PHARMACODYNAMICS Flashcards
The cellular macromolecule or macromolecule
complex with which the drug interacts to elicit a
cellular response
DRUG RECEPTOR/ DRUG TARGET
Other receptors can be in the form of
ion
channels, Enzymes and Transporters.
Binding of ATENOLOL to Beta receptor
stimulates conversion of _______ (producing
biologic effects by the activation of G-protein)
ATP to cAMP
Ex: Binding of amlodipine to calcium channel
Ion channels
_____ block NaCl transporter at the distal convoluted tubule
Thiazides
Magnitude of biologic effect is directly related to the fraction of ACTIVE STATE
Partial agonist
In reversible equilibrium, it favors more the
_____state.
inactive
Drugs that bind to physiological receptors and
mimic the regulatory effects of the endogenous
signalling compounds/ endogenous ligand.
AGONIST
Are drugs that would bind on the same
recognition site as the endogenous
ligand/agonist.
PRIMARY AGONIST
Drug binds to a different site but produces the
same effect as that of the endogenous ligand.
ALLOSTERIC/ ALLOTOPIC AGONIST
Transduction process that links drug occupancy
of receptors and pharmacological response
Coupling
After drug-receptor binding, _____
may occur then cause _____,
desensitization and down-regulation of the
receptor.
signal transduction; signal amplification
Signal amplification is only seen if the mechanism involves ______ and ______
second
messenger G-protein coupled receptors ;
enzyme-linked receptors.
Binding of ____(Beta agonist) to its
receptor would activate the receptor → Stimulates
G-protein coupled receptors (aka 7
Transmembrane receptors because it is a
protein located at the cell membrane; it passes
through it for about 7 times. It contains Alpha,
Beta and Gamma.)
Albuterol
3 TYPES OF G-PROTEIN COUPLED RECEPTORS
Gs/ STIMULATORY
Gi/ INHIBITORY
Gq
