Adult: Initially, 5 mg bid, may increase to 10 mg bid after 1 wk if tolerated.
Sublingual Acute manic episodes of bipolar disorder, Acute mixed episodes of bipolar disorder
Adult: As monotherapy or adjunct to lithium or valproate: Initially, 5 mg bid, may increase to 10 mg bid depending on clinical response and tolerability.
Severe (Child-Pugh Class C): Contraindicated.
Hypersensitivity to asenapine. Dementia-related psychosis. Severe (Child-Pugh Class C) hepatic impairment.
Patient w/ history of seizure disorder, known CV disease (e.g. heart failure, MI or ischaemia, arrhythmia), cerebrovascular disease, dehydration, bradycardia, hypovolaemia, hypokalaemia, Parkinson’s disease, dementia w/ Lewy Bodies (DLB). Moderate (Child-Pugh Class B) hepatic impairment. Pregnancy and lactation.
Avoid eating or drinking 10 min after admin. This drug may cause somnolence and sedation, if affected, do not drive or operate machinery.
Monitor mental status, electrolytes, vital signs, BP, BMI, waist circumference, CBC, fasting plasma glucose level (HbA1c) and fasting lipid panel, prolactin level, and liver function. Monitor for Parkinsonian signs; changes in menstruation, libido, galactorrhoea, erectile and ejaculatory function; and tardive dyskinesia (12 mthly or 6 mthly for high-risk patients).
Symptoms: Agitation, confusion, extrapyramidal symptoms (e.g. akathisia, orofacial dystonia), sedation, bradycardia, supraventricular complexes, intraventricular conduction delay, hypotension, circulatory collapse. Management: Symptomatic and supportive treatment. Maintain adequate airway, oxygenation, and ventilation. Monitor ECG. Treat hypotension and circulatory collapse w/ sympathomimetic agents (except epinephrine and dopamine) and IV fluids. Treat severe extrapyramidal symptoms w/ anticholinergic agents.
Increased plasma concentration w/ fluvoxamine. May enhance the effects of certain antihypertensive agents (due to its α1-adrenergic antagonism) and CNS depressants. May increase exposure of paroxetine. May antagonise the effects of levodopa and dopaminergics.
Reduced bioavailability w/ food and drink. May enhance CNS effects of alcohol.
Description: Asenapine, a dibenzo-oxepino pyrrole derivative, is a 2nd generation or atypical antipsychotic w/ mixed antagonistic activity. It has high affinity for serotonin (5-HT1A-B, 2A-C, 5-7), dopamine (D1-4), adrenergic (α1-2), and histamine (H1) receptors; and moderate affinity for H2 receptor. Pharmacokinetics: Absorption: Rapidly absorbed in the sublingual, supralingual, and buccal mucosa. Bioavailability: 35%. Reduced bioavailability w/ food and liq. Time to peak plasma concentration: W/in 0.5-1.5 hr. Distribution: Undergoes rapid and extensive extravascular distribution. Volume of distribution: Approx 20-25 L/kg. Plasma protein binding: 95%, including albumin and α1-acid glycoprotein. Metabolism: Metabolised in the liver mainly via direct glucuronidation by uridine diphosphate glucuronosyltransferase 1A4 (UGT1A4) and via oxidation mainly by CYP1A2 enzyme. Excretion: Via urine (approx 50%) and faeces (approx 40%). Terminal elimination half-life: Approx 24 hr.
Store between 20-25°C. Protect from light and moisture.
Any unused portions should be disposed of in accordance w/ local requirements.
N05AH05 - asenapine ; Belongs to the class of diazepines, oxazepines and thiazepines antipsychotics.
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