hydrochloride (trade name Serzone
) is an antidepressant
drug marketed by Bristol-Myers Squibb
. Its sale was discontinued in 2003 in some countries, due to the small possibility of hepatic (liver) injury, which could lead to the need for a liver transplant, or even death. The incidence of severe liver
damage is approximately one in 250,000 to 300,000 patient-years. On May 20, 2004, Bristol-Myers Squibb discontinued the sale of Serzone in the United States and Canada. Several generic formulations of nefazodone are still available.
Structure and mode of action
Nefazodone is most closely related to trazodone
(trade name Desyrel
). Nefazodone is not considered to be an SSRI
or tricyclic antidepressant
. It is not chemically related to either bupropion
, or venlafaxine
It operates by blocking post-synaptic serotonin type-2A receptors and, to a lesser extent, by inhibiting pre-synaptic serotonin and norepinephrine (noradrenaline) reuptake. Nefazodone is also a relatively potent alpha-1 adrenoceptor antagonist.
Nefazodone doses for adults typically start at 50 mg
twice daily uptitrated by 100 mg/day per week to a maximum of 600 mg (300 mg twice daily), according to Food and Drug Administration
(FDA) regulations. Some patients with severe depression were treated with more than 600 mg/day. Most patients were treated with 300 mg–600 mg daily.
Unlike most SNRIs and SSRIs, Nefazodone has no negative effects on libido or sexual functioning, and is actually sometimes used as an antidote to SSRI induced impotence and anorgasmia in men.
Nefazodone's claimed advantages over other antidepressants include reduced possibility of disturbed sleep or sexual dysfunction, and ability to treat some patients who did not respond to other antidepressant drugs.