Clomipramine (Anafranil)
TCA • Last reviewed 2025-09-27
General information
Clomipramine is a serotonin-preferring TCA approved for obsessive-compulsive disorder and used in treatment-resistant depression. Strong serotonergic, anticholinergic, and antihistamine effects increase side-effect burden.
Combined plasma levels (clomipramine + desmethylclomipramine) should stay within 150–300 ng/mL; higher concentrations significantly increase seizure and arrhythmia risk.
Patients require counseling regarding sexual dysfunction, orthostasis, and constipation.
Due to seizure risk, avoid rapid titration and use caution with other threshold-lowering drugs (bupropion, tramadol).
Dosing & administration
Start 25 mg at bedtime; increase by 25 mg every 3–4 days.
Target 100–250 mg/day divided; max 250 mg outpatient/300 mg inpatient.
Monitor plasma level after 3 weeks or with dose >150 mg/day.
Mechanism of action
Potent serotonin reuptake inhibition with secondary norepinephrine effect via active metabolite.
Metabolism & pharmacokinetics
Peak concentration 2–6 h post-dose. Half-life 32–37 h; hepatic metabolism via CYP2D6/CYP3A4 to desmethylclomipramine.
Drug interactions
Avoid MAOIs, cisapride, SSRIs (serotonin syndrome/QT).
CYP2D6/CYP3A4 inhibitors (fluoxetine, fluvoxamine, ketoconazole) increase levels; reduce dose.
Use caution with other anticholinergic or QT-prolonging agents.
Monitoring & safety checks
ECG baseline and after dose increases
Plasma level (goal 150–300 ng/mL)
Assess anticholinergic side effects and bowel regimen
Discontinuation guidance
Taper ≥4 weeks. Abrupt stop can provoke cholinergic rebound, anxiety, and insomnia.
References
- Clomipramine Prescribing Information — DailyMed
- APA OCD guideline (2020)
- Clomipramine therapeutic monitoring and safety — CNS Spectrums (2023)
Educational use only — verify details in current prescribing information and authoritative clinical guidelines before making prescribing decisions.