Asenapine is an atypical neuroleptic and is one of the psychotropic drugs. As a medicinal agent, asenapine is used for psychoses such as bipolar disorder type I. 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 may only be administered to adults.
What is asenapine?
As a medicinal agent, asenapine is used to treat psychosis such as bipolar disorder type I. Asenapine is a chemical, tetracyclic (four-ring) compound of ozepane and benzene, pyrrolidine, and chlorine. The active medical ingredient was developed in the Netherlands, and processing into an antipsychotic is done in the United States. As a psychotropic drug, asenapine is one of the atypical neuroleptics. “Atypical” refers to the specificity of side effects as opposed to comparable drugs. In tablet form with compressed salt, the drug has been on the market in Europe under the name Sycrest as a prescription medication for adults since the end of 2010. Sycrest is prescribed for psychosis with pronounced mania, such as bipolar I disorder. One sublingual tablet of Sycrest contains either 5 or 10 milligrams of asenapine.
Pharmacologic effects
The exact mode of action of asenapine is not clearly established in pharmacological and medical research. Attempts by scientists to explain it are based on conjecture. According to scientific studies, what triggers asenapine where and why in the brain can be approximated. It can be assumed that asenapine has an indirect rather than direct effect due to an antagonistic effect (one substance cancels out the effect of another): the chemical compound positively reverses the polarity of other substances that have a negative effect in the brain. To this end, asenapine docks with certain receptors and influences them. In this way, the action of neurotransmitters such as dopamine and serotonin can be directed in the desired direction by signals from asenapine. For example, the neurological signal for restlessness is reversed to fatigue. To be highly effective in the brain, the bioavailability (usability) of the drug must be maintained during transport through the body: When asenapine is taken orally (swallowed), less than 2 percent of the active ingredient arrives in the brain as its destination. Bioavailability can be increased to 35 percent by direct absorption through the oral mucosa: Asenapine is transported more quickly and without loss. Therefore, asenapine is commercially available as a sublingual tablet to be placed under the tongue.
Medicinal use and application
Asenapine is prescribed as a neuroleptic primarily for bipolar I disorder (formerly manic-depressive illness) during moderate to severe phases of mania. Insomnia and restlessness are dampened by administration of asenapine, as are strong irritability, overactivity, racing thoughts and slurred speech. The drug is to be taken in the morning and in the evening as prescribed by the doctor. The sublingual tablet is to be placed under the tongue directly from the package with dry hands. The salt with the drug pressed into the tablet quickly dissolves in the oral mucus and quickly enters the bloodstream. After taking the tablet, the patient must not eat or drink for ten minutes to improve the effect. The effect of asenapine is immediate and long-lasting. 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. For seniors 65 and older, dementia patients, and pregnant and breastfeeding women, medical experts advise against use due to uncertainty of effect based on a lack of scientific studies.
Risks and side effects
As an atypical neuroleptic, asenapine has different side effects than typical neuroleptics. For example, motor agitation and twitching are rare side effects after taking asenapine. Very common are increased urge to eat with weight gain, as well as fatigue and listlessness. Anxiety and dejection are other side effects. Dizziness, numbness of the mouth and impaired sense of taste may occur. Weaker side effects include uncontrolled movements, as in Parkinson’s disease, and an increased urge to move. Some patients complain of numbness in the arms and legs and stiff muscles.Laboratory tests show an increase in liver values due to asenapine. Patients with severe liver dysfunction are advised not to take it.
