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From “Goodman & Gilman's The Pharmacological Basis of Therapeutics” 11th ed by Brunton et al,and “Basic & Clinical Pharmacology” 11th ed. By Katzung et al

Definitions of terms in basic pharmacology

PharmacoDYNAMICS: actions of the drug ON the body; PharmacoKINETICS: actions OF the body on the drug POTENCY: need less of the drug to achieve the same 50% effect EFFICACY: how great a maximum response a drug can get EC50 = concentration at which 50% of the maximum effect is reached Low EC50 = potent drug ED50 = the DOSE (not concentration) at which the drug achieves its 50% effect LD50 is the dose required to kill 50% of the test animals Kd is the dose required to bind half of the receptors.

Low Kd = potent drug Spare receptors: receptors which have not bound the drug once maximum effect is reached Zero order kinetics: always cleared at the same rate, no matter the concentration. Because at the useful dose the elimination mechanisms are saturated

= half-life depends on the initial concentration First order kinetics: the higher the concentration, the higher the clearance rate = half-life is constant Michaelis-Menton: at a high enough concentration, , first-order elimination is saturated,

and the rate drops, becoming zero-order (irrespective of further rises in concentration) Flow-dependent elimination: depends on the rate of blood delivered to the organ (…liver) Zero-order absorption: rate is constant regardless of the concentration in the gut,

eg. sustained-release medications Phase 1 reactions: MEOS-mediated, to improve solubility in water. A polar group is added or unmasked

- OXIDATION - REDUCTION - HYDROLYSIS - De-something; deamination, dechlorination etc

Phase 2 reactions: conjugation and synthesis reactions, something is added - The –Ations: something gets –ated, - METHYLATION - SULPHATION - ACETYLATION - CONJUGATION eg. glucouronidation