all pharm Flashcards
affinity
efficacy
defn?
affinity : strength of binding to receptor
efficacy: ability to produce effect
AGONIST: AFFINITY w EFFICACY
ANTAGONIST: AFFINity but NO efficacy
= both determine potency
potency?
conc or dose required to produce effect, if drug is more potent dose can be reduced
Pharmokinetics : what body does to drug
absoprtion, distribution , metabolism , excretion
bioavailability vs absorption
site of admin into plasme - B
fraction of doe that reaches systemic circulation
mode of transfer - bulk flow or diffusional
what type of drug is likely to diffuse across a membrane?
unionised drug; lipid soluble
ionised drug require transport protein
T/F
true as water soluble
membranes are lipid
first pass metabolism
CYP450 action
SE hard to determine as this is genetically determined
Oral drug > small intestine absorption > hepatic portal circulation > liver
Liver heavily metabolises drug ∴ little active reaches systemic circulation
Presents a problem of bioavailbility for oral drugs > must admin higher doses
renal excretion
fast excretion= small molecules
lipid soluble drugs absorbed back
4problems w t2DM?
excess hepatic glucose production
resistance to action of circulating insulin
inadequate insulin production
excess glucose in circulation
excess hepatic glucose production
resistance to action of circulating insulin
inadequate insulin production
excess glucose in circulation
metformin
metformin, thiozolidinediones
sulphonylureas
DPP4-inhibitors
GLP-1 agonists
Alpha Glucosidase inhibitor
SGLT2 Inhibitor : renal glucose absorption blocked