Asenapine

Name: Asenapine

What side effects can this medication cause?

Asenapine may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • dry mouth
  • stomach pain
  • constipation
  • vomiting
  • heartburn
  • increased appetite
  • increase in amount of saliva in the mouth
  • change in taste
  • toothache
  • weight gain
  • loss of feeling in the lips or mouth
  • dizziness, feeling unsteady, or having trouble keeping your balance
  • excessive tiredness
  • restlessness or constant urge to keep moving
  • irritability
  • anxiety
  • depression
  • difficulty falling asleep or staying asleep
  • pain in the joints, arms, or legs

Some side effects can be serious. If you experience any of these symptoms, or those listed in the SPECIAL PRECAUTION section, call your doctor immediately or get emergency medical treatment:

  • hives
  • rash
  • itching
  • difficulty breathing or swallowing
  • swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
  • hoarseness
  • wheezing
  • fever
  • muscle stiffness or pain
  • spasm or tightening of the neck muscles
  • confusion
  • fast or irregular heartbeat
  • sweating
  • uncontrollable movements of the arms, legs, face, mouth, tongue, jaw, lips or cheeks
  • falling
  • seizures
  • sore throat, chills, cough, and other signs of infection
  • red or brown colored urine

Asenapine may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.

If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).

What are the side effects of asenapine?

The most common side effects of asenapine are

  • drowsiness,
  • headache, and
  • dizziness.

Other side effects are

  • fatigue,
  •  insomnia,
  • dry mouth,
  • feeling restlessness or difficulty sitting still,
  • stiffness and shuffling walk,
  • tremors, and
  • joint pain.

Less common but serious side effects include:

  • Neuroleptic malignant syndrome (NMS). NMS is a rare but serious side effects associated with the use of antipsychotics. NMS may result in death and must be treated in the hospital. Signs and symptoms of NMS may include high fever, sweating (diaphoresis), severe muscle stiffness or rigidity, confusion, loss of consciousness, high blood pressure, rapid heartbeat, and changes in your breathing.
  • Extrapyramidal side effects (EPS) including:
    • Dystonia: painful spasms of the oral, throat, or neck muscles that may cause problems with speech, swallowing, and stiff neck.
    • Akathisia: feelings of restlessness or difficulty sitting still.
    • Pseudoparkinsonis: drug induced Parkinson's symptoms.
  • Tardive dyskinesia (TD). TD usually occurs after long term use of antipsychotics and usually presents with movement problems affecting the tongue, lips, jaw, face, and extremities.
  • Metabolic changes including high blood sugar (hyperglycemia), diabetes mellitus, increase in blood cholesterol, and weight gain.
  • High blood levels of prolactin. Prolactin is a hormone that allows the production of breast milk. High levels of prolactin may cause menstrual abnormalities, leakage of milk from the breast, development of breasts in men (gynecomastia), and erection problems in men (erectile dysfunction).

Is asenapine safe to take if I'm pregnant or breastfeeding?

Fetuses exposed to antipsychotics during the third trimester of pregnancy are at risk for extrapyramidal and withdrawal symptoms after birth. Symptoms reported included agitation, hypertonia, hypotonia, tremor, somnolence, depressed breathing, and feeding disorder. Currently there is no data on the use of asenapine during pregnancy. Asenapine should only be used during pregnancy if the potential benefit to the mother outweighs the potential for side effects in the unborn baby.

A pregnancy exposure registry has been established to monitor the use of atypical antipsychotics, including asenapine, during pregnancy. All pregnant women treated with atypical antipsychotics are advised to enroll in this pregnancy registry and report any side effects.

Asenapine has not been evaluated in breastfeeding women.

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Reviewed on 6/29/2015 References REFERENCE: FDA Prescribing Information

Inform MD

Before taking asenapine, tell your doctor about all of your medical conditions. Especially tell your doctor if you:

  • are allergic to asenapine or to any of its ingredients
  • or anyone in your family has or has ever had diabetes
  • have severe diarrhea or vomiting or you think you may be dehydrated
  • have ever used street drugs or misused prescription medications
  • have or have ever had a prolonged QT interval (a rare heart problem that may cause irregular heartbeat, fainting, or sudden death)
  • have or have ever had low blood pressure
  • have or have ever had a heart attack or a slow or irregular heartbeat
  • have or have ever had a stroke or TIA (ministroke)
  • have or have ever had seizures
  • have or have ever had breast cancer
  • have or have ever had a low level of white blood cells in your blood or a decrease in white blood cells caused by a medication you have taken
  • have or have ever had a low level of potassium or magnesium in your blood
  • have or have ever had heart or liver disease
  • are pregnant, especially if you are in the last few months of your pregnancy, or if you plan to become pregnant. If you become pregnant while taking asenapine, call your doctor. Asenapine may cause problems in newborns following delivery if it is taken during the last months of pregnancy.
  • are breast-feeding
  • if you are having surgery, including dental surgery

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Asenapine and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if asenapine crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using asenapine. It is recommended that women receiving asenapine should not breast feed.

Asenapine FDA Warning

Warning: Increased Mortality in Elderly Patients with Dementia- Related Psychosis

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Asenapine is not approved for the treatment of patients with dementia-related psychosis.

 

What is asenapine?

Asenapine is an antipsychotic medication. It works by changing the actions of chemicals in the brain.

Asenapine is used to treat schizophrenia in adults, and bipolar I disorder in adults and children who are at least 10 years old.

Asenapine may also be used for purposes not listed in this medication guide.

What is the most important information I should know about asenapine?

You should not use asenapine if you are allergic to it, or if you have severe liver disease.

Asenapine can cause serious neurologic problems. Stop taking this medicine and call your doctor at once if you have: very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, feeling light-headed, tremors, twitching, or uncontrollable movements of your eyes, lips, tongue, face, arms, or legs.

Asenapine is not approved for use in psychotic conditions related to dementia. Asenapine may increase the risk of death in older adults with dementia-related conditions.

What happens if I miss a dose?

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Asenapine dosing information

Usual Adult Dose for Schizophrenia:

Acute treatment:
Starting dose: 5 mg sublingually twice a day
Recommended dose: 5 mg sublingually twice a day, if tolerated may increase to 10 mg sublingually twice a day after 1 week if necessary
Maximum dose: 10 mg sublingually twice a day

Comments: Controlled trials revealed no added benefit with the higher dose, but a clear increase in certain adverse reactions. The safety of doses above 10 mg twice daily has not been evaluated in clinical studies.

Maintenance Treatment:
Recommended dose: 5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day

Comments: There is no available evidence to answer the question of how long the schizophrenic patient should remain on therapy; it is generally recommended that responding patients be continued beyond the acute response.

Use: Treatment of schizophrenia.

Usual Adult Dose for Bipolar Disorder:

Monotherapy:
Starting dose: 10 mg sublingually twice a day
Recommended dose: 5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day

Comment: In controlled trials, the starting dose was 10 mg twice daily. On the second and subsequent days, the dose could be lowered to 5 mg twice daily, however less than 10% of patients had their dose reduced.

Adjunctive Therapy:
Starting dose: 5 mg sublingually twice a day
Maintenance dose: 5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day

Comments:
-The dose should be titrated based on clinical response and tolerability.
-There is no available evidence to answer the question of how long the patient should remain on therapy; it is generally recommended that responding patients be continued beyond the acute response.

Uses: For the acute treatment of manic or mixed episodes associated with bipolar 1 disorder either as monotherapy or as adjunctive therapy with either lithium or valproate.

Usual Pediatric Dose for Bipolar Disorder:

Age: 10 years or older
Starting dose: 2.5 mg sublingually twice a day
Dose titration: After 3 days, may increase to 5 mg sublingually twice daily, and after an additional 3 days to 10 mg twice a day, as needed and as tolerated
Recommended dose: 2.5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day

Comment: Pediatric patients appear to be more sensitive to dystonia with initial dosing and therefore gradual dose escalation is recommended. The safety of doses above 10 mg twice a day has not been studied.

Use: As monotherapy for the acute treatment of manic or mixed episodes associated with bipolar 1 disorder.

What other drugs will affect asenapine?

Taking asenapine with other drugs that make you sleepy or slow your breathing can cause dangerous or life-threatening side effects. Ask your doctor before taking a sleeping pill, narcotic pain medicine, prescription cough medicine, a muscle relaxer, or medicine for anxiety, depression, or seizures.

Tell your doctor about all your current medicines and any you start or stop using, especially:

  • an antibiotic;

  • an antidepressant;

  • anti-malaria medication;

  • cancer medicine;

  • heart or blood pressure medicine; or

  • other antipsychotic medications.

This list is not complete. Other drugs may interact with asenapine, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Usual Adult Dose for Schizophrenia

Acute treatment:
Starting dose: 5 mg sublingually twice a day
Recommended dose: 5 mg sublingually twice a day, if tolerated may increase to 10 mg sublingually twice a day after 1 week if necessary
Maximum dose: 10 mg sublingually twice a day

Comments: Controlled trials revealed no added benefit with the higher dose, but a clear increase in certain adverse reactions. The safety of doses above 10 mg twice daily has not been evaluated in clinical studies.

Maintenance Treatment:
Recommended dose: 5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day

Comments: There is no available evidence to answer the question of how long the schizophrenic patient should remain on therapy; it is generally recommended that responding patients be continued beyond the acute response.

Use: Treatment of schizophrenia.

Usual Pediatric Dose for Bipolar Disorder

Age: 10 years or older
Starting dose: 2.5 mg sublingually twice a day
Dose titration: After 3 days, may increase to 5 mg sublingually twice daily, and after an additional 3 days to 10 mg twice a day, as needed and as tolerated
Recommended dose: 2.5 to 10 mg sublingually twice a day
Maximum dose: 10 mg sublingually twice a day

Comment: Pediatric patients appear to be more sensitive to dystonia with initial dosing and therefore gradual dose escalation is recommended. The safety of doses above 10 mg twice a day has not been studied.

Use: As monotherapy for the acute treatment of manic or mixed episodes associated with bipolar 1 disorder.

Precautions

US BOXED WARNING: INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS:
INCREASED MORTALITY IN ELDERLY PATIENTS WITH DEMENTIA-RELATED PSYCHOSIS: Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. This drug is not approved for the treatment of patients with dementia-related psychosis.

Safety and efficacy have not been established in patients younger than 10 years.

Consult WARNINGS section for additional precautions.

Asenapine Pregnancy Warnings

Use is not recommended unless the benefit outweighs the risk to the fetus AU TGA pregnancy category: C US FDA pregnancy category: Not assigned Comments: -Neonates exposed to this drug during the third trimester should be monitored for extrapyramidal and/or withdrawal symptoms following delivery. -US: There is a pregnancy exposure registry that monitors pregnancy outcomes; for more information contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/

In animal studies, developmental toxicity was observed, but teratogenicity was not demonstrated. Agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, and feeding disorder have been reported in neonates exposed to antipsychotics during the third trimester. As with other drugs that antagonize dopamine D2 receptors, this drug elevates prolactin levels. 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. There is no controlled data in human pregnancy. AU TGA pregnancy category C: Drugs which, owing to their pharmacological effects, have caused or may be suspected of causing, harmful effects on the human fetus or neonate without causing malformations. These effects may be reversible. Accompanying texts should be consulted for further details. US FDA pregnancy category Not Assigned: The US FDA has amended the pregnancy labeling rule for prescription drug products to require labeling that includes a summary of risk, a discussion of the data supporting that summary, and relevant information to help health care providers make prescribing decision and counsel women about the use of drugs during pregnancy. Pregnancy categories A, B, C, D and X are being phased out.

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