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Lymipranil - antipsychotic (neuroleptic).
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.
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.
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.
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:
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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.
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.
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).
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.
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.
- Brand name: Lymipranil
- Active ingredient: Amisulpride
- Dosage form: Pills
- Manufacturer: Rivofarm
- Country of Origin: Switzerland
- Behavioral profile of amisulpride in agonistic encounters between male mice
- Liquid chromatography tandem mass spectrometry method for the quantification of amisulpride with LLOQ of 100 pg/mL using 100 µL of plasma
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- Electroanalytical Characteristics of Amisulpride and Voltammetric Determination of the Drug in Pharmaceuticals and Biological Media
- Amisulpride for the treatment of very-late-onset schizophrenia-like psychosis
- The acute and long-term effectiveness of amisulpride in patients with schizophrenia: results of a 12-month open-label prospective follow-up study
- A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers
- Dosage finding and outcome in the treatment of schizophrenic inpatients with amisulpride. Results of a drug utilization observation study
- Efficacy of amisulpride in treating primary negative symptoms in first-episode psychosis: a pilot study
- Treatment with amisulpride and olanzapine improve neuropsychological function in schizophrenia
- Stereospecific determination of amisulpride, a new benzamide derivative, in human plasma and urine by automated solid-phase extraction and liquid chromatography on a chiral column application to pharmacokinetics
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- Comparative validation of amisulpride determination in pharmaceuticals by several chromatographic, electrophoretic and spectrophotometric methods
- Selective and sensitive determination of amisulpride in human plasma by liquid chromatography–tandem mass spectrometry with positive electrospray ionisation and multiple reaction monitoring
- Enantioselective analysis of amisulpride in pharmaceutical formulations by means of capillary electrophoresis
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- Automated determination of amisulpride by liquid chromatography with column switching and spectrophotometric detection
- Rapid high-performance liquid chromatographic measurement of amisulpride in human plasma: application to manage acute intoxication
- Combined use of amisulpride and clozapine for patients with treatment-resistant schizophrenia
- Successful treatment with amisulpride of a woman with tourette's disorder: a case report
- Amisulpride versus bromocriptine in infantile autism: A controlled crossover comparative study of two drugs with opposite effects on dopaminergic function
- In vivo characteristics of dopamine D2receptor occupancy by amisulpride in schizophrenia
- Comparison of clozapine-amisulpride and clozapine-quetiapine combinations for patients with schizophrenia who are partially responsive to clozapine: A single-blind randomized study
- Amisulpride is an “atypical” antipsychotic associated with low weight gain