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178 Cards in this Set
- Front
- Back
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Time it takes for amount of drug to fall to half of its value; this is a 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 a 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 (4)
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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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Products of Phase II conjugation
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Glucuronate, acetic acid, and glutathione sulfate
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Type of kinetics when a constant percentage of substrate is 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 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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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; refers to the drug's strength
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Potency
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Maximum response achieveable from a drug
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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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Class of drugs with ability to decrease the maximal response to an agonist
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Noncompetitive antagonist
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A hormone whose mechanism of action (MOA) utilizes intracellular receptors
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Thyroid and steroid hormones
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A hormone whose MOA utilizes transmembrane receptors
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Insulin
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Time it takes for amount of drug to fall to half of its value; this is a 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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Metabolism
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This step of metabolism makes a 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 (4)
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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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Products of Phase II conjugation
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Glucuronate, acetic acid, and glutathione sulfate
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Type of kinetics when a constant percentage of substrate is 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 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
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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; refers to the drug's strength
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Potency
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Maximum response achieveable from a drug
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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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Class of drugs with ability to decrease the maximal response to an agonist
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Noncompetitive antagonist
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A hormone whose mechanism of action (MOA) utilizes intracellular receptors
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Thyroid and steroid hormones
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A hormone whose MOA utilizes transmembrane receptors
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Insulin
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Class of drugs whose 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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Term for a high margin of safety
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High therapeutic index
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Term for 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 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/anticholinesterase poisoning (2)
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Atropine, pralidoxime (2-PAM)
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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 (Mucomyst)
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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 (FFP)
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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 or fomepizole
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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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Digibind (also need to d/c 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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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 "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 (SE) 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 toxicity 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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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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CHOP (cyclophosphamide, doxorubicin, vincristine, and prednisone) plus rituximab
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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 (3 types)
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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 (4)
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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 ) antagonists
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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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Alkylating agent (part of MOPP) produces disulfiram-like reaction with ethanol
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Procarbazine
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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
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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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Thyroid and anti-thyroid drugs
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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 (4)
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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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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 glucocorticoids
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Cortisone and hydrocortisone (equivalent to cortisol)
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Intermediate acting glucocorticoids (4)
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Prednisone, methylprednisolone, prednisolone, and triamcinolone
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Long acting glucocorticoids
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Betamethasone and dexamethasone
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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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Inhibitors of corticosteroids biosynthesis
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Used for Cushing's syndrome (increased corticosteroid)
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Dexamethasone suppression test
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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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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 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 prophylaxis in women with risk factors for breast cancer
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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, oxymetholone, and oxandrolone
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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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