II. Indications
- Insomnia (as adjunct to SSRI)
-
Impotence
- See Impotence Management for more effective agents
III. Mechanism
- Triazolopyridine derivative
- Unrelated to Tricyclic Antidepressants
- Phenylpiperazine Antidepressant (Serzone prototype)
-
Serotonin Antagonist and Reuptake Inhibitor (SARI)
- Blocks 5-HT-2 postsynaptic receptor
- Low dose: Serotonin receptor Antagonist
- High dose: Serotonin Agonist
- Weaker than SSRIs as a Serotonin reuptake inhibitor
IV. Pharmacokinetics
- Serum Half Life: 4 to 9 hours
- Therapeutic plasma level: 800 to 1600
V. Efficacy: Major Depression
- As effective as Fluoxetine, Tricyclic Antidepressants
VI. Background
- Cost: $34 per month (generic)
VII. Dosing
-
Sleep
- Dose: 25-100 mg PO qhs
- Average: 50 mg PO qhs
-
Major Depression
- Start: 50 to 150 mg per day in divided doses
- Effective dose: 400 to 600 mg in divided doses
VIII. Adverse Effects
- Sedation
- Limits use as an Antidepressant
- Useful in Major Depression with Insomnia
-
Priapism
- See Priapism Management
- Serotonin Syndrome
- Cardiac Arrhythmia
-
Orthostatic Hypotension (Dizziness)
- Minimize by administering with food
X. Toxicity
- Less toxic in Overdose than Tricyclic Antidepressants
- Lower Incidence of Anticholinergic Toxicity
XI. References
- Sundberg (1995) Depression Primary Care, PGM, p. 45-57
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