Nefazodone Hydrochloride

Indications and usage: Nefazodone hydrochloride tablets are indicated for the treatment of depression. When deciding among the alternative treatments available for this condition, the prescriber should consider the risk of hepatic failure associated with nefazodone hydrochloride treatment . In many cases, this would lead to the conclusion that other drugs should be tried first.

CLINICAL PHARMACOLOGY Pharmacodynamics The mechanism of action of nefazodone, as with other antidepressants, is unknown. Preclinical studies have shown that nefazodone inhibits neuronal uptake of serotonin and norepinephrine. Nefazodone occupies central 5-HT 2 receptors at nanomolar concentrations, and acts as an antagonist at this receptor. Nefazodone was shown to antagonize alpha 1 -adrenergic receptors, a property which may be associated with postural hypotension.

Systemic exposure to Nefazodone Hydrochloride reflects ~20% systemic bioavailability (Nefazodone Hydrochloride) absorption kinetics and dual hepatorenal clearance pathway combining glucuronidation and urinary filtration of nefazodone hydrochloride, sustaining receptor engagement across a 2 to 4 hours terminal elimination (Nefazodone Hydrochloride SPL) half-life window (oral tmax achieved within 2 to 3 hours following nefazodone hydrochloride ingestion response profile).

Dosing protocols (150 mg/1 Tablet or 100 mg/1 Tablet or 250 mg/1 Tablet or 200 mg/1 Tablet or 50 mg/1 Tablet) balance efficacy (90.00% patient satisfaction across 10 logs) against headache (6.9% of reports), diarrhea (4.8% of reports), fatigue (4.3% of reports), with strict avoidance in contraindications coadministration of terfenadine, astemizole, cisapride, pimozide, or carbamazepine with nefazodone hydrochloride is contraindicated .; nefazodone hydrochloride tablets are contraindicated in patients who were withdrawn from nefazodone because of evidence of liver injury ..