Sulpirides
Sulpiride: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. For violations of liver function
- 12. In case of impaired renal function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Terms and conditions of storage
- 16. Reviews
- 17. Price in pharmacies
Latin name: Sulpirid
ATX code: N05AL01
Active ingredient: sulpiride (sulpiride)
Producer: Rosemont Pharmaceuticals Ltd (Great Britain), Organic (Russia)
Description and photo update: 2018-17-05
Prices in pharmacies: from 81 rubles.
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Sulpiride is an antipsychotic, atypical antipsychotic drug with antidepressant and antiemetic effects.
Release form and composition
Dosage forms:
- oral solution: colorless or yellowish liquid with a transparent structure, with a smell characteristic of lemon or anise (150 ml each in an orange glass bottle, 1 bottle in a cardboard box);
- tablets: round flat-cylindrical shape, white with a slight yellow tinge or white, with a chamfer, for 200 mg tablets - on one side there is a dividing line (10 pcs. in a blister strip, in a cardboard box 3 packs; 30 pcs. in a glass jar of dark color, in a cardboard box 1 can);
- capsules: hard gelatinous, cylindrical shape with rounded edges; in a dosage of 50 mg - white, size No. 1, in a dosage of 100 mg - white, size No. 0, in a dosage of 200 mg - yellow, size No. 0; the contents of the capsules are cream to white powder (10 capsules in a blister contour package, 3 packages in a cardboard box);
- solution for intramuscular (intramuscular) administration: transparent, slightly colored or colorless liquid (2 ml in an ampoule, 10 ampoules in a cardboard box complete with an ampoule knife or scarifier).
5 ml of oral solution contains:
- active substance: sulpiride - 200 mg;
- auxiliary components: propyl parahydroxybenzoate, methyl parahydroxybenzoate, citric acid monohydrate, propylene glycol, anise flavor (L559), liquid maltitol, lemon flavor (L573), purified water.
1 tablet contains:
- active substance: sulpiride - 50 mg or 200 mg;
- auxiliary components: potato starch, lactose monohydrate (milk sugar), microcrystalline cellulose, magnesium stearate, gelatin, talc (magnesium hydrosilicate).
1 capsule contains:
- active substance: sulpiride - 50 mg, 100 mg or 200 mg;
- auxiliary components: corn starch, magnesium stearate, lactose monohydrate, colloidal anhydrous silicon dioxide;
- the composition of the capsule: glycerin, titanium dioxide (E171), gelatin, sodium lauryl sulfate, purified water, additionally for 200 mg capsules - sunset yellow (E110) and quinoline yellow (E104) dyes.
1 ampoule with a solution for i / m administration contains:
- active substance: sulpiride - 100 mg;
- auxiliary components: sulfuric acid solution (0.2 M), sodium chloride, water for injection.
Pharmacological properties
Pharmacodynamics
Sulpiride is an atypical neuroleptic from the group of substituted benzamides, which has moderate neuroleptic activity and has a stimulating and thymoanaleptic (antidepressant) effect on the body.
The antipsychotic effect of sulpiride is manifested when the substance is taken at a dose of more than 600 mg. At a daily dose of up to 600 mg, antidepressant and stimulating effects are predominant.
Sulpiride has a slight effect on histamine, cholinergic, adrenergic, serotonin and GABA receptors (gamma-aminobutyric acid receptors).
The neuroleptic effect of sulpiride is associated with an antidopaminergic effect. This substance predominantly blocks the dopaminergic receptors of the limbic system and to a small extent affects the neostriatal system. Sulpiride has an antipsychotic effect with few side effects. The peripheral action of sulpiride is based on the suppression of presynaptic receptors. With an increase in the amount of dopamine in the central nervous system, an improvement in mood is observed, with a decrease, the development of depression.
Small doses of sulpiride can be used as an adjuvant in the treatment of psychosomatic diseases (for example, to relieve negative mental symptoms of gastric ulcer and duodenal ulcer). The use of sulpiride in irritable bowel syndrome can reduce the intensity of abdominal pain and improve the patient's clinical condition. Low doses of sulpiride (50 to 300 mg per day) are used for dizziness of various etiologies. This substance stimulates the secretion of prolactin, and also has a central antiemetic effect (inhibits the vomiting center).
Pharmacokinetics
When administered orally, the maximum plasma concentration of sulpiride is reached after 3–6 hours. The bioavailability of the substance when taken orally is 25–35%, binding to plasma proteins is less than 40%. The concentration in the central nervous system is 2–5% of the plasma concentration. In the human body, when taken orally, sulpiride is not metabolized and is excreted through the kidneys practically unchanged (approximately 95%).
The half-life after oral administration is 6 to 8 hours. In patients with moderate and severe renal insufficiency, this indicator increases significantly, so there is a need to reduce the dose and / or increase the interval between doses.
With intramuscular injection of sulpiride at a dose of 100 mg, the maximum concentration (2.2 mg / l) is reached after 0.5 hours. The substance quickly penetrates the kidneys and liver, more slowly - into the brain tissue (it accumulates mainly in the pituitary gland). Communication with plasma proteins - no more than 40%. Intramuscularly administered sulpiride practically does not undergo metabolism: 92% of the dose is excreted unchanged in the urine (by glomerular filtration). The half-life of sulpiride is 7 hours. Full clearance - 126 ml / min.
Sulpiride passes into breast milk (with intramuscular injection - 0.1% of the daily dose).
Indications for use
Oral solution
Taking Sulpiride in the form of a solution is indicated both for monotherapy and in combination with other psychotropic drugs:
- acute and chronic form of schizophrenia;
- depression;
- acute delirious conditions;
- neurotic disorders;
- dizziness with vertebrobasilar insufficiency, vestibular neuritis, Meniere's disease, otitis media, conditions after traumatic brain injury.
In addition, the drug is prescribed as an adjunct therapy for irritable bowel syndrome, gastric ulcer and duodenal ulcer.
Pills
- 200 mg each: acute form of psychotic disorders in adults, chronic forms of psychotic disorders in adults, including schizophrenia, non-schizophrenic chronic delusional states: chronic hallucinatory psychosis, paranoid delusions;
- 50 mg each: in adults - short-term symptomatic treatment of anxiety conditions with the ineffectiveness of traditional treatment methods; in children over 6 years old (including autism syndrome) - severe behavior disorders in the form of agitation, stereotypy, self-harm.
Capsules
- chronic and acute schizophrenic psychoses, accompanied by lethargy;
- chronic alcoholic psychoses;
- adjuvant therapy for alcohol dependence;
- psychosomatic, neurotic disorders;
- migraine;
- peptic ulcer of the stomach and duodenum;
- fainting of various origins (Meniere's disease).
Solution for i / m administration
Monotherapy and as part of combined treatment with other psychotropic drugs:
- depression;
- acute and chronic schizophrenia;
- delirious conditions in acute form.
Contraindications
- pheochromocytoma;
- period of breastfeeding;
- hypersensitivity to sulpiride or to other components of the drug.
During pregnancy, the appointment of Sulpiride is possible only if the expected effect of therapy for the mother exceeds the potential threat to the fetus.
Do not use solution for oral administration, tablets, solution for intramuscular administration with hyperprolactinemia, acute poisoning with hypnotics, alcohol, analgesics.
Oral solution
- epilepsy;
- hereditary fructose intolerance;
- a state of affect and aggression that poses a risk for provoking symptoms;
- age up to 14 years.
With care: impaired renal function, heart and blood vessel disease, Parkinson's disease, a history of convulsive disorders, dysmenorrhea, old age.
Pills
- syndrome of glucose-galactose malabsorption, lactase deficiency, galactosemia;
- prolactin-dependent tumors (including pituitary prolactinomas, breast cancer);
- acute porphyria;
- combination with dopamine receptor agonists (rotigotine, quinagolide, cabergoline, ropinirole);
- simultaneous use of levodopa;
- age up to 18 years (for 200 mg tablets);
- age up to 6 years (for 50 mg tablets).
With care: angina pectoris, arterial hypertension, severe heart disease, epilepsy, renal and / or hepatic failure, dysmenorrhea, a history of neuroleptic malignant syndrome, prostatic hyperplasia, glaucoma, urinary retention, old age.
Capsules
- significant psychomotor agitation;
- acute porphyria;
- simultaneous use of antacids and sucralfate (no earlier than 2 hours after taking them);
- children under 6 years of age.
It is recommended to use with caution in patients with Parkinson's disease, epilepsy, renal failure, diseases of the cardiovascular system, because of the risk of exacerbation of the disease - in patients with productive symptoms, especially with symptoms of mania.
Solution for i / m administration
- prolactin-dependent tumors (eg, pituitary prolactinomas and breast cancer);
- manic psychosis;
- seizures;
- affective disorders, aggressive behavior;
- combination with sultopride, dopaminergic receptor agonists (apomorphine, amantadine, cabergoline, entacapone, bromocriptine, lisuride, piribedil, pergolide, pramipexole, ropinirole, quinagolide) - except for patients with Parkinson's disease.
With care: arterial hypertension, severe heart disease, angina pectoris, dysmenorrhea, renal and / or hepatic failure, glaucoma, a history of neuroleptic malignant syndrome, epilepsy, prostatic hyperplasia, urinary retention, old age.
Instructions for the use of Sulpiride: method and dosage
Oral solution
The solution is taken orally, preferably in the first half of the day, after shaking the contents of the bottle.
Recommended dosage:
- chronic and acute schizophrenia, acute delirious psychosis: the initial dose (depending on clinical indications) is 600-1200 mg per day, divided into several doses. The maintenance dose can range from 300 to 800 mg per day;
- depression: 150-600 mg per day, divided into several doses;
- dizziness: 150-200 mg per day, to achieve the desired effect in severe conditions, the dose can be increased to 300-400 mg per day. Duration of treatment is 2 weeks or more;
- auxiliary therapy for irritable bowel syndrome, gastric ulcer and duodenal ulcer: 100–300 mg per day, the frequency of administration is 1–2 times.
The daily dose for adults should not exceed 1600 mg of sulpiride.
In case of impaired renal function, the dose should be reduced and / or the interval between taking the drug should be increased.
For children over 14 years old, the standard dose of the drug is 3-5 mg per 1 kg of body weight.
Pills
The tablets are taken orally with a sufficient amount of liquid, regardless of the meal, in the morning (no later than 16 hours) of the day.
Treatment should begin with the appointment of a low dose of the drug, appropriate to the clinical condition of the patient. Then, gradually increasing it, it is brought to the minimum effective dose.
Recommended dosage:
- chronic and acute psychotic disorders: adults - 200-1000 mg per day, divided into several doses;
- anxiety (symptomatic short-term therapy in the absence of effect from conventional treatments): 50-150 mg per day for 4 weeks;
- severe behavioral disturbances in children over 6 years old, especially with autism syndrome (self-harm, agitation, stereotypes): at the rate of 5-10 mg per 1 kg of body weight per day.
Capsules
Capsules are taken orally no later than 1 hour before and no earlier than 2 hours after meals.
Recommended daily dosage:
- schizophrenia: depending on symptoms - 200-1200 mg, divided into 2 doses, the maximum daily dose is 1200 mg;
- neurosis, psycho-functional disorders: 150–300 mg;
- migraine, dizziness (Meniere's syndrome): 50-200 mg, course - at least 2 weeks.
For peptic ulcer disease, the drug is taken at 50-100 mg 3 times a day as an adjunct therapy for 1.5-2 months.
The dose for children from 6 years old is 5-10 mg per 1 kg of body weight per day.
Elderly patients do not need dosage adjustment.
The doctor prescribes the duration of treatment individually, taking into account the patient's condition.
Solution for i / m administration
The solution is used in / m only for the treatment of adult patients.
It is necessary to start with the lowest dose, taking into account the clinical condition of the patient. Then, gradually increasing it, it is brought to the minimum effective dose.
The recommended daily dose is from 400 to 800 mg, the duration of treatment is 2 weeks.
In case of impaired renal function, the dose should be reduced and / or increased the interval between taking each of the forms of Sulpiride, depending on the creatinine clearance (CC):
- CC 30-60 ml / min: the dose is reduced by 1/3 and / or the intervals between doses are increased by 1.5 times;
- CC 10-30 ml / min: the dose is reduced by 2 times and / or the intervals between doses are increased by 2 times;
- CC less than 10 ml / min: the dose is reduced by 2/3 and / or the intervals between doses are increased by 3 times.
Initial dose sulpiride for elderly patients should correspond ¼- 1 / 2 doses for adults.
Side effects
- digestive system: dry mouth, nausea, vomiting, heartburn, constipation, increased activity of liver enzymes; in addition, oral solution - diarrhea or laxative effect, capsules (very rare) - fear of eating (sitophobia);
- nervous system: drowsiness, sedation, dizziness, tremors, headache; rarely - aphasia, extrapyramidal syndrome, early and late dyskinesias, oral automatism, akathisia; possibly (at low doses) - anxiety, sleep disorder, psychomotor agitation, irritability, impaired visual acuity;
- cardiovascular system: tachycardia; possibly - a decrease or increase in blood pressure; rarely - orthostatic hypotension, pirouette-type ventricular arrhythmia; in addition, tablets and oral solution - lengthening the QT interval;
- endocrine system: possibly - hyperprolactinemia, most often manifested in the form of menstrual irregularities, galactorrhea, less often in the form of gynecomastia, frigidity, impotence; in addition, tablets and oral solution - increased body weight, increased sweating;
- allergic reactions: possibly itching, rash, eczema.
Overdose
There are no specific symptoms of sulpiride overdose, blurred vision, the development of NZS (neuroleptic malignant syndrome), arterial hypertension, sedation, gynecomastia, the appearance of extrapyramidal symptoms, vomiting, nausea, dry mouth, increased sweating may be observed.
There is no specific antidote, symptomatic and supportive therapy is recommended.
special instructions
Since the drug lowers the threshold of seizure activity, patients with epilepsy are advised to conduct a clinical and electrophysiological examination prior to use.
With extrapyramidal disorders, it is necessary to reduce the dose of the drug or prescribe antiparkinsonian therapy.
Do not drink alcohol while using Sulpiride.
Abrupt withdrawal of the drug can cause a withdrawal syndrome in the patient.
The risk of death in elderly patients with dementia is usually associated with heart failure or infectious diseases (pneumonia).
In case of an unexplained increase in the patient's body temperature, treatment with the drug should be discontinued and immediately consult a doctor. Asymptomatic hyperthermia can be caused by the development of neuroleptic malignant syndrome; its characteristic symptoms include pallor, hyperthermia, muscle rigidity, and dysfunction of the autonomic nervous system. Before the onset of hyperthermia, the patient may experience increased sweating, instability of blood pressure and pulse. The genesis of the development of neuroleptic malignant syndrome has not been established; it is believed that congenital predisposition, dehydration, organic brain damage, and intercurrent infection may contribute to its appearance.
According to the instructions, Sulpiride should be used with caution to treat patients with risk factors for stroke.
Due to the possible development of hyperglycemia against the background of the use of atypical antipsychotic drugs, patients with diabetes mellitus or patients with risk factors for its development need to monitor blood sugar levels.
Long-term therapy with sulpiride is recommended to be accompanied by regular monitoring of the composition of peripheral blood, especially when a fever or infection of unknown etiology occurs. Significant hematological changes in the composition of peripheral blood are grounds for discontinuation of treatment.
To avoid the development of venous thromboembolic complications (pulmonary thromboembolism, deep vein thrombosis) during treatment, the use of the drug should be started after an appropriate examination and repeated periodically during therapy. This will allow you to identify the existing risk factors in time and take appropriate preventive measures.
Patients with Parkinson's disease receiving dopamine receptor agonists should be prescribed Sulpiride only in exceptional cases. After starting the use of the drug, it is necessary to gradually reduce the dose of dopamine receptor agonists until complete cancellation.
With neuroleptic-induced extrapyramidal syndrome, dopaminergic receptor agonists should not be used; anticholinergics should be used.
The use of the drug in the afternoon helps to increase the level of wakefulness.
During the period of treatment with sulpiride, patients are advised to be careful when driving vehicles and mechanisms.
Application during pregnancy and lactation
The appointment of Sulpiride during pregnancy is possible only after a careful assessment of the ratio of potential benefits to the mother and the possible risk to the fetus.
The use of the drug during breastfeeding is prohibited.
Pediatric use
It is forbidden to use Sulpiride in the treatment of children:
- under 6 years old - 50 mg tablets;
- up to 14 years old - oral solution, solution for intramuscular administration;
- up to 18 years old - 200 mg tablets.
For violations of liver function
When treating patients with hepatic impairment, Sulpiride should be used with caution.
With impaired renal function
The elimination of sulpiride from the body is carried out mainly through the kidneys, therefore, when using the drug, it is necessary to reduce the dose and / or increase the interval between doses.
Use in the elderly
When treating elderly patients, the initial dose of sulpiride should be 25-50% of the adult dose.
Drug interactions
With the simultaneous use of Sulpiride:
- levodopa - reduces its effectiveness;
- antihypertensive drugs - enhance their hypotensive effect, increasing the risk of orthostatic hypotension;
- narcotic analgesics, anxiolytic (tranquilizers) and hypnotics, antitussives of central action, clonidine - enhance their depressing effect;
- antacids (containing A13 + and / or Mg2 +), sucralfate - reduce bioavailability by 20–40%;
- class 1a antiarrhythmics (disopyramide, quinidine) and class III (sotalol, amiodarone, ibutilide, dofetilide), drugs that promote the development of hypokalemia [potassium-excreting diuretics, some laxatives, amphotericin B (intravenous), tetracosactide, glucocorticeposteroids (thioridazole), neurolidazole, chlorpromazine, trifluoperazine, amisulpride, cyamemazine, tiapride, droperidol, pimozide haloperidol), bradycardia-inducing agents (verapamil, pyridostigmine bromide, diltiazem, beta-blockers, guanfacine, clonidine, donutaminestep drugs, takepromostila ambenonium chloride), bepridil, diphemanil methyl sulfate, cisapride, erythromycin (intravenous), vincamine (intravenous), mizolastine, halofantrine, moxifloxacin, sparfloxacin,pentamidine - increase the risk of developing ventricular arrhythmias such as pirouette.
Terms and conditions of storage
Keep out of the reach of children at a temperature: tablets and ampoules - up to 30 ° C, vials with oral solution - up to 25 ° C, capsules - 15-25 ° C.
Protect tablets, ampoules and capsules from direct sunlight, ampoules - from moisture.
Shelf life: oral solution - 3 years (after opening - 12 weeks), tablets - 5 years, solution for intramuscular injection - 3 years, capsules - 3 years.
Reviews about Sulpiride
Reviews of Sulpiride indicate the high effectiveness of this drug. Side effects are rare.
Price for Sulpiride in pharmacies
The price of Sulpiride is: 30 capsules 50 mg - 104 rubles, 30 tablets 200 mg - 140 rubles, 10 ampoules with a solution for intramuscular administration - 143 rubles.
Sulpiride: prices in online pharmacies
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Drug name Price Pharmacy |
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Sulpiride Belupo capsules 200mg 12 pcs. 120 RUB Buy |
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Sulpiride 200mg tablets 30 pcs. 141 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
