TaperCommunityamitriptyline
Boxed Warning
Suicidality risk in children, adolescents, and young adults under 25 during initial treatment.
Amitriptyline is a tertiary amine tricyclic antidepressant (TCA) used for major depressive disorder. It is also widely used off-label for chronic pain, migraine prophylaxis, and insomnia. It has strong anticholinergic, antihistaminic, and alpha-adrenergic blocking properties.
10mg, 25mg, 50mg, 75mg, 100mg
Tablets: 10mg, 25mg, 50mg, 75mg, 100mg, 150mg
Category C (risk cannot be ruled out)
Inhibits reuptake of both serotonin and norepinephrine. Also has significant antagonist activity at histamine H1, muscarinic acetylcholine, and alpha-1 adrenergic receptors, contributing to its sedative, anticholinergic, and hypotensive effects.
Available in multiple tablet strengths and liquid formulation. Anticholinergic rebound common during withdrawal.
Multiple available strengths (10, 25, 50, 75mg) allow stepwise reduction. Liquid formulation available for fine adjustments.
Toxicity
Cardiotoxic in overdose (QRS widening, arrhythmias, cardiac arrest). Anticholinergic toxicity (urinary retention, delirium). Seizures. Low therapeutic index.
Pharmacokinetics
Rapidly absorbed after oral administration. Extensive first-pass metabolism; bioavailability ~30–60%. Tmax 2–5 hours.
~6–10 L/kg
Hepatic via CYP2D6, CYP2C19, CYP1A2, and CYP3A4 to the active metabolite nortriptyline (via demethylation) and hydroxylated metabolites.
Renal (primarily as metabolites). Enterohepatic recirculation contributes to variable half-life.
~96%
~46 L/hr (oral clearance, highly variable)
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