Pharmacology One-liners 1 Flashcards
(299 cards)
Half-life (T1/2)
Time it takes for amount of drug to fall to half its value, constant in first order kinetics (majority of drugs)
Volume of distribution (VD)
Relates the amount of drug in the body to the plasma concentration
Cp
Plasma concentration of a drug at a given time
Clearance (CL)
The ratio of the rate of elimination of a drug to its plasma concentration
First pass effect
Hepatic metabolism of the drug before it reaches the systemic circulation
Bioavailability (F)
The fraction of unchanged drug that reaches systemic circulation after administration
Steady state
When the rate of drug input equals the rate of drug elimination
Different Steps of Phase I
Oxidation
Reduction
Hydrolysis
Inducers of CYP450
Rifampin Phenobarbitol Carbamazepine Phenytoin St. John's wort
Inhibitors of CYP450
Macrolides Ketoconazole (azoles) Ritonavir (protease inhibitors) Cimetadine Grapefruit juice Quinidine Amiodarone
Phase II Conjugation reactions
Glucuronidation Acetylation Glutathione conjugation Glycine conjugation Sulfation Methylation Water conjugation
First-order kinetics
Constant percentage of drug metabolized per unit time
Zero-order kinetics
Constant amount of drug metabolized per unit time
Loading dose
Cp x (Vd/F) Target plasma concentration times [volume of distribution/bioavailability]
Maintenance dose
Cp x (CL/F) Concentration in the plasma times [clearance/bioavailability]
Affinity
Strength of interaction between drug and its receptor
Specificity
Selectivity of a drug for its receptor
Potency
Amount of drug necessary to elicit a biological effect compared with another drug
Efficacy
Ability of a drug to produce the maximal biological effect
Full agonist
Ability of a drug to produce maximal response after binding to the receptor
Partial agonist
Ability to produce less than maximal response after binding to the receptor
Competitive antagonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Noncompetitive antagonist
Ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site
Which substances use an intracellular receptor as the mechanism of action?
Steroids
Hormones