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Indications and Dosage
Sublingual
Schizophrenia 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.
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Hepatic Impairment
Severe (Child-Pugh Class C): Contraindicated.
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Contraindications
Hypersensitivity to asenapine. Dementia-related psychosis. Severe (Child-Pugh Class C) hepatic impairment.
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Special Precautions
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.
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Adverse Reactions
Significant: Extrapyramidal symptoms (e.g. pseudoparkinsonism, dystonia, akathisia, tardive dyskinesia) seizure, syncope, orthostatic hypotension, QT prolongation, dysphagia, hyperprolactinaemia, leukopenia, neutropenia.
Nervous: Somnolence, sedation, dizziness, oral hypoaesthesia, paraesthesia, speech disturbance, irritability, anxiety. CV: Tachycardia. GI: Constipation, nausea, dry mouth, glossodynia, hypersalivation, taste disturbance, swollen tongue. Genitourinary: Urinary retention. Endocrine: Galactorrhoea, gynaecomastia, amenorrhoea, impotence. Haematologic: Thrombocytopenia. Ophthalmologic: Blurred vision, mydriasis. Others: Fatigue. Potentially Fatal: Neuroleptic malignant syndrome (manifesting as hyperthermia, muscle rigidity, altered mental status, autonomic instability, elevated serum creatine phosphokinase levels, myoglobinuria, acute renal failure), agranulocytosis, hyperglycaemia (associated w/ ketoacidosis or hyperosmolar coma). |
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Patient Counseling Information
Avoid eating or drinking 10 min after admin. This drug may cause somnolence and sedation, if affected, do not drive or operate machinery.
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Monitoring Parameters
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).
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Overdosage
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.
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Drug Interactions
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.
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Food Interaction
Reduced bioavailability w/ food and drink. May enhance CNS effects of alcohol.
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Action
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. |
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Chemical Structure
 Source: National Center for Biotechnology Information. PubChem Database. Asenapine, CID=3036780, https://pubchem.ncbi.nlm.nih.gov/compound/Asenapine (accessed on Jan. 21, 2020) |
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Storage
Store between 20-25°C. Protect from light and moisture.
Any unused portions should be disposed of in accordance w/ local requirements. |
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MIMS Class
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ATC Classification
N05AH05 - asenapine ; Belongs to the class of diazepines, oxazepines and thiazepines antipsychotics.
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References
Anon. Asenapine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 03/04/2017. Buckingham R (ed). Asenapine Maleate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2017. Joint Formulary Committee. Asenapine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 03/04/2017. McEvoy GK, Snow EK, Miller J et al (eds). Asenapine Maleate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 03/04/2017. Saphris Tablet (Allergan USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 03/04/2017.
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