Vegaprat
Vegaprat: 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. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Vegaprat
ATX code: A03AE04
Active ingredient: prucalopride (prucalopride)
Producer: Obninsk Chemical-Pharmaceutical Company, CJSC (Russia)
Description and photo updated: 28.08.
Prices in pharmacies: from 465 rubles.
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Vegaprat is a laxative drug that stimulates serotonin receptors.
Release form and composition
Dosage form - film-coated tablets: almost white or white, round biconvex, the core is almost white or white (10 pcs in a blister strip, in a cardboard box 1, 2, 3, 4, 5 or 6 packages and instructions for the use of Vegaprat).
1 tablet contains:
- active substance: prucaloprid succinate - 1.321 mg or 2.642 mg, which is equivalent to 1 mg or 2 mg of prucaloprid;
- auxiliary components: sodium carboxymethyl starch, colloidal silicon dioxide, microcrystalline cellulose, magnesium stearate (without a shell, the weight of the tablet is 100 mg or 200 mg);
- shell composition: macrogol 6000, hypromellose 6cP, titanium dioxide, talc (with a shell, the weight of the tablet is 103 mg or 206 mg).
Pharmacological properties
Pharmacodynamics
The active substance of Vegaprat is prucaloprid, a dihydrobenzofurancarboxamide, which enhances intestinal motility. It is a selective, high-affinity agonist of 5HT 4 -serotonin receptors, which probably explains its effect on intestinal motility.
Binding to other types of receptors is observed only at concentrations of a substance that exceed its affinity for 5HT 4 -serotonin receptors by at least 150 times.
Pharmacokinetics
Prucaloprid is absorbed quickly; after a single oral dose of 2 mg, the maximum concentration is reached in 2-3 hours. The absolute bioavailability after oral administration is more than 90%. Taking the drug simultaneously with food does not affect this indicator.
The substance is distributed throughout the body, the volume of distribution in an equilibrium state is 567 liters. Binds to blood plasma proteins at a level of approximately 30%.
The metabolism of prucaloprid is very slow in the liver, with only a small amount of metabolites being formed. After oral administration of 14 C-labeled prucalopride, eight metabolites are found in small amounts in feces and urine. The main one is R107504, which is formed by O-demethylation of prucalopride and the oxidation of the resulting alcohol to a carboxylic acid. It is less than 4% of the administered dose.
As shown by the results of studies of a substance with a radioactive label, approximately 85% of prucaloprid remains unchanged; The metabolite R107504 in plasma is present in a small volume.
Most of the taken dose of the active substance is excreted unchanged (by the kidneys - about 60%, with feces - about 6%).
The excretion of unchanged substance by the kidneys includes active secretion and passive filtration. The clearance of prucaloprid from blood plasma averages 317 ml / min, the terminal half-life is approximately 24 hours.
The equilibrium state of prucaloprid is achieved within 3-4 days of therapy, while the minimum and maximum plasma concentrations in an equilibrium state when 2 mg of prucaloprid is taken once a day are 2.5 and 7 ng / ml, respectively. The coefficient k of the drug when taken 1 time per day ranges from 1.9–2.3.
The pharmacokinetic parameters of prucaloprid are linearly dependent on the dose up to 20 mg per day. With prolonged administration once a day, the pharmacokinetics of the substance does not depend on the duration of therapy.
When Vegaprat was administered to elderly patients 1 mg once a day, the maximum plasma concentration of prucalopride in the blood and AUC (area under the concentration-time curve) were 26% and 28% higher, respectively, than in young patients. This may be due to weakening renal function in elderly patients.
With mild and moderate renal impairment (in patients with creatinine clearance of 50–79 and 25–49 ml / min, respectively), the plasma concentration of prucaloprid in the blood after a single dose of 2 mg increases by 25% and 51%, respectively. In severe renal dysfunction (in patients with creatinine clearance less than 24 ml / min), the value of this indicator increases by 2.3 times.
Indications for use
The use of Vegaprat is indicated for the symptomatic treatment of chronic constipation in women in the absence of a sufficient effect from taking laxatives.
Contraindications
- functional or anatomical disorders of the intestinal wall, leading to its obstruction or perforation;
- mechanical intestinal obstruction;
- severe bowel inflammation (including ulcerative colitis, Crohn's disease, toxic megarectum, or megacolon);
- functional renal impairment requiring dialysis;
- the period of pregnancy and breastfeeding;
- age up to 18 years;
- hypersensitivity to the components of the drug.
With extreme caution, Vegaprat tablets should be used in case of a heart rhythm disorder or a history of coronary heart disease. With caution - with severe and clinically unstable concomitant pathologies: diseases of the lungs, kidneys, cardiovascular and endocrine systems, mental disorders, neurological, oncological diseases, AIDS.
Vegaprat, instructions for use: method and dosage
Vegaprat tablets are taken orally, 1 time at any time of the day, regardless of food intake.
Recommended dosage: the initial dose is 1 mg, in the absence of a sufficient therapeutic effect, it can be increased to 2 mg.
In case of severe impairment of liver or kidney function, the daily dose should not exceed 1 mg.
Side effects
- cardiovascular system: infrequently - palpitations;
- digestive system: very often - abdominal pain, nausea, diarrhea; often - dyspepsia, vomiting, flatulence, intestinal noises of a pathological nature, rectal bleeding; infrequently - anorexia;
- nervous system: very often - headache; often - dizziness; infrequently - tremor;
- urinary system: often - pollakiuria;
- general reactions: often - weakness; infrequently - feeling unwell, fever.
Overdose
The main symptoms of prucalopride overdose are due to an increase in known side effects. These include diarrhea, nausea, and headache.
Therapy: symptomatic and supportive. If there is a lot of fluid loss from vomiting / diarrhea, electrolyte imbalance may need to be corrected.
There is no specific antidote.
special instructions
Due to the mechanism of action characteristic of prucaloprid (stimulation of intestinal motility), the use of a dose of more than 2 mg per day does not guarantee an increase in the effect. In the absence of the effect of taking Vegaprat for one month, a second examination is required to confirm the feasibility of further therapy.
During the entire period of treatment, women of childbearing age should use reliable methods of contraception. Since Vegaprat can cause severe diarrhea and increase the risk of reducing the effectiveness of oral contraceptives, it is necessary to use additional barrier contraceptives.
Influence on the ability to drive vehicles and complex mechanisms
Due to the risk of dizziness and / or general weakness, especially at the beginning of therapy, caution should be exercised when driving vehicles and mechanisms.
Application during pregnancy and lactation
Vegaprat is not prescribed during pregnancy / lactation.
Pediatric use
Patients under 18 years of age are not prescribed Vegaprat.
With impaired renal function
Patients with impaired renal function requiring dialysis are contraindicated to use Vegaprat.
In case of kidney disease, therapy should be carried out with caution. Patients with severe renal impairment (glomerular filtration rate <30 ml / min / 1.73 m 2) should take 1 mg once a day. Patients with mild to moderate renal impairment do not need to adjust the dose.
For violations of liver function
Patients with severe hepatic impairment (Child-Pugh class C) should take 1 mg once a day. Patients with mild to moderate hepatic impairment do not need to adjust the dose of Vegaprat.
Drug interactions
Research results confirm the weak ability of therapeutic doses of prucalopride to affect the metabolism of concurrently taken drugs.
Active inhibitors of P-glycoprotein (including ketoconazole, verapamil, quinidine, cyclosporin A) do not have a clinically significant effect on prucaloprid.
With the simultaneous use of Vegaprat increases the concentration of erythromycin in the blood plasma by 30%.
Caution should be exercised with concomitant therapy with drugs that can cause prolongation of the QTc interval.
The activity of Vegaprat may decrease when combined with atropine-like substances.
Analogs
The analogue of Vegaprat is Resolor.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C in a dark place.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Vegaprat
Reviews about Vegaprat are mostly positive. Indicate that the drug is usually well tolerated, there are rare reports of headaches at the beginning of therapy. Also, the advantage of the remedy is considered to be the effect directly on the intestinal motility. In comparison with the analogue, the cost is estimated as affordable.
Price for Vegaprat in pharmacies
The approximate price for Vegaprat is 509–550 rubles. (30 tablets of 1 mg) or 855–909 rubles. (30 tablets, 2 mg each).
Vegaprat: prices in online pharmacies
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Drug name Price Pharmacy |
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Vegaprat 1 mg film-coated tablets 30 pcs. 465 RUB Buy |
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Vegaprat 2 mg film-coated tablets 30 pcs. 800 RUB Buy |
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Vegaprat tablets p.o. 2mg 30 pcs. 1044 RUB 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!
