Prosulpine, tablets 50 mg 30 pcs

Sulpiride is an atypical neuroleptic from the group of substituted benzamides. It has moderate neuroleptic activity in combination with stimulant and thymoanaleptic (antidepressant) action.

The neuroleptic effect is associated with antidopaminergic action. It blocks dopaminergic D2- and D3-receptors, acts insignificantly on the neostriate system, and has an antipsychotic effect. The antipsychotic effect of sulpiride is seen in doses greater than 600 mg/day, in doses up to 600 mg/day the 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 ulcer. In irritable colon syndrome it reduces the intensity of abdominal pain.

Low doses of sulpiride (50-300 mg/day) are effective for dizziness.

Stimulates prolactin secretion and has a central antiemetic effect (inhibition of the vomiting center).

Pharmacokinetics

After oral administration of a 200 mg dose, Cmax in plasma is reached after approximately 4.5 hours. Bioavailability is 25-35%. Binding to plasma proteins is less than 40%. It penetrates rapidly into the liver and kidneys, slower – into brain tissue (the main amount of the drug is accumulated in the pituitary gland). The concentration of sulpiride in CNS is 2-5% of the plasma concentration. It penetrates the placental barrier. It is excreted unchanged by the kidneys through glomerular filtration (92%). Total clearance is 126 ml/min. T1/2 is 6-8 hours. With breast milk 0.1% of daily dose is excreted.

Indications

– Psychosomatic diseases, incl.

– gastric and duodenal ulcers, stress ulcers of the GI tract, drug-induced ulcers, symptomatic ulcers, nonspecific ulcerative colitis and irritable bowel syndrome;

– dysphoric disorders;

– depression of various etiologies, including

– reactive (nosogenic) depression;

– neurosis;

– acute and chronic psychotic disorders of different etiology (including

– dizziness of various etiologies (vertebro-basilar insufficiency, vestibular neuritis, Meniere’s disease, conditions after craniocerebral injury, otitis media);

In children – psychosis, behavioral disorders.

Active ingredient

Composition

1 tablet contains:

The active ingredient:

sulpiride 50 mg

Excipients:

Microcrystalline cellulose granulated,

lactose monohydrate,

lactose granulated,

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 bowel syndrome: 100-300 mg/day in 1 or 2 doses, for 4-6 weeks.

Neuroses: 100-400 mg/day in 2-3 doses.

Depressions: from 150-300 mg/day, divided into several doses; the maximum dose is 600 mg/day.

Acute and chronic psychosis (including schizophrenia): depending on the clinical picture of the disease, prescribe 300-600 mg/day divided into several doses, the maximum dose is 1200 mg/day. For negative symptoms, 200-600 mg/day; for productive symptoms, 800-1200 mg/day; for motor retardation, 100-300 mg/day.

Dizziness, migraine: 150-300 mg/day, in severe states the daily dose can be increased to 300-400 mg. Duration of treatment of dizziness should be at least 14 days.

In case of impaired renal function, it is recommended to reduce the dose of sulpiride and/or to increase the interval between individual doses of the drug, depending on the CK values.

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

In children, the average daily dose is determined at the rate of 5 mg/kg body weight.

Interaction

Simultaneous use of sulpiride and CNS depressant drugs (opioid analgesics, hypnotics, antihistamines, barbiturates, tranquilizers, central cough suppressants) may increase the sedative effect of these drugs.

The combination of sulpiride with alcohol may also increase the sedative effect of ethanol. Concomitant administration with levodopa should be avoided because of mutual antagonism of the drugs and decreased efficacy of sulpiride.

The concomitant use of sulpiride and antihypertensive agents increases the hypotensive effect and the risk of orthostatic hypotension.

Sucralfate, antacids containing magnesium or aluminum decrease the bioavailability of sulpiride by 20-40%.

Special Instructions

Caution is used with the elderly, as this category of patients often has hypersensitivity to the drug.

Patients with cardiovascular disease, parkinsonism, and young women with irregular menstrual cycles should also use caution when prescribing sulpiride.

In patients with epilepsy, a preliminary clinical and electrophysiologic examination should be performed before starting treatment, because the drug lowers the seizure threshold.

Hyperthermia developed with sulpiride therapy may be an early sign of malignant neuroleptic syndrome. If hyperthermia develops, the drug should be stopped!

Impact on driving and operating machinery

At any time during treatment, refrain from driving, engaging in other potentially hazardous activities requiring increased attention and rapid psychomotor reactions, and – from drinking alcohol.

Contraindications

– acute poisoning with alcohol, sleeping pills, analgesics;

– hypertension stage 2-3;

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– pheochromocytoma;

– psychomotor agitation;

– hypersensitivity to sulpiride.

With caution – pregnancy, period of lactation, period of newborn old age, cardiovascular diseases; renal failure, parkinsonism, epilepsy.

Side effects

CNS disorders: sedation, somnolence, headache; rarely – tremor, akathisia, extrapyramidal disorders, dyskinesia, anxiety, irritability, insomnia.

Digestive system disorders: dry mouth, heartburn, vomiting, constipation.

Cardiovascular system disorders: possible increase in BP, tachycardia; rarely – arterial hypotension, orthostatic hypotension, dizziness.

Laboratory findings: increased activity of hepatic transaminases and alkaline phosphotase.

Endocrine system disorders: hyperprolactinemia; menstrual cycle disorders, decreased sexual activity, galactorrhea, gynecomastia, weight gain may occur.

Allergic reactions: skin rash, eczematous rashes, itching are possible.

Others: visual acuity disorders.

Overdose

Symptoms: dyskinesia (spasm of masticatory muscles, spastic torticollis), extrapyramidal disorders, in some cases – coma.

Treatment: symptomatic therapy, cholinoblockers of central action.

Pregnancy use

Pregnancy and lactation should be used with caution and in the lowest effective doses in cases where the estimated benefit to the mother exceeds the potential risk to the fetus. The mother, fetus, and newborn should be closely monitored. Extrapyramidal disorders may develop in newborns whose mothers have used sulpiride for a long time.

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