Sulpiride Belupo, 200mg capsules 12pcs

Composition

1 capsule contains:  Active ingredients:  sulpiride 200 mg; Auxiliary substances:  lactose monohydrate, corn starch, pre-gelatinized corn starch, magnesium stearate, titanium dioxide, gelatin.

Pharmacological action

of ATX: N. 05. A. L Benzamide Farmacodynamics: Sulpiride is an atypical antipsychotic from the group of substituted benzamides, has moderate neuroleptic activity in combination with stimulating and thymoanaleptic (antidepressant) effects. The neuroleptic effect is associated with an anti-dopaminergic effect. In the central nervous system (CNS), sulpiride blocks mainly dopaminergic receptors of the limbic system, the effect on the neostriatic system is insignificant. It has an antipsychotic effect and causes a small number of side effects. The peripheral effect of sulpiride is based on the inhibition of presynaptic receptors. An increase in the amount of dopamine in the central nervous system is associated with an improvement in mood, with a decrease in 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 effects predominate. Sulpiride has no significant effect on adrenergic, cholinergic, serotonin, histamine and gamma-aminobutyric acid receptors (GABA receptors). Sulpiride stimulates prolactin secretion and has a central antiemetic effect (inhibition of the emetic center)Pharmacokinetics: Absorption After oral use, the maximum plasma concentration of sulpiride is reached in 3-6 hours. Bioavailability is 25-35% and is characterized by significant individual variability. The pharmacokinetics of sulpiride remain linear in the dose range from 50 mg to 300 mg. Concomitant use of sulpiride with food reduces absorption by 30%. Distribution Sulpiride is rapidly distributed in the tissue, the volume of distribution at steady state is 0.94 l / kg. Binding to plasma proteins is approximately 40%. Small amounts of sulpiride are excreted in breast milk and pass through the placental barrier. Metabolism In humans, sulpiride is poorly metabolized. Excretion It is mainly excreted by the kidneys in unchanged form by glomerular filtration. The total clearance is 126 ml/min. The plasma half-life of the drug is 7 hours.

Indications

As monotherapy or in combination with other psychotropic drugs.

• acute and chronic schizophrenia;
• acute delirious states;
• depressions of various etiologies;
• neurotic disorders;
• dizziness of various etiologies (vertebrobasilar insufficiency, vestibular neuritis, Meniere’s disease, condition after traumatic brain injury, otitis media);
• auxiliary therapy for gastric and duodenal ulcers and irritable bowel syndrome.

Use during pregnancy and lactation

Experiments on animals did not reveal a teratogenic effect. There are very limited clinical data on the use of sulpiride in pregnant women, so the use of sulpiride to pregnant women is not recommended. Newborns who have been exposed to antipsychotic medications in utero during the third trimester of pregnancy are at an increased risk of developing adverse reactions, including extrapyramidal symptoms or withdrawal symptoms, which may vary in severity and duration (see section “Adverse effects”). Cases of agitation, muscle hypertonia, muscle hypotension, tremor, drowsiness, respiratory disorders or eating disorders have been reported, so newborns should be under constant medical supervision. Sulpiride passes into breast milk, so breast-feeding during treatment with sulpiride om should be discontinued.

Contraindications

• Hypersensitivity to sulpiride or excipients of the drug
• Children under 6 years of age (for 50 mg capsules)
• Children under 14 years of age (for 200 mg capsules)
• Prolactin-dependent tumors (pituitary prolactinomas and breast cancer)
• Hyperprolactinemia
• Pheochromocytoma or suspected pheochromocytoma
• Acute intoxication with alcohol, sleeping pills, narcotic analgesics
• Breast-feeding period
• Congenital galactosemia, glucose/galactose malabsorption syndrome, or lactase deficiency (due to the presence of lactose in the drug)
• Concomitant use of levodopa (see section “Interaction with other medicinal products”)
• Concomitant use of mechitazine, cabergoline, quinagolide, rotigotine, citalopram and escitalopram (see section “Interaction with other
• medicinal products”)

With caution:

• In patients with a predisposition to the development of cardiac arrhythmias
• with bradycardia less than 55 beats per minute;
• with disorders of electrolyte balance, particularly hypokalemia;
• with congenital prolonged QT interval;
• receiving both drugs can cause pronounced bradycardia (<55 BPM); hypokalemia; slowing of intracardiac conduction, or prolongation of the QT interval, since sulpiride may cause prolonged QT interval and increase the risk of severe ventricular arrhythmias, including the development of piruetas ventricular tachycardia (see section “Interaction with other medicinal products”, the “Special instructions”).
• In patients with a history of neuroleptic malignant syndrome (see sections “Side effects”, “Special instructions”).
• In the elderly (increased risk of sedation, orthostatic hypotension, extrapyramidal disorders).
• Aggressive behavior or agitation with impulsivity (may require simultaneous use of sedatives).
• In elderly patients with dementia (see section “Special instructions”).
• In patients with risk factors for stroke (see section “Special instructions”).
• In patients with Parkinson’s disease(see section “Special instructions”).
• In patients with risk factors for thromboembolism (see section “Special instructions”).
• If you have diabetes and there are risk factors for developing diabetes (risk of hyperglycemia, blood sugar monitoring is required).
• During pregnancy (limited experience of use) (see the section “Use during pregnancy and lactation”).
• If you have a history of epilepsy or convulsive seizures (risk of lowering the threshold of convulsive readiness) (see the section “Special instructions”).
• In case of renal insufficiency (correction of the dosage regimen is required) (see the section “Dosage and use”).
• Concomitant use of medicinal products containing ethanol (see the section “Interaction with other medicinal products
• “).
• Leukopenia, neutropenia, and agranulocytosis have been reported during antipsychotic therapy, including Sulpiride Belupo. The development of unexplained infections or an increase in body temperature may be signs of blood disorders, which requires immediate hematological studies.
• In patients with a history of glaucoma, intestinal obstruction, congenital stenosis of the digestive tract, urinary retention or prostatic hyperplasia (since the drug has m-holinoblocking properties).
• In patients (especially elderly patients) with arterial hypertension due to the risk of developing a hypertensive crisis (patients should be under medical supervision).
• Caution should be exercised when using sulpiride in children, as the efficacy and safety of sulpiride in this category of patients have not been sufficiently studied.

Side effects

To indicate the frequency of side effects, the following classification is used, according to WHO: very common (> 1/10), common (>1/100 and > < 1/10), infrequent (> 1/1000 and < 1/10), infrequent (>< 1/100), rare (> 1/10000 and < 1/100), rare (>< 1/1000), very rare (The adverse events resulting from the use of sulpiride are similar to those caused by other psychotropic drugs, but the frequency of their development is generally lower. From the endocrine system: often: hyperprolactinemia. From the liver and biliary tract: often: increased activity of “liver” enzymes. From the nervous system: often: sedation, drowsiness, extrapyramidal disorders (these symptoms are usually reversible after the appointment of antiparkinsonian drugs), parkinsonism, tremor, akathisia; infrequently: muscle hypertonus, dyskinesia, muscle dystonia;rarely: oculogir crisis; frequency unknown: neuroleptic malignant syndrome, hypokinesia, tardive dyskinesia (after taking for more than 3 months, as with taking other drugs). neuroleptics, while taking antiparkinsonian drugs is ineffective or may cause increased symptoms), seizures. From the cardiovascular system: infrequently: orthostatic hypotension; rarely: ventricular arrhythmias, ventricular fibrillation, ventricular tachycardia; frequency unknown: prolongation of the QT interval, pirouette ventricular tachycardia, cardiac arrest, sudden death, venous thromboembolic complications, including pulmonary embolism and deep vein thrombosis, sometimes fatal; increased blood pressure (seesection “Special instructions”). From the genitals and mammary glands: infrequently: breast enlargement, amenorrhea, orgasmic dysfunction, erectile dysfunction; often: breast tenderness, galactorrhea; frequency unknown: gynecomastia. Skin and subcutaneous tissue disorders: common: macular-papular rash. Common disorders: common: weight gain. From the blood and lymphatic system: infrequently: leukopenia; frequency unknown: neutropenia, agranulocytosis. From the side of the psyche: often: insomnia. From the gastrointestinal tract: infrequently: hypersalivation. Immune system disorders: frequency unknown: anaphylactic reactions (urticaria, shortness of breath, excessive lowering of arterial pressure, anaphylactic shock). Musculoskeletal and connective tissue disorders: frequency unknown: torticollis, trismus. Pregnancy, postpartum period and perinatal condition: frequency unknown: withdrawal syndrome in newborns (see section “Use during pregnancy and lactation”).

Interaction

Concomitant use of sulpiride and drugs that depress the central nervous system (narcotic analgesics, antihistamines, barbiturates, benzodiazepines, and other anxiolytics) may increase the sedative effect of these drugs.

The combination of sulpiride with alcohol can also increase the sedative effect of alcohol.

Concomitant use with levodopa should be avoided due to the mutual antagonism of levodopa and sulpiride. There is an increased risk of developing orthostatic hypotension when taking sulpiride and antihypertensive drugs at the same time. Sucralfate, antacids containing Mg2+and/or Al3+, reduce bioavailability by 20-40%.

Antagonism with dopaminergic receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, kinagolide, ropinirole) and neuroleptics. In neuroleptic-induced extrapyramidal syndrome, dopaminergic receptor agonists are not used, but anticholinergic drugs are used. 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 may lead to the development of neuroleptic malignant syndrome).

The risk of developing ventricular arrhythmias type “torsade de pointes” when applied simultaneously with: antiarrhythmic drugs 1 and class (quinidine, gedragingen, disopyramide) and class III (amiodarone, sotalol, mofetil, ibutilide), certain antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide), drugs that cause bradycardia (diltiazem, verapamil, beta-blockers, clonidine, guanfacine, preparations of digitalis, donepezil, rivastigmine, tacrine, amrinone chloride, galantamine, and pyridostigmine, neostigmin), drugs that cause hypokalemia (calivintage diuretics, some laxatives, amphotericin b in/in GCS, tetracosactide) and others (including bepridil, cisapride, was diphemanil, erythromycin intravenously, mizolastine, vincamine has I/, halofantrine, pentamidine, sparfloxacin, moxifloxacin).

How to take, course of use and dosage

Inside, before meals, with a small amount of liquid. The daily dose is divided into several doses. It is not recommended to take the drug in the afternoon (after 16 hours) due to an increase in the level of wakefulness. In all cases, the minimum effective dose of the drug should be used. If the patient’s clinical condition permits, treatment should begin with low doses. The minimum effective dose is selected by gradually increasing the dose until the desired effect is achieved. Adults: Short-term symptomatic treatment if conventional treatment methods are ineffective: the daily dose is 50 to 150 mg for no more than 4 weeks. Acute psychotic disorders, chronic psychotic disorders (schizophrenia, chronic non-schizophrenic delusions): the daily dose is 200-400 mg of sulpiride twice a day. If necessary, the dose can be increased to 1200 mg twice a day (the highest recommended dose is 2400 mg). Children over 6 years of age with severe behavioral disorders (agitation, self-harm, stereotypy), especially with autism syndrome: the daily dose is 5-10 mg/kg of body weight. Doses for the elderly The initial dose of sulpiride should be 1/4-1/2 of the adult dose. Doses in patients with impaired renal function Due to the fact that sulpiride is mainly excreted from the body through the kidneys, it is recommended to reduce the dose of sulpiride and/or increase the interval between individual doses of the drug, depending on creatinine clearance indicators.

Overdose

Symptoms (common to both dosage forms): dyskinesia (masticatory muscle spasm, spastic torticollis), extrapyramidal disorders. In some cases-severe Parkinsonism, coma.

When using tablets, there may be: blurred vision, arterial hypertension, sedation, nausea, dry mouth, vomiting, increased sweating and gynecomastia, development of NMS.

Treatment: symptomatic. Purpose of holinoblokatorov central action.

Special instructions

If hyperthermia occurs during treatment with Sulpiride Belupo, it should be discontinued. Hyperemia can be a sign of the development of neuroleptic malignant syndrome (manifested by hyperthermia, dyskinesia, autonomic disorders), described in the treatment with neuroleptics. Although there are no data on the development of the syndrome during treatment with Sulpiride Belupo, caution is necessary, especially when prescribing high doses of the drug.

When prescribing Sulpiride Belupo to patients with epilepsy, a preliminary clinical and electrophysiological examination should be performed before starting treatment, since the drug reduces the threshold of convulsive activity.

Influence on the ability to drive motor vehicles and manage mechanisms

During the treatment period, driving vehicles and working with mechanisms that require increased attention, as well as taking alcohol, are prohibited.

Active ingredient

Sulpiride

Conditions of release from pharmacies

By prescription

Dosage form

Capsules