LAGRIN [Sulpiride] 50 mg Tablets

instructions for medical use of the drug

LAGRIN

Tradename

Lagrin, Лагрин

International nonproprietary name

Sulpiride, Сульпирид

Compound

Each film-coated tablet contains:

active substance: sulpiride 50 mg

excipients: starch, dextrin, microcrystalline cellulose, sodium glycolate, hypromellose, talc, silicon dioxide, magnesium stearate.

Dosage form

Tablets.

Pharmacotherapeutic group

Antipsychotic (neuroleptic) drug .

Pharmacological properties

Pharmacodynamics

An atypical antipsychotic drug (neuroleptic), also has a stimulating, antidepressant and antiemetic effect.

The neuroleptic effect is associated with an antidopaminergic effect. In the central nervous system, sulpiride predominantly blocks dopaminergic receptors of the limbic system, has a slight effect on the neostriatal system, and has an antipsychotic effect.

The peripheral effect of sulpiride is based on inhibition of presynaptic receptors. An increase in the amount of dopamine in the central nervous system (hereinafter referred to as the CNS) is associated with an improvement in mood, and a decrease is associated with the development of symptoms of depression.

The antipsychotic effect of sulpiride is manifested in doses of more than 600 mg per day; in doses up to 600 mg per day, the stimulating and antidepressant effect predominates. Sulpiride does not have a significant effect on adrenergic, cholinergic, serotonin, histamine and gamma-aminobutyric acid receptors.

Sulpiride stimulates the secretion of prolactin and has a central antiemetic effect (suppression of the vomiting center) due to the blockade of dopamine D2 receptors in the trigger zone of the vomiting center.

Pharmacokinetics

Bioavailability - 27%. Plasma protein binding is less than 40%. The concentration of the drug in the central nervous system is 2-5% of the concentration in plasma. Excreted in breast milk.

It is not metabolized in the human body and is excreted almost unchanged through the kidneys.

The half-life (T1/2) is 6-8 hours. T1/2 increases significantly in patients with moderate and severe renal failure. Such patients should reduce the dose and/or increase the interval between doses of the drug.

Indications for use

As monotherapy or in combination with other psychotropic drugs:

·  neurotic disorders;

·  dizziness of various etiologies (vertebrobasilar insufficiency, vestibular neuritis, Meniere's disease , condition after traumatic brain injury, otitis media);

·  acute and chronic schizophrenia;

·  acute delirious states;

·  depression of various etiologies;

·  auxiliary therapy for gastric and duodenal ulcers and irritable bowel syndrome.

Contraindications

·  hypersensitivity to sulpiride or another ingredient of the drug;

·  prolactin-dependent tumors (for example, pituitary prolactinomas and breast cancer);

·  pheochromocytoma;

·  acute porphyria;

·  children under 6 years of age;

·  acute poisoning with alcohol, hypnotics, analgesics;

·  hyperprolactinemia;

·  simultaneous use of levodopa;

·  concomitant therapy with dopamine receptor agonists (cabergoline, quinagolide, ropinirole, rotigotine).

Directions for use and doses

The tablets are taken orally with a small amount of liquid, regardless of meals.
In all cases, the minimum effective dose of the drug should be used. If the patient's clinical condition allows, treatment should begin with low doses. The minimum effective dose is selected by gradually increasing the dose until the desired effect is achieved. Acute psychotic disorders in adults; chronic psychotic disorders in adults: the daily dose is divided into several doses and ranges from 200 to 1000 mg. It is not recommended to take the drug in the afternoon (after 16 hours) due to the possible activating effect of the drug. Doses in patients with impaired renal function: due to the fact that sulpiride is excreted from the body primarily through the kidneys, it is recommended to reduce the dose and/or increase the interval between the administration of individual doses of the drug depending on the creatinine clearance indicators: with a creatinine clearance of 30 - 60 ml/min, the dose of Lagrin should be reduced by 30%, and the intervals between doses should be increased by 1.5 times; with a creatinine clearance of 10-30 ml/min, the dose of Lagrin should be reduced by 2 times, and the interval between doses of the drug should be increased by 2 times; if creatinine clearance is less than 10 ml/min, the dose of Lagrin should be reduced by 70%, and the interval between doses of the drug should be increased by 3 times.
Short-term symptomatic treatment of anxiety conditions when conventional treatment methods are ineffective: the daily dose is 50 - 150 mg for no more than 4 weeks. Severe behavioral disorders (agitation, self-harm, stereotypies) in children over 6 years of age, especially with autism syndrome: daily dose is 5-10 mg/kg body weight.
Doses for the elderly: the initial dose of Lagrin should be 1/4 -1/2 the dose for adults.

Special instructions and precautions

Before using the drug, consult your doctor.

Use with caution in patients with parkinsonism and the elderly. In severe renal failure, a dose reduction or intermittent course of treatment is recommended.

In patients with epilepsy, before starting therapy, it is necessary to conduct a preliminary clinical and electrophysiological examination, because sulpiride lowers the threshold for convulsive readiness.

In case of hyperthermia, which is one of the elements of NMS, sulpiride should be discontinued immediately.

During the treatment period, avoid drinking alcohol.

Use with caution in children.

Impact on the ability to drive vehicles and machinery

During the treatment period, you should refrain from engaging in potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Use during pregnancy and breastfeeding

Prescription for pregnant women is not recommended, except in cases where the doctor, having assessed the balance of benefit and risk for the pregnant woman and the fetus, decides that the use of the drug is necessary.
The use of the drug during lactation (breastfeeding) is contraindicated.

Interaction with other drugs

When used simultaneously: with levodopa, the effectiveness of sulpiride is reduced; with antihypertensive drugs, their hypotensive effect is enhanced and the risk of developing orthostatic hypotension increases.

With drugs that depress the central nervous system (narcotic analgesics, hypnotics and anxiolytic drugs (tranquilizers), clonidine, antitussive drugs (central action), their inhibitory effect is enhanced.

Sucralfate, antacids containing magnesium and/or aluminum ions reduce bioavailability by 20-40%.

Antagonism with agonists of dopaminergic receptors (Amantadine, Apomorphine, Brokom-Riptin, Cabergoline, Entacapon, Lisurid, Pergoolid, Piribedil, Pramepexol, Hinagolyid, Ro-Pinirol) and neuroleptics. For extrapyramidal syndrome, induced by neuroptics, do not use neuroptics, do not use neurop dopaminergic receptor agonists , and use anticholinergic drugs.If it is necessary to treat patients with Parkinson's disease while using dopaminergic receptor agonists, the dose of the latter should be gradually reduced until complete withdrawal (abrupt withdrawal can lead to the development of neuroleptic malignant syndrome).

Sulpiride increases the risk of developing ventricular arrhythmias (including atrial fibrillation).

Risk of developing ventricular arrhythmias such as "torsade" de Pointes "with the simultaneous use of with: antiarrhythmic medicines of the 1st grade (quinidine, dysopiramid) and grade III (amiodarone, Sotalol, prefhylaid, ibulaid), some neuroleptics (thioridazine, chlorpromazine , leftompromazine, triflurazizin, cyamemazine, amisiprad, tiapid, haloproedol, drooperistol, pimozide), drugs that cause bradycardia (diltiazem, verapamil, beta blockers, clonidine, guanfacine, digitalis preparations, donepezil, rivastigmine, tacrine, and mbenonium chloride, galantamine, pyridostigmine bromide, neostigmine bromide), drugs that cause hypokalemia (potassium-sparing diuretics, some laxatives, amphotericin B intravenously (IV), glucocorticosteroids, tetracosactide) and others (including bepridil, cisapride, difemanil methyl sulfate, erythromycin IV, mizolastine, vincamine IV, halofantrine, pentamidine, sparfloxacin, moxifloxacin).

Side effect

From the side of the central nervous system: psychomotor agitation, anxiety, irritability, sleep disorder, impaired visual acuity, drowsiness, dizziness, headache, tremor, extrapyramidal syndrome, early and tardive dyskinesia, akatization , oral automatism, aphasia.

From the digestive system: dry mouth, heartburn, nausea, vomiting, constipation.

From the cardiovascular system: tachycardia, increase or decrease in blood pressure, possible development of orthostatic hypotension, prolongation of the QT interval, torsade- type arrhythmia de points ".

From the endocrine system: galactorrhea , menstrual irregularities, gynecomastia, impotence and frigidity; increased sweating, weight gain.
Allergic reactions: skin rash, itching.

Overdose

Symptoms: dyskinesia (spasm of masticatory muscles, spasmodic torticollis), extrapyramidal disorders. In some cases - severe parkinsonism, coma. The following may be observed: blurred vision, arterial hypertension, sedation, nausea, dry mouth, vomiting, increased sweating and gynecomastia, development of NMS.
Treatment: symptomatic. Centrally acting anticholinergics.

Storage conditions

Store in a dry place at a temperature not higher than 30°C.

Keep out of the reach of children!

Best before date

3 years. Do not use after the expiration date stated on the packaging.

Vacation conditions

Dispensed by prescription.

Release form

10 tablets in an aluminum foil blister. 3 blisters along with instructions for use in a cardboard box.