Also Known As: Nefazodone, Serzone

Nefazodone (Serzone, Nefadar) is an antidepressant marketed by Bristol-Myers Squibb. Its sale was discontinued in 2003 in some countries due to the rare incidence of hepatotoxicity (liver damage), which could lead to the need for a liver transplant, or even death. The incidence of severe liver damage is approximately 1 in every 250,000 to 300,000 patient-years. On June 14, 2004, Bristol-Myers Squibb discontinued the sale of Serzone in the United States and Canada. Several generic formulations of nefazodone are still available.

Nefazodone acts primarily as a potent antagonist at the 5-HT2A receptors (Kd 26 nM).[5] It also has moderate affinity for the α1-adrenergic receptor (Kd 48 nM) and 5-HT1A receptor (Kd 80 nM), and very low affinity for the α2-adrenergic receptor (Kd 640 nM) and D2 receptor (Kd 910 nM).[5] It acts as an antagonist at all of these sites.[5][6] Nefazodone has low affinity for the serotonin (200 nM), norepinephrine (360 nM), and dopamine (360 nM) transporters as well, and therefore acts as a weak serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[7] It has negligible affinity for the H1 receptor (24,000 nM) or muscarinic acetylcholine receptors (11,000 nM), and accordingly lacks any antihistamine or anticholinergic side effects.[7]

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