nefazodone SERZONE
Class: SARI/PhenylpiperazineFDA Indications: MDD, Relapse Prevention In MDD
Off-Label Use: PTSD, Panic Disorder
Prescribing
Forms: 50, 100, 150, 200, 250mg tabletDose Range: 200-600 mg/day
Starting: 100 mg bid, titrate as tolerated up to max dose 600 mg bid; typically most effective in the 300-600mg/day range
Precautions
Contraindications: active liver disease or with elevated baseline serum transaminasesSerious Side Effects: hepatotoxicity ~ 1 in 250,000 per year of treatment
Side Effects: nausea, xerostomia, constipation, dyspepsia, increased appetite, headache, dizziness, visual changes, sedation/somnolence, insomnia, agitation, confusion, ataxia, memory impairment, weakness/asthenia, paresthesia, orthostatic hypotension
Pharmacodynamics
1° MOA: Serotonin antagonist/reuptake inhibitor2° MOA: Norepinephrine reuptake inhibition
Target: Antagonism at:
Pharmacokinetics
t½: 3.5 (2-4)° TMAX: 1°Substrate of: 3A4
Inhibits: 3A4, 2D6; Induces: ∅
Active Metabolites: HO-NEF, mCPP, Triazole-dione
DDIs
- - DO NOT CO-PRESCRIBE WITH MAOIs
- - 3A4 inhibitors can ↑ levels; likewise, 3A4 inducers can ↓ levels
- - 2D6 inhibitors can increase levels of active secondary metabolite, mCPP
Misc
- - nonlinear pharmacokinetics; inhibits its own metabolism
- - Food delays the absorption and decreases its bioavailability ~20%
- - very effective antidepressant
- - more sedating than other antidepressants, but causes less sexual side effects
Special Populations
Category C—Although the animal data suggest moderate risk, the limited human pregnancy experience suggests that the risk of developmental toxicity is low. However, long-term studies on functional and/ or neurobehavioral deficits have not been conducted.
RID 0.3-0.45%; Limited Human Data—Potential Toxicity
Initiate at half the usual adult dose, and then follow same titration schedule as younger patients
No adjustments necessary
Contraindicated in patients with known hepatic impairment
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