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56 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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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, and glutathione sulfate
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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 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
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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/anticholinesterase 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 toxicity
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Protamine
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Antidote used for warfarin toxicity
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Vitamin 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
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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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