Nefazodona

Nefazodona Uses, Dosage, Side Effects, Food Interaction and all others data.

Nefazodona 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.

Nefazodona, 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.

Nefazodona
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Nefazodona
Availability	Prescription only
Generic	Nefazodone
Nefazodone Other Names	Nefazodona, Nefazodone, Nefazodonum
Related Drugs	Rexulti, sertraline, trazodone, Lexapro, Zoloft, citalopram, Cymbalta, Prozac
Type
Formula	C₂₅H₃₂ClN₅O₂
Weight	Average: 470.007 Monoisotopic: 469.224453
Protein binding	Greater than 99% (in vitro, human plasma proteins).
Groups	Approved, Withdrawn
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Nefazodona is an antidepressant used in the treatment of depression.

For the treatment of depression.

Nefazodona is also used to associated treatment for these conditions: Depression

How Nefazodona works

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. Nefazodona also antagonizes alpha(1)-adrenergic receptors, producing sedation, muscle relaxation, and a variety of cardiovascular effects. Nefazodona's affinity for benzodiazepine, cholinergic, dopaminergic, histaminic, and beta or alpha(2)-adrenergic receptors is not significant.

Toxicity

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

Food Interaction

Avoid alcohol.
Take at the same time every day.
Take with or without food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Nefazodona Drug Interaction

Major: duloxetine, duloxetine, quetiapine, quetiapine, alprazolam, alprazolamModerate: zolpidem, zolpidem, lorazepam, lorazepam, pregabalin, pregabalinUnknown: omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, lamotrigine, lamotrigine, levothyroxine, levothyroxine, cholecalciferol, cholecalciferol

Nefazodona Disease Interaction

Major: hypotension, liver diseaseModerate: angle closure glaucoma, mania, seizures, suicidality

Volume of Distribution

0.22 to 0.87 L/kg

Elimination Route

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

Half Life

2-4 hours

Elimination Route

Nefazodona 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.