Zukaria Sublingual Tablet

Zukaria is indicated for:

• Schizophrenia in adults
• Bipolar I disorder
• Acute monotherapy for manic or mixed episodes in adults and pediatric patients 10 to 17 years of age
• Adjunctive treatment to lithium or valproate in adults.
• Maintenance monotherapy treatment in adults

The mechanism of action of asenapine, in schizophrenia and bipolar I disorder, is unknown. It has been suggested that the efficacy of asenapine in schizophrenia could be mediated through a combination of antagonist activity at D2 and 5-HT 2A receptors.

Schizophrenia: adults:

• Initial dose: 5 mg sublingually, twice daily
• Recommended dose: 5 mg sublingually, twice daily
• Maximum dose: 10 mg sublingually, twice daily

Schizophrenia maintenance treatment in adults.

• Initial dose: 5 mg sublingually, twice daily
• Recommended dose: 5-10 mg sublingually, twice daily
• Maximum dose: 10 mg sublingually, twice daily

Bipolar mania in adults: acute and maintenance monotherapy.

• Initial dose: 5-10 mg sublingually, twice daily
• Recommended dose: 5-10 mg sublingually, twice daily
• Maximum dose: 10 mg sublingually, twice daily

Bipolar mania in pediatric patients (10-17 years): monotherapy.

• Initial dose: 2.5 mg sublingually, twice daily
• Recommended dose: 2.5-10 mg sublingually, twice daily
• Maximum dose: 10 mg sublingually, twice daily

Bipolar mania in adults: as an adjunct to lithium or valproate

• Initial dose: 5 mg sublingually, twice daily
• Recommended dose: 5-10 mg sublingually, twice daily
• Maximum dose: 10 mg sublingually, twice daily

Sublingual tablets should not be swallowed. It should be placed under the tongue and left to dissolve completely. It will dissolve in saliva within seconds. Eating and drinking should be avoided for 10 minutes after administration.

Zukaria should be used with caution in combination with:

• Antihypertensive, as it may cause hypotension
• Paroxetine (CYP2D6 substrate and inhibitor)

Asenapine is contraindicated in patients with:

• Severe hepatic impairment (Child-Pugh C).
• A history of hypersensitivity reactions to asenapine. Reactions have included anaphylaxis, angioedema, hypotension, tachycardia, swollen tongue, dyspnea, wheezing and rash.

The most common adverse reactions to asenapine are akathisia, somnolence, oral hypoesthesia, dizziness, extrapyramidal symptoms, nausea, increased appetite, fatigue, and increased weight.

May cause extrapyramidal and/or withdrawal symptoms in neonates with third trimester exposure. Lactation studies have not been conducted to assess the presence of asenapine in human milk, the effects of asenapine on the breastfed infant, or the effects of asenapine on milk production.

Caution should be exercised when asenapine is prescribed in elderly patients with dementia-related psychosis, QT prolongation, neuroleptic malignant syndrome, tardive dyskinesia, metabolic changes, orthostatic hypotension, leukopenia, neutropenia, agranulocytosis, seizures, and the potential for cognitive and motor impairment.

There is no specific antidote for asenapine. The management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and the management of symptoms. In cases of severe extrapyramidal symptoms, anticholinergic medication should be administered. Close medical supervision and monitoring should continue until the patient recovers.

Do not store above 30°C. Keep away from light and out of the reach of children.