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NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Diazepines, oxazepines, thiazepines and oxepines
asenapine
N05AH05
Forms & Strengths
- Sublingual tablets: 2.5 mg, 5 mg, 10 mg
- Transdermal patch: 3.8 mg/24h, 5.7 mg/24h, 7.6 mg/24h
Adult Dosing
- Schizophrenia (Sublingual): 5 mg sublingually twice daily; target 5-10 mg twice daily (Max: 10 mg twice daily)
- Bipolar Mania (Sublingual): 10 mg sublingually twice daily initially; may reduce to 5 mg twice daily
- Schizophrenia (Transdermal): 3.8 mg/24 hours applied once weekly initially; titrate to 5.7 mg or 7.6 mg/24 hours
Pediatric Dosing
- Safety and efficacy not established in pediatric patients under 18 years of age
Indications
- Acute treatment of schizophrenia in adults
- Acute treatment of manic or mixed episodes associated with bipolar I disorder in adults
Mechanism of Action
- Atypical antipsychotic with high affinity for serotonin (5-HT2A, 5-HT1A, 5-HT2C, 5-HT7) and dopamine (D2, D3, D4) receptors
- Moderate affinity for alpha-1 adrenergic and histamine H1 receptors
- Lacks appreciable affinity for muscarinic cholinergic receptors
Contraindications
- Severe hepatic impairment (Child-Pugh Class C)
- Known hypersensitivity to asenapine or any components of the formulation
Adverse Reactions
- Somnolence
- Oral hypoesthesia and paresthesia
- Dizziness
- Extrapyramidal symptoms
- Weight gain
- Increased alanine aminotransferase (ALT)
- Orthostatic hypotension
Drug Interactions
- CYP1A2 inhibitors (e.g., fluvoxamine) may increase asenapine concentrations
- Strong CYP1A2 inducers (e.g., smoking, carbamazepine) may decrease asenapine concentrations
- Additive CNS depressants (alcohol, sedatives) increase risk of sedation and orthostasis
- Antihypertensive agents may exhibit enhanced hypotensive effects
Curated Content: Needs Vetting Before Put to Clinical Use