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887 Cards in this Set
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Basic Pharmacokinetics
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Way to increase the renal elimination of a weak acid
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Alkalinize the urine
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1. volumes of plasma, blood, ECF, total body water for 70 kg. person?
2. Eq. for Vd, half life, Cl, Infusion rate, loading dose, maintanence dose? |
1. 3, 5, 12-14, 40-42
2. Vd=Dose/Conc. at time 0 half life=.7/k k=Cl/Vd it is the elimination constant Cl=k x Vd or elimination rate/plasma conc. Infusion rate (k0)=Cl x Steady state concentration LD= V(d) x steady state conc. MD= Cl x steady state conc. x dosing interval |
None
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Way to inc. the renal elimination of a weak base
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Acidify the urine
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1. Time to 50, 90, 95, 100 percent steady states?
2. What is the normal GFR? |
1. 1x half life, 3.3x half life, 4-5x half life, >7 half life
2. 120 ml/min. |
None
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Weak acid % ionized at pH-pKa of -2,-1,0,1,2
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1, 10, 50, 90, 99
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List 4 phases of clinical testing?
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1. small group volunteers w/o disease test safety. PHARMOCOKINETICS at different levels.
2. 100 or more pt. with disease COMPARE AGAINST PLACEBO to see effectiveness 3. 1000 or more pt. with disease compare with placebo. how well work with common SE. DOUBLE BLIND. Compare against gold standard. 4. out market. post market surveilance for AE. Less common and possible more severe toxicities. not rigidly regulated by FDA. |
None
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% weak base ionized at pH-pKa of -2, -1, 0, 1, 2
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99, 90, 50, 10, 1
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Time it takes for amount of drug to fall to half of its value, when is it constant, which kinetics? (majority of drugs)
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Half-life (T1/2)
first order kinetics constant |
None
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Relates the amount of drug in the body to the plasma concentration
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Volume of distribution (VD) VD=dose/plasma level
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Plasma concentration of a drug at a given time
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Cp
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The ratio of the rate of elimination of a drug to its plasma concentration
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Clearance (CL)
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The elimination of drug that occurs before it reaches the systemic circulation
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First pass effect
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The fraction of administered dose of a drug that reaches systemic circulation
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Bioavailability (F)
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When the rate of drug input equals the rate of drug elimination, # half lives it takes
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Steady state: math=7, clinically 4-5
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Measurement used to determine the safety and eficacy of generic drugs
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Bioequivalence
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Metabolism
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This step of metabolism makes drug more hydrophilic and hence augments elimination
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Phase I
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Different steps of Phase I
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Oxidation, reduction, hydrolysis
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Inducers of Cytochrome P450 (CYP450)
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Barbiturates, phenytoin, carbamazepine, and rifampin, ethanol, St. Johns Wart, isoniazid
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None
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Inhibitors of CYP450
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Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit, Adenavir, ethanol, Ritonavir
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None
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Products of Phase II conjugation
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Glucuronate, acetic acid, and glutathione sulfate
so put on glucuronic acid, acetic acid, sulfuric acid |
None
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Constant percentage of substrate metabolized per unit time, directly proportional to plasma conc.
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First order kinetics
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Drug elimination with a constant amount metabolized regardless of drug concentration
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Zero order kinetics
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Target plasma concentration times (volume of distribution divided by bioavailability)
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Loading dose (Cp*(Vd/F))
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Concentration in the plasma times (clearance divided by bioavailability)
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Maintenance dose (Cp*(CL/F))
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Pharmacodynamics
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Strength of interaction between drug and its receptor, compare 2 which better
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Affinity, closest to Y axis
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Selectivity of a drug for its receptor
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Specificity
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Amount of drug necessary to elicit a biologic effect, compare 2 which better
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Potency, closest Y axis
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Ability of drug to produce a biologic effect, compare two which better
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Efficacy, maximal height of curve
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A drug that will produce 100% of the maximum response regardless of the potency
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Full agonist
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None
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Will produce less than 100% of the response
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Partial agonist
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None
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Ability to bind reversibly to the same site as the drug and without activating the effector system
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Competitive antagonist
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Ability to bind to either the same or different site as the drug
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Noncompetitive antagonist
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Mechanism of action (MOA) utilizes intracellular receptors
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Thyroid and steroid hormones
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MOA utilizes transmembrane receptors
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Insulin
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MOA utilizes ligand gated ion channels
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Benzodiazepines and calcium channel blockers and Acetylcholine
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None
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Median effective dose required for an effect in 50% of the population
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ED50
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Median toxic dose required for a toxic effect in 50% of the population
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TD50
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Dose which is lethal to 50% of the population
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LD50
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Window between therapeutic effect and toxic effect and equation
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Therapeutic index TD50/ED50
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None
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Receptors linked to GS
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B1, B2, D1
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Receptors linked to Gq
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M1, M3, a1
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Receptors linked to Gi
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M2, A2
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Drug with a high margin of safety
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High therapeutic index
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Drug with a narrow margin of safety
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Low therapeutic index
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Antidotes and agents used in drug overdose
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Antidote used for lead, arsenic, mercury poisoning
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Dimercaprol, EDTA
a chelating agent |
None
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Antidote used for cyanide poisoning
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Nitrites: convert Hgb to methgb which cyanides bind stronger to rather than cytochrome oxidase
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None
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Antidote used for anticholinergic poisoning
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Physostigmine: cholinesterase inhibitor.
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None
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Antidote used for organophosphate/anticholinesterase poisoning (2)
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Atropine(antimuscarinic), pralidoxime (reactivates inhibited acetylcholinesterase by breaking bond of insecticide and enzyme) (2-PAM)
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None
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Antidote used for iron salt toxicity
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Deferoxamine, a chelating agent
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None
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Antidote used for acetaminophen (APAP) toxicity
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N-acetylcysteine (Mucomyst), inc. glutathione, inhibits formation metabolite, directly interacts with metabolite
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None
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Antidote for arsenic, mercury, lead, and gold poisoning
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Dimercaprol
Heavy metals act by chemically reacting with adjacent sulfhydryl residues on metabolic enzymes, creating a chelate complex that inhibits the affected enzyme's activity. Dimercaprol competes with the sulfhydryl groups for binding the metal ion, which is then excreted in the urine. |
None
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Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
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Penicillamine, a chelating agent or dimercaprol
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None
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Antidote used for heparin toxicity
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Protamine sulfate, a base
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None
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Antidote used for warfarin toxicity
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Vitamin K and Fresh frozen plasma (FFP)
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None
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Antidote for tissue plasminogen activator (t-PA), streptokinase
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Aminocaproic acid, inhibits plasminogen activation
It binds reversibly to the kringle domain of plasminogen and blocks the binding of plasminogen to fibrin and its activation to plasmin |
None
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Antidote used for methanol and ethylene glycol (2)
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Ethanol, which has higher affinity for alcohol dehydrogenase.
Fomepizole: alcohol dehydrogenase inhibitor. |
None
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Antidote used for opioid toxicity
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Naloxone (IV), naltrexone (PO)
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Antidote used for benzodiazepine toxicity
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Flumazenil: a GABA receptor antagonist
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None
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Antidote used for tricyclic antidepressants (TCA)
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Sodium bicarbonate to correct acidosis
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None
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Antidote used for carbon monoxide poisoning
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100% O2 and hyperbaric O2
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Antidote used for digitalis toxicity. What if they have become arrythmic
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Digibind: antibody fragments against digoxin (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
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None
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Antidote used for beta agonist toxicity (eg. Metaproterenol)
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Esmolol
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Antidote for methotrexate toxicity
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Leucovorin: Folinic acid is a 5-formyl derivative of tetrahydrofolic acid. It is readily converted to other reduced folic acid derivatives (e.g. tetrahydrofolate). Since it does not require the action of dihydrofolate reductase for its conversion, it will be unaffected by inhibition of this enzyme by drugs such as methotrexate.
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None
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Antidote for beta-blockers and hypoglycemia
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Glucagon
Glucagon binds to the glucagon receptor, a G protein-coupled receptor located in the plasma membrane. The conformation change in the receptor activates G proteins, alpha subunit specifically activates the next enzyme in the cascade, adenylate cyclase. Adenylate cyclase manufactures cAMP (cyclical AMP) which activates cAMP-dependent protein kinase. This enzyme in turn activates phosphorylase B kinase, which in turn, phosphorylates phosphorylase B. Phosphorylase B is the enzyme responsible for the release of glucose-1-phosphate from glycogen polymers in heart can inc. cAMP without having to use Beta receptor |
None
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Antidote useful for some drug induced Torsade de pointes
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Magnesium sulfate
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Antidote for hyperkalemia
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sodium polystyrene sulfonate (Kayexalate): it binds K+ in the gut
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None
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Antidote for salicylate intoxication
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Alkalinize urine, dialysis
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Cancer Chemotherapy
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Constant proportion of cell population killed rather than a constant number
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Log-kill hypothesis
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Treatment with cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
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Pulse therapy
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Toxic effect of anticancer drug can be lessened by rescue agents
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Rescue therapy
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Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
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Allopurinol
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Pyrimidine analog that causes "Thiamine-less death" given with leucovorin. Used for solid tumors.
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5-flouracil (5-FU): When goes into cells converted into 5-fDUMP which blocks thymidylate synthase
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None
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Drug used in cancer therapy causes Cushing-like symptoms
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Prednisone
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Side effect of Mitomycin and MOA
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SEVERE myelosuppression
Changed into alkylating agent so it crosslinks DNA to fight hypoxic tumors |
None
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MOA of cisplatin + use of
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Alkylating agent. Used for bladder, lung, ovary, testis
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None
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Common toxicities of cisplatin
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Nephro and ototoxicity
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Analog of hypoxanthine, needs HGPRTase for activation: INHIBITS purine metabolism. Used for acute leukemia.
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6-mercaptopurine (6-MP): after HGPRTase metabolite inhibtis enzymes of purine synthesis
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None
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Interaction with this drug requires dose reduction of 6-MP
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Allopurinol, because xanthine oxidase metabolized 6-MP
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None
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May protect against doxorubicin toxicity by scavenging free radicals and MOA of doxorubicin
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Dexrazoxane: inhibitor of iron mediated free radical generation to protect against cardiotoxicity.
It intercalates between base pairs, inhibitis topoisomerase II, generates free radicals |
None
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Breaks DNA via free redicals, Used for Hodgkins, squamous cell, testicular. What is the drug and what is limiting SE?
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Bleomycin
limiting SE is pulmonary fibrosis. |
None
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This regimen if used for testicular cancer produces near 100% response
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Bleomycin (free radicals) +vinblastine (prevent microtubule assembly)+etoposide (inc. degradation DNA via topo II and inhibts electron transport)+cisplatin (alkylating) produce almost a 100% response when all agents are used for this neoplasm
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None
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MOPP regimen used in Hodgkin's disease (HD) + MOA of each
How each work? |
Mechlorethamine (alkylating agent) + oncovorin (vincristine) (prevent assembly of microtubles) + procarbazine (forms hydrogen peroxide=free radicals and a alkylating agent), and prednisone
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None
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ABVD regimen used for HD, but appears less likely to cause sterility and secondary malignancies than MOPP
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Adriamycin (doxorubicin) (intercalates between bases of DNA) +bleomycin (free radicals), vinblastine (prevents formation of microtubules) +dacarbazine (alkalating agent)
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None
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Regimen used for non-Hodgkin's lymphoma
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COP (cyclophosphamide (alkylating agent), oncovorin(vincristine, prevents formatoin of microtubules), and prednisone)
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None
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Regimen used for breast cancer
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CMF (cyclophosphamide (alkylating agent), methotrexate (inhibits dihydrofolate reductase), and fluorouracil (thiamine less death) and tamoxifen if ER+
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None
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Alkylating agent, vesicant that causes tissue damage with extravasation.
What cancer used for? |
Mechlorethamine: spontaneously converts in body to reactive cytotoxic product.
Hodgkin disease |
None
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Anticancer drug also used in RA, SE is hemorrhagic cystitis. What cancers used for? what is this SE due to and how can you prevent it?
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non hodgkin, ovary, breast
Cyclophosphamide: The main effect of cyclophosphamide is due to its metabolite phosphoramide mustard. This metabolite is only formed in cells which have low levels of ALDH. Phosphoramide mustard forms DNA crosslinks between and within DNA strands. This leads to cell death. SE due to acrolein formation in the kidney. Give hydration and MESNA |
None
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Prevention of cyclophosphamide induced hemorrhagic cystitis
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Hydration and mercaptoethanesulfonate (MESNA): Mesna assists to neutralise these metabolites by binding through its sulfhydryl-moieties, and also increases urinary excretion of cysteine.
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None
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Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation. Used for acute leukemia, lymphomas, Kaposi, neuroblastoma, testicular.
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Vincristine and vinblastine
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None
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Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase. Advanced breast and ovarian cancer.
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Paclitaxel (taxol)
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None
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Toxicities include nephrotoxicity and ototoxicity, leading to a severe interaction with aminoglycosides
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Cisplatin
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Agent similar to cisplatin, less nephrotoxic, but what at more risk for?
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Carboplatin
Myelosuprresion |
None
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Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
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L-asparaginase
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Used for hairy cell leukemia; MOA
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Interferon alpha
activates NK cells |
None
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Anti-androgen used for prostate cancer
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Flutamide (Eulexin): androgen receptor antagonist
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None
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Anti-estrogen used for estrogen receptor + breast cancer
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Tamoxifen
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SERM used only for metastatic breast cancer. No risk of endometrial cancer.
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Toremifene (Fareston)
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None
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Some cell cycle specific anti-cancer drugs
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Bleomycin, vinca alkaloids, antimetabolites (eg., 5-FU, 6-MP, methotrexate, etoposide)
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Some cell cycle non-specific drugs
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Alkylating agents (eg., mechlorethamine, cyclophosphamide), antibiotics (doxorubicin, daunorubicin), cisplatin, nitrosourea
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Anti-emetics used in association with anti-cancer drugs. How do they work?
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Odansetron, granisetron
They are 5-HT3 (serotonin receptor subtype ) antagonist |
None
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Nitrosoureas with high lipophilicity, used for brain tumors
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Carmustine (BCNU) and lomustine (CCNU): alkylating agents
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None
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Produces disulfiram-like reaction with ethanol, also blocks MAO
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Procarbazine: alkylating agent also forms hydrogen peroxide generating free radicals
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None
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Endocrine drugs: hypothalamic and pituitary hormones
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Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma and other GH producing pituitary tumors
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Octreotide
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Somatotropin (GH) analog used in GH deficiency (dwarfism)
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Somatrem
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GHRH analog used as diagnostic agent
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Sermorelin
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GnRH agonist used for infertility or different types of CA depending on pulsatile or steady usage respectively Name 2.
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Leuprolide or goserelin
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None
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GnRH antagonist with more immediate effects, used for infertility
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Ganirelix, to prevent premature LH surge. Also cetrorelix.
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None
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Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
Name 3 |
Bromocriptine or pergolide or Cabergoline
Pergolide is in decreasing use, as it has been associated with fibrotic heart disease since 2003 [1]. This problem is thought to be due to pergolide's action at the 5-HT2B serotonin receptors of cardiac myocytes |
None
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Hormone inhibiting prolactin release
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Dopamine
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ACTH analog used for diagnosis of patients with corticosteroid abnormality
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Cosyntropin
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Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
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Desmopressin (DDAVP)
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Thyroid and anti-thyroid drugs
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Most widely used thyroid drugs contain this thyroid hormone. Name 2.
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L-thyroxine (T4)
Synthroid and Levoxyl |
None
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T3 compound less widely used
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Cytomel
Unlike synthroid, cytomel results in a rapid elevation in thyroid hormone levels that result in supraphysiological levels 2 to 6 hours after ingestion and a rapid clearance. |
None
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Anti-thyroid drugs
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Thioamides, iodides, radioactive iodine, and ipodate
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Thioamide agents used in hyperthyroidism
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Methimazole and propylthiouracil (PTU)
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Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses, and should be used with extreme caution in pregnancy
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PTU
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PTU (propylthiouracil) MOA
does PTU affect the iodide transporter in and if not who could |
PTU inhibits many steps in the synthesis of thyroid hormones, including the addition of iodide to thyroglobulin by the enzyme thyroperoxidase, a necessary step in the synthesis of thyroxine, and by inhibiting the enzyme 5'-deiodinase which converts T4 to T3.
PTU does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors such as perchlorate and thiocyanate. |
None
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Can be effective for short term therapy of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
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Iodide salts
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Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
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Radioactive iodine
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Radio contrast media that inhibits the conversion of T4 to T3
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Ipodate
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Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3 in peripheral how?
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Beta-blockers such as propranolol
via 5' deiodinase |
None
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Adrenocorticosteroid and adrenocortical antagonists
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3 zones of adrenal cortex and their products
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Glomerulosa (mineralocorticoids), fasciculata (glucocorticoid=GC), and reticularis (adrenal androgens)
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Pneumonic for 3 zones of adrenal cortex
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GFR
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Used for Addison's disease, Congenital Adrenal Hyperplasia (CAH), inflammation, allergies, and asthma (as a local inhalation)
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Glucocorticoids
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Short acting GC's
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Cortisone and hydrocortisone (equivalent to cortisol)
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Intermediate acting GC's (4)
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Prednisone, methylprednisolone, prednisolone, and triamcinolone
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None
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Long acting GC's
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Betamethasone, dexamethasone, and paramethasone
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Mineralocorticoids
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Fludrocortisone and deoxycorticosterone
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Some side effects of corticosteroids
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Osteopenia, impaired wound healing, inc. risk of infection, inc. appetite, HTN, edema, PUD, euphoria, psychosis
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Period of time of therapy after which GC therapy will need to be tapered
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5-7 days
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Inhibitors of corticosteroids biosynthesis
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Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test + MAO of drug
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Metyrapone: Metyrapone blocks cortisol synthesis by inhibiting 11B hydroxylase. this stimulates ACTH secretion, which in turn increases plasma 11- deoxycortisol levels. When excess ACTH secretion is the cause of hypercortisolism, the metyrapone test helps clarify if the source of the ACTH is pituitary or ectopic (non-pituitary).
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None
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Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
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Aminoglutethimide
Since cortisol helps break down muscle, aminoglutethimide is used by bodybuilders in a steroid cycle. |
None
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Antifungal agent used for inhibition of all gonadal and adrenal steroids
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Ketoconazole
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Antiprogestin used as potent antagonist of GC receptor
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Mifepristone
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Diuretic used to antagonize aldosterone receptors
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Spironolactone
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Common SE of spironolactone
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Gynecomastia and hyperkalemia
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Gonadal hormones and inhibitors
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Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable), has beneficial effects on bone loss
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Estrogen
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Antiestrogen drug used for fertility
antiestrogen drug used for breast cancer |
Clomiphene (acts by inhibiting the action of estrogen on the gonadotrope cells in the anterior pituitary gland "Sensing" low estrogen levels, follicle-stimulating hormone (FSH) release is increased, leading to a higher rate of ovulation ) and tamoxifen
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None
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Common SE of tamoxifen and raloxifene
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Hot flashes
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Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and currently being tested for treatment of breast cancer (Stars study)
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Raloxifene
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Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
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Diethylstilbestrol (DES)
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Estrogen mostly used in oral contraceptives (OC) (2)
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Ethinyl estradiol and mestranol which is metabolized to ethinyl estradiol
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None
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Anti-progesterone used as abortifacient
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Mifepristone (RU-486)
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Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
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Combination oral contraceptives (OC)
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Oral contraceptive available in a transdermal patch
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Ortho-Evra
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Converted to more active form DHT and by what enzyme?
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Testosterone: 5 alpha reductase
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None
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5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
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Finasteride (Proscar and Propecia respectively)
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Anabolic steroid that has potential for abuse
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Nandrolone and stanozolol
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Anti-androgen used for hirsutism in females (2)
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Cyproterone acetate or Spironolactone
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None
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Drug is used with testosterone for male fertility
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Leuprolide: GnRH agonist
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None
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Pancreatic hormones, antidiabetics, and hyperglycemics
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Alpha cells in the pancreas
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Produce glucagon
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Beta cells in the pancreas
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Produce insulin
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Beta cells are found. What type of compounds can increase the release of its product?
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Islets of Langerhans
Increased by glucose, sulfonylureas, M-activators, B2 agonists **Decreased by alpha 2 agonist |
None
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Delta cells in the pancreas
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Produce Somatostatin
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Product of proinsulin cleavage used to assess insulin abuse
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C-peptide
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Exogenous insulin
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Little C-peptide
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Lab measurement to determine source of insulin.
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C-peptide
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None
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Very rapid acting insulin, having fastest onset and shortest duration of action. Describe peak, duration
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Lispro (Humalog)
Peaks at 15-30 minutes and duration is 3-4 hours |
None
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Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia? Peak and duration? How treat diabetic ketoacidosis?
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Regular (Humulin R): Peak 30 min - 3 hours duration 5-7 2-4 min. IV,
Regular IV, fluids and electrolytes |
None
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Long acting insulin
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Ultralente (humulin U)
onset 3-4 hr, peak 8-16 hr, dur. 24-36 hr. |
None
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Ultra long acting insulin, has over a day duration of action
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Glargine (Lantus): has no peak and works greater 24 hr
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None
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Major SE of insulin
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Hypoglycemia
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|
Receptor for glucose found in the liver and pancreas and kidney
Describe the other receptors |
GLUT 2
1=RBC 3=neurons, placenta 4=muscle and adipose |
None
|
|
Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
|
GLUT 4
|
|
|
Examples of alpha-glucosidase inhibitors (AGI)
|
Acarbose, miglitol
|
|
|
MOA of AGI's
|
Act on intestine, delay absorption of glucose
|
|
|
SE of AGI's. What do you not want to give these pt.?
|
Flatulence (do not use beano to tx, Beano is an enzyme-based dietary supplement that is alleged by its manufacturer to reduce gas in the digestive tract, thereby preventing flatulence. It contains the enzyme alpha galactosidase. It is claimed that the human digestive tract does not contain alpha galactosidase; however acarbose may work against alpha galactosidase ), diarrhea, abdominal cramps
|
None
|
|
Alpha-glucosidase inhibitor associated with elevation of LFT's
|
Acarbose
|
|
|
Amino acid derivative with MOA similar to sulfonylureas but a shorter DOA
|
Nateglinide, a phenylalanine derivative
|
None
|
|
MOA of nateglinide
|
Insulin secretagogue, closes K+ channels causing depolarization
|
None
|
|
The only biguanide approved for treating type 2 diabetes?
|
Metformin
|
None
|
|
Drugs available in combination with metformin (4)
|
Glyburide, glipizide, and rosiglitazone, and pioglitazone
|
None
|
|
MOA of metformin
|
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity. Works via gene expression.
|
None
|
|
Most important potential SE of metformin
|
Lactic acidosis due to more glucose uptake by the cells. By blocking gluconeogenesis may impair hepatic metabolism of lactic acidosis esp. with renal insufficiency
|
None
|
|
Name a Meglitinide and use of.
|
Repaglinide: use just before meals due to short half life.
Also Nateglinide. |
None
|
|
MOA of repaglinide
|
Insulin release from pancreas. It achieves this by closing ATP-dependent potassium channels in the membrane of the beta cells. This depolarizes the beta cells, opening the cells' calcium channels, and the resulting calcium influx induces insulin secretion.; faster and shorter acting than sulfonylurea
|
None
|
|
First generation sulfonylureas. Which is ok with renal dysfunction? Which is most potent?
|
Chlorpropamide (most potent), tolbutamide (ok with renal dysfunction), tolazamide, Acetohexamide.
|
None
|
|
Second generation sulfonylureas. Which is dec. in dose with renal problems. Which with hepatic problems?
|
Glyburide (dec. with renal), glipizide (dec. with hepatic), glimepiride, etc.
|
None
|
|
MOA of both generations
|
Insulin release from pancreas by modifying K+ channels
|
|
|
Common SE of sulfonylureas, repaglinide, and nateglinide
|
Hypoglycemia
|
|
|
Sulfonylurea NOT recommended for elderly because of very long half life
|
Chlorpropamide
|
|
|
Name three Thiazolidinediones
|
Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
|
None
|
|
Reason troglitazone was withdrawn from market
|
Hepatic toxicity
|
|
|
MOA of thiazolindinediones
|
Stimulate PPAR-gamma receptor involved in transcription in insulin responsive genes. Senstitizes target tissues to insulin.
|
None
|
|
SE of Thiazolindinediones
|
Edema, mild anemia; interaction (they are inducers) with drugs that undergo CytP450 3A4 metabolism
|
None
|
|
Hyperglycemic agent to treat low serum glucose that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
|
Glucagon
|
None
|
|
Drugs used in bone homeostasis
|
|
|
|
Available bisphosphonates
|
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
(PARTE) |
None
|
|
MOA of Bisphosphonates
|
Inhibits osteoclast bone resorption and stabalize hydroxyapatite structure
|
None
|
|
Only bisphosphonates available IV
|
Etidronate
|
|
|
Uses of bisphosphonates
|
Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
**Alendronate DOC with HRT or for steroid induced osteoperosis |
None
|
|
Major SE of bisphosphonates
|
Chemical esophagitis esp. with alendronate when pt. has inadequate water intake
|
None
|
|
1. Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
2. Recombinant DNA PTH analog used used one time daily to stimulate osteoblasts. Name drug and major SE? |
1.Etidronate and Pamidronate
2. Teriparatide, with continous infustion stimulates osteoclasts. Also used more 2 years inc. risk of osteosarcoma. |
None
|
|
Used for prevention of postmenopausal osteoporosis in women
|
Estrogen (HRT-Hormone replacement therapy)
|
|
|
Increase bone density, also being tested for breast CA tx.
|
Raloxifene (SERM-selective estrogen receptor modulator)
|
|
|
Used intranasally and decreases bone resorption
|
Calcitonin (salmon prep)
|
|
|
Used especially in postmenopausal women, dosage should be 1500 mg
|
Calcium
|
|
|
Vitamin given with calcium to ensure proper absorption
|
Vitamin D
|
|
|
Drugs with important actions on smooth muscle
|
|
|
|
Disease caused by excess ergot alkaloids
|
St. Anthony's Fire: The symptoms can be roughly divided into convulsive symptoms and gangrenous symptoms.
|
None
|
|
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
|
Autocoids: local hormones made many places, not just endocrine glands. Formed by the tissues where they act.
|
None
|
|
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
|
Zollinger-Ellison Syndrome
|
|
|
Endogenous Drug that causes contraction of the uterus
|
Oxytocin
|
None
|
|
Distribution of histamine receptors H1, H2, and H3
|
Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
|
|
|
Prototype antagonist of H1 and H2 receptors respectively
|
Diphenhydramine and impromidine or cimetidine respectively
|
None
|
|
1st generation antihistamine that is highly sedating
|
Diphendydramine
|
|
|
1st generation antihistamine that is least sedating (2)
Name all 1st generation antihistamines |
Chlorpheniramine or cyclizine
Chlorpheniramine, cyclizine, diphenydramine, dimenhydrinate, doxepin, doxylamine, hydroxyzine, meclizine, promethazine |
None
|
|
2nd generation antihistamines, name 3
|
Fexofenadine, loratadine, and cetirizine
|
None
|
|
Generation of antihistamine that has the most CNS effects
|
First generation due to being more lipid-soluble
|
|
|
Major indication for H1 receptor antagonist
|
Use in IgE mediated allergic reaction
|
|
|
Antihistamine that can be used for anxiety and insomnia and is not addictive
|
hydroxyzine (Atarax)
H1 receptor antagonist and piperazine derivative used primarily as an antihistamine for the treatment of itches and irritations, an antiemetic for the reduction of nausea, as a weak analgesic and as an anxiolytic. Good for people with drug abuse who have anxiety. |
None
|
|
H1 antagonist used in motion sickness (5)
|
Dimenhydrinate, Diphenhydramine, cyclizine, meclizine, hydroxyzine
|
None
|
|
Most common side effect of 1st generation antihistamines
|
Sedation
|
|
|
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
|
Terfenadine and astemizole (have been removed from the market)
|
|
|
H2 blocker that causes the most interactions with other drugs
|
Cimetidine
|
|
|
Clinical use for H2 blockers
|
Acid reflux disease, duodenal ulcer and peptic ulcer disease
|
|
|
Receptors for serotonin are located. How do they work? MOA?
|
5 HT-1D : Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
5 HT-2 : Smooth muscle and platelets. 5 HT-3 : CNS. chemoreceptor area and vomiting center. |
None
|
|
5HT-1d agonist used for migraine headaches (3)
|
Sumatriptan, naratriptan, and rizatriptan
|
None
|
|
Triptan available in parenteral and nasal formulation
|
Sumatriptan
|
|
|
1.H1 blocker that is also a serotonin antagonist, what used for?
2. Two serotonin antagonists that have alpha 1 blocking properties? |
Cyproheptadine
antihistaminic and antiserotonergic agent. It acts as a 5-HT2 receptor antagonist and also blocks calcium channels. Cyproheptadine is used in the treatment of allergies (specifically Hay fever) and is also used to stimulate appetite in underweight people (e.g. anorexia nervosa). Cyproheptadine may also be used to combat SSRI-induced sexual dysfunction, but is used cautiously in this manner due to the fact that it may reverse the effects of the SSRI. Cyproheptadine is also used for the treatment of Cushing's Syndrome, the treatment of serotonin reactions secondary to meperidine, and may be used, though rarely, as a prophylactic drug for migraine headaches. 2. Ketanserin and Phenoxybenzamine |
None
|
|
5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction (3)
|
Ketanserin, cyproheptadine, phenoxybenzamine and ergot alkaloids (partial agonist of alpha and serotonin receptors)
|
None
|
|
Ergot Alkaloids
1. agent used for postpartum bleeding 2. agents for migraines, one for acute, one for prophylaxis |
1. ergonovine
2. acute=ergotamine: alpha VC prophylaxis=methysergide or ergonavine |
None
|
|
Serotonin or ergots:
Agents used in treatment of carcinoid tumor |
Ketanserin cyproheptadine, and phenoxybenzamine (all HT-2 antagonist) + methysergide
|
None
|
|
Serotonin antagonist used in chemotherapeutic induced emesis and which receptor do they work on? (4)
|
Ondansetron, granisetron, dolasetron and alosetron
5HT-3 |
None
|
|
5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
5 HT-3 antagonist Associated with fatal bowel complications |
Dolasetron
Alosetron |
None
|
|
DOC of chemo induced nausea and vomiting
|
Odansetron
|
|
|
Drug used in ergot alkaloids overdose, ischemia and gangrene
|
Nitroprusside: counteracts the alpha and HT VC of the ergot alkaloids
|
None
|
|
Reason ergot alkaloids are contraindicated in pregnancy
|
Uterine contractions
|
|
|
SE of ergot alkaloids
|
Hallucinations resembling psychosis (LSD), others see GI distress and prolonged vasoconstriction
|
None
|
|
Ergot alkaloid used as an illicit drug
|
LSD
Partial dope agonist and The hallucinogenic effects of LSD are attributed to its strong partial agonist effects at 5-HT2A receptors as specific 5-HT2A agonist drugs are hallucinogenic and largely 5-HT2A specific antagonists block the hallucinogenic activity of LSD.[14] Exactly how this produces the drug's effects is unknown, but it is thought that it works by increasing glutamate release and hence excitation in the cortex, specifically in layers IV and V |
None
|
|
Dopamine agonist used in hyperprolactinemia
|
Bromocriptine
|
|
|
Peptide causing increased capillary permeability and edema (2)
|
Bradykinin and histamine
|
None
|
|
Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
|
Bradykinin
|
|
|
Drug causing depletion of substance P (vasodilator)
|
Capsaicin
|
|
|
Prostaglandins that cause abortions
|
Prostaglandin E1 (misoprostol) PGE2, and PGF2alpha
|
|
|
Difference between COX 1 and COX 2 "
|
COX 1 is found throughout the body and COX 2 is only in inflammatory tissue
|
|
|
3 Drugs that selectively inhibits COX 2
|
Celecoxib, valdecoxib, and rofecoxib
|
None
|
|
Inhibitor of lipoxygenase that can help treat asthma
|
Zileuton: selective and specific inhibitor of 5-lipooxygenase
|
None
|
|
Major SE of zileuton
|
Liver toxicity
|
|
|
Inhibitor of leukotrienes (LTD4) receptors and used in asthma prophylaxis
|
Zafirlukast and montelukast
|
None
|
|
Used in pediatrics to maintain patency of ductus arteriosis
|
PGE1
|
|
|
Prostaglandin Approved for use in severe pulmonary HTN
|
PGI2 (epoprostenol)
Prostacyclin acts chiefly to prevent platelet formation and clumping involved in blood clotting. It is also an effective vasodilator. |
None
|
|
Prostaglandin used in the treatment impotence
|
Alprostadil (PGE1)
|
None
|
|
Irreversible, nonselective COX inhibitor
|
Aspirin
|
|
|
Class of drugs that reversibly inhibit COX
|
NSAIDS
|
|
|
Primary endogenous substrate for Nitric Oxidase Synthase
|
Arginine
|
|
|
MOA and effect of nitric oxide
|
Stimulates cGMP which leads to vascular smooth muscle relaxation
mechanism: cGMP facilitates the dephosphorylation and inactivation of myosin light chains |
None
|
|
Long acting beta 2 agonist used in asthma (2)
|
Salmeterol and Formoterol
|
None
|
|
Muscarinic antagonist used in asthma for people unable to tolerate adrenergic agonists. (2)
|
Ipratropium and Tiotropium
|
None
|
|
MOA action of cromolyn
|
Mast cell stabilizer
|
|
|
Enzyme which theophylline inhibits
|
Phosphodiesterase this leads to an inc. of cAMP which causes smooth muscle dilation
|
None
|
|
Methylxanthine derivative used as a remedy for intermittent claudication
|
Pentoxifylline
|
|
|
Antidote for severe CV toxicity of theophylline
|
Beta blockers
|
|
|
MOA of corticosteroids"
|
inhibit phospholipase A2
|
|
|
SE of long term (>5 days) corticosteroid therapy and remedy
|
Adrenal suppression and weaning slowly, respectively
|
|
|
Antimicrobials
|
|
|
|
MOA of quinolones
|
Inhibit Topoisomerase II (DNA gyrase) blocking relaxation of supercoiled DNA. Also block Topo 4 which is required for DNA seperation.
|
None
|
|
MOA of penicillin
|
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
|
|
|
Drug used for MRSA
|
Vancomycin
|
|
|
Vancomycin MOA
|
Blocks peptidoglycan synthesis, the D-ala-D-ala pentapeptide linkage
|
None
|
|
Type of resistance found with vancomycin
|
Point mutation: Terminal D-ala replaced by D-lactate
|
None
|
|
N. Meningitidis prophylaxis in exposed patients and drug MOA
|
Rifampin: inhibits DNA-dependent RNA polymerase
|
None
|
|
Technique used to diagnose perianal itching, and the drug used to treat it. MOA of drug
|
Scotch tape technique and mebendazole (selectively inhibits microtubule synthesis and glucose uptake in nematodes)
|
None
|
|
Two toxicities of aminoglycosides
|
nephro and ototoxicity
|
|
|
DOC for Legionnaires' disease
|
Erythromycin
|
|
|
Complete MOA of sulfonamides
|
Competes with PABA, Inhibiting dihydropteroate synthase
PABA uses dihydropteroate synthase to go to dihydrofolic acid. This uses dihydrofolate reductase to go to tetrahydrofolic acid. This is used to make purines |
None
|
|
Penicillins active against penicillinase secreting bacteria
|
Methicillin, nafcillin, and dicloxacillin
|
|
|
Cheap wide spectrum antibiotic DOC of otitis media and backup drug for Lyme disease
|
Amoxicillin
|
None
|
|
Class of antibiotics that have 10% cross sensitivity with penicillins
|
Cephalosporins
|
|
|
PCN active against pseudomonas
|
Carbenicillin, piperacillin and ticarcillin
|
|
|
Antibiotic causing red-man syndrome, and prevention
|
Vancomycin, infusion at a slow rate and antihistamines
|
|
|
Drug causes teeth discoloration
|
Tetracycline
|
|
|
MOA of tetracycline
|
Decreases protein synthesis by inhibiting 30S ribosome
|
|
|
Drug that causes gray baby syndrome and aplastic anemia
|
Chloramphenicol (50S)
|
None
|
|
Drug notorious for causing pseudomembranous colitis
|
Clindamycin (50S)
|
None
|
|
DOC for tx of pseudomembranous colitis + MOA
|
Metronidazole: good for anaerobes
Metronidazole is selectively taken up by anaerobic bacteria and sensitive protozoal organisms because of the ability of these organisms to reduce metronidazole to its active form intracellularly. The nitro group of metronidazole is chemically reduced by ferredoxin (or ferredoxin-linked metabolic process) and the products are responsible for disrupting the DNA helical structure, thus inhibiting nucleic acid synthesis |
None
|
|
Treatment of resistant pseudomembranous colitis
|
ORAL vancomycin: It is a large hydrophilic molecule which partitions poorly across the gastrointestinal mucosa
|
None
|
|
Anemia caused by trimethoprim
|
Megaloblastic anemia: it may inhibit dyhdrofolate in humans also
|
None
|
|
Reason fluoroquinolones are contraindicated in children and pregnancy
|
Cartilage damage
|
|
|
Name 4 bugs that metronidazole is the DOC for?
|
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
|
None
|
|
Treatment for TB patients
|
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
I saw a red pyre burning the liver |
None
|
|
Metronidazole SE if given with alcohol and mechanism
|
Disulfiram-like reaction because it inhibits acetaldehyde dehydrogenase
|
None
|
|
Common side effect of Rifampin
|
Red urine discoloration: metabolites are red-orange color
|
None
|
|
MOA of nystatin
|
nystatin binds to ergosterol, a major component of the fungal cell membrane. When present in sufficient concentrations, it forms pores in the membrane that lead to K+ leakage and death of the fungus
|
None
|
|
Neurotoxicity with isoniazid (INH) prevented by
|
Administration of Vit. B6 (pyridoxine) as this drug inc. excretion of pyridoxine in slow acetylators
|
None
|
|
Toxicity of amphotericin
|
Nephrotoxicity
|
|
|
SE seen only in men with administration of ketoconazole
|
Gynecomastia because it blocks steroid synthesis
|
None
|
|
Topical DOC in impetigo + MOA
|
Topical mupirocin (Bactroban)
It has a unique mechanism of action, which is selective binding to bacterial isoleucyl-tRNA synthetase, which halts the incorporation of isoleucine into bacterial proteins. Because this mechanism of action is not shared with any other antibiotic, mupirocin has few problems of antibiotic cross-resistance |
None
|
|
DOC for influenza A
|
Amantadine: prevents uncoating of influenza A
The drug interferes with a viral protein, M2 (an ion channel), which is needed for the viral particle to become "uncoated" once it is taken inside the cell by endocytosis. |
None
|
|
DOC for RSV
|
Ribavirin: inhibits viral RNA polymerase
|
None
|
|
DOC for CMV retinitis
|
Ganciclovir: block RNA polymerase of virus
|
None
|
|
SE for ganciclovir
|
Neutro, leuko and thrombocytopenia
|
|
|
Anti-viral agents associated with Stephen Johnson syndrome
|
Nevirapine, amprenavir
|
|
|
HIV antiviral class known to have severe drug interactions by causing inhibition of metabolism
|
Protease inhibitors
|
|
|
Antivirals that are teratogens
|
Delavirdine, efavirenz, and ribavirin
|
|
|
Antivirals associated with neutropenia
|
Ganciclovir, zidovudine, saquinavir, and interferon
|
|
|
HIV med used to reduce transmission during birth
|
AZT (zidovudine)
|
|
|
Drug used for African sleeping sickness
|
Suramin
|
|
|
Drug used in Chagas disease
|
Nifurtimox: T cruzi lacks catalase and this drug makes oxygen free radicals
|
None
|
|
Cephalosporins able to cross the BBB
|
Cefixime (2nd) and 3rd generation
|
|
|
Drug used for N. gonorrhea in females
|
Ceftriaxone because most gonorrhea resistant to penicillin
|
None
|
|
Cephalosporin causes kernicterus in neonates
|
Ceftriaxone or cefuroxime; these may cause hemolytic anemia
|
None
|
|
SE of Isoniazid
|
Peripheral neuritis due to pyridoxine deficiency and hepatitis due to toxic metabolite
|
None
|
|
Aminoglycoside that is least ototoxic
|
Streptomycin
|
|
|
Drug used in exoerythrocytic cycle of malaria
|
Primaquine
|
|
|
Oral antibiotic of choice for moderate inflammatory acne
|
Minocycline
|
|
|
Drug of choice for leprosy and MOA
|
Dapsone: PABA antagonist to inhibit folate synthesis.
|
None
|
|
DOC for herpes and its MOA
|
Acylovire
It is selectively converted into a monophosphate form by viral thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase. Subsequently, the monophosphate form is further phosphorylated into the active triphosphate form, aciclo-GTP, by cellular kinases. Aciclo-GTP is a very potent inhibitor of viral DNA polymerase; it has approximately 100 times higher affinity to viral than cellular polymerase. Its monophosphate form also incorporates into the viral DNA, resulting in chain termination |
None
|
|
Anti-microbials that cause hemolysis in G6PD-deficient patients
|
Sulfonamides
|
|
|
MOA of erythromycin
|
Inhibition of protein synthesis at the 50s subunit of ribosome
|
|
|
Anti-biotic frequently used for chronic UTI prophylaxis and MOA
|
sulfamethoxazole/ trimethoprim
sulf inhibits incorporation of PABA into folic acid, tri prevents reduction of dihydrofolate to tetrahydrofolate. Both excreted in urine. |
None
|
|
Lactam that can be used in PCN allergic patients
|
Aztreonam
|
|
|
SE of imipenem
What drug should you combine with this? |
Seizures
Cilastin |
None
|
|
Anti-viral with a dose limiting toxicity of pancreatitis
|
Didanosine
|
|
|
Sedative Hypnotics
|
|
|
|
Common side effect of hypnotic agents
|
Sedation
|
|
|
Occurs when sedative hypnotics are used chronically or at high doses
|
Tolerance
|
|
|
The most common type of drug interaction of sedative hypnotics with other depressant medications
|
Additive CNS depression
|
|
|
Name Benzodiazepines (8)
|
Diazepam, Alprazolam, chlordiazepoxide, clonazepam, flurazepam, lorazepam, oxazepam, triazolam
|
None
|
|
Major effect of benzodiazepines on sleep at high doses
|
REM is decreased
|
|
|
Neurologic SE of benzodiazepines
|
Anterograde amnesia: why at high doses can be used as date rape drug
|
None
|
|
Reason benzos are used cautiously in pregnancy
|
Ability to cross the placenta
|
|
|
Main route of metabolism for benzodiazepines
|
Hepatic
|
|
|
Benzodiazepines (3) that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
|
Lorazepam, oxazepam, and temazepam
|
None
|
|
MOA for benzodiazepines (key word)
|
increase the FREQUENCY of GABA-mediated chloride ion channel opening
|
None
|
|
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
|
Flumazenil: benzodiazepine receptor antagonist
|
None
|
|
Benzodiazepine with useful relaxant effects in skeletal muscle spasticity of central origin
|
Diazepam
|
|
|
Benzodiazepine that has efficacy against absence seizures and in anxiety states, such as agoraphobia
|
Clonazepam
|
|
|
Benzodiazepines that are the most effective in the treatment of panic disorder
|
Alprazolam and Clonazepam
|
|
|
Benzodiazepine that is used for anesthesia. It is the shortest acting benzo.
|
Midazolam
|
None
|
|
Name two drugs useful with status epelepticus. Which one is the preffered agent for a child with a febrile seizure?
|
Diazepam and Lorazapam
febrile=diazepam |
None
|
|
Two Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
|
Chlordiazepoxide and Diazepam
|
None
|
|
Agents having active metabolites, long half lives, and a high incidence of adverse effects (4)
|
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
|
None
|
|
Name 5 Barbiturates
|
Phenobarbital, Amobarbital, Pentobarbital, Secobarbital, thiopental
|
None
|
|
Barbiturates may precipitate this hematologic condition
|
Acute intermittent porphyria
|
|
|
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
|
Liver enzyme INDUCTION
|
|
|
Barbiturates MOA KEY WORD
|
Increase the DURATION of GABA-mediated chloride ion channels
|
None
|
|
Barbiturate used for the induction of anesthesia
|
Thiopental
|
|
|
Alcohols
|
|
|
|
Important drug interaction with chloral hydrate
|
May displace coumadin from plasma proteins
|
|
|
Others
|
|
|
|
Site of action for zaleplon and zolpidem and their advantage
|
Benzodiazepine receptor BZ1 (although are not considered benzodiazepines). Bind more specifically to this receptor. Cause less daytime impairment and do not effect sleep as much.
|
None
|
|
Good hypnotic activity with less CNS SE than most benzodiazepines
|
Zolpidem, zaleplon
|
|
|
Agent that is a partial agonist for the 5-HT1A receptor but that may not be reason it helps you sleep
|
Buspirone
|
None
|
|
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
|
Buspirone
|
|
|
Alcohols
|
|
|
|
Two systems that will metabolize ethanol
|
metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
|
None
|
|
Is ethanol first order or zero order
|
Zero order
|
None
|
|
Rate limiting step of alcohol metabolism
|
Aldehyde dehydrogenase
|
|
|
System that increases in activity with chronic exposure and may contribute to tolerance
|
MEOS
|
|
|
Agent that metabolize acetaldehyde to acetate
|
Aldehyde dehydrogenase
|
|
|
Agents that inhibit aldehyde dehydrogenase
|
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
|
None
|
|
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing, and hypotension
|
Disulfiram
|
|
|
The most common neurologic abnormality in chronic alcoholics
|
Peripheral neuropathy (also excessive alcohol use is associated with HTN, anemia, and MI)
|
|
|
Agent that is teratogen and causes a fetal syndrome
|
Alcohol
|
|
|
Agent that is the antidote for methanol overdose
|
Alcohol
|
|
|
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
|
Fomepizole
|
|
|
Name Anti seizure Drugs by seizure type and back up drugs
|
1. TC and Partial = carbamazepine, phenytoin, valproic acid
2. abcense = ethosuximibe, valproic acid, clonazepam 3. myoclonic = valproic acid, clonazepam 4. back up = felbamate, gabapentin, lamotrigine, phenobarbital, tiagabine, topiramate, |
None
|
|
Most frequent route of metabolism
|
Hepatic enzymes
|
|
|
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
|
Sodium blockade in neuron = prolongation of inactivated state of Na+ channel
|
None
|
|
MOA for benzodiazepines and barbiturates
|
GABA-related targets
|
|
|
MOA for Ethosuximide
|
T type Calcium channels esp. in thalamic neurons that act as pacemakers
|
None
|
|
MOA for Valproic acid at high doses
|
Affect calcium, potassium, and sodium channels
|
|
|
Three Drugs of choice for generalized tonic-clonic and partial seizures
|
Valproic acid and Phenytoin and Carbamezepine
|
None
|
|
DOC for seizures in infants
|
Phenobarbital
|
None
|
|
Drugs of choice for absence seizures
|
Ethosuximide and valproic acid
|
|
|
Drug of choice for myoclonic seizures
|
Valproic acid
|
|
|
Drugs of choice for status epilepticus
|
IV diazepam or phenytoin (for prolonged therapy not acute)
|
|
|
Drugs that can be used for infantile spasms
|
Corticosteroids
|
|
|
Anti-seizure drugs used also for bipolar affective disorder (BAD) (4)
|
Valproic acid, carbamazepine, phenytoin and gabapentin
|
None
|
|
Anti-seizure drug of choice used also for Trigeminal neuralgia
|
Carbamazepine
|
None
|
|
Anti-seizure drugs used also for pain of neuropathic orgin
ex. postherpetic neuralgia |
Gabapentin
|
None
|
|
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes fetal hydantoin syndrome, and stimulates hepatic metabolism
|
Phenytoin
|
|
|
SE of phenytoin
|
Gingival hyperplasia, nystagmus, diplopia and ataxia
|
|
|
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacial anomalies and spina bifida
|
Carbamazepine
|
|
|
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
|
Valproic acid
|
|
|
Laboratory value required to be monitored for patients on valproic acid
|
Serum ammonia and LFT's
|
|
|
SE for Lamotrigine
|
Stevens-Johnson syndrome
|
|
|
SE for Felbamate
|
Aplastic anemia and acute hepatic failure
|
|
|
Anti-seizure medication also used in the prevention of migraines
|
Phenytoin and Gabapentin
|
None
|
|
Antiseizure medicine that may cause agranulocytosis
|
Carbamazepine
|
None
|
|
Anti-seizure drugs used as alternative drugs for mood stabilization (4)
|
Carbamazepine, gabapentin, phenytoin, and valproic acid
|
None
|
|
General Anesthetics: inhaled and IV
|
Halothane, Enflurane, desflurane, isoflurane, sevoflurane, nitrous, theopental, fentanyl, propofol, midazolam, ketamine, etomidate
|
None
|
|
MOA of general anesthetics
|
Unclear, thought to increase the threshold for firing of CNS neurons
|
|
|
Inhaled anesthetic with a low blood/gas partition coefficient
|
Nitrous oxide
|
|
|
Inversely related to potency of anesthetics
|
Minimum alveolar anesthetic concentration (MAC): alveolar conc. req to eliminate the response to a painful stimuli in 50% of pt.
|
None
|
|
2 Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
|
Halothane and methoxyflurane
|
None
|
|
Most inhaled anesthetics SE
|
Decrease arterial blood pressure
|
|
|
Inhaled anesthetics are myocardial depressants
|
Enflurane and halothane
|
|
|
Inhaled anesthetic causes peripheral vasodilation
|
Isoflurane
|
|
|
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholamines and has produced hepatitis
|
Halothane
|
|
|
Inhaled anesthetics, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
|
Nitrous oxide
|
|
|
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
|
Methoxyflurane
|
|
|
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
|
Nitrous oxide
|
|
|
Pungent inhaled anesthetic which leads to high incidence of coughing and vasospasm
|
Desflurane
|
|
|
DOC for malignant hyperthermia that may be caused by use of halogenated anesthetics
|
Dantrolene: prevents release of calcium from sarcoplasmic reticulum
|
None
|
|
IV barbiturate used as a pre-op anesthetic
|
Thiopental
|
|
|
Benzodiazepine used adjunctively in anesthesia
|
Midazolam
|
|
|
Benzodiazepine receptor antagonist, it accelerates recovery from benzodiazepine overdose
|
Flumazenil
|
|
|
This produces "dissociative anesthesia", is a cardiovascular stimulant which may increases intracranial pressure, and hallucinations occur during recovery
|
Ketamine
|
|
|
Opioid associated with respiratory depression, but is used in high risk patients who may not survive full general anesthetia
|
Fentanyl
|
|
|
State of analgesia and amnesia produced when fentanyl is used with droperidol and nitrous oxide
|
Neuroleptanesthesia
|
|
|
Produces both rapid anesthesia and recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
|
Propofol
|
|
|
Local Anesthetics
|
ester: tetracaine, procaine, benzocaine, cocaine
amides: bupivacaine, ropivacaine, lidocaine, prilocaine |
None
|
|
MOA of local anesthetics (LA's)
|
Block voltage-dependent sodium channels
|
|
|
This may enhance activity of local anesthetics
|
Hyperkalemia
|
|
|
This may antagonize activity of local anesthetics
|
Hypercalcemia
|
|
|
Almost all local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
|
Vasodilation
|
|
|
Local anesthetic with vasoconstrictive property, favored for head, neck, and pharyngeal surgery
|
Cocaine
|
|
|
Longer acting local anesthetics which are less dependent on vasoconstrictors
|
Tetracaine and bupivacaine
|
|
|
These LA's have surface activity
|
Cocaine and benzocaine
|
|
|
Most important toxic effects of most local anesthetics
|
CNS toxicity
|
|
|
Commonly abused LA which has cardiovascular toxicity including severe hypertension with cerebral hemorrhage, cardiac arrhythmias, and myocardial infarction
|
Cocaine
|
|
|
LA causing methemoglobinemia
|
Prilocaine
|
|
|
Skeletal Muscle Relaxants
|
depolarizing: succinylcholine
non: tubocurarine, pancuronium, vecuronium, atracurium, mivacurium |
None
|
|
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artifical ventilation. Full doses lead to respiratory paralysis and require ventilation
|
Neuromuscular blocking drugs
|
|
|
These drugs strongly potentiate and prolong effect of neuromuscular blockade (NMB)
|
Inhaled anesthetics, especially isoflurane, aminoglycosides, and antiarrhythmic
|
|
|
These prevent the action of Ach at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
|
Nondepolarizing type antagonists
|
|
|
Agent with long duration of action and is most likely to cause histamine release
|
Tubocurarine
|
None
|
|
Non-depolarizing antagonist has short duration x2. Why?
|
Mivacurium: because it is metabolized by plasma cholinesterase
Atracurium: Hoffman |
None
|
|
Agent can block cardiac muscarinic receptors
|
Pancuronium
|
None
|
|
Agent undergoing Hofmann elimination (breaking down spontaneously)
|
Atracurium
|
|
|
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis. SE?
|
Succinylcholine: causes muscle pain postoperatively and myoglobinuria may occur
|
None
|
|
During Phase I these agents worsen the paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
|
Cholinesterase inhibitors
|
|
|
Spasmolytic drugs
|
diazepam, baclofen, cyclobenzaprine, dantrolene, tizanidine, botulinum,
|
None
|
|
Agents acting in the CNS or in the skeletal muscle, used to reduce abnormally elevated tone caused by neurologic or muscle end plate disease
|
Spasmolytic drugs
|
|
|
Spasmolytic drug that Facilitates GABA presynaptic inhibition
|
Diazepam
|
None
|
|
GABA agonist in the spinal cord
|
Baclofen
|
|
|
Similar to clonidine and may cause hypotension
|
Tizanidine
|
|
|
DOC for malignant hyperthermia by acting on the sacroplasmic reticulum or skeletal muscle
|
Dantrolene
|
|
|
Agent used for acute muscle spasm
|
Cyclobenzaprine
|
|
|
Drugs Used in Parkinsonism & Other Movement Disorders
|
levodopa, benztropine, selegiline, trihexyphenidyl, amantadine, pergolide, bromocriptine, pramipexole, entacapone
|
None
|
|
What drugs can cause drug induced Parkinsonism?
|
Antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog) and is irreversible
|
None
|
|
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
|
L-dopa
|
|
|
This is combined with L-dopa, and mechanism of.
|
Carbidopa
inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias) |
None
|
|
Clinical response that may fluctuate in tx of Parkinson's dx
|
"On-off-phenomenon"
|
|
|
Anti-Parkinson's drug which increases intraocular pressure and is contraindicated in closed angle glaucoma
|
Levodopa
|
|
|
2 Ergot alkaloids that is are used for patients who are refractory or cannot tolerate levodopa, Common SE?
|
Bromocriptine or Pergolide: work at D2 agonist
Erythromelalgia: a rare disorder in which blood vessels, usually in the extremities and especially in the feet, are blocked and inflamed, causing a painful burning and throbbing sensation and red skin |
None
|
|
Non ergot dopamine receptor agonists agents used as first-line therapy in the initial management of Parkinson's
|
Pramipexole and ropinirole
|
None
|
|
Enhances dopaminergic neurotransmission. SE's include CNS excitation, acute toxic psychosis and livedo reticularis
|
Amantadine
|
None
|
|
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed pt's
|
Selegiline
|
|
|
Inhibitors of catechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
|
Entacapone and Tolcapone
|
|
|
2 Agent decreases the excitatory actions of cholinergic neurons. May improve tremor and rigidity but have LITTLE effect on what?. Atropine-like side effects
|
Benztropine or trihexyphenidyl both antimuscarinics
Little effect on bradykinesia |
None
|
|
Agent effective in physiologic and essential tremor
|
Propranolol
|
|
|
Agents used in Huntington's Disease
|
Tetrabenazine + reserpine (both amine depleting drug), Haloperidol (antipsychotic that is a dopamine receptor antag.)
|
None
|
|
Agents used in Tourette's dx and why they work
|
Haloperidol or pimozide
both block dopamine 2 receptor |
None
|
|
Chelating agent used in Wilson's disease
|
Penicillamine
|
|
|
|
|
|
|
Antipsychotics
|
older: haloperidol, chlorpromazine, fluphenazine, tribluoperazine, thioridazine
newer: clozapin, olanzapine, quetiapine, risperidone, ziprasidone |
None
|
|
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
|
Older antipsychotic agents, D2 receptors
|
|
|
Side effects occuring in antipsychotics that block dopamine
|
Hyperprolactinemia, menorrhea, galactorrhea, confusion, mood changes, decreased sexual interest, and weight gain
|
|
|
Antipsychotics that reduce positive symptoms only
|
Older antipsychotics
|
|
|
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
|
Clozapine, Risperidone, Olanzapine, aripiprazole, and sertindole
|
None
|
|
Antipsychotic used in the treatment of psychiatric symptoms in patients with dementia
|
Risperidone
|
|
|
Atypical antipsychotic causing high prolactin levels
|
Risperidone
|
|
|
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain, and adversely affect diabetes
|
Olanzapine
|
|
|
Agent more frequently associated with extrapyramidal side effects that can be treated with benzodiazepine, diphenhydramine or muscarinic blocker
|
Haloperidol
|
|
|
Drug used in neuroleptic malignant syndrome
|
Dantrolene
|
|
|
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
|
Muscarinic blockers
|
|
|
Antipsychotic having the strongest autonomic effects
|
Thioridazine
|
|
|
Antipsychotic having the weakest autonomic effects
|
Haloperidol
|
|
|
Antipsychotic that does not block muscarinic or histamine receptors, and it prolongs the QT interval
|
Sertindole
|
|
|
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
|
Thioridazine
|
|
|
Agent having no effect on D2 receptors, blocks D4, reserved for resistant schizophrenia, and can cause agranulocytosis
|
Clozapine
|
|
|
Anti-psychotic not shown to cause tardive dyskinesia
|
Clozapine
|
|
|
Anti-psychotics available in depot preparation
|
Fluphenazine and haloperidol
|
|
|
Reduced seizure threshold
|
Low-potency typical antipsychotics and clozapine
|
|
|
Orthostatic hypotension and QT prolongation
|
Low potency older agents (esp ziprasidone) and risperidone
|
None
|
|
Increased risk of developing cataracts
|
Quetiapine
|
|
|
Lithium
|
|
|
|
Major route of elimination for Lithium
|
Kidneys
|
|
|
Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
|
Lithium toxicity
|
|
|
Drug increases the renal clearance hence decreases levels of lithium
|
Theophylline
|
|
|
Lithium is associated with this congenital defect
|
Cardiac anomalies and is contraindicated in pregnancy or lactation
|
|
|
DOC for bipolar affective disorder
|
Lithium
|
|
|
SE of lithium
|
Tremor, sedation, ataxia, aphasia, thyroid enlargement, and reversible diabetes insipidus
|
|
|
Antidepressants
|
TCA: amytriptyline, doxepin, nortriptyline, imipramine, clomipramine, desipramine
SSRI: paroxetine, fluoxetine, sertraline, fluvoxemine, citolapram, Heterocyclics: 2= maprotiline, buproprion, trazadone, amoxapine 3=mirtazapine, venlafaxine, nefazadone MAO : moclobemide, isocarboxazid, phenelzine, tranylcypromine |
None
|
|
Example of three antidepressants that are indicated for obsessive compulsive disorder
|
Clomipramine, fluoxetine and fluvoxamine
|
|
|
Neurotransmitters affected by the action of antidepressants
|
Norepinephrine and serotonin
|
|
|
Usual time needed for full effect of antidepressant therapy
|
2 to 3 weeks
|
|
|
Population group especially sensitive to side effects of antidepressants
|
Elderly patients
|
|
|
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
|
Side-effect profile and prior pt response
|
|
|
Well-tolerated and are first-line antidepressants (3)
|
SSRI's, bupropion, and venlafaxine
|
None
|
|
Monoamine oxidase inhibitors (MAOI)
|
|
|
|
Most useful in patients with significant anxiety, phobic features, hypochondriasis, and resistant depression
|
Monamine oxidase inhibitors
|
|
|
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese, and pickled meats)
|
Hypertensive crisis
|
|
|
MAOI should not be administered with SSRI's or potent TCA's due to development of this condition
|
Serotonin syndrome: muscle rigidity, myoclonus, hyperthermia, cardio instability, seizures
|
None
|
|
Tricyclic antidepressants (TCA)
|
|
|
|
Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
|
Tricyclic antidepressants (TCA)
|
|
|
Three C's associated with TCA toxicity
|
Coma, Convulsions, Cardiac problems (arrhythmias and wide QRS)
|
|
|
Agents having higher sedation and antimuscarinic effects than other TCA's
|
Tertiary amines: amitriptyline and doxepin
|
None
|
|
TCA used in chronic pain, a hypnotic, and has marked antimuscarinic effects
|
Amitriptyline
|
|
|
TCA used in chronic pain, enuresis, and ADD
|
Imipramine
|
|
|
TCA with greatest sedation of this group, and marked antimuscarinic effects, used for sleep
|
Doxepin
|
|
|
TCA used in obsessive compulsive disorder (OCD), most significant of TCA's for risk of seizure, weight gain, and neuropsychiatric signs and symptoms
|
Clomipramine
|
|
|
Secondary amines that have less sedation and more excitation effect
|
Nortriptyline, Desipramine
|
|
|
Heterocyclics
|
|
|
|
Antidepressant associated with neuroleptic malignant syndrome
|
Amoxapine
|
|
|
2 Antidepressant associated with seizures and cardiotoxicity
|
Maprotiline + amoxapine
|
None
|
|
Antidepressant having stimulant effects similar to SSRI's and can increase blood pressure
|
Venlafaxine
|
|
|
Antidepressant inhibiting norepinephrine, serotonin, and dopamine reuptake
|
Venlafaxine
|
|
|
Antidepressant also used for sleep that causes priapism
|
Trazodone
|
|
|
2 Antidepressants which is inhibitor of CYP450 enzymes and may be associated with hepatic failure
|
Nefazodone + venlafaxine
|
None
|
|
Heterocyclic antidepressants least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth, aggravation of psychosis, and seizures
|
Bupropion
|
|
|
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5-HT and NE, blocks histamine receptors, and is sedating
|
Mirtazapine
|
|
|
SE of mirtazapine
|
Liver toxicity, increased serum cholesterol
sedation and WG |
None
|
|
Selective serotonin reuptake inhibitors (SSRI)
|
|
|
|
Except for these agents all SSRI have significant inhibition of CytP450 enzymes
|
Citalopram and its metabolite escitalopram
|
|
|
SSRI with long T1/2 and can be administered once weekly for maintenance, not acute tx
|
Fluoxetine
|
|
|
SSRI indicated for premenstrual dysphoric disorder
|
Fluoxetine (Sarafem)
|
|
|
Some of SSRIs' therapeutic effects beside depression (name 5 others)
|
Panic attacks, social phobias, bulimia nervosa, and PMDD premenstrual dysphoric disorder), OCD
|
None
|
|
SSRI's less likely to cause a withdrawal syndrome
|
Fluoxetine
|
|
|
Opioid Analgesics & Antagonists
|
agonists: morphine, fentanyl, heroin, methadone, meperidine, codeine, oxycodone, propoxyphene
mixed: buprenorphine, nalbuphine, pentazocine antagonists: naloxone, naltrexone, nalmefene |
None
|
|
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
|
Ascending pathways
|
|
|
Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
|
Presynaptic mu, delta, and kappa receptors
|
|
|
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
|
Postsynaptic Mu receptors
|
|
|
Tolerance to all effects of opioid agonists can develop except
|
Miosis and constipation
|
|
|
All opioids except this agent (which has a muscarinic blocking action) cause pupillary constriction
|
Meperidine
|
|
|
Name SE of opioid analgesics?
Name 10! |
dependence, withdrawal syndrome, sedation, euphoria, respiratory depression nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone, and reduction in uterine tone
|
None
|
|
Strong opioid agonists
|
Morphine, methadone, meperidine, and fentanyl
|
|
|
Opioids used in anesthesia
|
Morphine and fentanyl
|
|
|
Opioid used in the management of withdrawal states
|
Methadone
|
|
|
Opioid available trans-dermally
|
Fentanyl
|
|
|
Opioid that can be given PO, by epidural, and IV, which helps to relieve the dyspnea of pulmonary edema
|
Morphine
|
|
|
Use of this opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serotonin syndrome
|
Meperidine
|
|
|
Moderate opioid agonists
|
Codeine, hydrocodone, and oxycodone
|
|
|
Weak opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
|
Propoxyphene
|
|
|
Partial agonist or mixed antagonists
|
Partial=buprenorphine
mixed=pentazocine, nalbuphine, butorphanol |
None
|
|
Partial opioid agonist, considered a strong analgesic, has a long duration of action and is resistant to naloxone reversal
|
Buprenorphine
|
|
|
Opioid antagonist that is given IV and had short DOA
|
Naloxone
|
|
|
Opioid antagonist that is given orally in alcohol dependency programs
|
Naltrexone
|
|
|
These agents are used as antitussive
|
Dextromethorphan, Codeine
|
|
|
These agents are used as antidiarrheal
|
Diphenoxylate, Loperamide: Loperamide is an opioid receptor agonist and acts on the μ-opioid receptors in the myenteric plexus large intestines; it does not affect the central nervous system like other opioids.
|
None
|
|
Drugs of Abuse
|
|
|
|
Inhalant anesthetics
|
NO, chloroform, and diethyl ether
|
|
|
Toxic to the liver, kidney, lungs, bone marrow, peripheral nerves, and cause brain damage in animals, sudden death has occurred following inhalation
|
Fluorocarbons and Industrial solvents
found in gasoline, paint thinner, glues, cements |
None
|
|
Cause dizziness, tachycardia, hypotension, and flushing
|
Organic nitrites such as amyl nitrite, isobutyl nitrite "poppers"
|
None
|
|
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
|
Steroids
|
|
|
Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
|
Changes in heart rate, blood pressure, respiration, body temperature, sweating, bowel signs, and pupillary responses
|
|
|
Opioid Analgesics
|
|
|
|
5 Most commonly abused in health care professionals
|
Heroin, morphine, oxycodone, meperidine and fentanyl
|
None
|
|
This route is associated with rapid tolerance and psychologic dependence
|
IV administration
|
|
|
Leads to respiratory depression progressing to coma and death
|
Overdose of opioids
|
|
|
Describe abstinence syndrome of the opoids
|
Lacrimation, rhinorrhea, yawning, sweating, weakness, gooseflesh, nausea, and vomiting, tremor, muscle jerks, and hyperpnea are signs of this syndrome
|
None
|
|
Treatment for opioid addiction
|
Methadone, followed by slow dose reduction
|
|
|
This agent may cause more severe, rapid and intense symptoms to a recovering addict
|
Naloxone
|
|
|
Sedative-Hypnotics
|
|
|
|
Sedative-Hypnotics action
|
Reduce inhibition, suppress anxiety, and produce relaxation
|
|
|
Additive effects when Sedative-Hypnotics used in combination with these agents
|
CNS depressants
|
|
|
Common mechanism by which overdose result in death
|
Depression of medullary and cardiovascular centers
|
|
|
"Date rape drug" (3)
|
Flunitrazepam (rohypnol): a potent rapid onset benzo with marked amnestic properties
also chloral hydrate or gamma hydroxybutyrate |
None
|
|
The most important sign of withdrawal syndrome
|
Excessive CNS stimulation (seizures)
|
|
|
Treatment of withdrawal syndrome involves
|
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
|
|
|
These agents are CNS depressants
|
Ethanol, Barbiturates, and Benzodiazepines
|
|
|
Stimulants
|
|
|
|
Withdrawal from this drug causes lethargy, irritability, and headache
|
Caffeine
|
|
|
W/D from this drug causes anxiety and mental discomfort
|
Nicotine
|
|
|
Treatments available for nicotine addiction
|
Patches, gum, nasal spray, psychotherapy, and bupropion
|
|
|
Chronic high dose abuse of nicotine leads to
|
Psychotic state, overdose causes agitation, restlessness, tachycardia, hyperthermia, hyperreflexia, and seizures
|
|
|
Tolerance is marked and abstinence syndrome occurs
|
Amphetamines
|
|
|
Amphetamine agents
|
Dextroamphetamines and methamphetamine
effects by binding to the monoamine transporters and increasing extracellular levels of the biogenic amines dopamine, norepinephrine and serotonin. It is hypothesized that d-amphetamine acts primarily on the dopaminergic systems, while l-amphetamine is comparatively norepinephrinergic. The primary reinforcing and behavioral-stimulant effects of amphetamine, however, are linked to enhanced dopaminergic activity, primarily in the mesolimbic DA system. Amphetamine binds to the dopamine transporter (DAT) and blocks the transporters ability to clear DA from the synaptic space. In addition, amphetamine is transported into the cell which leads to dopamine efflux (DA is transported out of the cell and into the synaptic space via reverse transport of the DAT |
None
|
|
These agents are congeners of Amphetamine
|
DOM, STP, MDA, and MDMA "ecstasy"
Serotonin is a neurotransmitter believed to play a role in the regulation of mood and pleasure. MDMA causes serotonin vesicles in the neurons to release quantities of serotonin into the synapses. Although popular press accounts focus on the role of serotonin release, the mechanism by which MDMA causes its unusual psychoactivity is largely unknown. In vitro and nonhuman animal studies have established that MDMA also induces dopamine, norepinephrine, and acetylcholine release, and can act directly on a number of receptors, including a2-adrenergic (adrenaline) and 5HT2A(serotonin) receptors. MDMA promotes the release of several hormones including prolactin and the antidiuretic hormone vasopressin, which may be important in its occasional production of water intoxication or hyponatremia |
None
|
|
Overdoses of this agent with powerful vasoconstrictive action may result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
|
Cocaine "super-speed"
|
|
|
Hallucinogens
|
|
|
|
Most dangerous of the currently popular hallucinogenic drugs, OD leads to nystagmus, marked hypertension, and seizures, presence of this which is pathognomonic
|
PCP: phencyclidine or angel dust.
both horizontal and vertical nystagmus is pathognomonic NMDA antagonist |
None
|
|
Removal of PCP may be aided
|
Urinary acidification and activated charcoal or continual nasogastric suction
|
|
|
THC is active ingredient, SE's include impairment of judgment, and reflexes, decreases in blood pressure and psychomotor performance occur
|
Marijuana
|
|
|
Cholinoreceptor-Activating & Cholinesterase-Inhibiting Drugs
|
Activating: Acetylcholine, carbachol, bethanechol, pilocarpine
Indirect: Neostigmine, pyridostigmine, physostigmine, edrophonium, echothiophate, parathion and malathion |
None
|
|
Direct-Acting Cholinomimetic Agonists
|
|
|
|
Muscarinic agonists or parasympathomimetic
|
|
|
|
This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
|
Bethanechol
|
|
|
Only direct acting agent that is very lipid soluble and used in glaucoma
|
Pilocarpine also carbachol
|
None
|
|
These agents are used to treat dry mouth in Sjögren's syndrome
|
Cevimeline + pilocarpine
|
None
|
|
Indirect-Acting ACh Agonist, alcohol, short DOA and used in diagnosis of myasthenia gravis
|
Edrophonium
|
|
|
Carbamate with intermediate action postoperative and used for neurogenic ileus and urinary retention
|
Neostigmine
|
None
|
|
Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
|
Physostigmine
|
|
|
Treatment of myasthenia gravis
|
Pyridostigmine
|
|
|
2 drugs used in the treatment of Alzheimers
|
Donepezil, tacrine
|
|
|
Organophosphates
|
|
|
|
Antiglaucoma organophosphate
|
Echothiophate
|
|
|
Associated with an increased incidence of cataracts in patients treated for glaucoma
|
Long acting cholinesterase inhibitors
|
|
|
Scabicide organophosphate
|
Malathion
|
|
|
Organophosphate anthelmintic agent with long DOA
|
Metrifonate
|
|
|
Toxicity of organophosphate:
|
DUMBELSS (diarrhea, urination, miosis, bronchoconstriction, excitation of skeletal muscle and CNS, lacrimation, salivation, and sweating)
|
|
|
The most important cause of acute deaths in cholinesterase inhibitor toxicity
|
Respiratory failure
|
|
|
The most toxic organophosphate
|
Parathion
|
|
|
Treatment of choice for organophosphate overdose
|
Atropine and/or pralidoxime
|
None
|
|
This agent regenerates active cholinesterase and is a chemical antagonist used to treat organophosphate exposure
|
Pralidoxime
|
|
|
Cholinoreceptor Blockers & Cholinesterase Regenerators
|
blockers: atropine, scopolamine, glycopyrrolate, ipratropium, tropicamide, oxybutynin, benztropine
Regenerator: Pralidoxime |
None
|
|
Prototypical Nonselective Muscarinic Antagonists
|
Atropine
|
None
|
|
Treat manifestations of Parkinson's disease and EPS
|
Benztropine, trihexyphenidyl
|
|
|
Treatment of motion sickness, may cause short term memory block
|
Scopolamine
|
|
|
Antispasmodic, antisecretory, antiulcer, does not enter the CNS
|
Glycopyrrolate
|
|
|
Treatment of Antimuscarinic toxicity
|
Symptomatic + physostigmine(blocks acetylcholinesterase)
|
|
|
Name 6 other classes of drugs that have antimuscarinic effects as a SE
|
Antihistamine, Tricylic Antidepressants, Antipsychotics, Quinidine, Amantadine, Meperidine
|
|
|
Produce mydriasis and cycloplegia (4)
|
Atropine, homatropine, tropicamide, cyclopentolate
|
None
|
|
Bronchodilation in asthma and COPD
|
Ipratropium
|
|
|
Reduce transient hyper GI motility (3)
|
Dicyclomine, methscopolamine, glycopyrrolate
|
None
|
|
Cystitis, postoperative bladder spasms, or incontinence (4)
|
Oxybutynin, dicyclomine, glycopyrrolate, tolterodine
|
None
|
|
Toxicity of anticholinergics
|
block SLUD (salivation, lacrimation, urination, defecation
dry as a bone, red as a beet, mad as a hatter |
None
|
|
Another pneumonic for anticholinergic toxicity
|
"dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat"
|
|
|
Atropine fever is the most dangerous effect and can be lethal in this population group
|
Infants
|
|
|
Contraindications to use of atropine
|
Infants, closed angle glaucoma, prostatic hypertrophy
|
|
|
Nicotinic Antagonists
|
|
|
|
Prototype ganglion blocker
|
Hexamethonium and Mecamylamine
|
|
|
Limiting adverse effect of ganglion blockade that patients usually are unable to tolerate
|
Combined block of sympathetics and parasympathetics ex. postureal hypotension, dry mouth, blurred vision, constipation, sexual dysfunction
|
None
|
|
Main use for ganglionic blocker
|
Block ANS reflexes, allowing to see if change HR direct or autonomic
|
|
|
Will reverse the blockade by neuromuscular blockers
|
Cholinesterase inhibitors
|
None
|
|
Tubocurarine is the prototype, pancuronium, atracurium, vecuronium are newer short acting agent, produce competitive block at end plate nicotinic receptor, causing flaccid paralysis
|
Nondepolarizing Neuromuscular Blockers
|
|
|
Only member of depolarizing neuromuscular blocker, causes fasciculation during induction and muscle pain after use
|
Succinylcholine
|
|
|
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
|
Cholinesterase Regenerators
|
|
|
Used to treat patients exposed to insecticides such as parathion
|
Pralidoxime
|
|
|
Sympathomimetics
|
1. epinephrine: general agonist
2. norepe: a1,a2,b1 3. phenylephrine, methoxamine, a1>a2 4. clonidine: a2>a1 5. isoproterenol: b1=b2 6. dobutamine b1>b2 7. terbutaline, albuterol: b2>b1 8. dopamine and bromocriptine: dop agonist |
None
|
|
Which beta receptor does heart and which does lungs
|
You have 1 heart (Beta 1) and 2 lungs (Beta 2)
|
None
|
|
|
|
|
|
Location of alpha 1 receptors (name at least 5)
|
Eye(myd), arterioles +veins = constrict, inhibits bladder, male sex organs, kidney(dec. renin), prostate(contract)
|
None
|
|
Location of alpha 2 receptors (name at least 3)
|
Prejunctional nerve terminals, aggregates platelets, pancreas(dec. insulin), fat cells to inhibit lipolysis
|
None
|
|
Location B1 receptors
|
nodes, heart muscle, kidney(inc. renin)
|
|
|
As increase dose of dopamine from low to high name receptor changes occuring
|
Low=D1, mid=also B1, high also a1
|
|
|
MAO of the liver
|
A
|
|
|
MAO of the brain
|
B
|
|
|
Locatoin B2 receptors (name at least 5)
|
all BV(dil), uterus, bronchioles, skeletal muscle get tremor, liver glycogenolysis, pancreas(inc. insulin)
|
None
|
|
This is the drug of choice for anaphylactic shock
|
Epinephrine
|
|
|
Differ high dose epinephrine with norepinephrine
|
Alpha 1 blocker. See hypotension with epi.
|
|
|
Phenylisopropylamines that are used legitimately and abused for narcolepsy, attention deficit disorder, and weight reduction
|
Amphetamines
|
|
|
At low dose epi is alpha or beta effect more prominent? High dose?
|
Low dose beta more responsive as more senstitive. High dose alpha due to being more numerous.
|
|
|
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
|
Phenylephrine
|
|
|
Epinephrine and dipivefrin are used for and MOA
|
Glaucoma: increase outflow via the uveoscleral veins
|
None
|
|
Newer alpha 2 agonist mechanism to treat glaucoma and name the two drugs
|
Reduce aqueous synthesis
(apraclonidine and brimonidine) |
None
|
|
Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis, name two others that would work
|
Albuterol
two others: terbutaline, metaproterenol |
None
|
|
Longer acting Beta 2 agonists is recommended for prophylaxis of asthma
|
Salmeterol
|
|
|
These agents increase blood flow and may be beneficial in treatment of acute heart failure and some types of shock
|
Beta1 agonists
|
|
|
These agents decrease blood flow or increase blood pressure, are local decongestant, and used in therapy of spinal shock (temporary maintenance of blood pressure which may help maintain perfusion
|
Alpha1 agonists
|
|
|
Shock due to septicemia or myocardial infarction is made worse by
|
Vasoconstrictors because Increasing afterload and tissue perfusion declines
|
None
|
|
Often mixed with local anesthetic to
|
Reduce the loss from area of injection
|
|
|
Chronic orthostatic hypotension can be treated with
|
Midodrine a new oral a1 agonist or ephedrine
|
None
|
|
2 Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
|
Terbutaline or ritodrine (relax smooth muscle)
|
None
|
|
Long acting sympathomimetic, sometimes used to improve urinary continence in children and elderly with enuresis
|
Ephedrine
|
|
|
Alpha 1 agonist toxicity
|
Hypertension
|
|
|
Beta 1 agonist toxicity
|
Sinus tachycardia and serious arrhythmias
|
|
|
Beta 2 agonist toxicity
|
Skeletal muscle tremor
|
|
|
The selective agents loose their selectivity at
|
high doses
|
|
|
Adrenoceptor Blocker
|
1. nonselective alpha blocker: phentolamine and pehnoxybenzamine
2. alpha 1 selective: prazosin, terazosin, doxazosin 3. alpha 2 selective: yohimbine 4. nonselective beta blocker: propranolol, carvedilol, labetalol, nadolol, timolol 5. beta 1 selective: metoprolol, atenolol, esmolol |
None
|
|
Nonselective alpha-blocking drug, long acting and irreversible, and used to treat pheochromocytoma. Blocks 5-HT, so occasionaly used for carcinoid tumor. Blocks H1 and used in mastocytosis
|
Phenoxybenzamine
|
|
|
Nonselective alpha-blocking drug, short acting and reversible, used for rebound HTN from rapid clonidine withdrawal, and Raynaud's phenomena
|
Phentolamine
|
|
|
Selective Alpha 1 blocker used for hypertension, BPH, may cause first dose orthostatic hypotension
|
Prazosin, terazosin, doxazosin
|
|
|
Selective Alpha 2 blocker used for impotence (controversial effectiveness)
|
Yohimbine
|
|
|
Beta-Blocking Drugs
|
|
|
|
SelectiveB1 Receptor blockers that may be useful in treating patients that you have to worry about asthma in
|
Acebutolol, atenolol, esmolol, metoprolol
|
None
|
|
Combined alpha and beta blocking agents that may have application in treatment of CHF
|
Labetalol and carvedilol
|
|
|
Beta blockers partial agonist activity (intrinsic sympathomimetic activity) cause some bronchodilation and may have an advantage in treating patients with asthma
|
Pindolol and acebutolol
|
|
|
This beta blocker lacks local anesthetic activity (decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
|
Timolol: decreases aqueous secretion
|
None
|
|
This parenteral beta blocker is a short acting
|
Esmolol
|
|
|
This beta blocker is the longest acting
|
Nadolol
|
|
|
These beta blockers are less lipid soluble
|
Acebutolol and atenolol and nadolol
|
None
|
|
This beta blocker is highly lipid soluble and may account for side effects such as nightmares
|
Propranolol
|
|
|
Clinical uses of these agents include treatment of HTN, angina, arrhythmias, and chronic CHF
|
Beta blockers
|
|
|
Why is B1 selective blockers CI with diabetes
|
Block the symp reflexes (tachycardia, tremor and anxiety) seen with hypoglycemia
|
None
|
|
Contraindications to beta blockers
|
Asthma, vasospastic disorders, diabetes
|
|
|
B blockers ok to give to hyperlipidemia patients
|
Acebutolol, Pindolol
|
|
|
Toxicity of these agents include bradycardia, AV blockade, exacerbation of acute CHF, signs of hypoglycemia may be masked (tachycardia, tremor, and anxiety)
|
Beta blockers
|
|
|
Glaucoma (all agents topical except for diuretics)
|
|
|
|
Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction
|
Pilocarpine, carbachol, physostigmine
|
|
|
Nonselective alpha agonists that increases outflow, probably via the uveoscleral veins
|
Epinephrine, dipivefrin
|
|
|
Selective alpha agonists that decreases aqueous secretion
|
Apraclonidine, brimonidine: both alpha 2 selective agents
|
None
|
|
These Beta blockers decrease aqueous secretion
|
Timolol (nonselective), betaxolol (beta 1 selective)
|
None
|
|
Pt. with dilated pupil. Symp agonist or parasympathetic antagonist?
|
Ask about blurred vision
|
|
|
Treatments for angle closure glaucoma
|
Pilocarpine or Mannitol
|
|
|
This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urine may precipitate calcium salts, hypokalemia, acidosis. Only oral treatment.
|
Acetazolamide
|
|
|
This agent cause increased aqueous outflow
|
Prostaglandin PGF2a (Latanoprost)
|
|
|
Antihypertensive Agents
|
|
|
|
Inhibit angiotensin-converting enzyme (ACE)
|
Ace inhibitors
|
|
|
Captopril and enalapril (-OPRIL ending) are
|
Ace inhibitors
|
|
|
SE of ACE inhibitors (2)
|
Dry cough, hyperkalemia (due to dec. aldosterone)
|
None
|
|
Ace inhibitors are contraindicated in
|
pregnancy (renal toxicity to baby) and with K+
|
None
|
|
Name two drugs that block the angiontensin receptor
|
Losartan and valsartan
|
None
|
|
Angiotensin receptor blockers do NOT cause
|
Dry cough
|
|
|
Block L-type calcium channel
|
Calcium channel blockers
|
|
|
CCB contraindicated in CHF
|
Verapamil
|
|
|
CCB with predominate effect on arteriole dilation
|
Nifedipine
|
|
|
SE of CCB (3)
|
Constipation, edema, and headache
|
None
|
|
Reduce heart rate, contractility, and O2 demand
|
Beta-blockers
|
|
|
B-blockers that are more cardioselective
|
Beta 1-selective blockers
|
None
|
|
Cardioselective Beta 1-blockers
|
Atenolol, acebutolol, and metoprolol, esmolol
|
None
|
|
Beta-blockers should be used cautiously in (3)
|
Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease
|
None
|
|
Non-selective Beta-blocker also used for migraine prophylaxis
|
Propranolol
|
|
|
SE of beta blockers (3-4)
|
Bradycardia, SEXUAL DYSFUNCTION, decrease in HDL, and increase in Triglycerols (TG)
|
None
|
|
Alpha 1selective blockers
|
Prazosin, terazosin and doxazosin (-AZOSIN ending)
|
|
|
Non-selective Alpha1blockers use to treat pheochromocytoma
|
Phenoxybenzamine
|
|
|
For rebound HTN from rapid clonidine withdrawal
|
Phentolamine: nonselective alpha blocker
|
None
|
|
A1a-selective blocker used for BPH
|
Tamsulosin (Flomax)
|
|
|
SE of alpha blockers
|
Orthostatic hypotension (especially with first dose) and reflex tachycardia
|
|
|
Presynaptic Alpha 2 agonist used in HTN
|
Clonidine, and methyldopa
|
|
|
SE of methyldopa
|
Positive Comb's test, depression
|
|
|
Methyldopa is contraindicated in
|
Geriatrics due to its CNS (depression) effects
|
|
|
SE of clonidine
|
Rebound HTN, sedation, dry mouth
|
|
|
Ganglionic blockers formerly used in HTN
|
Trimethaphan, and hexamethonium
|
|
|
Direct vasodilator of arteriolar smooth muscle
|
Hydralazine: release of nitric oxide from endothelial cells
|
None
|
|
SE of hydralazine
|
Lupus-like syndrome
|
|
|
Arterial vasodilator that works by opening K+ channels
|
Minoxidil
|
|
|
SE of minoxidil
|
Hypertrichosis
|
|
|
IV Drug used Hypertensive Crisis
|
Nitroprusside
|
|
|
Nitroprusside vasodilates
|
Arteries and veins
|
|
|
Toxicity caused by nitroprusside and treatment
|
Cyanide toxicity treated with sodium thiosulfate
|
|
|
Diuretics
|
|
|
|
Carbonic anhydrase inhibitor
|
Acetazolamide
|
|
|
Diuretic used for mountain sickness and glaucoma
|
Acetazolamide
|
|
|
SE of acetazolamide
|
Paresthesias, alkalization of the urine (which may ppt. Ca salts: alkalinization = precipitation), hypokalemia (due to inc. sodium in tubules), acidosis (cannot exchange sodium and Hydrogen), and encephalopathy in patients with hepatic impairment (may have inc. ammonia reabsorption)
|
None
|
|
MOA of loop diuretics
|
inhibits Na+/K+/2Cl- cotransport
|
|
|
Site of action of loop diuretics
|
Thick ascending limb
|
|
|
SE of loop (furosemide) diuretics
|
Hyperuricemia, hypokalemia and ototoxicity, hypomagnesemia (may enhance digoxin), hypocalcemia, alkalosis, sulfur allergy
|
None
|
|
Aminoglycosides used with loop diuretics potentiate adverse effect
|
Ototoxicity
|
|
|
Loops lose and thiazide diuretics retain
|
Calcium: lower intracellular sodium increased Basolateral sodium/calcium transporter
|
None
|
|
MOA of thiazide diuretics
|
Inhibit Na+/Cl- cotransport
|
|
|
Site of action of thiazide diuretics
|
Work at early distal convoluted tubule
|
|
|
Class of drugs that may cause cross-sensitivity with thiazide diuretics
|
Sulfonamides: carbonic anhydrase inhibitors, loops except EA, sulfa ab, celexocib
|
None
|
|
SE of thiazide (HCTZ) diuretics
|
Hyperuricemia, hypokalemia and hyperglycemia (high calcium opens K+ channels), sulfur allergy, alkalosis, hyperlipidemia (due to less insulin),
|
None
|
|
Potassium sparing diuretics inhibit
|
Na+/K+ exchange
|
|
|
Diuretic used to treat primary aldosteronism
|
Spironolactone
|
|
|
SE of spironolactone
|
Gynecomastia (also block steroid receptors), hyperkalemia, and impotence
|
None
|
|
Osmotic diuretic used for increased intracranial pressure
|
Mannitol
|
|
|
Antidiuretic hormone (ADH) agonist and antagonist
|
|
|
|
ADH agonist used for pituitary diabetes insipidus
|
Desmopressin (DDAVP)
|
|
|
Used for SIADH
|
Demeclocycline (antagonist of ADH at V2 receptor)
|
None
|
|
SE of demeclocycline
|
Bone marrow and teeth discoloration (chelate with cations) for children under 8 years of age
|
None
|
|
Antiarrhythmic agents
|
|
|
|
MOA of class I A, class IB, and class IC antiarrhythmics
+ prototype of each class |
Ia: blocks fast Na channels in open state and K+ channels-quinidine + procainamide
Ib: block fast Na channels that are inactivated- lidocaine Ic: block fast Na channels esp. Purkinje-Flecainide and Encainide |
None
|
|
SE of procainamide
|
Lupus-like syndrome (slow acetylator)
|
|
|
Limiting side effect of Quinidine
|
Prolongs QT interval (Torsad)
|
|
|
Other side effects of Quinidine
|
Thrombocytopenic purpura, and CINCHONISM (autonomic side effects from M2 and alpha block)
|
None
|
|
Major drug interaction with Quinidine
|
Increases concentration of Digoxin (will displace digoxin from tissue binding sites)
|
None
|
|
MOA of class 1a
|
blocks activated Na channels and also blocks K channels
|
|
|
Treating Pt. for A fib with quinidine, what needs to be done first
|
Initial digitalization to slow AV conduction becuase due to M2 block quinidine inc. heart rate and AV conduction
|
None
|
|
Proarrythmic effects of quinidine
|
M block, alpha block
|
|
|
Class 1a effect on AP and ERP
|
Increase both
|
|
|
DOC for management of acute Ventricular arrhythmias
|
Lidocaine, least cardiotoxic of all
|
|
|
MOA class 1B drugs
|
Block inactivated Na channels, preferring hypoxic tissue (minor affect on normal)
|
|
|
Affect of 1B on APD
|
decrease, bringing ischemic tissue back to speed
|
|
|
IB drugs given orally
|
Mexiletine and Tocainide
|
|
|
DOC for digoxin induced arrhythmias
|
Phenytoin: sometimes classified as a class IB antiarrhythmic agent
|
None
|
|
SE of phenytoin
|
Gingival hyperplasia
|
|
|
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents
|
Class IC (flecainide, encainide, propafenone, moricizine)
|
|
|
Class II antiarrhythmics are
|
B-blockers
|
|
|
Antiarrhythmic that exhibits Class II and III properties
|
Sotalol: has two enantiomers one for beta and one for potassium channels
|
None
|
|
Side effect of sotalol
|
prolongs QT and PR interval
|
|
|
Used intravenously for acute arrhythmias during surgery
|
Esmolol: by dec. cAMP decreases sodium and calcium currents and AV node particularly sensitive
|
None
|
|
Anti-arrhythmics that decrease mortality
|
B-blockers
|
|
|
MOA of class III antiarrhythmics
|
Potassium channel blockers, slow phase 3
|
|
|
Class III antiarrhythmic that exhibits properties of all 4 classes
|
Amiodarone
|
|
|
Specific pharmacokinetic characteristic of amiodarone
|
Prolonged half-life, up to six weeks (iodine slowly metabolized, may become antigenic)
|
|
|
Antiarrhythmic effective in most types of arrhythmia
|
Amiodarone
|
|
|
SE of Amiodarone
|
Dysfunction, photosensitivity, skin (blue smurf syndrome) because iodine reacts withs starches, Pulmonary fibrosis, thyroid and corneal deposits
|
None
|
|
MOA of class IV antiarrhythmics
|
Calcium channel blockers, dec. activity nodes, dec. slope phase 4
|
|
|
SE of class IV agents
|
Constipation, dizziness, AV block, CI with Beta blocker or digoxin and hypotension
|
None
|
|
Class IV drugs used
|
Verapamil, Diltiazem
|
|
|
Life threatening cardiac event that prolong QT leads to
|
Torsades de pointes
|
|
|
Agent to treat torsades de pointes
|
Magnesium sulfate
|
|
|
Drug used supraventricular arrhythmias
|
Digoxin: due to parasympathomimetic effect
|
None
|
|
DOC for paroxysmal supraventricular tachycardia (PSVT) + AV nodal arrythmias
|
Adenosine: activates A receptors = Gi coupled dec. in cAMP = inc. K + efflux = membrane hyperpolarization
|
None
|
|
Adenosine's MOA
|
Activates acetylcholine sensitive K+ channels in SA and AV node causing hyperpolarization
|
|
|
Anti-arrhythmic with 15 second duration of action
|
Adenosine
|
|
|
Vasodilators and treatment of angina
|
|
|
|
MOA of sildenafil (Viagra)
|
Inhibits phosphodiesterase-5, enhancing effects of nitric oxide-activated increases in cGMP because it prvents PD5 from converting cGMP to GMP
|
None
|
|
|
|
|
|
Drugs used in the management of angina
|
Aspirin, Nitrates, CCB, and Beta blockers
|
|
|
Aspirin reduces mortality in unstable angina by
|
Platelet aggregation inhibition
|
|
|
MOA of nitrates
|
Relax vascular smooth muscle by activating guanylyl cyclase to from cGMP = promotes the dephosphorylation of myosin light chani phosphate preventing interaction with actin.
at low doses dilate veins and at high doses dilate arterioles |
None
|
|
Nitrate used for acute anginal attacks
|
Nitroglycerin sublingual tablets
|
|
|
Nitrate used to prevent further attacks
|
Oral and transdermal forms of nitroglycerin
|
|
|
Nitrate free intervals are needed due to
|
Tolerance: cysteine gets used up
|
None
|
|
SE of nitrates
|
Postural hypotension, reflex tachycardia, hot flashes, and throbbing headache due to meningeal artery dilation
|
|
|
CCB are DOC for
|
Prinzmetal's angina
|
|
|
Beta blockers are used for which type of anginal attack
|
Classic
|
|
|
Drugs used to treat CHF
|
|
|
|
MOA of Cardiac glycosides (eg. digoxin)
|
Indirectly increase intracellular calcium and cardiac contractility by inhibit Na+/K+ ATPase, this keeps higher Na in the cell so Ca/Na pump will not work
|
None
|
|
|
|
|
|
Digoxin is used in
|
Atrial fibrillation and CHF
|
|
|
Digoxin toxicity can be precipitated by
|
Hypokalemia: Potassium complets with digoxin for binding spots
also hypomagnesemia, hypercalcemia, quinidine, NSAID, amiodarone, verapamil, sympathomimetics, erthromycin |
None
|
|
Antidote for digoxin toxicity
|
Digibind: antibody to digoxin
|
None
|
|
Phosphodiesterase inhibitors that increase mortality and have been found to have NO beneficial effects
|
Amrinone and milrinone
|
|
|
SE of amrinone
|
Thrombocytopenia
|
|
|
Beta 1 agonists used in acute CHF
|
Dobutamine and dopamine: inc. cAMP = protein kinase A activatoin of Calcium channel
|
None
|
|
Diuretics work in CHF by
|
Reducing preload
|
|
|
Beta blockers work in CHF by
|
Reducing progression of heart failure (never use in acute heart failure)
|
|
|
Agent used in CHF that is a selective alpha and nonselective beta blocker
|
Carvedilol
|
|
|
Agent used in acutely decompensated CHF resembling natriuretic peptide
|
Nesiritide (Natrecor): recombinant BNP. has guanylate cyclase activity, inc. cGMP, relaxes SM of arterioles and veins. Also causes diuresis.
|
None
|
|
Drugs used in coagulation disorders
|
|
|
|
Vitamin K dependent anticoagulant
|
Warfarin (PT)
|
|
|
Warfarin is contraindicated in
|
Pregnancy
|
|
|
Anticoagulant of choice in pregnancy
|
Heparin
|
|
|
Heparin (PTT) increases activity of
|
Antithrombin 3
|
|
|
Route of administration of warfarin
|
Oral
|
|
|
Routes of administration of heparin
|
IM (only LMW) and IV
|
|
|
SE of both warfarin and heparin
|
Bleeding
|
|
|
SE of heparin
|
Heparin induced thrombocytopenia (HIT): some people produce an Ab that binds to complex heparin + platelet factor 4
|
None
|
|
Alternative anticoagulant used if HIT develops
|
Lepirudin and argatroban: binds to the active sites of thrombin and sthrombin substrates.
|
None
|
|
Antidote to reverse actions of warfarin
|
Vitamin K or fresh frozen plasma
|
|
|
Antidote to reverse actions of heparin
|
Protamine sulfate: is a basic compound so binds to acidic heparine (high arginines)
|
None
|
|
MOA of aspirin
|
Irreversibly blocking cyclooxygenase
|
|
|
Agent used to treat MI and to reduce incidence of subsequent MI
|
Aspirin
|
|
|
SE of Aspirin
|
GI bleeding
|
|
|
Antiplatelet drug reserved for patients allergic to aspirin
|
Ticlopidine + Clopdogrel: irreversible inhibition of ADP receptor and ADP mediated platelet aggregation
|
None
|
|
SE for ticlopidine
|
Neutropenia and agranulocytosis
|
|
|
Effective in preventing TIA's
|
aspirin, Clopidogrel and ticlopidine
|
None
|
|
Prevents thrombosis in patients with artificial heart valve
|
Dipyridamole
|
|
|
Block glycoprotein IIb/IIIa involved in platelet cross-linking
|
Abciximab, tirofiban and eptifibatide
|
|
|
MOA of thrombolytics
|
Degradation of fibrin clots (takes plasminogen to plasmin) and are administered
|
None
|
|
Thrombolytics are used for
|
Pulmonary embolism and DVT
|
|
|
Thrombolytic that can cause allergic reaction
|
Streptokinase: Pt. with previous streptokinase infection may have made antibodies
|
None
|
|
Thrombolytic used for acute MI and ischemic (non hemorrhagic) CVA
|
Tissue plasmin activator
|
|
|
SE of tPA
|
Cerebral hemorrhage
|
|
|
Antidote for thrombolytics
|
Aminocaproic acid: inhibit plasminogen activation
|
None
|
|
Agents used in anemias and hematopoietic growth factors
|
|
|
|
Agent to treat hypochromic microcytic anemias
|
Ferrous sulfate
|
|
|
Chelating agent used in acute iron toxicity
|
Deferoxamine
|
|
|
Agent for pernicious anemia
|
Cyanocobalamin (Vit B12)
|
|
|
Agent used for neurological deficits in megaloblastic anemia
|
Vitamin B12
|
|
|
Agent used for megaloblastic anemia (but does NOT reverse neurologic symptoms) and decrease neural tube defects during pregnancy
|
Folic acid
|
|
|
Agent used for anemias associated with renal failure
|
Erythropoietin
|
|
|
Agent used neutropenia especially after chemotherapy
|
G-CSF (filgrastim) and GM-CSF (sargramostim)
|
|
|
Treatment of patients with prior episodes of thrombocytopenia after a cycle of cancer chemotherapy
|
Interleukin 11 (oprelvekin)
Interleukin eleven (IL-11) is a thrombopoietic growth factor that directly stimulates the proliferation of hematopoietic stem cells and megakaryocyte progenitor cells and induces megakaryocyte maturation resulting in increased platelet production |
None
|
|
Antihyperlipidemics
|
|
|
|
Decrease intestinal absorption of cholesterol
|
Bile acid-binding resins:cholestyramine, colestipol, colesevelam
Ezetimibe |
None
|
|
Cholestyramine and colestipol are
|
Bile acid-binding resins
|
|
|
Major nutritional side effect of bile acid-binding resins
|
Impair absorption of fat soluble vitamin absorption (A,D,E,K)
|
|
|
Mechanism of statins
|
inhibits HMG COA reductase
|
None
|
|
Name the important statins
|
Prodrugs: lovastatin and simvastatin
others: atorvastatin, pravastatin, fluvastatin |
None
|
|
HMG CoA reductase inhibitors are contraindicated in
|
Pregnancy
|
|
|
Drug or foods (grapefruit juice) that increase statin effect mechanism of
|
Inhibit Cytochrome P450 3A4
|
None
|
|
SE of HMG COA reductase inhibitors
|
Rhabdomyolysis and Hepatotoxicity
|
|
|
Monitoring parameter to obtain before initiation of STATINS
|
LFT's
|
|
|
Decreases liver triglycerol synthesis
|
Niacin
|
|
|
SE of niacin
|
Cutaneous flush: can pretreat with NSAID
|
None
|
|
Name the fibrates
|
Gemfibrozil, Fenofibrate, Clofibrate
|
None
|
|
Fibrates (gemfibrozil) increase activity of
|
Lipoprotein lipase by activating PPAR
|
None
|
|
Most common SE of fibrates
|
Nausea
|
|
|
Fibrates are contraindicated in
|
Pregnancy
|
|
|
Concurrent use of fibrates and statins increases risk of
|
Rhabdomyolysis
|
|
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with the Statins
|
Ezetimibe (Zetia)
|
|
|
NSAIDS and DMARDS
|
|
|
|
MOA of NSAIDS
|
inhibit prostaglandin synthesis by inhibiting cyclo-oxygenase (cox)
|
|
|
Difference between aspirin and other NSAIDS
|
Aspirin irreversibly inhibits cyclooxygenase
|
|
|
Four main actions of NSAIDS
|
Anti-inflammatory, analgesia, antipyretic and antiplatelet activity
|
|
|
Agent used for closure of patent ductus arteriosus
|
Indomethacin
|
|
|
Aspirin is contraindicated in children with viral infection
|
Potential for development of Reye's syndrome
|
|
|
SE of salicylates
|
Tinnitus, GI bleeding
|
|
|
NSAID also available as an ophthalmic preparation
|
Diclofenac
|
|
|
NSAID available orally, IM and ophthalmically
|
Ketoralac: used mainly for analgesia not for anti-inflammatory
|
None
|
|
NSAID that is used for acute condition, such as pre-op anesthesia and has limited duration (<5 days) of use due to nephrotoxicity
|
Ketoralac
|
|
|
Newer NSAIDs that selectively inhibit COX-2
|
Celecoxib and rofecoxib
|
|
|
COX 2 inhibitors may have reduced risk of
|
Gastric ulcers and GI Bleeding
|
|
|
COX 2 inhibitors should be used cautiously in pts with
|
Pre-existing cardiac or renal disease
|
|
|
Acetaminophen only has
|
Antipyretic and analgesic activity
|
|
|
SE of acetaminophen
|
Hepatotoxicity
|
|
|
Antidote for acetaminophen toxicity
|
N-acetylcysteine: Acetylcysteine is the N-acetyl derivative of the amino acid L-cysteine, and is a precursor in the formation of the antioxidant glutathione in the body. The thiol (sulfhydryl) group confers antioxidant effects and is able to reduce free radicals.
|
None
|
|
Drugs-Modifying Anti-Rheumatic Agents (DMARDS)
|
|
|
|
DMARDs are slow acting drugs for
|
Rheumatic disease
|
|
|
MOA of gold salts
|
Alter activity of macrophages and suppress phagocytic activity of PMNs
|
|
|
SE of gold salts
|
Dermatitis of the mouth aplastic anemia and agranulocytosis
|
|
|
Causes bone marrow suppression
|
Methotrexate
|
|
|
SE of penicillamine
|
Aplastic anemia and renal
|
|
|
Interferes with activity of T-lymphocytes
|
Hydroxychloroquine
|
|
|
Anti-malarial drug used in rheumatoid arthritis (RA)
|
Hydroxychloroquine
|
|
|
SE of hydroxychloroquine
|
Retinal destruction and dermatitis
|
|
|
MOA of Leflunomide (newer agent)
|
Inhibiting Dihydroorotate Dehydrogenase which leads to decreased pyrimidine synthesis
Cell is stuck in G1 phase |
None
|
|
Proteins that prevent action of tumor necrosis factor alpha (TNF-alpha)
|
Infliximab and etanercept and Adalimumab
|
None
|
|
Anti-rheumatic agent also used for ulcerative colitis
|
Sulfasalazine: dec. rheumatoid factor
|
None
|
|
Drugs used in Gout
|
|
|
|
NSAIDS used in gout
|
Indomethacin and phenylbutazone
|
|
|
NSAID contraindicated in gout
|
Aspirin: can inhibit the secretion of uric acid
|
None
|
|
SE of phenylbutazone
|
Aplastic anemia and agranulocytosis
|
|
|
MOA of Colchicine (used in acute gout)
|
Selective inhibitor of microtubule assembly by binding to tubulin
|
None
|
|
SE of colchicine
|
Kidney and liver toxicity
|
|
|
Agent used to treat chronic gout by increasing uric acid secretion
|
Probenecid and sulfinpyrazone: these are weak organic acids that inhibit the urate-anion exchanger in the prox convuluted tubule
|
None
|
|
Allopurinol treats chronic gout by inhibiting
|
Xanthine oxidase: xanthine and hypoxanthine are more soluble
|
None
|