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NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTIDEPRESSANTS › Other antidepressants
nefazodone
N06AX06
Forms & Strengths
- Tablet: 50 mg
- Tablet: 100 mg
- Tablet: 150 mg
- Tablet: 200 mg
- Tablet: 250 mg
Adult Dosing
- Initial: 200 mg/day administered in two divided doses
- Titration: Increase in increments of 100 to 200 mg/day at intervals of no less than 1 week
- Maintenance range: 300 to 600 mg/day administered in two divided doses
Pediatric Dosing
- Safety and effectiveness in pediatric patients below the age of 18 have not been established
Indications
- Treatment of major depressive disorder
Mechanism of Action
- Serotonin antagonist and reuptake inhibitor (SARI)
- Inhibits neuronal reuptake of serotonin and norepinephrine
- Antagonist at postsynaptic 5-HT2 receptors and alpha-1 adrenergic receptors
Contraindications
- Pre-existing hepatic disease or elevated baseline transaminases
- Concurrent use of monoamine oxidase inhibitors (MAOIs)
- Coadministration with CYP3A4 substrates such as terfenadine, astemizole, cisapride, or pimozide
- Known hypersensitivity to nefazodone or phenylpiperazine antidepressants
Adverse Reactions
- Severe hepatotoxicity, liver failure, and potential need for liver transplantation
- Somnolence, dizziness, and fatigue
- Dry mouth, nausea, and constipation
- Orthostatic hypotension
- Blurred vision
- Suicidality in children, adolescents, and young adults
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole) significantly increase nefazodone plasma concentrations
- CYP3A4 substrates (e.g., triazolam, alprazolam, simvastatin): nefazodone markedly increases their concentrations and risk of toxicity
- Monoamine oxidase inhibitors (MAOIs): risk of serious, sometimes fatal serotonin syndrome
- Additive CNS depressants (alcohol, sedatives): increased sedation and psychomotor impairment
Curated Content: Needs Vetting Before Put to Clinical Use