Pharm 1 liners kinetics and dynamics Flashcards
Time required to reduce amount of drug in the body by half during elimination, 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)
Hepatic metabolism of the drug before it reaches the systemic circulation
First pass effect
The fraction of unchanged drug that reaches systemic circulation after administration
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
Different steps of Phase I
Oxidation, reduction, hydrolysis
Rifampin, phenobarbital, carbamazepine, phenytoin, St. Johns wort
Inducers of CYP450
Macrolides, ketoconazole (azoles), ritonavir (protease inhibitors), cimetidine, grapefruit juice, quinidine, amiodarone
Inhibitors of CYP450
Name three Phase II conjugation reactions
Glucuronidation, acetylation, glutathione conjugation, sulfation, methylation
Constant fraction of drug eliminated per unit time
First order kinetics
Constant amount of drug eliminated per unit time
Zero order kinetics
A higher dose given to rapidly achieve effective blood levels
Loading dose (Cp*(VD/F))
Amount of drug required to keep a desired mean steady-state concentration in the body
Maintenance dose (Cp*(CL/F))
Ability of a drug to bind to a receptor
Affinity
Selectivity of a drug for its receptor
Specificity
Amount of drug necessary to elicit a biologic effect compared with another drug
Potency
Ability of drug to produce the maximal effect
Efficacy
Ability of a drug to produce maximal response after binding to the receptor
Full agonist
Ability to produce less than maximal response after binding to the receptor
Partial agonist
Ability to bind reversibly to the active site without activating the effector system
Competitive antagonist
Ability to bind irreversibly to the active site or bind to an allosteric site without activating the effector system
Noncompetitive antagonist
Mechanism of action utilizes intracellular receptors
Steroids and hormones
Mechanism of action utilizes transmembrane receptors that have intrinsic enzymatic activity
Insulin, EGF, TGFbeta, PDGF, BNP
Mechanism of action utilizes ligand gated ion channels
Acetylcholine, nicotine
Dose that produces therapeutic response in 50% of the population
ED50
Dose that is toxic to 50% of the population
TD50
Dose that is lethal to 50% of a population of animals
LD50
Window between therapeutic effect and toxic effect
Therapeutic index
Drugs that have a large margin of safety is indicated by
High therapeutic index
Drugs that have a narrow margin of safety is indicated by
Low therapeutic index