Prosulpine, tablets 200 mg 30 pcs

Prosulpine (Sulpiride) is an atypical neuroleptic from the group of substituted benzamides.

It has moderate neuroleptic activity combined with stimulant and thymoanaleptic (antidepressant) effects.

The neuroleptic effect is associated with antidopaminergic action. It blocks dopaminergic D 2 and D 3 receptors, has little effect on the neostriatal system, has antipsychotic action.

The antipsychotic effects of sulpiride are seen in doses over 600 mg per day; in doses under 600 mg per day, stimulant and antidepressant effects predominate.

Sulpiride has no significant effect on noradrenergic, acetylcholine, serotonin, histamine and GABA receptors.

In low doses, sulpiride may be used as an adjunctive agent in the treatment of psychosomatic diseases, particularly gastric and duodenal ulcers.

In irritable bowel syndrome it reduces the intensity of abdominal pain.

Low doses of sulpiride (50-300 mg per day) are effective for dizziness. It stimulates prolactin secretion and has a central antiemetic effect (inhibition of the vomiting center).

Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient:

sulpiride 200 mg.

the excipients:

Microcrystalline cellulose granulated,

lactose monohydrate,

lactose granulated,

sodium carboxymethylaminopectin,

corn starch,

magnesium stearate,

povidone 90.

How to take, the dosage

It is not recommended to take the drug in the afternoon (after 4 p.m.) due to increased wakefulness.

– Psychosomatic disorders, including gastric and duodenal ulcers, stress gastrointestinal ulcers, drug-induced ulcers, symptomatic ulcers, nonspecific ulcerative colitis, irritable colon syndrome 100-300 mg daily in one or two doses, for 4-6 weeks.

– Neuroses 100-400 mg per day in 2 to 3 doses.

– Depressions From 150-300 mg per day, divided into several doses. Maximum dose-600mg per day.

– Acute and chronic psychosis (including schizophrenia): Depending on the clinical picture of the disease, prescribe 300 – 600 mg per day, divided into several doses. The maximum dose is 1200 mg per day. With negative symptoms – 200-600 mg per day. In productive – 800-1200 mg per day. With motor retardation – 100-300 mg per day.

– Vertigo, migraine 150-300 mg per day, in severe states the daily dose can be increased to 300-400 mg. The duration of treatment of dizziness should be at least 14 days.

– With impaired renal function: If renal function is impaired, it is recommended to reduce the dose of sulipiride and/or increase the interval between individual doses of the drug, depending on creatinine clearance rates. Table Creatinine clearance (ml/min) Dose of sulpiride versus standard (%) Increase interval between doses of sulpiride 30-60 ml/min 70 1.5 times 10-30 ml/min 50 2 times less than 10 ml/min 34 3 times

– For the elderly: The starting dose is 1/4 to 1/2 of the adult dose.

– Children: The average daily dose is determined at the rate of 5 mg/kg body weight.

Interaction

Contraindicated combinations

Dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole), except in Parkinson’s disease patients./p>

There is mutual antagonism between dopamine receptor agonists and neuroleptics. In extrapyramidal syndrome induced by neuroleptics, dopamine receptor agonists are not used; anticholinergic agents are used in these cases.

Sultopride

The risk of ventricular arrhythmias, particularly atrial fibrillation, is increased.

No recommended combinations

Drugs that can cause torsade des pointes ventricular arrhythmias: Class Ia (quinidine, hydroquinidine, disopyramide) and Class III (amiodarone, sotalol, dofetilide, ibutilide) antiarrhythmic agents, some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, thiapride, haloperidol, droperidol, pimozide) and other drugs such as bepridil, cisapride, difemanil, IV erythromycin, misolastin, IV vincamine, etc.д.

Alcohol

Alcohol increases the sedative effects of neuroleptics. Impaired attention creates a hazard for driving vehicles and working with mechanisms requiring increased attention. Consumption of alcoholic beverages and use of medicinal products containing alcohol should be avoided.

Levodopa

Mutual antagonism between levodopa and neuroleptics. Parkinson’s disease patients should be prescribed the minimum effective dose of both drugs.

Dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lysuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole) in Parkinson’s disease patients

Agonists in Parkinson’s disease

There is mutual antagonism between dopamine receptor agonists and neuroleptics. The aforementioned drugs can cause or exacerbate psychosis. If it is necessary to treat a neuroleptic patient with Parkinson’s disease who is receiving a dopamine receptor antagonist, the dose of the latter should be gradually reduced until withdrawn (abrupt withdrawal of dopamine receptor agonists can lead to the development of a malignant neuroleptic syndrome).

Halofantrine, pentamidine, sparfloxacin, moxifloxacin

The risk of ventricular arrhythmias, particularly “torsade des pointes” is increased. If possible, the antimicrobial drug causing the ventricular arrhythmia should be stopped. If the combination cannot be avoided, the QT interval should be checked beforehand and the ECG should be monitored.

Combinations requiring caution

Drugs that cause bradycardia (bradycardic BCCs: diltiazem, verapamil, beta-adrenoblockers, clonidine, guanfacine, cardiac glycosides; cholinesterase inhibitors: donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine bromide, neomycin methyl sulfate

The risk of ventricular arrhythmias, particularly “torsade des pointes” is increased. Clinical and cardiographic monitoring is recommended.

Potassium-lowering drugs (potassium withdrawing diuretics, stimulant laxatives, amphotericin B (IV), GCS, tetracosactide

The risk of ventricular arrhythmias, particularly “torsade des pointes” is increased. Hypokalemia should be corrected and clinical and cardiographic controls and electrolyte concentrations should be established before prescribing the drug.

Combinations to consider

Antihypertensive drugs

Augment the hypotensive effect and increase the possibility of postural hypotension (additive effect).

Other CNS depressants: Morphine derivatives (narcotic analgesics, cough suppressants and substitution therapy), barbiturates, benzodiazepines and other anxiolytics, sleeping pills, sedatives, antidepressants, sedative H1-histamine receptor blockers, centrally acting hypotensive agents, baclofen, thalidomide

CNS depression. Impairment of attention creates a hazard for driving vehicles and working with mechanisms requiring increased attention.

Sucralfate, antacids containing Mg2+ and/or A13+ reduce the bioavailability of oral dosage forms by 20-40%. Sulpiride should be administered 2 h before their administration.

Special Instructions

Malignant neuroleptic syndrome: If hyperthermia of unknown etiology develops, sulpiride should be stopped because this may be one of the signs of the malignant neuroleptic syndrome described with neuroleptics (pale skin, hyperthermia, autonomic dysfunction, impaired consciousness, rigidity of muscles).

Signs of autonomic dysfunction, such as increased sweating and labile BP may precede the onset of hyperthermia, and therefore represent early warning signs. Although these effects of neuroleptics may be idiosyncratic in origin, it appears that certain risk factors may predispose to them, such as dehydration or organic brain damage.

Longening of the QT interval: Sulpiride prolongs the QT interval in a dose-dependent manner. This effect, which is known to increase the risk of serious ventricular arrhythmias such as “torsade des pointes”, is more pronounced in the presence of bradycardia, hypokalemia or congenital or acquired prolonged QT interval (combination with a QT interval prolongator drug). If the clinical situation allows, it is recommended to verify that there are no factors that may contribute to this type of arrhythmia before prescribing the drug:

– bradycardia with a heart rate less than 55 bpm.

– congenital prolongation of the QT interval;

– concomitant treatment with a drug that can cause significant bradycardia (less than 55 bpm), hypokalemia, and/min), hypokalemia, intracardiac conduction delays, or QT interval prolongation.

Except in urgent cases, patients who require treatment with neuroleptics are advised to have an ECG as part of the status evaluation. Except in exceptional cases, this drug should not be used in patients with Parkinson’s disease.

In patients with impaired renal function, reduced doses of sulpiride should be used and monitoring should be increased; intermittent courses of treatment are recommended in severe renal failure.

Control during treatment with sulpiride should be increased:

In patients with epilepsy because the seizure threshold may be lowered;

In the treatment of elderly patients who show greater sensitivity to postural hypotension, sedation and extrapyramidal effects.

During treatment with Prosulpine®, driving and operating machinery requiring increased attention, and taking alcohol or using medications containing alcohol are prohibited.

Contraindications

– Acute alcohol poisoning, sleeping pills, analgesics.
– Hypersensitivity to sulpiride.
– Hypertension stage 2-3.
– Pheochromocytoma.
– Psychomotor agitation.

With caution:

– Pregnancy.
– Period of lactation.
– Period of newborn.
– Older age.
– Cardiovascular disease.
– Kidney failure.
– Parkinsonism.
– Epilepsy.

Side effects

CNS disorders: sedation, drowsiness, dizziness, tremor, early dyskinesia (spastic torticollis, oculogyric crises, trismus), resolving with administration of central m-cholinoblockers; rarely – extrapyramidal syndrome and related disorders: akinesia, sometimes combined with muscle hypertonicity and partially resolved by administration of central m-cholinoblockers, hyperkinesia-hypertonus, motor agitation, akathisia.

There have been cases of tardive dyskinesia characterized by involuntary rhythmic movements, mainly of the tongue and/or face during long courses of treatment, which can be observed during courses of treatment with all neuroleptics: the use of antiparkinsonian drugs is ineffective or may cause a worsening of symptoms.

The drug should be discontinued if hyperthermia develops, as elevated body temperature may indicate the development of malignant neuroleptic syndrome.

Endocrine system disorders: reversible hyperprolactinemia may develop, the most common manifestations of which are galactorrhea, amenorrhea, dysmenorrhea; impotence and frigidity are less common.

In treatment with sulpiride, increased sweating and weight gain may occur.

Digestive system disorders: increased liver enzyme activity.

Particular system disorders: tachycardia; possible increase or decrease of BP; in rare cases orthostatic hypotension, prolongation of QT interval; very rare cases of “torsade des pointes” syndrome.

Hematological and lymphatic system disorders: hemolytic anemia, aplastic anemia, leukocytosis, thrombocytopenic purpura, granulocytosis.

Allergic reactions: skin rash is possible.

Overdose

Symptoms. There is limited experience with sulpiride overdose. There are no specific symptoms; the following may be observed: dyskinesia with spastic torticollis, tongue protrusion and trismus, blurred vision, increased BP, sedation, nausea, extrapyramidal symptoms, dry mouth, vomiting, increased sweating and gynecomastia, development of MNS is possible. Parkinsonism in some patients.

Treatment. Sulpiride is partially excreted by hemodialysis. Because of absence of specific antidote, symptomatic and supportive therapy with careful monitoring of respiratory function and constant control of cardiac activity (risk of QT interval prolongation) should be used; cholinoblockers of central action are prescribed if marked extrapyramidal syndrome develops.

Pregnancy use

In pregnancy and during lactation, use with caution and in the lowest effective doses when the estimated benefit to the mother exceeds the potential risk to the fetus.

The condition of the mother, the fetus, and the newborn should be monitored closely.

The development of extrapyramidal disorders is possible in newborns whose mothers have used sulpiride for a long time.

Similarities