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Asenapine – Effect, Application & Risks

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Asenapine is an atypical neuroleptic and is one of the psychotropic drugs . Asenapine is used as a medical agent in psychoses such as bipolar type I disorder. The drug is manufactured in the USA. In Europe, asenapine, available in the form of sublingual tablets (to be placed under the tongue), has been marketed under the brand name Sycrest® since 2010. The drug requires a prescription and can only be administered to adults.

What is asenapine?

Asenapine is a chemical tetracyclic (four ring) compound of ocepane and benzene, pyrrolidine and chlorine. The medicinal substance was developed in the Netherlands and processed into an antipsychotic in the USA.

Asenapine is one of the atypical neuroleptics. “Atypical” refers to the peculiarity of the side effects in contrast to comparable drugs.

In tablet form with pressed salt, the drug has been on the market in Europe under the name Sycrest® as a prescription drug for adults since the end of 2010. Sycrest® is prescribed for psychoses with pronounced manias such as bipolar I disorder. A Sycrest® sublingual tablet contains either 5 or 10 milligrams of asenapine.

Pharmacological action

The exact mode of action of asenapine has not been clearly established in pharmacological and medical research. Scientists’ attempts at explanations are based on assumptions. What asenapine triggers where and why in the brain can be approximately understood according to scientific studies.It can be assumed that asenapine has an indirect instead of a direct effect through an antagonistic effect (one substance neutralizes the effect of another): the chemical compound reverses the polarity of other substances that have a negative effect in the brain. To do this, asenapine docks with certain receptors and influences them.

In this way, the effects of messenger substances such as dopamine and serotonin can be steered in the desired direction by signals from asenapine. For example, the neurological signal for restlessness is reversed to become tired .

In order to be able to have a high-level effect in the brain, the bioavailability (usability) of the drug must be maintained during transport through the body: When asenapine is taken orally (swallowed down), less than 2 percent of the active substance arrives in the brain as its destination. The bioavailability can be increased to 35 percent by direct absorption through the oral mucosa : the asenapine is transported faster and with less loss. Therefore, asenapine is marketed as a sublingual tablet to be placed under the tongue.

Medical Application & Use

Asenapine is prescribed as a neuroleptic, especially for bipolar I disorders (formerly: manic-depressive illness) during moderate to severe phases of mania. Insomnia and restlessness are dampened by doses of asenapine, as is severe irritability , over-activity, racing thoughts and confused speech .

The drug is to be taken in the morning and evening as prescribed by the doctor. The sublingual tablet should be placed under the tongue straight from the packaging with dry hands . The salt with the medicinal substance pressed into a tablet quickly dissolves in the oral mucus and quickly enters the bloodstream . After ingestion, the patient is not allowed to eat or drink for ten minutes to improve the effect.

The effect of asenapine occurs promptly and sustainably. According to studies, the first positive symptoms appear on the second day after ingestion and last for several weeks.

The prescription is approved for adults and excludes children and adolescents. Doctors advise against taking it for seniors over 65 years of age, people with dementia , and pregnant and breastfeeding women due to the lack of scientific studies due to the uncertainty of its effectiveness.

Risks & side effects

As an atypical neuroleptic, asenapine has different side effects than typical neuroleptics. Motor restlessness and twitching are rare side effects after taking asenapine.Increased urge to eat with weight gain as well as tiredness and listlessness can be observed very often . Anxiety and depression are other side effects. Dizziness and numbness in the mouth and disturbed sense of taste may occur .

Uncontrolled movements as in Parkinson’s disease and an increased urge to move occur as weaker side effects . Some patients complain of numbness in their arms and legs and stiff muscles. Laboratory tests show that asenapine increases liver enzymes. Patients with severe liver dysfunction are advised not to take it.

Lisa Newlon
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.