imipramine TOFRANIL

Class: TCA/​Dihydrodibenzazepine
FDA Indications: MDD
Off-Label Use: Enuresis, Anxiety, Chronic Pain, Sleep Terrors, Somnambulism, ADHD, Migraines, Neuropathic Pain, Eating Disorders, PTSD
Prescribing
Forms: 10, 25, 50mg tablet; 75, 100, 125, 150 mg Tofranil-PM™ capsule
Dose Range: 75-300 mg/day
Starting: 25 mg qd qhs, ↑ by 25 mg q3-7 days, max dose 300 mg qd
Stopping: ↓ 50% x3 days, then ↓ another 50% x3 days, then D/C entirely.
Monitoring: Suggested plasma level 500-800 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: 32 (11-25)° TMAX: 1-2°
Substrate of: 2D6, 2C19; 1A2, 3A4
Inhibits: ∅ ; Induces:
Active Metabolites: desipramine
DDIs
  • - DO NOT CO-PRESCRIBE WITH MAOIs (need a 14-day washout period)
  • - caution combining with other CNS depressants & anticholingerics
Misc
  • - the first antidepressant, first approved in 1959
  • - its 2° metabolite, desipramine, is the most noradrenergic of all the TCAs
  • - most preferred TCA for treating enuresis in children
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 0.15%


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.

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Last updated July 08 2018 15:58:23. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.