Vegaprat tablets p / o 1mg, No. 30

Symptomatic treatment of chronic constipation in women in whom laxatives have not provided a sufficient effect in eliminating symptoms.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally, regardless of food intake, at any time of the day. The initial dose is 1 mg 1 time / day, if necessary, the dose is increased to 2 mg 1 time / day.

For patients with severely impaired renal or hepatic function, the dose is 1 mg 1 time / day.

Active substance:

prucaloprid succinate - 1.321 mg, which corresponds to the content of prucaloprid - 1 mg

Excipients: microcrystalline cellulose - 96 mg, sodium carboxymethyl starch - 1.419 mg, magnesium stearate - 0.9 mg, colloidal silicon dioxide - 0.36 mg.

Uncoated tablet weight - 100 mg.

The composition of the shell: hypromellose 6 cP - 1.8 mg, macrogol 6000 - 0.6 mg, titanium dioxide - 0.5 mg, talc - 0.1 mg.

The weight of the coated tablet is 103 mg.

• impaired renal function requiring dialysis;

• intestinal perforation or obstruction due to anatomical or functional disorders of the intestinal wall, mechanical intestinal obstruction, severe intestinal inflammation, incl. Crohn's disease, ulcerative colitis, and toxic megacolon / megarectum;

• hypersensitivity to prucaloprid.

Description:

Film-coated tablets of white or almost white color, round, biconvex, on a cross-section the core of the tablet is white or almost white.

Ingredients: 1 tab.

Active substance:

prucaloprid succinate - 1.321 mg, which corresponds to the content of prucaloprid - 1 mg

Excipients: microcrystalline cellulose - 96 mg, sodium carboxymethyl starch - 1.419 mg, magnesium stearate - 0.9 mg, colloidal silicon dioxide - 0.36 mg.

Uncoated tablet weight - 100 mg.

The composition of the shell: hypromellose 6 cP - 1.8 mg, macrogol 6000 - 0.6 mg, titanium dioxide - 0.5 mg, talc - 0.1 mg.

The weight of the coated tablet is 103 mg.

Clinical and pharmacological group: Selective agonist of serotonin 5-HT4 receptors

Pharmaco-therapeutic group: Serotonin receptor stimulant

pharmachologic effect

An agent that increases intestinal motility, dihydrobenzofurancarboxamide. The effect on intestinal motility is most likely due to the selectivity and high affinity of prucalopride for serotonin 5-HT4 receptors.

Pharmacokinetics

After a single oral administration, prucaloprid is rapidly absorbed from the gastrointestinal tract. After taking a dose of 2 mg, Cmax is achieved after 2-3 hours. The absolute bioavailability after oral administration exceeds 90%. Taking with food does not affect bioavailability. Prucaloprid is widely distributed in the body, Vd at equilibrium is 567 liters. Plasma protein binding is approximately 30%.

The equilibrium state is achieved after 3-4 days of administration, and when prucaloprid is taken at a dose of 2 mg 1 time / day, Cmin and Cmax in blood plasma in equilibrium are 2.5 and 7 ng / ml, respectively.

The pharmacokinetics of prucaloprid is linearly dependent on the dose in the range of up to 20 mg / day. With long-term administration 1 time / day, pharmacokinetics does not depend on the duration of administration.

The metabolism of prucalopride in the human liver in vitro is very slow, and only a small amount of metabolites is formed. After oral administration of 14C-labeled prucalopride in a person, 8 metabolites are found in urine and feces in small amounts. The main metabolite (R107504, formed by O-demethylation of prucalopride and oxidation of the resulting alcohol to carboxylic acid) is less than 4% of the dose. Studies with a radioactive label have shown that about 85% of the active substance remains unchanged; The metabolite R107504 is present in plasma in small amounts.

Most of the orally taken dose is excreted unchanged (approximately 60% by the kidneys and at least 6% in the feces). Excretion of unchanged prucalopride by the kidneys includes passive filtration and active secretion. The clearance of prucalopride from blood plasma averages 317 ml / min, the final T1 / 2 is about 1 day.

Indications of the active substances of the drug Vegaprat

Symptomatic treatment of chronic constipation in women in whom laxatives have not provided a sufficient effect in eliminating symptoms.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken orally, regardless of food intake, at any time of the day. The initial dose is 1 mg 1 time / day, if necessary, the dose is increased to 2 mg 1 time / day.

For patients with severely impaired renal or hepatic function, the dose is 1 mg 1 time / day.

Side effect

From the digestive system: very often - nausea, diarrhea, abdominal pain; often - vomiting, dyspepsia, rectal bleeding, flatulence, abnormal bowel sounds; infrequently - anorexia.

From the nervous system: very often - headache; often - dizziness; infrequently - tremor.

From the side of the cardiovascular system: infrequently - palpitations.

From the urinary system: often - pollakiuria.

General reactions: often - weakness; infrequently - fever, feeling unwell.

Contraindications for use

Kidney dysfunction requiring dialysis; intestinal perforation or obstruction due to anatomical or functional disorders of the intestinal wall, mechanical intestinal obstruction, severe intestinal inflammation, incl. Crohn's disease, ulcerative colitis, and toxic megacolon / megarectum; hypersensitivity to prucaloprid.

Application during pregnancy and lactation

Not recommended for use during pregnancy and lactation (breastfeeding).

In clinical studies, cases of miscarriage have been reported, although, given the presence of other risk factors, the relationship of these phenomena with the use of prucaloprid remains unproven.

Women of childbearing age should use reliable methods of contraception during treatment.

Prucaloprid is excreted in breast milk, however, when used in therapeutic doses, the effect on newborns / infants is unlikely. There are no data on use in nursing mothers.

In preclinical studies on animals, no direct or indirect adverse effects on the course of pregnancy, development of the embryo / fetus, childbirth and postnatal development of offspring have been revealed; any effect on the fertility of males and females.

special instructions

Use with caution in patients with severe and clinically unstable concomitant diseases (liver disease, lungs, cardiovascular, neurological, endocrine diseases, mental disorders, cancer, AIDS) has not been studied, use with extreme caution in patients with cardiac arrhythmias or coronary artery disease history.

Due to the specific mechanism of action of prucalopride (stimulation of intestinal motility), an increase in the daily dose of more than 2 mg is unlikely to lead to an increase in the effect. If taking prucaloprid 1 time / day for 4 weeks does not give an effect, the patient should be re-examined and the expediency of continuing treatment should be determined.

In severe diarrhea, the effectiveness of oral contraceptives may decrease, and it is recommended to use additional methods of contraception to prevent the decrease in the effectiveness of oral contraceptives.

Use in pediatrics

Not recommended for use in children and adolescents under 18 years of age.

Influence on the ability to drive vehicles and use mechanisms

In some cases, the use of prucalopride was associated with the development of dizziness and weakness, especially in the first days of treatment, which may affect the ability to drive vehicles and moving mechanisms.

Drug interactions

In vitro data indicate the weak ability of prucaloprid to interact, and at therapeutic concentrations it is unlikely to affect the metabolism of simultaneously used drugs carried out by enzymes of the cytochrome system. Although prucalopride may bind weakly to P-glycoprotein, it does not inhibit P-glycoprotein activity at clinically relevant concentrations.

A potent inhibitor of the isoenzyme CYP3A4 and P-glycoprotein ketoconazole at a dose of 200 mg 2 times / day increased the AUC of prucaloprid by about 40%. This effect is not clinically significant, and is most likely associated with the suppression of the active transport of prucalopride in the kidneys by P-glycoprotein. The same interaction as with ketoconazole can be observed with other active inhibitors of P-glycoprotein, for example, verapamil, cyclosporine A and quinidine. Prucalopride is also likely to be transported in the kidney and other vectors. In theory, suppression of the activity of all carriers involved in the active secretion of prucalopride in the kidneys (including P-glycoprotein) can increase the level of its systemic exposure by 75%.

With the simultaneous use of prucalopride and erythromycin, the concentration of the latter in the blood plasma increases by 30%. The mechanism of this interaction is not completely clear, but the available data indicate that it is most likely not the result of the direct action of prucalopride, but a consequence of the high variability of the pharmacokinetics of erythromycin itself.

Use with caution in conjunction with drugs that can lengthen the QTc interval.

Atropine-like substances can weaken the effects of prucaloprid, mediated through serotone 5-HT4 receptors.

Terms and conditions of storage

The medicine should be stored in a dark place at a temperature not exceeding 25 ? C. Keep out of the reach of children. Shelf life is 2 years.

Conditions of dispensing from pharmacies

In pharmacies, the drug is sold by prescription.