Limipranil
Limipranil: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Lymipranil
ATX code: N05AL05
Active ingredient: amisulpride (Amisulpride)
Manufacturer: Rivopharm S. A. (Switzerland)
Description and photo updated: 2018-29-11
Limipranil is a neuroleptic, antipsychotic drug.
Release form and composition
Dosage forms:
- tablets: round, almost white or white, on one side there is a dividing line and inscriptions: dosage of 50 mg - "C", on the other side "AK"; dosage of 100 mg - "C" and "AL"; dosage 200 mg - "C" and "AM" (10 pcs. in blisters, in a cardboard box of 1, 2, 3 or 5 blisters; for hospitals - in a cardboard box of 20, 50 or 100 blisters);
- film-coated tablets: almost white or white, biconvex, oval, with a dividing line (10 pcs in blisters, in a cardboard box of 3, 6 or 10 blisters; for hospitals - in a cardboard box of 20, 40, 50 or 100 blisters).
Each pack also contains instructions for the use of Limipranil.
Composition of 1 tablet:
- active substance: amisulpride - 50, 100 or 200 mg;
- auxiliary components: lactose monohydrate, colloidal silicon dioxide, methylcellulose 400 cP, corn starch, magnesium stearate.
Composition of 1 film-coated tablet:
- active substance: amisulpride - 400 mg;
- auxiliary components: lactose monohydrate, sodium carboxymethyl starch, methylcellulose 400 cP, microcrystalline cellulose, magnesium stearate;
- film shell: copolymer of methyl methacrylate, dimethylaminoethyl methacrylate and butyl methacrylate (Eudragit E100), macrogol 6000, magnesium stearate, titanium dioxide (E171), talc.
Pharmacological properties
Pharmacodynamics
Limipranil is a neuroleptic drug with the active ingredient amisulpride. The mechanism of action of amisulpride is due to its property of absolute selective binding to the D 2 or D 3 subtypes of dopaminergic receptors and a complete lack of affinity for the remaining subtypes (D 1, D 4, D 5).
Amisulpride is distinguished from classical and atypical neuroleptics by the absence of affinity for the H 1 -histamine receptor, alpha-adrenergic, cholinergic and serotonin receptors. Moreover, it does not associate with sigma sites.
When used in high doses, Limipranil blocks postsynaptic D 2 receptors located in limbic structures, without affecting analogous receptors in the striatum. Does not cause catalepsy and does not lead to the development of increased sensitivity of D 2 -dopamine receptors after repeated treatment. Amisulpride in low doses affects mainly the process of blocking presynaptic D 2 or D 3 receptors, causing the release of dopamine, which is responsible for its inhibitory effects.
Amisulpride has an atypical pharmacological profile, which may explain the antipsychotic effect of amisulpride in high doses, which occurs as a result of blockade of postsynaptic dopamine receptors, and its effectiveness against negative symptoms at low doses due to blockade of presynaptic dopamine receptors.
It is believed that due to the predominant limbic activity while taking amisulpride, extrapyramidal side effects are less common.
In the treatment of acute attacks of schizophrenia, Limipranil acts on secondary negative symptoms and affective disorders (including depressive mood, retardation).
Pharmacokinetics
Absorption of amisulpride occurs in two stages. At the first stage, the maximum plasma concentration (C max) is reached quickly and within 1 hour after taking Limipranil at a dose of 50 mg is 36–42 ng / ml. Then, between 3 and 4 hours, the second peak of C max is noted, where its value is 50–58 ng / ml.
The absolute bioavailability of the drug is 48%.
Against the background of the simultaneous consumption of food rich in carbohydrates containing 68% liquid, there is a decrease in the total concentration of the drug in the blood plasma, the time to reach and the size of C max of amisulpride. Taking a tablet after taking a fatty meal does not affect the pharmacokinetics of the drug.
The volume of distribution (V d) is 5.8 l / kg.
Plasma protein binding is 16%, therefore, interaction of amisulpride with other drugs is unlikely.
About 4% of amisulpride is metabolized to form two inactive metabolites.
T 1/2 (half-life) is approximately 12 hours.
It is excreted unchanged through the kidneys, the renal clearance of amisulpride is approximately 330 ml / min (20 l / h).
After taking repeated doses, the pharmacokinetics of the drug remains unchanged, amisulpride does not accumulate in the body.
Indications for use
The use of Limipranil is indicated for the treatment of patients with acute and chronic schizophrenia, which is accompanied by severe productive disorders (delirium, thought disorder, hallucinations, etc.) and / or negative disorders (lack of emotionality, affective flatness, withdrawal from communication, etc.), including number in case of predominance of negative symptoms.
Contraindications
Absolute:
- pituitary prolactinoma, breast cancer and other prolactin-dependent neoplasms;
- pheochromocytoma;
- concomitant therapy with the following drugs (due to an increased risk of atrial fibrillation): class IA antiarrhythmics (procainamide, quinidine, disopyramide) and class III (sotalol, amiodarone), halofantrine, pentamidine, bepridil, cisapride, sparfloxacin, sultopride, thioridazine, intravenous administration of erythromycin and vincamine;
- simultaneous administration of levodopa;
- childbearing age in women - in the absence of a guarantee of their use of adequate contraception;
- period of pregnancy;
- lactation;
- age up to 15 years;
- hypersensitivity to the components of the drug.
With caution, Limipranil tablets should be prescribed for renal failure, epilepsy, parkinsonism, in old age.
Limipranil, instructions for use: method and dosage
The tablets are taken orally.
When prescribing Limipranil in a daily dose of more than 400 mg, it should be divided into 2 doses.
Do not use the drug in a daily dose of more than 1200 mg.
Recommended daily dosage of Limipranil:
- acute psychotic episodes: 400-800 mg, in some cases - 1200 mg. An increase in the daily dose must be made taking into account individual tolerance;
- mixed negative and productive symptoms of schizophrenia: the dose is selected individually, the initial dose should provide optimal control over productive symptoms, the maintenance dose is set at the minimum effective level;
- schizophrenia with a predominance of negative symptoms: 50-300 mg, the dose is selected individually.
Elderly patients dose selection of Limipranil should be done with extreme caution, monitoring the patient's condition for the development of excessive sedation or arterial hypotension.
With renal failure, dose adjustment is required, it is reduced depending on the patient's creatinine clearance (CC). With CC 30-60 ml / min, the daily dose is prescribed in the amount of ½ of the usual dose, with CC 10-30 ml / min - in the amount of ⅓ of the usual dose.
No dose adjustment of Limipranil is required in case of liver dysfunction.
Side effects
- from the central nervous system: often - anxiety, agitation, insomnia; infrequently - drowsiness; perhaps - acute dystonia (including spastic torticollis, trismus, oculogyric crises); very rarely (in the treatment of schizophrenia with a predominance of negative symptoms in a daily dose of 50 to 300 mg) - increased blood pressure (BP), akathisia, tremor, hypersalivation, hypokinesia; against the background of long-term therapy - tardive dyskinesia (the appearance of rhythmic involuntary movements, predominantly of the tongue and / or face; the use of antiparkinsonian drugs is ineffective and can worsen the condition); isolated cases - seizures, neuroleptic malignant syndrome;
- on the part of the cardiovascular system: rarely - prolongation of the QT interval, bradycardia, arterial hypotension; very rarely - atrial fibrillation;
- from the digestive system: infrequently - dry mouth, nausea, vomiting, constipation; rarely - an increase in the activity of liver enzymes (mainly transaminases);
- from the endocrine system: against the background of a reversible increase in the level of prolactin in the blood plasma - chest pain, galactorrhea, amenorrhea, gynecomastia, impotence, weight gain;
- others: rarely - allergic reactions.
Overdose
Symptoms: increased pharmacological effects of amisulpride (drowsiness, sedation), the development of arterial hypotension, extrapyramidal symptoms, in severe cases - coma.
Treatment: the appointment of symptomatic therapy. Due to the increased risk of lengthening the QT interval, it is necessary to carefully monitor the functions of the heart, it is also recommended to monitor other vital functions of the body. In the event of severe extrapyramidal symptoms, anticholinergics are indicated.
There is no specific antidote. Hemodialysis is ineffective.
When diagnosing an acute overdose, one should take into account the possibility of interaction of simultaneously taken drugs.
special instructions
Against the background of the use of Limipranil, there is a risk of developing neuroleptic malignant syndrome. Its characteristic features include: hyperthermia, muscle stiffness, dysfunction of the peripheral nervous system, elevated levels of creatine phosphokinase. In the case of hyperthermia, especially when taking high doses of amisulpride, drug treatment should be discontinued.
Complication of the patient's condition in the form of acute dystonia is reversible. In this case, the appointment of anticholinergic antiparkinsonian drugs is recommended.
Regular monitoring of the state of renal function is required; if functional disorders of the kidneys are detected, the dose of Limipranil should be reduced. Particular care in dose selection is required in the treatment of patients with severe renal failure (CC less than 10 ml / min), since there are no recommendations for the treatment of this category of patients.
When treating patients with a history of epilepsy, it should be borne in mind that Limipranil is characterized by a decrease in the seizure threshold, and ensure they are constantly monitored throughout the entire period of therapy.
In Parkinson's disease, the combination of dopamine agonists and amisulpride can worsen the patient's condition, therefore, the use of Limipranil is possible only for health reasons.
Due to the risk of severe ventricular arrhythmias, it is recommended to take into account the property of Limipranil to cause a dose-dependent prolongation of the QT interval. The likelihood of this effect increases if the patient has bradycardia, hypokalemia, congenital or acquired lengthening of the QT interval.
Influence on the ability to drive vehicles and complex mechanisms
Limipranil has a negative effect on the patient's ability to drive vehicles or work with complex mechanisms.
Application during pregnancy and lactation
The use of Limipranil is contraindicated during gestation and breastfeeding.
Pediatric use
The appointment of Limipranil is contraindicated for the treatment of patients under the age of 15 years.
With impaired renal function
With caution, Limipranil tablets should be prescribed to patients with renal insufficiency.
With renal failure, dose adjustment is required. With CC 30-60 ml / min, the daily dose should be ½ of the usual dose, with CC 10-30 ml / min - ⅓.
For violations of liver function
No dose adjustment is required for liver dysfunction.
Use in the elderly
Elderly patients are prescribed Limipranil with extreme caution.
When choosing a dose, the patient's condition should be carefully monitored for the development of excessive sedation or arterial hypotension.
Drug interactions
- quinidine, disopyramide, procainamide (class IA antiarrhythmics), amiodarone, sotalol (class III antiarrhythmics), sultopride, thioridazine, bepridil, cisapride, halofantrine, sparfloxacin, pentamidine, iv administration of erythromycin and vincamine: cause a significant increase in the risk of developing ventricular arrhythmias of the "pirouette" type, therefore, their appointment in combination with amisulpride is contraindicated;
- levodopa: antipsychotics in combination with levodopa have a mutual antagonism of action;
- ethanol: there is an increase in the inhibitory effect of alcohol on the central nervous system (CNS);
- beta-blockers, calcium channel blockers (including diltiazem and verapamil), guanfacine, clonidine, digitalis drugs: drugs that cause bradycardia can increase the likelihood of ventricular arrhythmias of the "pirouette" type, so their appointment should be done with great care;
- potassium-excreting diuretics, amphotericin B, laxatives, glucocorticoids, tetracosactides: can cause hypokalemia, therefore, it is recommended to be careful when taking them simultaneously with Limipranil;
- pimozide, haloperidol (antipsychotics), imipramine (other antidepressants of this type), lithium preparations: the use of these drugs is undesirable or requires special care;
- drugs that depress the function of the central nervous system (including antipsychotics, narcotic analgesics), antihistamines with a sedative effect, barbiturates, benzodiazepines and other anxiolytics: when combined with Limipranil, they cause a pronounced increase in its inhibitory effect;
- antihypertensive drugs: an increase in the antihypertensive effect of antihypertensive drugs should be considered.
Analogs
Limipranil analogs are: Solian, Eglonil, Clozasten, Finlepsin, Moditen Depot, Thioridazin, Rispaxol, Egolanza, Leponex, Betamax, Prosulpin, Tiaprid.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Limipranil
Reviews of Limipranil are rare. Most often, patients discuss the degree of effectiveness of the active substances of antipsychotic drugs. Reviews about amisulpride are mostly positive.
Price for Limipranil in pharmacies
The price for Limipranil for a pack containing 30 pcs. May be:
- tablets 200 mg - 1509-1934 rubles;
- film-coated tablets, 400 mg - 2782–3235 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
