化合物信息

Drug Groups

approved; withdrawn

Description

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, which could lead to the need for a liver transplant, or even death. The incidence of severe liver damage is 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. [Wikipedia]

Indication

For the treatment of depression.

Pharmacology

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.

Toxicity

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

Affected Organisms

Biotransformation

Hepatic.

Absorption

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

Half Life

2-4 hours

Protein Binding

Greater than 99% (in vitro, human plasma proteins).

Elimination

Nefazodone is extensively metabolized after oral administration by n-dealkylation and aliphatic and aromatic hydroxylation, and less than 1% of administered nefazodone is excreted unchanged in urine.

Distribution

* 0.22 to 0.87 L/kg

References

External Links