asenapine maleate: clinical use

Prescribing considerations

• Confirm reliable sublingual technique; swallowed bioavailability is very low.
• Use caution with cardiovascular or cerebrovascular disease, hypotension risk, seizures, diabetes risk, dysphagia, Parkinson's disease, dementia with Lewy bodies, impaired temperature regulation and increased falls risk.
• Not approved or recommended for dementia-related psychosis.
• Use cautiously in older adults; exposure may be higher and efficacy data are limited.
• Moderate hepatic impairment may increase exposure in some patients; severe renal impairment has not been adequately studied.
• Assess suicide risk and supervise high-risk patients appropriately.

Contraindications and cautions

• Hypersensitivity to asenapine or any product excipient.

Monitoring

• Clinical response, adherence and sublingual technique.
• Weight, blood glucose and lipids, particularly with diabetes or metabolic risk.
• Blood pressure, dizziness, syncope and falls risk.
• Extrapyramidal symptoms and tardive dyskinesia.
• Prolactin-related symptoms, liver function and relevant cardiovascular or ECG risk factors when clinically indicated.

Clinical pharmacology

Asenapine is a multi-receptor antagonist with high affinity for dopamine, serotonin, alpha-adrenergic and histamine receptors. It is metabolised mainly through UGT1A4 glucuronidation and CYP1A2-mediated oxidation, with lesser CYP2D6 and CYP3A4 contributions; the parent compound provides the principal activity.

Formulation and product differences

• The selected product is an unflavoured sublingual tablet containing gelatin and mannitol.
• It dissolves rapidly in saliva but must remain under the tongue; swallowing substantially reduces absorption.
• The selected Sycrest sublingual tablet products are marked discontinued on eMC.