PCOL2012

LECTURE 2: PRINCIPLES OF DRUG ACTION

Drug receptors:

Enable extracellular molecules to alter intracellular events

o Agonists occupy and activate the receptor causing signal transduction
o Antagonists occupy but do not activate the receptor, resulting in no effect

ion channels:

Allow ions to cross membranes and are voltage-gated or ligand-gated

o Blockers prevent ions from getting through
o Modulators increases/decreases the ion channel from being opened

Enzyme:

Metabolise substrates to products

o Inhibitors prevent metabolism
o False substrates compete with substrates to use the enzyme and produce abnormal
metabolites
o Pro-drugs are drugs which are converted into active drugs by the enzyme

Transporters

Carry substrates across the membrane

o Inhibitors block the transport of exogenous compounds
o False substrates cause abnormal compounds to accumulate within a cell

LECTURE 3: THEORY AND EXPERIMENTAL DESIGN

Distribution
Substrate specificity
Function

ache
Limited NMJ and
synapse
Narrow Ach and
methacholine
Hydrolyses and
terminates ACh action

buche
Widespread liver, skin, brain, GI
smooth muscle
Broad: Buche, ach, suxamethonium
Unclear for physiological functions,
pharmacologically important to
anaethetists