Asenapine

Bipolar Disorder, Schizophrenia

DRUG STATUS

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Approvals

US(FDA), UK(BNF)

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Essential Medicine

NO

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Teratogenicity

Unlisted

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Pharmaceutical Class

Atypical Antipsychotic

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Drug Ingredient

Asenapine

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Summary

  • Asenapine is used to treat schizophrenia and bipolar I disorder in adults, and manic or mixed episodes in bipolar I disorder in children aged 10 years and older.

  • Asenapine works by blocking certain receptors in the brain, including dopamine D2 and serotonin 5HT2A receptors. This helps to balance neurotransmitters and reduce symptoms such as hallucinations, mood swings, and disorganized thinking.

  • For adults, the usual dose for schizophrenia is 5 mg twice daily. For bipolar I disorder, the dose ranges from 5 mg to 10 mg twice daily. In children aged 10 to 17 years, the starting dose is 2.5 mg twice daily. Asenapine is taken as a sublingual tablet, placed under the tongue to dissolve.

  • Common side effects of Asenapine include drowsiness, weight gain, and oral numbness. Serious adverse effects can include neuroleptic malignant syndrome, tardive dyskinesia, and metabolic changes like high blood sugar.

  • Asenapine carries a risk of increased mortality in elderly patients with dementia-related psychosis and is not approved for treating this condition. It should not be used in patients with severe liver impairment or those with a history of hypersensitivity to the drug.

Indications and Purpose

What is Asenapine used for?

Asenapine is indicated for the treatment of schizophrenia in adults and for the treatment of manic or mixed episodes associated with bipolar I disorder in adults and children aged 10 years and older. It helps manage symptoms like mood swings, hallucinations, and disorganized thinking.

How does Asenapine work?

Asenapine works by blocking certain receptors in the brain, including dopamine D2 and serotonin 5-HT2A receptors. This action helps to balance neurotransmitters, reducing symptoms of schizophrenia and bipolar disorder such as hallucinations, mood swings, and disorganized thinking.

Is Asenapine effective?

Asenapine's effectiveness in treating schizophrenia and bipolar I disorder has been demonstrated in clinical trials. In trials, it showed superior efficacy to placebo in reducing symptoms of mania and schizophrenia. Maintenance of efficacy was also demonstrated in long-term studies, supporting its use for ongoing management of these conditions.

How does one know if Asenapine is working?

The benefit of Asenapine is evaluated through regular follow-up appointments with your doctor, who will assess symptom control and side effects. Blood tests may be conducted to monitor metabolic changes, and weight should be checked regularly to ensure the medication is working effectively and safely.

Directions for Use

What is the usual dose of Asenapine?

For adults, the usual dose of Asenapine for schizophrenia is 5 mg twice daily. For bipolar I disorder, the dose ranges from 5 mg to 10 mg twice daily. In children aged 10 to 17 years with bipolar I disorder, the starting dose is 2.5 mg twice daily, which can be increased to 5 mg or 10 mg twice daily based on response and tolerability.

How do I take Asenapine?

Asenapine is taken as a sublingual tablet, placed under the tongue to dissolve completely. It should not be swallowed, chewed, or taken with food or drink for at least 10 minutes after administration. There are no specific food restrictions, but avoid eating or drinking immediately after taking the medication.

For how long do I take Asenapine?

Asenapine is typically used as a long-term treatment to manage symptoms of schizophrenia and bipolar I disorder. The duration of use depends on the individual's response to the medication and the doctor's recommendation. It is important to continue taking Asenapine even if you feel well, and not to stop without consulting your doctor.

How long does it take for Asenapine to start working?

Asenapine may start to show effects within a few days, but it can take several weeks to experience the full benefits. It is important to continue taking the medication as prescribed and attend follow-up appointments to monitor progress and adjust the dosage if necessary.

How should I store Asenapine?

Asenapine should be stored at room temperature, between 20°C to 25°C (68°F to 77°F), and kept in its original packaging to protect from moisture and light. It should be kept out of reach of children and not stored in the bathroom to avoid exposure to humidity.

Warnings and Precautions

Who should avoid taking Asenapine?

Key warnings for Asenapine include increased mortality in elderly patients with dementia-related psychosis, risk of neuroleptic malignant syndrome, tardive dyskinesia, and metabolic changes like hyperglycemia. It is contraindicated in patients with severe hepatic impairment and those with a history of hypersensitivity to the drug.

Can I take Asenapine with other prescription drugs?

Asenapine can interact with antihypertensive drugs, potentially enhancing their effects. It may also interact with strong CYP1A2 inhibitors like fluvoxamine, increasing Asenapine levels. Caution is advised when used with other CNS depressants, as it may enhance sedative effects. Always inform your doctor of all medications you are taking.

Can I take Asenapine with vitamins or supplements?

There are no specific known interactions between Asenapine and vitamins or supplements. However, it is important to inform your doctor about all supplements you are taking, as they can provide guidance on any potential interactions based on your overall health and medication regimen.

Can Asenapine be taken safely while pregnant?

Asenapine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. There is a risk of extrapyramidal and/or withdrawal symptoms in newborns exposed during the third trimester. There is limited human data, so consult your doctor for personalized advice if you are pregnant or planning to become pregnant.

Can Asenapine be taken safely while breastfeeding?

It is not known if Asenapine is excreted in human milk, but it is excreted in rat milk. Due to potential risks to the infant, breastfeeding is not recommended while taking Asenapine. Discuss with your doctor the risks and benefits of continuing the medication while breastfeeding.

Is Asenapine safe for the elderly?

Elderly patients using Asenapine, especially those with dementia-related psychosis, are at an increased risk of death. Asenapine is not approved for treating dementia-related psychosis. Elderly patients should be monitored closely for side effects like orthostatic hypotension and falls. Dosage adjustments may be necessary based on individual tolerance.

Is it safe to exercise while taking Asenapine?

Asenapine may cause dizziness, drowsiness, and fatigue, which can affect your ability to exercise safely. It is important to assess how the medication affects you before engaging in physical activities. Consult your doctor if you have concerns about exercising while taking Asenapine.

Is it safe to drink alcohol while taking Asenapine?

Drinking alcohol while taking Asenapine can worsen the side effects of the medication, such as drowsiness and dizziness. It is generally advised to avoid alcohol consumption while on this medication to ensure safety and effectiveness. Always consult with your doctor for personalized advice.