Trazodone

sleep · nervous · digestive · Oral

Trazodone, a sleep compound. Primary action is potent 5-HT2A receptor antagonism with weak serotonin reuptake inhibition — at low doses (<100… Oral half-life 6.7 h.

Primary action is potent 5-HT2A receptor antagonism with weak serotonin reuptake inhibition — at low doses (<100 mg) 5-HT2A blockade + H1/α1 antagonism dominate, producing sedation without meaningful SSRI-like effects; at antidepressant doses (>200 mg) SERT engagement contributes. Active metabolite m-chlorophenylpiperazine (mCPP) is a 5-HT2C agonist and can be anxiogenic in CYP2D6 poor metabolisers who clear it slowly.

Pharmacokinetics

• Oral — t½ 6.7 h · F 65% · Vd 70 L

Sources: PMID:36191287, PMID:15322733