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Amoxapine

ASENDIN

What it isTricyclic antidepressant that is also a D2 antagonist; depression.

Why it mattersIt combines antidepressant and antipsychotic action in one molecule, which occasionally suits psychotic depression.

What it changes⚑ The D2 blockade brings extrapyramidal effects, tardive dyskinesia and neuroleptic malignant syndrome — unexpected from a tricyclic. It is the metabolite of loxapine.

FDA-approved for

FDA label

BOXED WARNING Increased risk of suicidal thinking and behavior in children, adolescents, and young adults with antidepressant use.
FDA dosingPopulationStartTargetMax
DepressionAdult50 mg BID-TID200-300 mg/day400 mg/day (600 mg/day in hospitalized refractory patients)
DepressionElderly25 mg BID-TID100-150 mg/day300 mg/day

Titration Maintain 300 mg/day for at least 2 weeks before increasing above 300 mg/day.

Renal Undefined

Hepatic Undefined

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy No teratogenic effect in animals; embryotoxicity and fetotoxic effects (intrauterine death, stillbirth, decreased birth weight) seen in animals at 3-10x human dose.

Lactation Undefined

⚠ BOXED WARNING

Cost, est. cash$10–$500/month

Generic entry1989

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger4 / 4
Weight-gain liability1 / 4
Sedation liability1 / 4
QT / Torsades1 / 4
Direct muscarinic antagonism1 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilitySeizures, coma, arrhythmia and neuroleptic-like toxicity make overdose especially dangerous.

Active metabolites

Mechanism of action: Amoxapine ballicule

Amoxapine ballicule: receptor binding, kinetics and half-life diagram

Open Amoxapine in the interactive console ↗

Memory aids: mascots and interaction avatars

Amoxapine ASENDIN mascot mnemonic cartoon
“Ammo mocks A send-in”
Tricycle symbol → tricyclic antidepressant (TCA)
Spooky mascot → D2-blocking like an antipsychotic
He’s ascendin’ and holding a “send-in”
Amoxapine CYP2D6 substrate avatar
CYP2D6 substrate

Open Amoxapine in the interactive console ↗