amitriptyline ELAVIL

Class: TCA/​3° Amine Dibenzocycloheptadiene
FDA Indications: MDD, Nocturnal Enuresis In Children
Off-Label Use: Neuropathic Pain, Postherpetic Neuralgia, Postherpetic Neuralgia, Migraines, Insomnia, Eating Disorders, Fibromyalgia
Prescribing
Forms: 10, 25, 50, 75, 100, 125, 150mg tablet; 10 mg/mL IM
Dose Range: 50-300 mg/day
Starting: 25 mg qd qhs, ↑ by 25 mg q3-7 days, increase to 150 mg. May be taken in divided doses.
Stopping: ↓ 50% x3 days, then ↓ another 50% x3 days, then D/C entirely.
Monitoring: Suggested plasma level 250-825 nmol/L (recommended for MDD)

NAMI drug fact sheet

Precautions
Contraindications: Concomitant use of MAOIs; patient s/p MI; coadministration of other QT-prolonging agents; h/o QT ↑ or arrhythmia; caution in patients with hypo-K+ or hypo-Mg2+
Serious Side Effects: 5HT syndrome; ↓ seizure threshold; QT↑, arrhythmias, tachycardia, orthostatic hypotension
Side Effects: weight gain, sexual dysfunction, anticholinergic side effects
Pharmacodynamics
1° MOA: Tricyclic antidepressant
Target: SERT, NET, H1, α1, M1, 5HT2A
Pharmacokinetics
t½: 21 (10-46)° TMAX: 2-12°
Substrate of: 2C19, 3A4; 2D6
Inhibits: 2D6, 2C19; Induces:
Active Metabolites: nortriptyline (t½ 18-44°)
DDIs
  • - DO NOT CO-PRESCRIBE WITH MAOIs (need a 14-day washout period)
  • - caution combining with other CNS depressants & anticholinergics
  • - CBZ can ↓ levels by ~50% via 3A4 induction
  • - VPA may ↑ levels
Misc
  • - popular TCA in treatment of headaches and numerous chronic pain syndromes
  • - commonly used for insomnia
  • - addition of T3 may potentiate effects
Special Populations

Category C—A case-control study showed ∅ ↑ congenital malformations with 1st trimester use & a review (n=209) showed ∅ assoc with congenital malformations or developmental delay.

RID 1.9-2.8%


Avoid due to its anticholinergicity and high sedation, especially when combining with other CNS depressants and/or anticholingerics. Caution regarding orthostatic hypotension (fall risk!). Can impair cognition.

No dosage adjustment necessary.


All TCAs are hepatically metabolzed, highly protein bound and will accumulate, and associated with ↑ LFTs. Especially sedating TCAs (e.g. amitriptyline) should be avoided.

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Last updated January 20 2018 15:32:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.