Amisure IV Infusion

Amisure 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.

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.

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.

With medicine: Consumption of alcohol while taking this medicine can cause CNS depression characterized by confusion, lack of focus, anxiety, drowsiness etc. As the risk of adverse effects are increasingly high uptake of alcohol along with Amisure, so uptake of alcohol while taking this medicine should be avoided. Drug Interaction may occur with Diltiazem, Pregabalin, Tramadol, Amiodarone, Quinidine, Bromocriptine, Ropinirole. Concomitant use of Amisure with other anti-psychotics may increase the risk of developing neuroleptic malignant syndrome. Co-administration of Amisure and clozapine may lead to an increase in plasma levels of Amisure. Amisure may enhance the effects of the following medicines:

• CNS depressants including narcotics, anaesthetics, analgesics, sedative H1 antihistamines, barbiturates, benzodiazepines and other anxiolytic medicines, clonidine and derivatives.
• Antihypertensive medicines and other hypotensive medications.

With food and others: Can be taken with or without food causes no interaction.

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.

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.

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.

Neuroleptic Malignant Syndrome (NMS) is a potentially fatal syndrome that has been reported in association with anti-psychotic medicines, including Amisure. 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 Amisure should be discontinued. Amisure can lower the seizure threshold. Therefore patients with a history of seizures should be closely monitored during Amisure 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 Amisure. Therefore gradual withdrawal of Amisure is advisable. Amisure causes an increase in plasma prolactin levels. This may result in galactorrhoea, amenorrhoea, gynaecomastia, breast pain, orgasmic dysfunction and impotence.

Use in elderly: Amisure should be used with particular caution because of a possible risk of hypotension or sedation.

Use in children & adolescents: Efficacy and safety of Amisure in children and adolescents under 18 years of age have not been established. If absolutely required, treatment of adolescents from 15 to 18 years of age must be initiated and performed physician experienced in treating schizophrenia in this age group.

Use in hepatic impairment: Since Amisure is weakly metabolized, a dosage reduction should not be necessary.

Patients with kidney problems: Treatment should be given at a lower dose. This may be half or a third of the usual daily dose, depending on how well your kidneys are working.

Use in renal impairment: Amisure is eliminated by the renal route. In renal insufficiency, the dose should be reduced to half in patients with creatinine clearance (CRCL) between 30-60 mL/min and to a third in patients with CRCL between 10-30 mL/min. As there is no experience in patients with severe renal impairment (CRCL<10 mL/min) particular is recommended in these patients.

Experience with Amisure in overdosage is limited. Exaggeration of the known pharmacological and effects of Amisure have been reported. These may include drowsiness, sedation, hypotension, extrapyramidal symptoms and coma. Fatal outcomes have been reported mainly in combination with other psychotropic agents.

Atypical neuroleptic drugs

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