Nefazodone

Absorption

Nefazodone is rapidly and completely absorbed. Its absolute bioavailability is low (about 20%).

Toxicity

Cases of life-threatening hepatic failure have been reported in patients treated with nefazodone.

Chemical properties

Crystalline Solid

Originator

Dutonin,Bristol-Myers Squibb,USA

The Uses of Nefazodone

A selective serotonin 5-HT2 receptor antagonist. An antidepressant

Indications

For the treatment of depression.

Background

Nefazodone 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. Drug-induced hepatic injuries were associated with an risk of elevated need for a liver transplant, or even death, with the incidence of severe liver damage was shown to be approximately 1 in 250,000 to 300,000 patient-years. On May 20, 2004, Bristol-Myers Squibb discontinued the sale of Serzone in the United States.

Definition

ChEBI: Nefazodone is a N-arylpiperazine, a N-alkylpiperazine, a member of triazoles, a member of monochlorobenzenes and an aromatic ether. It has a role as an antidepressant, a serotonergic antagonist, a serotonin uptake inhibitor, an alpha-adrenergic antagonist and an analgesic.

brand name

Serzone (Bristol-Myers Squibb).

Therapeutic Function

Antidepressant

Biological Functions

Although nefazodone (Serzone) is structurally related to trazodone, it is less sedating. It does not block α₁- adrenoreceptors, and its use is not associated with priapism. Nefazodone inhibits the neuronal reuptake of serotonin and blocks 5HT2A receptors. Its short half-life requires dosing twice a day. Nefazodone is not associated with weight gain or sexual dysfunction. It inhibits the cytochrome P450 3A4 isoenzyme that is responsible for 50% of known oxidative metabolism, and therefore, nefazodone can elevate levels of drugs dependent on this pathway for metabolism.

Pharmacokinetics

Nefazodone, an antidepressant synthetically derived phenylpiperazine, is used to treat major depression. Although it is structurally similar to trazodone, nefazodone has a mechanism of action different from other antidepressants and, hence, lacks the risk for major cardiovascular toxicity seen with tricyclics and insomnia and inhibition of REM sleep seen with the selective serotonin reuptake inhibitors.

Metabolism

Hepatic.