General Flashcards
3 mechanisms of action
Direct-acting
Indirect-acting
Mixed-acting
(Direct activation + indirect release)
Direct-acting drugs
stimulate postsynaptic receptors
Selective vs. Nonselective
NOT reduced by pretreatment w/ Reserpine
Indirect-acting drugs
increase availability of NE or E
- -releasing or displacing NE from sympathetic nerve varicosities
- -Blocking transport of NE into neurons (i.e. cocaine)
- -Blocking metabolizing enzymes (i.e. MAO or COMT)
ABOLISHED by pretreatment w/ Reserpine
Releasing agents vs. Cocaine, MAO, COMTI, etc.
Mixed-acting drugs
direct activation + indirect release
REDUCED by pretreatment w/ Reserpine
Selective Direct-acting adrenergic agonists
a1- phenylephrine
a2- clonidine
b1- dobutamine
b2- terbutaline
Non-selective Direct-acting adrenergic agonists
a–oxymetazoline
b–isoproterenol
a and b–epinephrine
a and b1–norepinephrine
Indirect-acting releasing agents
Tyramine
Amphetamines
Pretreatment w/ Reserpine…
Direct-acting drug
No effect,
may even increase b/c upregulation of receptors/enhancement of signalling pathway due to chronic treatment of reserpine
Pretreatment w/ Reserpine…
Indirect-acting
Abolished
Pretreatment w/ Reserpine…
Mixed-acting
Reduced
Tachyphalaxis
Rapid loss of pharmacological effect (happens faster than desensitization)