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387 Cards in this Set
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Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)
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Half-life (T1/2)
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Relates the amount of drug in the body to the plasma concentration
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Volume of distribution (VD)
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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
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Steady state
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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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Products of Phase II conjugation
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Glucuronate, acetic acid, and glutathione sulfate
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Inducers of Cytochrome P450
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Barbiturates, phenytoin, carbamazepine, and rifampin
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Inhibitors of CYP450
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Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
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Constant percentage of substrate metabolized per unit time
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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 multiplied by (volume of distribution divided by bioavailability)
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Loading dose (Cp*(Vd/F))
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Concentration in the plasma multiplied by (clearance divided by bioavailability)
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Maintenance dose (Cp*(CL/F))
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Strength of interaction between drug and its receptor
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Affinity
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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
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Potency
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Ability of drug to produce a biologic effect
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Efficacy
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Ability of a drug to produce 100% of the maximum response regardless of the potency
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Full agonist
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Ability to produce less than 100% of the response
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Partial agonist
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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
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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
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Therapeutic index
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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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Antidote used for lead poisoning
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Dimercaprol, EDTA
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Antidote used for cyanide poisoning
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Nitrites
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Antidote used for anticholinergic poisoning
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Physostigmine
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Antidote used for organophosphate and anticholinesterase poisoning
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Atropine, pralidoxime
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Antidote used for iron salt toxicity
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Deferoxamine
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Antidote used for acetaminophen (APAP) toxicity
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N-acetylcysteine
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Antidote for arsenic, mercury, lead, and gold poisoning
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Dimercaprol
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Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
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Penicillamine
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Antidote used for heparin overdose
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Protamine
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Antidote used for warfarin toxicity
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Vitamin K and Fresh frozen plasma
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Antidote for tissue plasminogen activator (t-PA), streptokinase
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Aminocaproic acid
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Antidote used for methanol and ethylene glycol
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Ethanol
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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
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Antidote used for tricyclic antidepressants (TCA)
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Sodium bicarbonate
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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
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Digi-Bind (also need to stop digoxin, normalize K+, and lidocaine if pt. is arrhythmic)
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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
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Antidote for beta-blockers and hypoglycemia
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Glucagon
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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)
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Antidote for salicylate intoxication
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Alkalinize urine, dialysis
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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 "Thymine-less death" given with leucovorin rescue
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5-flouracil (5-FU)
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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
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SEVERE myelosuppression
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MOA of cisplatin
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Alkylating agent
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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
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6-mercaptopurine (6-MP)
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Interaction with this drug requires dose reduction of 6-MP
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Allopurinol
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May protect against doxorubicin toxic by scavenging free radicals
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Dexrazoxane
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Blows DNA (breaks DNA strands), limiting SE is pulmonary fibrosis
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Bleomycin
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Bleomycin+vinblastine+etoposide+cisplatin produce almost a 100% response when all agents are used for this neoplasm
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Testicular cancer
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MOPP regimen used in Hodgkin's disease (HD)
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Mechlorethamine+ oncovorin (vincristine)+ procarbazine, and prednisone
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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) +bleomycin, vinblastine +dacarbazine
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Regimen used for non-Hodgkin's lymphoma
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COP (cyclophosphamide, oncovin(vincristine), and prednisone)
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Regimen used for breast cancer
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CMF (cyclophosphamide, methotrexate, and fluorouracil) and tamoxifen if ER+
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Alkylating agent, vesicant that causes tissue damage with extravasation
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Mechlorethamine
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Anticancer drug also used in RA, produces acrolein in urine that leads to hemorrhagic cystitis
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Cyclophosphamide
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Prevention of cyclophosphamide induced hemorrhagic cystitis
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Hydration and mercaptoethanesulfonate (MESNA)
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Microtubule inhibitor that causes peripheral neuropathy, foot drop (eg. ataxia), and "pins and needles" sensation
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Vincristine
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Interact with microtubules (but unlike vinca which prevent disassembly of tubules), it stabilizes tubulin and cells remain frozen in metaphase
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Paclitaxel (taxol)
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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 greater myelosuppression
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Carboplatin
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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; it stimulates NK cells
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Interferon alpha
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Anti-androgen used for prostate cancer
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Flutamide (Eulexin)
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Anti-estrogen used for estrogen receptor + breast cancer
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Tamoxifen
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Aromatase inhibitor used in breast cancer
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Letrozole, anastrozole
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Newer estrogen receptor antagonist used in advanced breast cancer
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Toremifene (Fareston)
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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 that are 5-HT3 (serotonin receptor subtype ) antagonist
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Odansetron, granisetron
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Nitrosoureas with high lipophilicity, used for brain tumors
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Carmustine (BCNU) and lomustine (CCNU)
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Produces disulfiram-like reaction with ethanol
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Procarbazine
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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
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Leuprolide
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GnRH antagonist with more immediate effects, used for infertility
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Ganirelix
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Dopamine (DA) agonist (for Parkinson's disease), used also for hyperprolactinemia
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Bromocriptine
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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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SE of OCs
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Increased thromboembolic events
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Most widely used thyroid drugs such as Synthroid and Levoxyl contain
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L-thyroxine (T4)
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T3 compound less widely used
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Cytomel
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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
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Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
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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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Dose may need to be increased during pregnancy or with Ocs due to increased TBG in plasma
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Thyroxine
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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
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Beta-blockers such as propranolol
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Vitamins containing iron should NOT be taken simultaneously with levothyroxine because
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Iron deiodinates thyroxine
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Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
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Estogens increase maternal TBG
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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
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Prednisone, methylprednisolone, prednisolone, and triamcinolone
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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, stria, thinning of skin
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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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Used for Cushing's syndrome (increased corticosteroid) and sometimes for adrenal function test
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Metyrapone
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Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosteroid synthesis
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Aminoglutethimide
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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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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 drugs used for fertility and breast cancer respectively
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Clomiphene and tamoxifen
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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)
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Ethinyl estradiol and mestranol
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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 by 5 alpha-reductase
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Testosterone
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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
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Cyproterone acetate
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Drug is used with testosterone for male fertility
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Leuprolide
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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
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Islets of Langerhans
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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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Endogenous insulin
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Normal C-peptide
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Very rapid acting insulin, having fastest onset and shortest duration of action
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Lispro (Humalog)
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Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia
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Regular (Humulin R)
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Long acting insulin
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Ultralente (humulin U)
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Ultra long acting insulin, has over a day duration of action
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Glargine (Lantus)
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Major SE of insulin
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Hypoglycemia
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Important in synthesis of glucose to glycogen in the liver
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GLUT 2
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Important in muscle and adipose tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
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GLUT 4
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Examples of alpha-glucosidase inhibitors (AGI)
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Acarbose, miglitol
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MOA of AGI's
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Act on intestine, delay absorption of glucose
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SE of AGI's
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Flatulence (do not use beano to tx), diarrhea, abdominal cramps
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Alpha-glucosidase inhibitor associated with elevation of LFT's
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Acarbose
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Amino acid derivative
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Nateglinide
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MOA of nateglinide
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Insulin secretagogue
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Biguanide
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Metformin
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Drugs available in combination with metformin
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Glyburide, glipizide, and rosiglitazone
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MOA of metformin
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Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
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Most important potential SE of metformin
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Lactic acidosis
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Meglitinide
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Repaglinide
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MOA of repaglinide
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Insulin release from pancreas; faster and shorter acting than sulfonylurea
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First generation sulfonylurea
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Chlorpropamide, tolbutamide, tolazamide, etc.
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Second generation sulfonylurea
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Glyburide, glipizide, glimepiride, etc.
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MOA of both generations
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Insulin release from pancreas by modifying K+ channels
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Common SE of sulfonylureas, repaglinide, and nateglinide
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Hypoglycemia
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Sulfonylurea NOT recommended for elderly because of very long half life
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Chlorpropamide
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Thiazolidinediones
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Pioglitazone, Rosiglitazone, Troglitazone (withdrawn/d from market)
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Reason troglitazone was withdrawn from market
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Hepatic toxicity
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MOA of thiazolindinediones
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Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
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SE of Thiazolindinediones
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Edema, mild anemia; interaction with drugs that undergo CytP450 3A4 metabolism
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Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
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Glucagon
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Available bisphosphonates
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Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
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MOA of Bisphosphonates
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Inhibits osteoclast bone resorption
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Only bisphosphonates available IV
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Etidronate
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Uses of bisphosphonates
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Osteoporosis, Paget's disease, and osteolytic bone lesions, and hypercalcemia from malignancy
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Major SE of bisphosphonates
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Chemical esophagitis
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Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
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Etidronate
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Used for prevention of postmenopausal osteoporosis in women
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Estrogen (HRT-Hormone replacement therapy)
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Increase bone density, also being tested for breast CA tx.
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Raloxifene (SERM-selective estrogen receptor modulator)
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Used intranasally and decreases bone resorption
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Calcitonin (salmon prep)
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Used especially in postmenopausal women, dosage should be 1500 mg
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Calcium
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Vitamin given with calcium to ensure proper absorption
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Vitamin D
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Disease caused by excess ergot alkaloids
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St. Anthony's Fire
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Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
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Autocoids
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Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
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Zollinger-Ellison Syndrome
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Drug that causes contraction of the uterus
|
Oxytocin
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Distribution of histamine receptors H1, H2, and H3
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Smooth muscle; stomach, heart, and mast cells; nerve endings, CNS respectively
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Prototype antagonist of H1 and H2 receptors
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Diphenhydramine and cimetridine, respectively
|
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1st generation antihistamine that is highly sedating
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Diphendydramine
|
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1st generation antihistamine that is least sedating
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Chlorpheniramine or cyclizine
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2nd generation antihistamines
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Fexofenadine, loratadine, and cetirizine
|
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Generation of antihistamine that has the most CNS effects
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First generation due to being more lipid-soluble
|
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Major indication for H1 receptor antagonist
|
Use in IgE mediated allergic reaction
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Antihistamine that can be used for anxiety and insomnia and is not addictive
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hydroxyzine (Atarax)
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H1 antagonist used in motion sickness
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Dimenhydrinate, meclizine, and other 1st generation
|
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Most common side effect of 1st generation antihistamines
|
Sedation
|
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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)
|
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H2 blocker that causes the most interactions with other drugs
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Cimetidine
|
|
Clinical use for H2 blockers
|
Acid reflux disease, duodenal ulcer and peptic ulcer disease
|
|
Receptors for serotonin (5HT-1) are located
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Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
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|
5HT-1d agonist used for migraine headaches "
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Sumatriptan, naratriptan, and rizatriptan
|
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Triptan available in parenteral and nasal formulation
|
Sumatriptan
|
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H1 blocker that is also a serotonin antagonist
|
Cyproheptadine
|
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Agents for reduction of postpartum bleeding
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Oxytocin, ergonovine and ergotamine
|
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Agents used in treatment of carcinoid tumor
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Ketanserin cyproheptadine, and phenoxybenzamine
|
|
5HT-3 antagonist used in chemotherapeutic induced emesis
|
Ondansetron, granisetron, dolasetron and alosetron
|
|
5ht-3 antagonist that has been associated with QRS and QTc prolongation and should not be used in patients with heart disease
|
Dolasetron
|
|
DOC of chemo induced nausea and vomiting
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Odansetron
|
|
Drug used in ergot alkaloids overdose, ischemia and gangrene
|
Nitroprusside
|
|
Reason ergot alkaloids are contraindicated in pregnancy
|
Uterine contractions
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|
SE of ergot alkaloids
|
Hallucinations resembling psychosis
|
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Ergot alkaloid used as an illicit drug
|
LSD
|
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Dopamine agonist used in hyperprolactinemia
|
Bromocriptine
|
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Peptide causing increased capillary permeability and edema
|
Bradykinin and histamine
|
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Mediator of tissue pain, edema, inactivated by ACE, and may be a contributing factor to the development of angioedema
|
Bradykinin
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Drug causing depletion of substance P (vasodilator)
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Capsaicin
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Prostaglandins that cause abortions
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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
|
|
Drug that selectively inhibits COX 2
|
Celecoxib and rofecoxib
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|
Inhibitor of lipoxygenase
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Zileuton
|
|
Major SE of zileuton
|
Liver toxicity
|
|
Inhibitor of leukotrienes (LTD4) receptors and used in asthma
|
Zafirlukast and montelukast
|
|
Used in pediatrics to maintain patency of ductus arteriosis
|
PGE1
|
|
Approved for use in severe pulmonary HTN
|
PGI2 (epoprostenol)
|
|
Prostaglandin used in the treatment impotence
|
Alprostadil
|
|
Irreversible, nonselective COX inhibitor
|
Aspirin
|
|
Class of drugs that reversibly inhibit COX
|
NSAIDS
|
|
Primary endogenous substrate for Nitric Oxidase Synthase
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Arginine
|
|
MOA and effect of nitric oxide
|
Stimulates cGMP which leads to vascular smooth muscle relaxation
|
|
Long acting beta 2 agonist used in asthma
|
Salmeterol
|
|
Muscarinic antagonist used in asthma
|
Ipratropium
|
|
MOA action of cromolyn
|
Mast cell stabilizer
|
|
Methylxanthine derivative used as a remedy for intermittent claudication
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Pentoxifylline
|
|
MOA of corticosteroids
|
inhibit phospholipase A2
|
|
SE of long term (>5 days) corticosteroid therapy and remedy
|
Adrenal suppression and weaning slowly, respectively
|
|
MOA of quinolones
|
Inhibit DNA gyrase
|
|
MOA of penicillin
|
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
|
|
Drug used for MRSA
|
Vancomycin
|
|
Vancomycin MOA
|
Blocks peptidoglycan synthesis
|
|
Type of resistance found with vancomycin
|
Point mutation
|
|
Meningitis prophylaxis in exposed patients
|
Rifampin
|
|
Technique used to diagnose perianal itching, and the drug used to treat it
|
Scotch tape technique and Mebendazole
|
|
Two toxicities of aminoglycosides
|
nephro and ototoxicity
|
|
DOC for Legionnaires' disease
|
Erythromycin
|
|
MOA of sulfonamides
|
Inhibit dihydropteroate synthase
|
|
Penicillins active against penicillinase secreting bacteria
|
Methicillin, nafcillin, and dicloxacillin
|
|
Cheap wide spectrum antibiotic DOC of otitis media
|
Amoxicillin
|
|
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 anti-histamines
|
|
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
|
|
Drug notorious for causing pseudomembranous colitis
|
Clindamycin
|
|
DOC for tx of pseudomembranous colitis
|
Metronidazole
|
|
Treatment of resistant pseudomembranous colitis
|
ORAL vancomycin
|
|
Anemia caused by trimethoprim
|
Megaloblastic anemia
|
|
Reason fluoroquinolones are contraindicated in children and pregnancy
|
Cartilage damage
|
|
DOC for giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
|
Metronidazole
|
|
Treatment for TB patients (think RIPE)
|
Rifampin, Isoniazid, Pyrazinamide, and Ethambutol
|
|
Metronidazole SE if given with alcohol
|
Disulfiram-like reaction
|
|
Common side effect of Rifampin
|
Red urine discoloration
|
|
MOA of nystatin
|
Bind ergosterol in fungal cell membrane
|
|
Neurotoxicity with isoniazid (INH) prevented by
|
Administration of Vit. B6 (pyridoxine)
|
|
Toxicity of amphotericin
|
Nephrotoxicity
|
|
SE seen only in men with administration of ketoconazole
|
Gynecomastia
|
|
Topical DOC in impetigo
|
Topical mupirocin (Bactroban)
|
|
DOC for influenza A
|
Amantadine
|
|
DOC for RSV
|
Ribavirin
|
|
DOC for CMV retinitis
|
Ganciclovir
|
|
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
|
|
Cephalosporins able to cross the BBB
|
Cefuroxime (2nd generation) and Ceftazidime
|
|
Cephalosporins that do NOT cross BBB
|
Cefixime (3rd gen)
|
|
Drug used for N. gonorrhea in females
|
Ceftriaxone
|
|
Cephalosporin causes kernicterus in neonates
|
Ceftriaxone or cefuroxime
|
|
SE of INH
|
Peripheral neuritis and hepatitis
|
|
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
|
Dapsone
|
|
DOC for herpes and its MOA
|
Acyclovir; incorporated into viral DNA and chain termination
|
|
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
|
sulfamethoxazole/ trimethoprim
|
|
Lactam that can be used in PCN allergic patients
|
Aztreonam
|
|
SE of imipenem
|
Seizures
|
|
Anti-viral with a dose limiting toxicity of pancreatitis
|
Didanosine
|
|
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
|
|
Benzodiazepines used to promote sleep
|
Temazpam, trizolam, flurazepam
|
|
Benzodiazepine used for anxiety
|
Alprazolam
|
|
Non-benzodiazepine used as an anxiolytic
|
Buspirone
|
|
Non-benzodiazepine used for sleep
|
Zolpidem
|
|
Major effect of benzodiazepines on sleep at high doses
|
REM is decreased
|
|
Neurologic SE of benzodiazepines
|
Anterograde amnesia
|
|
Reason benzos are used cautiously in pregnancy
|
Ability to cross the placenta
|
|
Main route of metabolism for benzodiazepines
|
Hepatic
|
|
Benzodiazepine that undergo extrahepatic conjugation (which are useful in older or hepatically impaired)
|
Lorazepam, oxazepam, and temazepam
|
|
MOA for benzodiazepines
|
increase the FREQUENCY of GABA-mediated chloride ion channel opening
|
|
Antidote to benzodiazepine overdose (antagonist that reverses the CNS effects)
|
Flumazenil
|
|
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
|
Midazolam
|
|
DOC for status epilepticus
|
Diazepam
|
|
Longer acting benzodiazepines used in the management of withdrawal states of alcohol and other drugs
|
Chlordiazepoxide and Diazepam
|
|
Agents having active metabolites, long half lives, and a high incidence of adverse effects
|
Diazepam, Flurazepam, chlordiazepoxide, and clorazepate
|
|
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
|
Increase the DURATION of GABA-mediated chloride ion channels
|
|
Barbiturate used for the induction of anesthesia
|
Thiopental
|
|
Site of action for zaleplon and zolpidem
|
Benzodiazepine receptor BZ1 (although are not considered benzodiazepines)
|
|
Good hypnotic activity with less CNS SE than most benzodiazepines
|
Zolpidem, zaleplon
|
|
Agent that is a partial agonist for the 5-HT1A receptor
|
Buspirone
|
|
Drug of choice for generalized anxiety disorder, NOT effective in acute anxiety
|
Buspirone
|
|
Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
|
Ethanol
|
|
Agent with zero-order kinetics
|
Ethanol
|
|
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 alcohol dehydrogenase
|
Disulfiram, metronidazole, certain sulfonylureas and cephalosporins
|
|
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
|
Ethanol
|
|
Agent that is the antidote for methanol overdose
|
Ethanol
|
|
Drug that inhibits alcohol dehydrogenase and is used in ethylene glycol exposure
|
Fomepizole
|
|
Most frequent route of metabolism
|
Hepatic enzymes
|
|
Mechanisms of action for Phenytoin, Carbamazepine, Lamotrigine
|
Sodium blockade
|
|
MOA for benzodiazepines and barbiturates
|
GABA-related targets
|
|
MOA for Ethosuximide
|
Calcium channels
|
|
MOA for Valproic acid at high doses
|
Affect calcium, potassium, and sodium channels
|
|
Drugs of choice for generalized tonic-clonic and partial seizures
|
Valproic acid and Phenytoin
|
|
DOC for febrile seizures
|
Phenobarbital
|
|
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 for short term (acute) treatment; phenytoin for prolonged therapy
|
|
Drugs that can be used for infantile spasms
|
Corticosteroids
|
|
Anti-seizure drugs used also for bipolar affective disorder (BAD)
|
Valproic acid, carbamazepine, phenytoin and gabapentin
|
|
Anti-seizure drugs used also for Trigeminal neuralgia
|
Carbamazepine
|
|
Anti-seizure drugs used also for pain of neuropathic orgin
|
Gabapentin
|
|
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
|
Valproic acid
|
|
Carbamazepine may cause
|
Agranulocytosis
|
|
Anti-seizure drugs used as alternative drugs for mood stabilization
|
Carbamazepine, gabapentin, lamotrigine, and valproic acid
|
|
MOA of general anesthetics
|
Most are thought to act at GABA-A receptor - chloride channel
|
|
Inhaled anesthetic with a low blood/gas partition coefficient
|
Nitrous oxide
|
|
Inversely related to potency of anesthetics
|
Minimum alveolar anesthetic concentration (MAC)
|
|
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
|
Halothane and methoxyflurane
|
|
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 anesthetic, 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
|
|
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
|