amoxapine ASENDIN

Class: TeCA/​Dibenzoxazepine
FDA Indications: MDD
Off-Label Use: Treatment-resistant Psychotic Depression, Treatment-resistant Depression
Prescribing
Forms: 25, 50, 100, 150mg tablet
Dose Range: 50-600 mg/day
Starting: 25 mg 2-3 times/ day; increase gradually to 100 mg 2-3 times/day or a single dose at bedtime; maximum 400 mg/day (may dose up to 600 mg/ day in inpatients)
Stopping: Taper to avoid withdrawal effects. Many patients tolerate 50% dose reduction for 3 days, then another 50% reduction for 3 days, then discontinuation.
Monitoring: Baseline ECG is recommended

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: , Tardive dyskinesia, Hyperprolactinemia
Side Effects: headache, sedation/somnolence, dizziness, weakness/asthenia, weight gain, hyperhidrosis, nausea, sexual dysfunction, anticholinergic side effects, EPS, restlessness
Pharmacodynamics
1° MOA: Tetracyclic antidepressant
Target: SERT, NET, 5HT2A, 5HT7, D2, D4, H1 (moderate), M1 (weak)
Pharmacokinetics
t½: 8 (6-16)° TMAX: 1.5°
Substrate of: 2D6; 3A4
Inhibits: ∅ ; Induces:
Active Metabolites: 8-hydroxyamoxapine, 7-hydroxyamoxapine
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
  • - less potent inhibitor of neuronal NE reuptake compared with the other secondary TCAs
  • - the most potent D2 antagonist of all antidepressants, which may explain some of its clinical effects – though it has 8.5x less affinity for D2 than chlorpromazine, it can still cause EPS
  • - amoxapine is the N-demethylated metabolite of loxapine
  • - may have a faster onset of action than some other antidepressants
Special Populations

Category C—No published reports linking the use of amoxapine with congenital defects have been located. The animal data suggest risk, but the human pregnancy experience is too limited to assess the embryo-fetal risk. Until such data are available, the safest course may be to avoid amoxapine during organogenesis. TCAs have a potential for neonatal abstinence syndrome when used near term.

Amoxapine and its metabolite are excreted into breast milk. In 2001, the American Academy of Pediatrics classified amoxapine as a drug whose effect on the nursing infant is unknown but may be of concern.

In general, lower dosages are recommended for these patients. Recommended starting dosage of amoxapine is 25 mg two or three times daily. If no intolerance is observed, dosage may be increased by the end of the first week to 50 mg two or three times daily. Although 100 to 150 mg daily may be adequate for many elderly patients, some may require higher dosage. Careful increases up to 300 mg daily are indicated in such cases.

Use with caution – may require lower than usual adult dose

Use with caution – may require lower than usual adult dose

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Last updated December 05 2018 19:19:12. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.