nortriptyline PAMELOR
Class: TCA/2° Amine DibenzocyclohepteneFDA Indications: MDD
Off-Label Use: IBS, Panic Disorder, Enuresis, Migraines, Neuropathic Pain, TMJD
Prescribing
Forms: 10, 25, 50, 75mg capsule; 10mg/5mL po solnDose Range: 75-300 mg/day
Starting: 10-25 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 150-500 nmol/L (recommended for MDD)
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
Possible Risk of TdP
Side Effects: anticholinergic side effects, weight gain, sexual dysfunction
Pharmacokinetics
t½: 30 (18-44)° TMAX: 2-6°Substrate of: 2D6; 1A2, 3A4, 2C19
Inhibits: 2D6 (weak), 2C19; Induces: ∅
Active Metabolites: ∅
DDIs
- - DO NOT CO-PRESCRIBE WITH MAOIs (need a 14-day washout period)
- - caution combining with other CNS depressants & anticholingerics
- - 2D6 inhibitors can ↑ serum levels; 2D6 inducers can ↓ serum levels
Misc
- - major 2° metabolite of amitriptyline
- - plasma level monitoring has been well-studied
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 1.7-3.1%
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.
2019 BEE℞S Recommendation: Avoid. Highly anticholinergic, sedating, and cause orthostatic hypotension.
No dosage adjustment necessary.
All TCAs are hepatically metabolzed, highly protein bound and will accumulate, and associated with ↑ LFTs.
References
Applied Clinical Pharmacokinetics And Pharmacodynamics Of Psychopharmacological AgentsConcise Guide To Drug Interaction Principles For Medical Practice
Foye's Principles Of Medicinal Chemistry
Pharmacology For Women's Health
Drug Interactions In Psychiatry, 3rd Ed.
Antidepressant Use During Pregnancy
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