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56 Cards in this Set
- Front
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time it takes for amount of drug to fall to half of its value; this is 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 in 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
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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, 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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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 effec
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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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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/antichoinesterase poisoning
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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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antidose used for warfarin toxicity
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vitamin K and fresh frozen flasma (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
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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 an 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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