Terms Test Flashcards
Emax
maximum response a drug can produce.
EC50.
Molar concentration of a drug that produces half the maximal response for that drug.
Kd
affinity of drug for receptor - ‘concentration of drug to occupy 50% of receptorsat eqm.’
dissociation constant - high affinity = low Kd - slow dissociation rate.
potency ratio.
comparison of EC50 values of two drugs with same action.
EC50 (test) / EC50 (standard).
Dose Ratio.
[agonist] producing same response in presence and absence of antagonist.
(reversible competitive antagonist Dr increases linearly with [antagonist].)
non-competitive antagonist.
act at different site on receptor or ANOTHER MOLECULE closely associated –> BOTH reversible or irreversible.
competitive antagonist.
compete with agonist forsame siteon receptor but don’t activate (affinity but no efficacy). [if reversible parallel shift to right].
pA2
NEGATIVE LOG of [antagonist] that requires you to double the [agonist] to produce same response (DR = 2)
AFFINITY ofreversible competitive antagonist.
Pharmacologically speaking what is a drug?
Chemically defined agent used to provoke a measurable response in a biological system.
Exogenously APPLIED and mimic or block activity of endogenous molecules.
how do agonists and antagonists differ?
agonist activates receptor (affinity and efficacy).
antagonist PREVENTS activation (affinity but no efficacy).
what is pharmacodynamics concerned with?
what a DRUG DOES to an organism.
what are the three factors to consider in pharmacokinetics?
absorption, distribution, metabolism & excretion.
briefly outline combinatorial chemical synthesis.
KNOWN synthetic pathway to many UNIDENTIFIED chemical products.
briefly outline the phases of clinical trials.
0 - sub-therapeutic doses in animals/tissues
1 - healthy volunteers (dose)
2 - patient volunteers (effective)
3 - patient volunteers (compare to current medicine)
AGENCY REGISTRATION
4 - long term safety.
does competitive or non-competitive stay colourless?
competitive.
