Drug reference

Asenapine

Atypical Antipsychotic · Antimanic

Also known as Asenapine maleate

Atypical AntipsychoticAntimanic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Use only if potential benefit outweighs risk—toxicity in animal studies.

FDA category + note

Top interactionssee all 12 →

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Mechanism

Asenapine is a second-generation (atypical) antipsychotic agent. These agents are characterized by an improved neurological risk profile and lower risk of extrapyramidal symptoms compared to typical antipsychotics. Asenapine also exhibits a favorable metabolic profile.

Indications

Monotherapy for the treatment of moderate to severe manic episodes associated with bipolar disorderCombination therapy for the treatment of moderate to severe manic episodes associated with bipolar disorderSchizophreniaacute mania

Dosing

Adult: Monotherapy: Initially 10 mg twice daily by mouth, reduced to 5 mg twice daily, adjusted according to response. Combination therapy: Initially 5 mg twice daily by mouth, increased if necessary to 10 mg twice daily, adjusted according to response.
Renal adjustment: Use with caution if eGFR less than 15 mL/minute/1.73 m2.
Hepatic adjustment: Manufacturer advises caution in moderate impairment; avoid in severe impairment (risk of increased exposure).

Pharmacokinetics

Peak effect

1 h (sublingual), 12–24 h (transdermal)

Half-life

30 h (sublingual), 24 h (transdermal)

Bioavailability

32%–40% (sublingual after 10 min buccal residence), <2% (oral, if swallowed). Transdermal: 3.8 mg/24 h is bioequivalent to 5 mg BID sublingual; 5.7 mg/24 h to 15 mg/day sublingual; 7.6 mg/24 h to 10 mg BID sublingual.

Metabolism

Primarily CYP1A2 and direct glucuronidation by UGT1A4. Minor pathways: CYP3A4 and CYP2D6. No active metabolites.