Amitriptyline (Elavil)
TCA • Last reviewed 2025-09-27
General information
Amitriptyline is a tertiary amine TCA indicated for depression but frequently used off-label for neuropathic pain and migraine prophylaxis. Strong antihistamine and anticholinergic effects drive sedation and weight gain.
Metabolism to nortriptyline provides additional noradrenergic effect. Combined plasma levels (amitriptyline + nortriptyline) should remain between 80–200 ng/mL to balance response and toxicity.
Cardiac conduction changes (QT prolongation, bundle branch block) and anticholinergic delirium are key safety considerations.
Elderly patients are particularly susceptible to orthostatic hypotension and cognitive impairment; consider lower starting doses and slow titration.
Dosing & administration
Start 25–50 mg at bedtime; increase by 25–50 mg every 3–7 days.
Typical antidepressant target 100–150 mg/day; max 300 mg/day inpatient.
Lower doses (10–75 mg) used for pain/migraine with slower titration.
Mechanism of action
Inhibits serotonin and norepinephrine reuptake; potent H1, muscarinic, and α1 antagonist leading to sedation, dry mouth, and orthostasis.
Metabolism & pharmacokinetics
Peak concentration 4–6 h post-dose. Half-life 21–24 h; metabolized via CYP2D6/CYP2C19 to nortriptyline. Accumulates in hepatic impairment.
Drug interactions
Avoid MAOIs, cisapride (QT), and agents lowering seizure threshold.
CYP2D6 inhibitors increase levels; enzyme inducers (carbamazepine) reduce efficacy.
Additive anticholinergic burden with antihistamines, antipsychotics.
Monitoring & safety checks
ECG at baseline and dose increases
Serum level (combined 80–200 ng/mL)
Discontinuation guidance
Gradually taper ≥4 weeks; abrupt cessation may cause cholinergic rebound, insomnia, irritability.
References
- Amitriptyline Prescribing Information — DailyMed
- CANMAT TCA guidance (2024)
- APA guidance on TCAs for chronic pain (2021)
Educational use only — verify details in current prescribing information and authoritative clinical guidelines before making prescribing decisions.