]> 2013-06-18T23:48:09-07:00 Nefazodone taken from DrugBank uncurated http://www.drugbank.ca/drugs/DB01149 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) 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. Mechanism of action: Within the serotonergic system, nefazodone acts as an antagonist at type 2 serotonin (5-HT2) post-synaptic receptors and, like fluoxetine-type antidepressants, inhibits pre-synaptic serotonin (5-HT) reuptake. These mechanisms increase the amount of serotonin available to interact with 5-HT receptors. Within the noradrenergic system, nefazodone inhibits norepinephrine uptake minimally. Nefazodone also antagonizes alpha(1)-adrenergic receptors, producing sedation, muscle relaxation, and a variety of cardiovascular effects. Nefazodone's affinity for benzodiazepine, cholinergic, dopaminergic, histaminic, and beta or alpha(2)-adrenergic receptors is not significant. Drug type: Approved. Small Molecule. Withdrawn. Drug category: Analgesics. Antidepressants. Antidepressive Agents, Second-Generation. Serotonin Agents CHEBI: 7494 Nefazodone 2010-03-16T00:00:00 Molecule Nefazodona (Spanish) Nefazodone Hcl Nefazodone Hydrochloride Nefazodonum (Latin) Dutonin Serzone Molecule Synonym SuperCategory Sodium-dependent serotonin transporter Alpha1B receptor Alpha1A receptor Sodium-dependent noradrenaline transporter 5-hydroxytryptamine 2A receptor RelatedTo ModifiedDate Label Id Drug Has role Definition DefiningCitation Ab Curator CurationStatus Comment