Asenapine

What it is used for

Asenapine sublingual tablets are indicated for:

• Schizophrenia in adults
• Bipolar I disorder
  • Acute monotherapy of 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

Side effects, and when to stop

The following adverse reactions are discussed in more detail in other sections of the labeling:

• Use in Elderly Patients with Dementia-Related Psychosis
• Neuroleptic Malignant Syndrome
• Tardive Dyskinesia
• Metabolic Changes
• Hypersensitivity Reactions
• Orthostatic Hypotension, Syncope, and other Hemodynamic Effects
• Falls
• Leukopenia, Neutropenia, and Agranulocytosis
• QT Interval Prolongation
• Hyperprolactinemia
• Seizures
• Potential for Cognitive and Motor Impairment
• Body Temperature Regulation
• Dysphagia

The most common adverse reactions (≥5% and at least twice the rate of placebo) reported with acute treatment in adults with schizophrenia were akathisia, oral hypoesthesia, and somnolence. The safety profile of asenapine sublingual tablets in the maintenance treatment of schizophrenia in adults was similar to that seen with acute treatment. The most common adverse reactions (≥5% and at least twice the rate of placebo) reported with acute monotherapy treatment of manic or mixed episodes associated with bipolar I disorder in adults were somnolence, oral hypoesthesia dizziness, extrapyramidal symptoms (excluding akathisia) and akathisia; and during the adjunctive therapy trial in bipolar I disorder in adults were somnolence and oral hypoesthesia. The rates were lower at the 5mg twice daily dose than the 10mg twice daily dose for all of these most common adverse reactions. The safety profile of asenapine sublingual tablets in the maintenance treatment of manic or mixed episodes associated with bipolar I disorder in adults was similar to that seen with acute treatment. The adult information below is derived from a clinical trial database for asenapine sublingual tablets consisting of over 5,355 patients and/or healthy subjects exposed to one or more sublingual doses of asenapine sublingual tablets. A total of 1,427 asenapine-treated patients were treated for at least 24 weeks and 785 asenapine sublingual tablets-treated patients had at least 52 weeks of exposure at therapeutic doses. In a 3-week monotherapy trial, the most common adverse reactions (≥5% and at least twice the rate of placebo) reported in pediatric patients with bipolar I disorder treated with asenapine sublingual tablets were somnolence, dizziness, dysgeusia, oral hypoesthesia, nausea, increased appetite, fatigue, and increased weight. No new major safety findings were reported from a 50-week, open-label, uncontrolled safety trial. A total of 651 pediatric patients were treated with asenapine sublingual tablets. Of these patients, 352 pediatric patients were treated with asenapine sublingual tablets for at least 180 days and 58 pediatric patients treated with asenapine sublingual tablets had at least 1 year of exposure. The safety of asenapine sublingual tablets was evaluated in 403 pediatric patients with bipolar I disorder who participated in a 3-week, placebo-controlled, double-blind trial, of whom 302 patients received asenapine sublingual tablets at fixed doses ranging from 2.5 mg to 10 mg twice daily.

The stated frequencies of adverse reactions represent the proportion of individuals who experienced a treatment- emergent adverse event of the type listed. A reaction was considered treatment emergent if it occurred for the first time or worsened while receiving therapy following baseline evaluation.

Who should not take it

Asenapine sublingual tablets are 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.