Asenapine

What is Asenapine?

• Asenapine (Saphris) is an atypical antipsychotic used to treat schizophrenia and acute mania associated with bipolar disorder.

Asenapine

Asenapine-3D-balls

Asenapine Structural Formulae V.2

What are the uses of this medicine?

Asenapine (Saphris) is used:

• for the treatment of schizophrenia.
• for the acute treatment of manic or mixed episodes associated with bipolar I disorder.
• as adjunctive therapy with either lithium or valproate for the acute treatment of manic or mixed episodes associated with bipolar I disorder.

How does this medicine work?

• Asenapine (a sen' a peen) is a second generation antipsychotic agent which appears to act as a dopamine type 2 (D2) and serotonin (5-HT)-2A receptor antagonist.
• It is a somewhat unique antipsychotic agent that has a tetracyclic structure similar to that of mirtazapine, and it is administered as a sublingual tablet, being poorly absorbed by the oral route.
• Several randomized controlled trials have shown that sublingual asenapine improves symptoms of schizophrenia with effects comparable to risperidone and olanzapine.
• It also has beneficial activity in acute manic and mixed episodes associated with bipolar 1 disorder.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• with a known hypersensitivity to the product.

What drug interactions can this medicine cause?

• Caution should be used when it is taken in combination with other centrally acting drugs or alcohol.
• Cautiously approach coadministration of SAPHRIS with Fluvoxamine (strong CYP1A2 inhibitor) and Paroxetine (CYP2D6 substrate and inhibitor).

Is this medicine FDA approved?

• Asenapine was approved for use in the United States in 2009 and is available in sublingual tablets of 2.5, 5 and 10 mg under the brand name Saphris.

How should this medicine be used?

Recommended dosage: Schizophrenia:

• Usual Dose for Acute Treatment in Adults:

The recommended starting and target dose of SAPHRIS is 5 mg given twice daily. 

• Maintenance Treatment:

Efficacy was demonstrated with SAPHRIS in a maintenance trial in patients with schizophrenia. The starting dose in this study was 5 mg twice daily with an increase up to 10 mg twice daily after 1 week based on tolerability.

Bipolar Disorder:

• Monotherapy:

The recommended starting dose of SAPHRIS, and the dose maintained by 90% of the patients studied, is 10 mg twice daily. The dose can be decreased to 5 mg twice daily if warranted by adverse effects or based on individual tolerability.

• Adjunctive Therapy:

The recommended starting dose of SAPHRIS is 5 mg twice daily when administered as adjunctive therapy with either lithium or valproate. Depending on the clinical response and tolerability in the individual patient, the dose can be increased to 10 mg twice daily.

Administration:

• Do not swallow tablet.
• SAPHRIS sublingual tablets should be placed under the tongue and left to dissolve completely.
• The tablet will dissolve in saliva within seconds.
• Eating and drinking should be avoided for 10 minutes after administration.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Sublingual tablets: 5 mg and 10 mg

Sublingual tablets, black cherry flavor: 5 mg and 10 mg

This medicine is available in fallowing brand namesː

• SAPHRIS

What side effects can this medication cause?

The most common side effects of this medicine include: in case of Schizophrenia:

• akathisia
• oral hypoesthesia
• somnolence

In case of Bipolar Disorder (Monotherapy):

• somnolence
• dizziness
• extrapyramidal symptoms other than akathisia
• weight increased

In case of Bipolar Disorder (Adjunctive):

• somnolence
• oral hypoesthesia

What special precautions should I follow?

• An increased incidence of cerebrovascular adverse events (e.g., stroke, transient ischemic attack) has been seen in elderly patients with dementia-related psychoses treated with atypical antipsychotic drugs.
• A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with administration of antipsychotic drugs, including SAPHRIS. Manage with immediate discontinuation and close monitoring.
• A syndrome of potentially irreversible, involuntary, dyskinetic movements can develop in patients treated with antipsychotic drugs. Discontinue if clinically appropriate.
• Increases in weight have been observed in pre-marketing clinical trials with SAPHRIS. Patients should receive regular monitoring of weight.
• Hypersensitivity reactions, including anaphylaxis and angioedema, have been observed in patients treated with asenapine.
• SAPHRIS may induce orthostatic hypotension and syncope in some patients, especially early in treatment, because of its α1-adrenergic antagonist activity. Use with caution in patients with known cardiovascular or cerebrovascular disease, and in antipsychotic-naïve patients.
• In clinical trial and postmarketing experience, events of leukopenia/neutropenia have been reported temporally related to antipsychotic agents, including SAPHRIS. Patients with a pre-existing low white blood cell count (WBC) or a history of leukopenia/neutropenia should have their complete blood count (CBC) monitored frequently during the first few months of therapy and SAPHRIS should be discontinued at the first sign of a decline in WBC in the absence of other causative factors.
• At these doses, SAPHRIS was associated with increases in QTc interval ranging from 2 to 5 msec compared to placebo. avoid use with drugs that also increase the QT interval and in patients with risk factors for prolonged QT interval.
• Like other drugs that antagonize dopamine D2 receptors, SAPHRIS can elevate prolactin levels, and the elevation can persist during chronic administration.
• Seizures were reported in patients treated with doses of 5 mg and 10 mg twice daily of SAPHRIS. Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.
• Somnolence was reported in patients treated with SAPHRIS.
• Disruption of the body's ability to reduce core body temperature has been attributed to antipsychotic agents.
• The possibility of a suicide attempt is inherent in schizophrenia and bipolar disorder. Closely supervise high-risk patients.
• Esophageal dysmotility and aspiration have been associated with antipsychotic drug use. Dysphagia was reported with SAPHRIS. SAPHRIS is not indicated for the treatment of dementia-related psychosis, and should not be used in patients at risk for aspiration pneumonia.
• Monitor patients for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia, and weakness. Monitor glucose regularly in patients with, and at risk for, diabetes.
• Patients should be cautioned about performing activities requiring mental alertness, such as operating hazardous machinery or operating a motor vehicle, until they are reasonably certain that SAPHRIS therapy does not affect them adversely.
• Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy, but has not been linked to instances of clinically apparent acute liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• agitation and confusion

Management of overdosage:

• There is no specific antidote to SAPHRIS.
• An electrocardiogram should be obtained and management of overdose should concentrate on supportive therapy, maintaining an adequate airway, oxygenation and ventilation, and management of symptoms.
• Hypotension and circulatory collapse should be treated with appropriate measures, such as intravenous fluids and/or sympathomimetic agents.
• In case of severe extrapyramidal symptoms, anticholinergic medication should be administered.
• Close medical supervision and monitoring should continue until the patient recovers.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies of SAPHRIS in pregnant women.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• Asenapine Maleate

Inactive ingredients:

• gelatin
• mannitol

Who manufactures and distributes this medicine?

Manufactured for: Merck Sharp & Dohme Corp., a subsidiary of MERCK & CO., INC., Whitehouse Station, NJ, USA

Manufactured by: Catalent UK Swindon Zydis Ltd., Blagrove, Swindon, Wiltshire, UK

What should I know about storage and disposal of this medication?

• Store at 15°-30°C (59°-86°F).

Antipsychotic agents

First Generation

• Phenothiazines
  • Chlorpromazine, Fluphenazine, Perphenazine, Prochlorperazine, Thioridazine, Trifluoperazine

• Other
  • Haloperidol, Lithium, Loxapine, Molindone, Pimozide

Second Generation (Atypicals)

• Aripiprazole, Asenapine, Brexpiprazole, Cariprazine, Clozapine, Iloperidone, Lurasidone, Olanzapine, Paliperidone, Pimavanserin, Quetiapine, Risperidone, Ziprasidone

• Dailymed label info on Asenapine
• FDA Asenapine

Asenapine Resources
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