Asenapine

Asenapine is a prescription medication used for the treatment of schizophrenia and bipolar disorder.

• Asenapine is available under the following different brand names: Saphris

Adult and pediatric dosage

Sublingual tablet

• 2.5mg
• 5mg
• 10mg

Schizophrenia

Adult dosage

• 5 mg sublingual every 12 hours initially; maintenance: after 1 week, may be increased up to 10 mg orally every 12 hours.

Bipolar disorder

Adult dosage

• Monotherapy: 10 mg orally every 12 hours initially; may be decreased to 5 mg orally every 12 hours on day 2 and subsequent days if warranted by adverse effects or individual tolerance (90% of patients typically remain on a higher dose)
• Adjunct to lithium or valproate: 5 mg orally every 12 hours initially; may be increased to 10 mg orally every 12 hours if warranted

Pediatric dosage

• Children below 10 years: Safety and efficacy not established
• Children between 10-17 years: 2.5 sublingual every 12 hours initially; may increase to 5 mg sublingual every 12 hours after 3 days and to 10 mg sublingual every 12 hours after 3 additional days

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

Common side effects of the Asenapine include:

• dizziness,
• drowsiness,
• feeling tired,
• restlessness,
• inability to sit still,
• numbness or tingling inside or around the mouth,
• ulcers, blisters, swelling, or peeling of the gums,
• nausea,
• altered sense of taste,
• increased appetite, and
• weight gain.

Serious side effects of the Asenapine include:

• very stiff (rigid) muscles,
• high fever,
• sweating,
• confusion,
• fast or uneven heartbeats,
• lightheadedness,
• tremors,
• twitching,
• uncontrollable movements of the eyes, lips, tongue, face, arms or legs,
• slow heartbeats,
• lightheadedness,
• breast pain, or swelling,
• nipple discharge,
• trouble swallowing,
• sudden weakness,
• ill-feeling,
• fever,
• chills,
• sore throat,
• swollen gums,
• painful mouth sores,
• skin sores,
• cold or flu symptoms,
• cough,
• sudden numbness or weakness,
• sudden severe headache,
• slurred speech, and
• problems with vision or balance.

Rare side effects of the Asenapine include:

• none 

This is not a complete list of side effects and other serious side effects or health problems that may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Asenapine has severe interactions with the following drugs:
  • amisulpride
• Asenapine has serious interactions with at least 59 other drugs.
• Asenapine has moderate interactions with at least 215 other drugs.
• Asenapine has minor interactions with at least 54 other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Known hypersensitivity
• Severe hepatic impairment (Child-Pugh C)

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Asenapine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Asenapine?”

Cautions

• Type 1 hypersensitivity reactions, including anaphylaxis and angioedema, have been reported (n=52), in several cases occurring after the first dose; symptoms include anaphylaxis, angioedema, hypotension, tachycardia, tongue, and laryngeal edema, difficulty breathing, wheezing, or rash
• Neuroleptic malignant syndrome associated with use; monitor for symptoms and discontinue if necessary
• Hyperglycemia (monitor patients with diabetes mellitus for worsening of glucose control); assess fasting plasma glucose before or soon after initiation of antipsychotic medication, and monitor periodically during long-term treatment
• Weight gain may occur; monitor weight at baseline and frequently thereafter; monitor weight in pediatric patients and assess against that expected for normal growth
• Hypotension and syncope, especially during initial dose titration and when increasing dose; orthostatic vital signs should be monitored in patients who are vulnerable to hypotension (elderly patients, patients with dehydration, hypovolemia, concomitant treatment with antihypertensive medications, patients with known cardiovascular disease (history of myocardial infarction or ischemic heart disease, heart failure, or conduction abnormalities), and patients with cerebrovascular disease; monitoring of orthostatic vital signs should be considered in such patients, and dose reduction considered if hypotension occurs
• Leukopenia, neutropenia, and agranulocytosis are reported with use; perform a complete blood count (CBC) during the first few months of therapy; in such patients, consider discontinuation of therapy at the first sign of clinically significant decline in WBC in absence of other causative factors
• Concurrent use of CNS-acting drugs or alcohol may increase toxicity
• Use with caution in patients with a history of seizures or with conditions that potentially lower seizure threshold; conditions that lower seizure threshold may be more prevalent in patients 65 years or older
• Cognitive or motor impairment may occur due to CNS depression; caution patients about operating hazardous machinery, including motor vehicles, until they are reasonably certain that therapy does not affect them adversely
• Dysphagia, dysmotility, and aspiration may occur; use cautiously in patients at risk for aspiration
• Potential disruption of body temperature regulation; strenuous exercise, exposure to extreme heat, dehydration, and anticholinergic medications may contribute to an elevation in core body temperature; use with caution in patients who may experience these conditions
• Not recommended with severe hepatic impairment (Child-Pugh class C)
• Inherent suicide risk in the population treated warrants close supervision when drug therapy is changed
• Atypical antipsychotic drugs have been associated with metabolic changes including hyperglycemia, dyslipidemia, and body weight gain, which may increase cardiovascular/ cerebrovascular risk; all of the drugs in the class have been shown to produce some metabolic changes but each drug has its specific risk profile
• Monitor weight gain in pediatric patients and assess against that expected for normal growth
• Can elevate prolactin levels, and elevation can persist during chronic administration; hyperprolactinemia may suppress hypothalamic GnRH, resulting in reduced pituitary gonadotropin secretion; this, in turn, may inhibit reproductive function by impairing gonadal steroidogenesis in both female and male patients
• Orthostatic vital signs should be monitored in patients who are vulnerable to hypotension (elderly patients, patients with dehydration, hypovolemia, concomitant treatment with antihypertensive medications
• May cause somnolence, postural hypotension, and motor and sensory instability, which may lead to falls and, consequently, fractures or other injuries; perform complete fall risk assessments when initiating antipsychotic treatment and recurrently for patients on long-term antipsychotic therapy
• Extrapyramidal symptoms, including acute dystonic reactions, pseudoparkinsonism, akathisia, and tardive dyskinesia reported
• QT prolongation
  • Based on clinical trials, therapy should be avoided in combination with other drugs known to prolong QTc including Class 1A antiarrhythmics (eg, quinidine, procainamide) or Class 3 antiarrhythmics (e.g., amiodarone, sotalol), antipsychotic medications (eg, ziprasidone, chlorpromazine, thioridazine), and antibiotics (eg, gatifloxacin, moxifloxacin)
  • Treatment should also be avoided in patients with a history of cardiac arrhythmias and in other circumstances that may increase the risk of occurrence of torsade de pointes and/or sudden death in association with the use of drugs that prolong QTc interval, including bradycardia; hypokalemia or hypomagnesemia; and presence of congenital prolongation of QT interval
• Tardive dyskinesia
  • Risk of tardive dyskinesia and the likelihood that it will become irreversible increase with the duration of treatment and cumulative dose
  • The syndrome can develop after a relatively brief treatment period, even at low doses; may also occur after discontinuation of treatment; prescribe in a manner most likely to reduce the risk of tardive dyskinesia
  • Chronic antipsychotic treatment should generally be reserved for patients who suffer from a chronic illness that is known to respond to antipsychotic drugs and for whom alternative, effective, but potentially less harmful treatments are not available or appropriate; some patients may require treatment despite the presence of a syndrome
  • In patients who do require chronic treatment, use the lowest dose and shortest duration of treatment producing a satisfactory clinical response; periodically reassess the need for continued treatment

Pregnancy and Lactation

• Use with caution if benefits outweigh risks during pregnancy
• Neonates exposed to antipsychotic drugs during 3rd trimester of pregnancy are at risk for EPS or withdrawal symptoms after delivery; these complications vary in severity, with some being self-limited and others requiring ICU unit support and prolonged hospitalization
• Lactation
  • Excretion in milk is unknown; use with caution.