Nefazodone

	Email		Print
	Bookmark		Link

Nefazodone

Nefazodone hydrochloride (trade name Serzone, Nefadar) is an antidepressant

Antidepressant

An antidepressant is a psychiatric medication used for alleviating major depressive disorder or dysthymia. Drug groups known as MAOIs, tricyclics, and second-generation antidepressants such as SSRIs, and serotonin-norepinephrine reuptake inhibitors are particularly associated with the term....
drug marketed by Bristol-Myers Squibb

Bristol-Myers Squibb

Bristol-Myers Squibb , colloquially referred to as BMS, is a pharmaceutical corporation, formed by a 1989 merger between pharmaceutical companies Bristol-Myers Company, founded in 1887 by William McLaren Bristol and John Ripley Myers in Clinton, NY , and E.R....
. 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

Liver

The liver is a vital organ present in vertebrates and some other animals; it has a wide range of functions, a few of which are detoxification, protein synthesis, and production of biochemicals necessary for digestion....
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.

Discussion

Ask a question about 'Nefazodone'

Start a new discussion about 'Nefazodone'

Answer questions from other users

Full Discussion Forum

Encyclopedia

Nefazodone hydrochloride (trade name Serzone, Nefadar) is an antidepressant

Antidepressant

Bristol-Myers Squibb

Liver

Structure and mode of action

Nefazodone is most closely related to trazodone

Trazodone

Trazodone is a psychoactive compound with sedative, anxiolytic, and antidepressant properties. The various manufacturers claim that the antidepressant becomes active in the first week of therapy....
(trade name Desyrel). Nefazodone is not considered to be an SSRI, MAOI or tricyclic antidepressant

Antidepressant

Bupropion

Bupropion is an atypical antidepressant that acts as a norepinephrine reuptake inhibitor and dopamine reuptake inhibitor, and nicotinic antagonist....
/amfebutamone, or venlafaxine

Venlafaxine

Venlafaxine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class first introduced by Wyeth in 1993. It is prescribed for the treatment of major depressive disorder and anxiety disorders, among other uses....
.

It operates by blocking post-synaptic serotonin

Serotonin

Serotonin is a monoamine neurotransmitter synthesized in serotonergic neurons in the central nervous system and enterochromaffin cells in the gastrointestinal tract of animals including humans....
type-2_A

5-HT2A receptor

The mammalian 5-HT2A receptor is a subtype of the 5-HT2 receptor which belongs to the serotonin receptor family and is a GPCR ....
receptors and, to a lesser extent, by inhibiting pre-synaptic serotonin and norepinephrine

Norepinephrine

Norepinephrine or noradrenaline is a catecholamine with dual roles as a hormone and a neurotransmitter.As a stress hormone, norepinephrine affects parts of the brain where attention and responding actions are controlled....
(noradrenaline) reuptake. Nefazodone is also a relatively potent alpha-1 adrenoceptor

Adrenergic receptor

The adrenergic receptors are a class of G protein-coupled receptors that are targets of the catecholamines. Adrenergic Receptor s specifically bind and are activated by their endogenous ligands, the catecholamines adrenaline and noradrenaline ....
antagonist

Receptor antagonist

A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a Receptor , but blocks or dampens agonist-mediated responses....
.

Dosing

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

Food and Drug Administration

The U.S. Food and Drug Administration is an Government agency of the United States Department of Health and Human Services and is responsible for regulating and supervising the safety of foods, dietary supplements, Medications, vaccines, Biopharmaceutical, blood transfusion, medical devices, Electromagnetic radiation-emitting devices, veteri...
(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.

Side effects

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.

Interactions

Nefazodone is a potent inhibitor

Enzyme inhibitor

Enzyme inhibitors are molecules that bind to enzymes and decrease their enzyme activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolism imbalance, many drugs are enzyme inhibitors....
of CYP3A4

CYP3A4

Cytochrome P450 3A4 , a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body....
, an isozyme

Isozyme

Isozymes are enzymes that differ in amino acid sequence but catalyze the same chemical reaction. These enzymes usually display different kinetic parameters , or different regulatory properties....
of the cytochrome P450 system, and may therefore interact adversely

Drug interaction

A drug interaction is a situation in which a substance affects the activity of a medication, i.e. the effects are increased or decreased, or they produce a new effect that neither produces on its own....
with many commonly-used medications

CYP3A4

Cytochrome P450 3A4 , a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body....
that are metabolized by CYP3A4.

Advantages

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.