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

– Psychosomatic diseases, incl. gastric and duodenal ulcers, gastrointestinal stress ulcers, drug-induced ulcers, symptomatic ulcers, ulcerative colitis and irritable bowel syndrome.

– Dysphoric disorders.

– Depression, of various etiologies, incl. reactive (nosogenic).

– Neuroses.

– Acute and chronic psychotic disorders of various etiologies (including schizophrenia).

– Migraine.

– Dizziness of various etiologies (vertebrobasilar insufficiency, vestibular neuritis, Meniere’s disease, condition after traumatic brain injury, otitis media).

– In children – psychoses, behavioral disorders.

Pharmacological effect

Prosulpin (Sulpiride) is an atypical antipsychotic from the group of substituted benzamides.

It has moderate neuroleptic activity in combination with stimulating and thymoanaleptic (antidepressive) effects.

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

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 noradrenergic, acetylcholine, serotonin, histamine and GABA receptors.

In small doses, sulpiride can be used as an adjuvant in the treatment of psychosomatic diseases, in particular gastric and duodenal ulcers.

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

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

Special instructions

Malignant neuroleptic syndrome: if hyperthermia of unknown etiology develops, sulpiride should be discontinued, because this may be one of the signs of neuroleptic malignant syndrome described with the use of neuroleptics (pallor of the skin, hyperthermia, autonomic dysfunction, impaired consciousness, muscle rigidity).

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

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

– bradycardia with a heart rate less than 55 beats/min;

– hypokalemia;

– congenital prolongation of the QT interval;

– simultaneous treatment with a drug that can cause severe bradycardia (less than 55 beats/min), hypokalemia, slowing of intracardiac conduction or prolongation of the QT interval.

Except in cases of urgent intervention, patients who require treatment with antipsychotics are recommended to undergo an ECG during the assessment process. 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; in severe forms of renal failure, intermittent courses of treatment are recommended.

Control during treatment with sulpiride should be strengthened:

– in patients with epilepsy, because the seizure threshold may be reduced;

– in the treatment of elderly patients who are more sensitive to postural hypotension, sedation and extrapyramidal effects.

During treatment with Prosulpin®, driving vehicles and operating machinery that require increased attention, as well as drinking alcohol or using drugs containing alcohol are prohibited.

Active ingredient

Sulpiride

Composition

1 tablet contains:

active substance:

sulpiride 200 mg.

excipients:

granulated microcrystalline cellulose,

lactose monohydrate,

granulated lactose,

sodium carboxymethylaminopectin,

corn starch,

magnesium stearate,

povidone 90.

Pregnancy

During pregnancy and lactation, it should be used with caution and in minimally effective doses, in cases where the expected benefit to the mother outweighs the potential risk to the fetus.

Careful monitoring of the condition of the mother, fetus, and newborn is necessary.

It is possible to develop extrapyramidal disorders in newborns whose mothers have used sulpiride for a long time.

Contraindications

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

With caution:

– Pregnancy.
– Lactation period.
– Newborn period.
– Old age.
– Cardiovascular diseases.
– Kidney failure.
– Parkinsonism.
– Epilepsy.

Side Effects

From the side of the central nervous system: sedation, drowsiness, dizziness, tremor, early dyskinesia (spasmodic torticollis, oculogyric crises, trismus), which resolves with the prescription of central m-anticholinergic drugs; rarely – extrapyramidal syndrome and associated disorders: akinesia, sometimes combined with muscle hypertonicity and partially eliminated by prescribing central m-anticholinergic drugs, hyperkinesia-hypertonicity, 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 antipsychotics: the use of antiparkinsonian drugs is ineffective or may cause worsening of symptoms.

If hyperthermia develops, the drug should be discontinued, because an increase in body temperature may indicate the development of neuroleptic malignant syndrome.

From the endocrine system: the development of reversible hyperprolactinemia is possible, the most common manifestations of which are galactorrhea, amenorrhea, dysmenorrhea; less often – impotence and frigidity.

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

From the digestive system: increased activity of liver enzymes.

From the cardiovascular system: tachycardia, possible increase or decrease in blood pressure; in rare cases, orthostatic hypotension and QT interval prolongation may develop; very rare cases of the development of torsade des pointes syndrome.

From the circulatory and lymphatic systems: hemolytic anemia, aplastic anemia, leukocytosis, thrombocytopenic purpura, granulocytosis.

Allergic reactions: possible skin rash.

Interaction

Contraindicated combinations

Dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole), except for patients with Parkinson’s disease

There is mutual antagonism between dopamine receptor agonists and antipsychotics. For extrapyramidal syndrome induced by antipsychotics, dopamine receptor agonists are not used; in such cases, anticholinergic drugs are used.

Sultopride

The risk of ventricular arrhythmias, in particular atrial fibrillation, increases.

Not recommended combinations

Drugs that can cause ventricular arrhythmias of the “torsade des pointes” type: antiarrhythmic drugs of class Ia (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilide), some antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide) and other drugs such as bepridil, cisapride, difemanil, IV erythromycin, mizolastine, IV vincamine, etc.

Alcohol

Alcohol enhances the sedative effect of neuroleptics. Impaired attention creates a danger for driving vehicles and working with mechanisms that require increased attention. The consumption of alcoholic beverages and the use of medications containing alcohol should be avoided.

Levodopa

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

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

There is mutual antagonism between dopamine receptor agonists and antipsychotics. The above drugs may cause or worsen psychosis. If treatment with a neuroleptic is necessary for a patient with Parkinson’s disease and receiving a dopamine receptor antagonist, the dose of the latter should be gradually reduced until discontinuation (abrupt withdrawal of dopamine receptor agonists can lead to the development of neuroleptic malignant syndrome).

Halofantrine, pentamidine, sparfloxacin, moxifloxacin

The risk of ventricular arrhythmias increases, in particular, “torsade des pointes”. If possible, the antimicrobial drug causing ventricular arrhythmia should be discontinued. If the combination cannot be avoided, the QT interval should first be checked and ECG monitoring should be ensured.

Combinations requiring caution

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

The risk of ventricular arrhythmias increases, in particular, “torsade des pointes”. Clinical and cardiac monitoring is recommended.

Drugs that reduce the concentration of potassium in the blood (potassium-sparing diuretics, stimulant laxatives, amphotericin B (iv), corticosteroids, tetracosactide

The risk of ventricular arrhythmias increases, in particular, “torsade des pointes”. Before prescribing the drug, hypokalemia should be eliminated, clinical and cardiac monitoring should be established, as well as monitoring of electrolyte concentrations.

Combinations to Consider

Antihypertensive drugs

Strengthening the hypotensive effect and increasing the possibility of postural hypotension (additive effect).

Other CNS depressants: morphine derivatives (narcotic analgesics, antitussives and replacement therapy), barbiturates, benzodiazepines and other anxiolytics, hypnotics, sedatives, antidepressants, sedating H1-blockers, centrally acting antihypertensives, baclofen, thalidomide

CNS depression. Impaired attention creates a danger for driving vehicles and working with mechanisms that require increased attention.

Sucralfate, antacids containing Mg2+ and/or A13+, reduce the bioavailability of oral dosage forms by 20–40%. Sulpiride should be prescribed 2 hours before taking them.

Overdose

Symptoms. Experience with overdose of sulpiride is limited. There are no specific symptoms, but the following may be observed: dyskinesia with spasmodic torticollis, tongue protrusion and trismus, blurred visual perception, increased blood pressure, sedation, nausea, extrapyramidal symptoms, dry mouth, vomiting, increased sweating and gynecomastia, possible development of NMS. Some patients have parkinsonism.

Treatment. Sulpiride is partially eliminated by hemodialysis. Due to the lack of a specific antidote, symptomatic and supportive therapy should be used with careful monitoring of respiratory function and constant monitoring of cardiac activity (risk of prolongation of the QT interval), which should continue until the patient recovers completely; Centrally acting anticholinergics are prescribed for the development of severe extrapyramidal syndrome.

Storage conditions

In a dry place, protected from light, at a temperature of 15–25 °C

Shelf life

2 years

Manufacturer

PRO.MED.CS Prague, Czech Republic