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Asenapine

Brands and Forms

  • Saphris
    • sublingual dissolving tablet: 5mg, 10mg
  • Sycrest
    • sublingual dissolving tablet: 5mg, 10mg

Uses of Asenapine

Asenapine is indicated in the treatment of Schizophrenia and Bipolar Disorder, and may also be used for treating other Psychotic Disorders, Depressive Disorders, PTSD, OCD, and Tic Disorder.

Asenapine can also be used in the management of behavioral disturbances, such as agitation and impulsivity, that can occur in various conditions like Impulse-Control Disorders, Disruptive Behavior Disorders, and Borderline Personality Disorder.

How Asenapine Works

Asenapine is an Atypical Antipsychotic. Its mechanism of action is not completely understood, but it has affinity for various serotonergic, dopamingeric and adrenergic receptors in the central nervous system. In particular, it functions as an antagonist of D2 and 5-HT2A receptors.

Cautions when Using Asenapine

In elderly individuals with Dementia, use of Antipsychotics has been associated with increased rates of sudden death. It is unclear whether the antipsychotic use is a cause, or simply a marker, of deteriorating health in these individuals.

Weight gain and metabolic side-effects (elevated glucose, lipids and cholesterol) can be pronounced in some individuals. Regular monitoring of these metabolic parameters is required when on Asenapine.

Individuals with Parkinson disease or Lewy-Body Dementia may have increased sensitivity to Asenapine, which may manifest as confusion, obtundation, severe extrapyramidal symptoms, and neuroleptic malignant syndrome.

Use with caution in people at risk for seizures or aspiration pneumonia.

People using Asenapine should become familiar with its effects before driving or operating heavy machinery.

Dosing of Asenapine

Asenapine is usually started at 5mg twice daily, and can be increased to 10mg twice daily after a week, if necessary.

In some situations, such as acute Mania, Asenapine can be started directly at 10mg twice daily.

It is important that when taking this medication, the tablet be placed under the tongue and allowed to dissolve completely; it should not be crushed, chewed, or swallowed, and one should not eat or drink for 10 minutes after taking a dose.

When wanting to stop this medication, the dose should be decreased gradually over a period of 4 weeks or more.

Onset of action

Symptoms of Mania and Psychosis can improve within 1 week of use, but full therapeutic effect may take several weeks. If there is no significant effect after 4-6 weeks, including a couple of weeks at doses above 4mg/day, then it may not work at all.

Acute agitation can improve after a single dose.

For other conditions, 4-6 weeks may be needed to see a therapeutic effect.

Kidney impairment

No dose adjustment required

Liver impairment

Asenapine should be avoided in people with severe liver failure, as its exposure can be up to 7 times higher than in healthy individuals.

Side-effects of Asenapine

Below is a list of most of the reported side-effects of Asenapine. Most of these side-effects occur in only a minority of individuals, and many also resolve with time while the medication is continued.

Cardiovascular: Orthostatic hypotension; hypertension (rare); cardiac arrhythmias and QTc prolongation (rare).

Central Nervous System: somnolence; insomnia; extrapyramidal symptoms including akathisia; headaches; dizziness; faintness; fatigue; depression; irritability; seizures (rare); stroke (rare).

Endocrine/Metabolic: Weight gain; metabolic syndrome (insulin resistance, elevated blood sugars, hyperlipidemia and hypercholesterolemia); elevated prolactin; breast pain, enlargement, or milk production in men and women; trouble conceiving; hyperthermia; SIADH.

Gastrointestinal: Constipation; vomiting; stomach upset; increased appetite; salivary hypersecretion (drooling); dry mouth; toothache.

Genitourinary: urinary incontinence; amenorrhea; ejaculation failure; erectile dysfunction; impotence; urinary frequency; priapism.

Hematologic: leukopenia and neutropenia (rare).

Musculoskeletal: muscle stiffness; muscle pains; muscle spasms; neuroleptic malignant syndrome (rare).

Psychiatric: anxiety; depression; irritability.

Respiratory: pulmonary embolism (rare).

Common side-effects of Asenapine

Somnolence/drowsiness, insomnia, headaches, dizziness, extrapyramidal symptoms including akathisia, constipation, vomiting, increased appetite, weight gain, metabolic syndrome (elevated blood sugars, lipids and cholesterol).

Rare but serious side-effects of note of Asenapine

  • severe hypoglycemia with associated ketoacidosis
  • increased risk of sudden death in elderly individuals with Dementia.
  • neuroleptic malignant syndrome
  • cardiac arrhythmias including QTc prolongation
  • seizures

Asenapine overdose

Agitation and confusion, extrapyramidal symptoms, sedation, and cardiac arrhythmias (bradycardia, supraventricular complexes, intraventricular conduction delay).

Asenapine and pregnancy

Category C: some animal studies show adverse effects at very high doses, but no controlled human studies have been done; should only be used in pregnancy if clearly needed and if benefits outweigh potential risks.

Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk of extrapyramidal and/or withdrawal symptoms following delivery.

Asenapine, weight gain and metabolic syndrome

About 15% of people taking Asenapine will gain about 7% of their total body weight within a year of starting the medication. Metabolic side-effects, including elevated glucose and lipids can also occur, which in the long-term increase the risk for heart disease and vascular problem.

See here for further information on these side-effects, and how they can be managed.

Medical Monitoring for Asenapine

Monitoring for weight gain and a metabolic syndrome requires the following measures to be taken prior to starting the medication, then monthly for the first 3 months of use, and then every 3 months:

  • Body Mass Index (BMI)
  • waistline circumference at umbilicus
  • blood pressure
  • fasting blood glucose
  • fasting blood lipids and cholesterol

To monitor for elevated prolactin, prolactin levels should be measured prior to starting the medication, and then one month after starting and after every dose increase.

Drug Interactions with Asenapine

  • No food or drink should be consumed within 10 minutes of taking Asenapine.
  • Asenapine may enhance the effects of some antihypertensives.
  • Avoid combining with medications that can prolong the QTc interval, including Gatifloxacin, Moxifloxacin, Chlorpromazine, Thioridazine, Ziprasidone, class IA antiarrhythmic agents (eg. Procainamide, Quinidine), class III antiarrhythmic agents (eg. Amiodarone, Sotalol).
  • Asenapine blood concentrations can be reduced by Paroxetine.
  • Asenapine blood concentrations can be increased by Fluvoxemine, Imipramine.
  • Asenapine can reduce blood concentrations of dextromethorphan
  • Asenapine can increase blood concentrations of Paroxetine.