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56 Cards in this Set

  • Front
  • Back
Time it takes for amount of drug to fall to half of its value, constant in first order kinetics (majority of drugs)
Half-life (T1/2)
Relates the amount of drug in the body to the plasma concentration
Volume of distribution (VD)
Plasma concentration of a drug at a given time
Cp
The ratio of the rate of elimination of a drug to its plasma concentration
Clearance (CL)
The elimination of drug that occurs before it reaches the systemic circulation
First pass effect
The fraction of administered dose of a drug that reaches systemic circulation
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
This step of metabolism makes drug more hydrophilic and hence augments elimination
Phase I
Different steps of Phase I
Oxidation, reduction, hydrolysis
Inducers of Cytochrome P450 (CYP450)
Barbiturates, phenytoin, carbamazepine, and rifampin
Inhibitors of CYP450
Cimetidine, ketoconazole, erythromycin, isoniazid and grapefruit
Products of Phase II conjugation
Glucuronate, acetic acid, and glutathione sulfate
Constant percentage of substrate metabolized per unit time
First order kinetics
Drug elimination with a constant amount metabolized regardless of drug concentration
Zero order kinetics
Target plasma concentration times (volume of distribution divided by bioavailability)
Loading dose (Cp*(Vd/F))
Concentration in the plasma times (clearance divided by bioavailability)
Maintenance dose (Cp*(CL/F))
Strength of interaction between drug and its receptor
Affinity
Selectivity of a drug for its receptor
Specificity
Amount of drug necessary to elicit a biologic effect
Potency
Ability of drug to produce a biologic effect
Efficacy
Ability of a drug to produce 100% of the maximum response regardless of the potency
Full agonist
Ability to produce less than 100% of the response
Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
Ability to bind to either the same or different site as the drug
Noncompetitive antagonist
Mechanism of action (MOA) utilizes intracellular receptors
Thyroid and steroid hormones
MOA utilizes transmembrane receptors
Insulin
MOA utilizes ligand gated ion channels
Benzodiazepines and calcium channel blockers
Median effective dose required for an effect in 50% of the population
ED50
Median toxic dose required for a toxic effect in 50% of the population
TD50
Dose which is lethal to 50% of the population
LD50
Window between therapeutic effect and toxic effect
Therapeutic index
Drug with a high margin of safety
High therapeutic index
Drug with a narrow margin of safety
Low therapeutic index
Antidote used for lead poisoning
Dimercaprol, EDTA
Antidote used for cyanide poisoning
Nitrites
Antidote used for anticholinergic poisoning
Physostigmine
Antidote used for organophosphate/anticholinesterase poisoning
Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity
Deferoxamine
Antidote used for acetaminophen (APAP) toxicity
N-acetylcysteine (Mucomyst)
Antidote for arsenic, mercury, lead, and gold poisoning
Dimercaprol
Antidote used in poisonings: copper (Wilson's disease), lead, mercury, and arsenic
Penicillamine
Antidote used for heparin toxicity
Protamine
Antidote used for warfarin toxicity
Vitamin and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase
Aminocaproic acid
Antidote used for methanol and ethylene glycol
Ethanol
Antidote used for opioid toxicity
Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity
Flumazenil
Antidote used for tricyclic antidepressants (TCA)
Sodium bicarbonate
Antidote used for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote used for digitalis toxicity
Digibind (also need to d/c digoxin, normalize K+, and lidocaine if pt. Is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol)
Esmolol
Antidote for methotrexate toxicity
Leucovorin
Antidote for beta-blockers and hypoglycemia
Glucagon
Antidote useful for some drug induced Torsade de pointes
Magnesium sulfate
Antidote for hyperkalemia
sodium polystyrene sulfonate (Kayexalate)
Antidote for salicylate intoxication
Alkalinize urine, dialysis