Amisulpride

Amisulpride is an atypical antipsychotic used for both acute and chronic schizophrenia. It selectively binds to human dopaminergic D2 and D3 receptors with no affinity for D1, D4 and D5 receptor subtypes. It blocks pre-synaptic D2/D3 dopamine receptors to increase dopamine release. With low affinity for serotonin, alpha-adrenergic and histamine receptors, it causes fewer side effects compared to classical antipsychotics.

Schizophrenia (acute and chronic) with prominent positive symptoms (delusions, hallucinations, thought disorders) and/or negative symptoms (blunted affect, social withdrawal).

Atypical Neuroleptic

Selective Dopamine D2/D3 Receptor Antagonist

Amisulpride is an atypical antipsychotic that selectively binds to dopaminergic D2 and D3 receptors. It blocks pre-synaptic D2/D3 receptors to increase dopamine release. With low affinity for serotonin, alpha-adrenergic and histamine receptors, it causes fewer side effects compared to classical antipsychotics. It does not induce catalepsy and does not produce D2 hypersensitivity after repeated use.

Amisulpride controls schizophrenia symptoms by blocking dopamine D2 and D3 receptors in the brain, reducing hallucinations, delusions, thought disorders (positive symptoms) and emotional withdrawal, social withdrawal (negative symptoms).

Oral: Acute psychotic episodes: 400-800 mg/day (divided doses), max 1200 mg/day. Mixed positive-negative symptoms: adjust based on positive symptom control. Predominant negative symptoms: 50-300 mg once daily. Elderly: dose reduction may be needed. Children (under 18): not recommended. Injection (PONV): Prevention: 5 mg IV (1-2 min) at anesthesia induction; Treatment: 10 mg IV (1-2 min) for nausea/vomiting.

May be taken before or after meals (preferably before meals). Take at the same time each day. Swallow tablet whole; do not chew. Renal adjustment: CrCl 30-60 mL/min: half dose; CrCl 10-30 mL/min: one-third dose.

If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.

Common: Tremor, muscle stiffness or spasm, slow movement, excess saliva, restlessness, uncontrolled movements (head, neck, jaw or eyes), insomnia, anxiety, agitation, drowsiness, constipation, nausea, vomiting, dry mouth, weight gain, low blood pressure, dizziness, blurred vision, increased prolactin. Rare: Neuroleptic Malignant Syndrome (NMS), seizures, osteoporosis, aspiration pneumonia.

Do not stop suddenly without consulting your doctor (withdrawal symptoms may occur). Caution while driving (drowsiness and dizziness). Avoid alcohol completely (increases CNS depression). Weight gain, blood sugar and cholesterol may increase; healthy diet and exercise are recommended. Dose adjustment needed in kidney disease. Do not use during pregnancy and breastfeeding.

Hypersensitivity to amisulpride; prolactin-dependent tumors (prolactinoma, breast cancer); pheochromocytoma; children before puberty; pregnancy and lactation; concomitant use with Class I and II antiarrhythmics.

CNS depressants (alcohol, narcotics, anesthetics, benzodiazepines): increased sedation. Antihypertensives: increased hypotensive effect. Other antipsychotics: increased risk of NMS. Clozapine: increased amisulpride plasma levels. Quinidine, amiodarone, sotalol: may prolong QT interval. Levodopa: reduced efficacy.

Alcohol consumption is strictly prohibited (increases CNS depression).

Pregnancy Category: C. Safety of amisulpride during pregnancy has not been established; use only if clearly needed with medical advice.

Pregnancy Category: C — always consult a doctor before taking during pregnancy.

Amisulpride is excreted in breast milk; use during breastfeeding is contraindicated.

Under 18 years: Safety and efficacy have not been established. If absolutely required, adolescents 15-18 years should be treated under the supervision of a physician experienced in schizophrenia.

Use with caution in elderly patients (higher risk of hypotension or sedation).

Renal impairment: CrCl 30-60 mL/min: half dose; CrCl 10-30 mL/min: one-third dose; CrCl <10 mL/min: caution required (no experience). Hepatic impairment: No dose adjustment needed (weakly metabolized).

Overdose symptoms: drowsiness, sedation, hypotension, extrapyramidal symptoms, coma. Treatment: symptomatic and supportive measures.

Store below 30C in a cool and dry place, protected from light. Keep out of reach of children.

C17H27N3O4S (Molecular weight: 369.48 g/mol)