5-HT receptor antagonists

Question 1

MOA: weak inhibitor SERT but metabolite m-cpp potently inhibits 5-HT2a receptors
-weak presynaptic alpha-adrenergic blocker
-modest antagonist of H1 receptor
-5-HT2a receptors are distributed throughout the neocortex
Use: hypnotic not associated with dependence or tolerance; MDD, anxiety disorders
Metab: short half-life but can be given once at night for hypnotic effect
Interactions: increased levels associated with ritonavir or ketaconazole which inhibit CYP3A4

Answer 1

trazadone

Desyrel

Question 2

MOA: two primary metabolites inhibit 5-HT2a receptor; weak inhibitor of NET & SERT
Use: MDD, anxiety disorders
No longer commonly prescribed due to hepatotoxicity (lethal)
Metab: short half-life
-few sexual side effects
Interactions: potent inhibitor of CYP3A4 so can raise levels of triazolam & simvastatin

Answer 2

nefazodone