PHRM2500 random terms

what are targets for drug action? when interacting with molecules in the organism where do drugs act?

receptors, enzymes, ion channels, carrier molecules

what are other modes of drug action?

chelation and/or neutralisation reaction, physical effects, antimicrobials

unbound drug concentration in plasma is in ____ with unbound drug concentration at the site of action

equilibrium

what are receptors and ligands?

receptors are protein molecules with complex 3d structures which have pockets that can be occupied by a ligand. ligands are small molecules that bind to the receptor.

4 types of receptors

ligand-gated ion channels

g-protein-coupled receptors

kinase-linked and related receptors

intracellular receptors

ligand-gated ion channels (time and example)

rapid action (milliseconds) eg. nicotinic acetylcholine receptor

g-protein-coupled receptors (time and example)

slow signal transduction (secs to mins) eg. beta-adrenoreceptor)

kinase-linked and related receptors (time and example)

very slow response (mins to hours) eg. insulin receptor

intracellular receptors (time and example)

very slow response (hours) eg. oestrogen receptor

agonists (or full agonists)

drugs that bind to a receptor and produce a maximal response comparable to endogenous ligands of the receptor (eg. hormones)

partial agonists

drugs that bind to receptors and produce a sub-maximal response even when a significant number of receptors are occupied