Indications

Amisulpride is indicated for the treatment of acute and chronic schizophrenic disorders, in which positive symptoms (such as delusions, hallucinations, and thought disorders) and/or negative symptoms (such as blunted affect, emotional and social withdrawal) are prominent, including patients characterized by predominant negative symptoms.

Composition

Pharmacology

Amisulpride belongs to a group of medicines called antipsychotics, which help to control the symptoms of a mental illness called schizophrenia. Amisulpride binds selectively to the human dopaminergic D2 and D3 receptor without any affinity for all, D4 and D5 receptor subtypes. Unlike classical and atypical neuroleptics amisulpride displays low affinity for serotonin, a-adrenergic, histamine receptor subtypes, muscarinic receptors and sigma sites. In addition, it does not induce catalepsy and it does not produce D2 hypersensitivity after repeated treatment. Moreover, it preferentially blocks pre-synaptic D2/D3 dopamine receptors, producing dopamine release responsible for its disinhibitory effects.

Dosage & Administration

Oral dose : For acute psychotic episodes, oral doses between 400 mg/day and 800 mg/day are recommended in individual cases. The daily dose may be increased up to 1200 mg/day. Doses above 800 mg/day have not been shown to be superior to lower doses and may increase the incidence of adverse events. No specific titration is required when initiating the treatment with Amisulpride. Doses should be adjusted according individual response. Dose should preferably be administered before meal. For patients with mixed positive negative symptoms, doses should be adjusted to obtain optimal control of positive symptoms. Maintenance treatment should be established individually with the minimally effective dose. For patients characterized by predominant negative symptoms, oral doses between 50 mg/day and 300 mg/day are recommended. Doses should be adjusted individually. Injectable dose : The recommended injectable adult dosage of Amisulpride and infusion rate by indication is shown in the table below: Prevention of postoperative nausea and vomiting : 5 mg as a single intravenous injection infused over 1 to 2 minutes at the time of induction of anesthesia. Treatment of postoperative nausea and vomiting : 10 mg as a single intravenous injection infused over 1 to 2 minutes in the event of nausea and/or vomiting after a surgical procedure.

Contraindications

Amisulpride is contraindicated if hypersensitivity to the active ingredient or to other ingredients of the drug occurs. Concomitant prolactin-dependent tumours, e.g. pituitary gland prolactinomas and breast cancer. It is also contraindicated in pheochromocytoma, children up to puberty, pregnancy & lactation. In combination with the following medication: Class-I anti-arrhythmic agents such as quinidine and disopyramide Class-II anti-arrhythmic agents such as amiodarone and sotalol Other medications such as bepridil, cisapride, sultopride, thioridazine, metha done, intravenous erythromycin intravenous vincamine, halofantrine, pentamidine, sparfloxacin & levodopa. In hepatic impairment amisulpride may be contraindicated to avoid the possible risk of adverse events due to an influence of the disease on amisulpride metabolism.

Side Effects

Common : Trembling, muscle stiffness or spasm, slow movement, producing more saliva than usual or feeling restless. Movements that patient cannot control, mainly of the head, neck, jaw or eyes. Difficulty sleeping (insomnia) or feeling anxious or agitated, feeling drowsy or sleepy, constipation, feeling or being sick, dry mouth, putting on weight, low blood pressure, dizziness, difficulty reaching orgasm, blurred vision, Increased blood levels of prolactin. Rare : Movements that you cannot control, mainly of the face or tongue, Osteoporosis (condition, when your bones are more likely to break) or osteopenia (bone weakening), aspiration pneumonia (a type of lung infection that occurs when food, saliva, liquids, or vomit is breathed into the lungs or airways leading to the lungs, instead of being swallowed into the esophagus and stomach.

Pregnancy & Lactation

The safety of amisulpride during human pregnancy has not been established, and therefore amisulpride is not recommended during pregnancy and in women of child bearing potential not using effective contraception, unless the benefits justify the potential risks and the administered dose and duration of treatment should be as low and as short as possible. Amisulpride has been found in breast milk of treated women. Breast-feeding is contraindicated.

Precautions & Warnings

Neuroleptic Malignant Syndrome (NMS) is a potentially fatal syndrome that has been reported in association with anti-psychotic medicines, including amisulpride. Neuroleptic malignant syndrome is characterized by hyperthermia, muscle rigidity, autonomic instability, and elevated CPK, may occur. In the event of any symptoms which could suggest NMS particularly with high daily doses, all antipsychotic medicines including Amisulpride should be discontinued. Amisulpride can lower the seizure threshold. Therefore patients with a history of seizures should be closely monitored during amisulpride therapy. Withdrawal symptoms have been described after abrupt cessation of high therapeutic doses of antipsychotic drugs. The emergence of involuntary movement disorders (such as akathisia, dystonia and dyskinesia) has been reported with amisulpride. Therefore gradual withdrawal of amisulpride is advisable. Amisulpride causes an increase in plasma prolactin levels. This may result in galactorrhoea, amenorrhoea, gynaecomastia, breast pain, orgasmic dysfunction and impotence.

Therapeutic Class

Atypical neuroleptic drugs

Storage Conditions

Store below 30°C in a cool and dry place, away from light. Keep all the medicine out of the reach of the children.