Amipride200 mg

Amipride is an atypical antipsychotic (substituted benzamide) used mainly for the treatment of schizophrenia. Its use is classified below by strength of evidence.

Established / guideline-supported uses

• Acute and chronic schizophrenia — at higher oral doses, Amipride is effective against positive symptoms (hallucinations, delusions, thought disorder) and, at lower doses, against predominant negative symptoms (blunted affect, social withdrawal, apathy).
• Prevention and treatment of postoperative nausea and vomiting (PONV) in adults — an intravenous, low-dose formulation of Amipride is approved for this use, given alone or combined with an antiemetic of a different class.

Lower-dose / limited-evidence use

• In some countries, very low oral doses of Amipride (below the antipsychotic range) have been used for dysthymia and mild depressive states; this dosing context is different from schizophrenia treatment and is not a globally established indication.

Amipride is not approved for treating psychosis related to dementia in elderly patients (see Precautions and Warnings).

Each tablet contains Amisulpride as the active ingredient, commonly available in strengths such as 50 mg, 100 mg, and 200 mg. An intravenous formulation containing Amisulpride 5 mg/2 mL is also available for prevention/treatment of postoperative nausea and vomiting. Tablets contain standard pharmaceutical excipients (e.g., lactose, microcrystalline cellulose, magnesium stearate); the exact excipient list may vary by manufacturer — refer to the specific product's package insert.

Amipride is a substituted benzamide derivative classified as an atypical (second-generation) antipsychotic. Unlike many other antipsychotics, Amipride has a relatively selective action, at recommended doses, on dopamine D2 and D3 receptors in specific brain pathways, which is thought to underlie its dual efficacy against both positive and negative symptoms of schizophrenia depending on dose.

Amipride is used orally for schizophrenia and, as a separate low-dose intravenous formulation, for the prevention and treatment of postoperative nausea and vomiting.

Amipride belongs to the atypical antipsychotic class, specifically the substituted benzamide subgroup of antipsychotic agents.

Amisulpride selectively blocks dopamine D2 and D3 receptors. At low doses, it preferentially blocks presynaptic D2/D3 autoreceptors, increasing dopamine release and producing a disinhibiting effect useful for negative symptoms. At higher doses, it predominantly blocks postsynaptic D2/D3 receptors in the mesolimbic pathway, reducing positive psychotic symptoms.

Amisulpride has low affinity for serotonergic, histaminergic, cholinergic, and alpha-adrenergic receptors, which may contribute to a lower incidence of sedation and anticholinergic effects compared with typical antipsychotics, though extrapyramidal symptoms and prolactin elevation remain dose-dependent risks.

Pharmacokinetics

• Absorption: Oral bioavailability is approximately 48%; absorption is not significantly affected by food.
• Distribution: Large volume of distribution; low plasma protein binding (~16%).
• Metabolism: Minimal hepatic metabolism.
• Elimination: Excreted largely unchanged via the kidneys; elimination half-life is approximately 12 hours.

Oral Amipride tablets may be taken with or without food and should be swallowed whole with a glass of water. Doses above 400 mg/day are usually split into two administrations (morning and evening) to improve tolerability. The intravenous formulation of Amipride is administered by a healthcare professional as a slow injection over 1–2 minutes and is not intended for self-administration.

The following are well-documented, clinically significant interactions with Amipride:

• QT-prolonging drugs (e.g., Class IA/III antiarrhythmics such as quinidine and amiodarone, certain antipsychotics, some antibiotics such as moxifloxacin): concurrent use with Amipride is contraindicated due to an additive risk of QT prolongation and life-threatening arrhythmia (e.g., torsades de pointes).
• Drugs causing bradycardia or electrolyte disturbance (e.g., beta-blockers, diltiazem, certain diuretics causing hypokalemia): increase the risk of QT-related arrhythmia when combined with Amipride; concurrent use should be avoided or requires close monitoring.
• CNS depressants (alcohol, benzodiazepines, opioids, sedating antihistamines): additive sedation and CNS depression can occur with Amipride; combinations should be used cautiously.
• Dopamine agonists (e.g., levodopa): mutual antagonism of effect; concurrent use with Amipride is generally avoided unless clinically necessary.
• Antihypertensive agents: Amipride may enhance the blood-pressure-lowering effect, increasing the risk of hypotension.

Side effects of Amipride are generally dose-related.

Common

• Insomnia, anxiety, agitation
• Extrapyramidal symptoms (tremor, rigidity, akathisia) — more frequent at higher doses
• Elevated prolactin levels, which may cause galactorrhea, menstrual irregularities, gynecomastia, or sexual dysfunction
• Weight gain
• Constipation, dry mouth, nausea
• Drowsiness, dizziness

Uncommon/Rare but serious

• QT interval prolongation and, rarely, serious arrhythmia (see Precautions and Warnings)
• Neuroleptic malignant syndrome (rare, potentially life-threatening — see Precautions and Warnings)
• Tardive dyskinesia with long-term use
• Seizures
• Allergic reactions (rash, angioedema)

Amipride should be used in pregnancy only if clearly needed and if the potential benefit justifies the potential risk to the fetus; safety in human pregnancy has not been firmly established. Neonates exposed to antipsychotics, including Amipride, during the third trimester are at risk of extrapyramidal and/or withdrawal symptoms after delivery, and should be monitored.

Amipride is excreted into breast milk. Breastfeeding is generally not recommended during treatment with Amipride unless a physician determines the benefit outweighs the risk to the infant. A physician should always be consulted before use in pregnancy or while breastfeeding.

Increased mortality in elderly patients with dementia-related psychosis

As with other antipsychotics, Amipride is associated with an increased risk of death when used in elderly patients with dementia-related psychosis. Amipride is not approved for this use.

QT prolongation

Amipride causes dose- and concentration-dependent prolongation of the QT interval, which can lead to a life-threatening arrhythmia (torsades de pointes). Use with caution, and consider ECG monitoring, in patients with cardiac disease, electrolyte abnormalities (particularly hypokalemia or hypomagnesemia), a family history of QT prolongation, or concurrent use of other QT-prolonging drugs. Avoid use in patients with congenital long QT syndrome.

Neuroleptic malignant syndrome (NMS)

A rare but potentially fatal reaction characterized by high fever, muscle rigidity, altered mental status, and autonomic instability has been reported with Amipride and other antipsychotics. If NMS is suspected, Amipride should be discontinued immediately and supportive treatment given.

Hyperprolactinemia

Amipride substantially increases serum prolactin, which may cause galactorrhea, amenorrhea, gynecomastia, sexual dysfunction, and, with long-term use, may be associated with reduced bone mineral density.

Extrapyramidal symptoms and tardive dyskinesia

Amipride can cause extrapyramidal symptoms in a dose-dependent manner and, with prolonged use, tardive dyskinesia, which may be irreversible.

Seizures and other precautions

Use cautiously in patients with a history of seizures or conditions predisposing to seizures. Use caution in patients with Parkinson's disease, as Amipride may worsen symptoms. Do not stop Amipride abruptly after prolonged use; discontinue gradually under medical supervision.

Overdose with Amipride may present with exaggeration of known pharmacological effects, including drowsiness, sedation, extrapyramidal symptoms, hypotension, and QT prolongation with the risk of serious arrhythmia. There is no specific antidote. If an overdose of Amipride is suspected, seek immediate medical attention or contact emergency services/poison control. Treatment is supportive, typically with continuous cardiac (ECG) monitoring for at least several hours and management of complications in a hospital setting; do not attempt to manage a suspected overdose at home.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Pediatric use

The safety and efficacy of Amipride in children and adolescents under 18 years of age have not been established, and its use is generally not recommended in this age group. Where used in adolescents (approximately 15–18 years) for severe illness, this should only be under the direct supervision of an experienced psychiatrist.

Elderly

Elderly patients, particularly those with dementia-related psychosis, are at increased risk of mortality and stroke with Amipride and other antipsychotics (see Precautions and Warnings); Amipride is not approved for this use. Elderly patients are also more susceptible to hypotension, sedation, and extrapyramidal effects; consider starting at the lower end of the dosing range.

Renal impairment

Dose reduction is required; avoid use in severe renal impairment (see Dosage and Administration and Contraindications).

Hepatic impairment

No specific dose adjustment is generally required, as Amipride undergoes minimal hepatic metabolism, but caution is advised.

Duration of treatment with Amipride for schizophrenia is individualized and typically long-term, guided by ongoing assessment of symptom control, tolerability, and physician follow-up; many patients require maintenance therapy for extended periods to prevent relapse. Treatment should not be stopped abruptly and should only be adjusted or discontinued under medical supervision. For prevention/treatment of postoperative nausea and vomiting, Amipride injection is given as a single dose (or repeated per physician judgment) in the perioperative period only.

Atypical antipsychotic; Substituted benzamide; Antiemetic (low-dose intravenous formulation)

Amisulpride selectively antagonizes dopamine D2 and D3 receptors. Low doses preferentially block presynaptic autoreceptors, enhancing dopaminergic transmission (beneficial for negative symptoms), while higher doses block postsynaptic D2/D3 receptors in mesolimbic pathways, reducing positive psychotic symptoms. In the chemoreceptor trigger zone, D2/D3 receptor blockade by Amisulpride also underlies its antiemetic effect used for postoperative nausea and vomiting.

The safety and efficacy of Amipride have not been established in children and pre-pubertal patients, and use in this population is contraindicated/not recommended. In adolescents (approximately 15–18 years) with severe schizophrenia, Amipride may occasionally be used under the direct supervision of an experienced psychiatrist, with close monitoring for extrapyramidal symptoms, prolactin-related effects, and QT prolongation. Amipride should not be used for behavioral disorders in children outside of this specialist context.