Amisulpride

Brand Rivofarm

In stock 1401 Items

Available since: 2019-09-19

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Clinical Pharmacology

Lymipranil - antipsychotic (neuroleptic).

Pharmacodynamics

Amisulpride binds selectively with high affinity to subtypes D₂/ D₃ dopaminergic receptors, while not having affinity for subtypes D₁, D₄ and D₅.
Unlike classical and atypical antipsychotics, amisulpride has no affinity for the serotonin receptor, histamine H₁, alpha adrenergic and cholinergic receptors. In addition, amisulpride does not bind to sigma regions. When used in high doses, blocks postsynaptic D₂ receptors localized in the limbic structures (does not affect the analogous receptors in the striatum). Does not cause catalepsy and does not lead to the development of hypersensitivity D₂dopamine receptors after repeated treatment.
In low doses, it predominantly blocks presynaptic D₂/ D₃ receptors, causing the release of dopamine responsible for its disinhibitory effects. This atypical pharmacological profile may explain the high-dose antipsychotic effect of amisulpride due to the blockade of postsynaptic dopamine receptors and its effectiveness against negative symptoms at low doses as a result of the blockade of presynaptic dopamine receptors.
In addition, amisulpride to a lesser extent causes extrapyramidal side effects, which may be due to its preferential limbic activity.
In patients with schizophrenia with acute attacks, amisulpride acts on both secondary negative symptoms and affective symptoms, such as depressive mood and retardation.

Pharmacokinetics

Amisulpride has two absorption peaks: one is reached quickly, one hour after the dose, and the second between 3 and 4 hours after ingestion. Concentration in plasma, respectively, is 39 ± 3 and 54 ± 4 ng / ml, after administration of 50 mg.
The volume of distribution is 5.8 l / kg. Since plasma protein binding is low (16%), interaction with other drugs is unlikely.
Absolute bioavailability is 48%. Amisulpride is poorly metabolized (about 4%), two inactive metabolites have been identified. Amisulpride does not accumulate, and its pharmacokinetics remain unchanged after repeated doses. The elimination half-life (T1 / 2) of amisulpride is approximately 12 hours after the oral dose.
Amisulpride is excreted in the urine unchanged. Renal clearance is approximately 20 l / h or 330 ml / min.
Food rich in carbohydrates (containing 68% liquid) reliably reduces the AUC (area under the concentration / time curve), the time to reach the maximum concentration and the maximum concentration of amisulpride itself, but there were no changes in pharmacokinetics after ingestion of fatty foods. However, the significance of these observations in everyday clinical practice is unknown.

Indications

Acute and chronic schizophrenia, accompanied by pronounced productive (delusions, hallucinations, mental disorders) and / or negative (affective flatness, lack of emotion and withdrawal from communication) disorders, including patients with a predominance of negative symptoms.

Composition

active substance: Amisulpride 400 mg;

Excipients: corn starch, lactose monohydrate, methylcellulose 400 cP, colloidal silicon dioxide, magnesium stearate

Amisulpride is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Lymipranil	Rivofarm	Switzerland	pills
Solian	Sanofi-aventis	France	pills

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Dosage and Administration

In acute psychotic episodes It is recommended to use orally in a dose of 400 to 800 mg per day. In some cases, the daily dose may be increased to 1200 mg per day. Doses should be increased taking into account individual tolerance. The safety of doses exceeding 1200 mg per day has not been adequately investigated, so they should not be used.
For patients with mixed negative and productive symptoms doses should be adjusted to provide optimal control of productive symptoms. Maintenance treatment must be set individually at the level of the minimum effective dose.
For patients with a predominance of negative symptoms It is recommended the appointment of an inside dose of 50 to 300 mg per day. Selection of doses should be individual. In doses exceeding 400 mg per day, Lymipranil should be administered in 2 doses.

Adverse reactions

From the nervous system and sense organs: insomnia, anxiety, agitation, drowsiness, extrapyramidal disorders, tardive dyskinesia, convulsive seizures, neuroleptic malignant syndrome.

On the part of the digestive tract: constipation, nausea, vomiting, dry mouth.

Other: hyperprolactinemia (including pain in the mammary glands, amenorrhea, galactorrhea, gynecomastia, sexual dysfunction, impotence), weight gain, hypotension, bradycardia, prolongation of the QT interval on the electrocardiogram, increased liver transaminase levels, allergic reactions.

Contraindications

Hypersensitivity, concomitant prolactin-dependent tumor (pituitary prolactinoma and breast cancer), pheochromocytoma, severe CRF (CC less than 10 ml / min); concomitant use of sultoprid, dopamine agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolid, piribedil, pramipexol, quinagolid, ropinirole, selegilin), with the exception of patients with Parkinson's disease; lactation period, child age (up to 14 years).

Drug interactions

Risk of developing ventricular arrhythmias of the "pirouette" type: anti-arrhythmic drugs of class Ia (quinidine, disopyramide), class III (amiodarone, sotalol), etc., such as bepridil, cisapride, sultopride, thioridazine, erythromycin (for i / v administration), vincamine (for iv administration), halofantrine, pentamidine, sparfloxacin. These combinations are not recommended. Drugs that increase the risk of ventricular arrhythmias such as "pirouette": Drugs that cause bradycardia (beta-blockers, diltiazem, and verapamil), clonidine, guanfacine, and digitalis preparations; Drugs that cause hypokalemia (potassium diuretics, laxatives, amphotericin B, GCS, tetracosactide); neuroleptics (pimozide, haloperidol), antidepressants (imipramine), drugs Li +. Levodopa: mutual antagonism of the action of levodopa and neuroleptics. Amisulpride enhances the inhibitory effect on the central nervous system ethanol. Drugs that inhibit the function of the central nervous system (narcotic analgesics, antipsychotics, sedative antihistamines, barbiturates, benzodiazepines, anxiolytics) - a marked increase in the inhibitory effect. With antihypertensive drugs - increased hypotensive action.

Special instructions

Before using the drug Lymipranil, previous hypokalemia should be adjusted. With the development of hyperthermia, especially during the use of high doses, the drug must be discontinued. Amisulpride may reduce the convulsive threshold, so patients with a history of epilepsy require constant monitoring during therapy. Amisulpride causes a dose-dependent increase in the duration of the Q-T interval, which increases the risk of developing serious ventricular arrhythmias, especially against the background of bradycardia, hypokalemia, existing congenital or acquired lengthening of the Q-T interval. Before prescribing and during the treatment period, it is recommended to control factors that may contribute to the development of this rhythm disorder (bradycardia less than 55 / min, hypokalemia, congenital lengthening of the QT interval, simultaneous administration of drugs causing marked bradycardia, hypokalemia, decrease in conductivity or lengthening of the QT interval. In the period of treatment is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and psychomotor reactions.