pharmacology Flashcards
pharmacodynamics
biological effects of a drug and mechanism of action
pharmacokinetics
absorption, distribution, metabolism and excretion of a drug and its metabolites
affinity
the strength of association between ligand and receptor
efficacy
the ability of a drug to evoke a cellular response
efficacy of partial agonists compared to agonists
lower
competitive antagonist
binding of agonist and antagonist occurs at the same site, causes a right parallel shift on the curve
non competitive antagonist
agonist binds at the orthosteric site, antagonist binds to allosteric site, no activation when the antagonist is bough, depresses slope on curve
what is potency
drug concentration needed for given effect
factors affecting absorption
solubility, chemical stability, lipid to water partition coefficient (lipid solubility), degree of ionization (depends on pKa and pH at absorption site, physicochemical interactions, tablet form, GI motility
what is pKa
pH when 50% of the drug is ionised and 50% is unionised
what is EC50
agonist concentration that elicits a half maximal response
what does equipotent mean
working over the same concentration range
first order kinetics
elimination rate directly proportional to the drug conc, plasma conc falls exponentially
elimination rate in 1st order kinetics equation
elimination rate = plasma conc x Cl
what is steady state
rate of drug elimination = rate of drug administration
when is steady state reached
after approx 5 half lifes
relationsip required for iV to reach steady state
hyperbolic
oral bioavailabili
F, fraction of drug administered that enters systemic circulation
zero order saturation kinetics
initially eliminated at constamt rate - not proportional to concentration, when plasma concentration > Km of an enzyme that metabolites it it becomes first order
what is drug metabolism
m converting drugs into more polar/less active metabolites that arent reabsorbed by the renal tubure for excretio by the liver
what drugs gain activity from metabolism
codiene - morphine
what drug is unchanged by drug metabolism
diazepam - nordiazepam
phase 1 metabolism
makes a drug more polar and reactive
example of phase 1 reactions
oxidation, reduction, hydrolysis
what are cytochrome p450 CYP proteins
monooxygenases, haem proteins in hepatocytes
what do cytochrome p450 CYP proteins do
mediate oxidation reactions of lipid soluble drugs
what happens in phase 2 reactions
conjugation
what happens in conjugation
adds an endogenous compound, increasing polarity, occurs in the liver
example of a endogenous compound
glucuronyl, sulphate, methyl, acetyl group
what is glucuronidation
transfer of glucuronic acid ti electron rich atoms on substrate by UDP-glucuronyl transferase
drug excretion
by kidney, glomerular filtration, tubular secretion, drug leaves in urine
what state does the drug leave in
unchanged(charged) or more polar