The active ingredient amisulpride is a benzamide and sulpiride derivative. It is marketed under several names and is used as an atypical neuroleptic for schizophrenia therapy. Amisulpride is available by prescription.
What is amisulpride?
Amisulpride is sold under several names and is used as an atypical neuroleptic for schizophrenia therapy. The full chemical name for amisulpride is (RS)-4-amino-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-(ethylsulfonyl)-2-methoxybenzamide. Amisulpride is a dopamine receptor antagonist and is used as a so-called racemate for the therapy of acute and chronic schizophrenia. In individual cases, therapeutic success has also been observed in Tourette’s syndrome. Amisulpride is available as 50 mg, 100 mg, 200 mg and 400 mg tablets and as a 1 ml oral solution containing 100 mg of the active substance. The treating physician decides the dosage form and dose. The neuroleptic amisulpride has an antipsychic and sedative effect. Unlike most neuroleptics, benzides such as amisulpride do not have a depressant effect, but rather a mood-lifting and activating effect. Taking amisulpride causes fewer side effects than common neuroleptics. In particular, phenomena such as movement disorders or fatigue occur much less frequently.
Pharmacologic effects
Chemically, amisulpride belongs to the group of substituted benzamides and it is a derivative of sulpiride. Neuroleptics interfere with neural activity in the brain by altering the concentrations of neurotransmitters in the brain. This affects perception and emotional life. While most of the typical neuroleptics act on the neurotransmitter dopamine and thus on the corresponding receptors, amisulpride, as an atypical neuroleptic, has an additional inhibitory effect on other neurotransmitters and their binding sites in the brain. This also includes serotonin. As a drug for psychoses such as schizophrenia, the atypical neuroleptic amisulpride has two effects:
1. amisulpride affects “positive symptomatology”: it dampens delusions. 2. amisulpride also influences “negative symptomatology”: it reduces effects such as a patient’s social withdrawal, isolation, decreased drive, and flattening of emotions. Amisulpride thus has an increased mood-lifting and activating effect, rather than a fatiguing and depressant effect like typical neuroleptics. The active ingredient amisulpride can interact with other centrally acting drugs and enhance their effects. On levodopa, an anti-Parkinsonian drug, amisulpride exerts an opposite effect, weakening its effect. Occasionally, again, during therapy with amisulpride, supplemental administration of an anti-Parkinson’s drug is recommended to relieve side effects such as impaired motor abilities, body stiffness, or cramping. Other possible side effects of amisulpride include: Tardive dyskinesia, hyperprolactinemia, menstrual irregularities, impotence, loss of libido, gastrointestinal distress, epileptic seizures, hypotension, and prolongation of the cardiac QT interval. Extrapyramidal motor side effects rarely occur with amisulpride treatment compared with other neuroleptics.
Medical Application and Use
Amisulpride as an atypical neuroleptic is used for the treatment of schizophrenia as well as other psychoses. These are, in detail:
- Schizophrenia – acute and chronic.
- Psychoses, delusions, thought disorders, hallucinations.
- Personality disorders
As a non-depressant and for it the mood lifting and activating drug amisulpride counteracts this in a positive way in behavioral forms such as social distrust to hostility – especially towards strangers, social withdrawal, impoverished or flattened emotional life and lack of drive. Under therapy with amisulpride, patients who have hitherto been very lethargic manage to free themselves from their self-imposed isolation due to a lack of drive by approaching other people with interest again. Despite an indication also for acute schizophrenia, amisulpride has limited potential specifically in this setting.
Risks and side effects
In certain cases, amisulpride is contraindicated for:
- Parkinson’s disease, as it counteracts the drug Lepodova.
- Alcohol abuse
- Severely impaired renal function
- Allergy to the active substance amisulpride
- Combination with medications that can cause serious cardiac arrhythmias
It should also be noted that amisulpride can potentiate the effects of other psychotropic drugs. Children and adolescents under 15 years of age are excluded from amisulpride prescription. Similarly, use is discouraged in those 15 to 18 years of age and over 65 years of age. Amisulpride should not be taken during pregnancy or lactation; if necessary, breastfeeding should be continued for that length of time. As with other neuroleptics, malignant neurologic syndrome may occur with amisulpride; therefore, if appropriate symptoms such as muscle rigidity, high fever, autonomic disturbances (pallor, sweating, and circulatory instability), and clouding of consciousness occur, contact a physician immediately and discontinue the drug.