Vegaprat pills 2 mg 30 pcs
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Active ingredients
Prucalopride
Release form
Pills
Composition
Prukaloprid succinate 2.642 mg,; which corresponds to the content of Procruloprid 2 mg; Excipients: microcrystalline cellulose - 192 mg, sodium carboxymethyl starch - 2.838 mg, magnesium stearate - 1.8 mg, silicon dioxide, colloidal - 0.72 mg; The composition of the shell: hypromellose 6 cP - 3.6 mg, macrogol 6000 - 1.2 mg, titanium dioxide - 1 mg, talc - 0.2 mg.
Pharmacological effect
A means that improves intestinal motility, dihydrobenzofurancarboxamide. The action on intestinal motility is most likely due to the selectivity and high affinity of prucalopride for serotonin 5-HT4 receptors.
Pharmacokinetics
After a single ingestion of prukaloprid rapidly absorbed from the gastrointestinal tract. After taking a dose of 2 mg Cmax is achieved in 2-3 hours. The absolute bioavailability after oral administration exceeds 90%. Reception during meals does not affect bioavailability. Prukaloprid is widely distributed in the body, Vd in the equilibrium state is 567 l. Plasma protein binding is approximately 30%. The equilibrium state is reached after 3-4 days of administration, and when taking prucaloprid at a dose of 2 mg 1 time / day, Cmin and Cmax in plasma are 2.5 and 7 ng / ml in equilibrium, respectively .; The pharmacokinetics of prucalopride is linearly dependent on the dose in the range of up to 20 mg / day. With long-term administration of 1 time / day, the pharmacokinetics do not depend on the duration of administration.; In vitro, the metabolism of prucalopride in the human liver proceeds very slowly, and only a small amount of metabolites is formed. After oral ingestion of 14C-labeled prukaloprid in the urine and feces by humans, 8 metabolites are detected in a small amount. 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 have shown with a radioactive label, about 85% of the active substance remains unchanged; metabolite R107504 is present in plasma in a small amount.; Most of the orally taken dose is excreted unchanged (approximately 60% by the kidneys and at least 6% with feces). The elimination of unchanged prucalopride by the kidneys includes passive filtration and active secretion.The plasma clearance of prucaloprid is on average 317 ml / min, the final T1 / 2 is about 1 day.
Indications
Symptomatic therapy of chronic constipation in women whose laxatives have not provided sufficient effect in eliminating the symptoms.
Contraindications
Impaired renal function requiring dialysis; perforation or obstruction of the intestine due to anatomical or functional disorders of the intestinal wall, mechanical intestinal obstruction, severe inflammation of the intestine, including Crohn's disease, ulcerative colitis and toxic megacolon / megarectum; hypersensitivity to prucaloprid
Use during pregnancy and lactation
It is not recommended to use during pregnancy and lactation (breastfeeding) .; There have been cases of miscarriage in clinical studies, although, given the presence of other risk factors, the relationship of these phenomena with the use of prucalopride remains unproven.; Women of childbearing age should use reliable methods during treatment. contraception.; Prukaloprid is excreted in breast milk, but when used in therapeutic doses, the effect on the newborn / infant is unlikely. There are no data on use in nursing mothers. In preclinical studies in animals, no direct or indirect adverse effect on the course of pregnancy, embryo / fetus development, childbirth, or postnatal development of offspring has been identified; any effect on the fertility of males and females.
Dosage and administration
Is ingested, regardless of the meal, 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 liver function, the dose is 1 mg 1 time / day.
Side effects
On the part of the digestive system: very often - nausea, diarrhea, abdominal pain; often - vomiting, dyspepsia, rectal bleeding, flatulence, abnormal intestinal noise; infrequently - anorexia. From the nervous system: very often - headache; often - dizziness; infrequently - tremor.; From the side of the cardiovascular system: infrequently - heartbeat.; From the part of the urinary system: often - pollakiuria.; General reactions: often - weakness; infrequently - fever, feeling unwell.
Interaction with other drugs
In vitro data indicate a weak ability of prucaloprid to interact, and at therapeutic concentrations it is unlikely to affect the metabolism of simultaneously used drugs by enzymes of the cytochrome system. Although prucalopride may poorly bind to P-glycoprotein, in clinically significant concentrations it does not inhibit the activity of P-glycoprotein.; A powerful inhibitor of the CYP3A4 isoenzyme and P-glycoprotein ketoconazole 200 mg 2 times / day increased the AUC of prucalopride by about 40%. This effect is not clinically significant, and is most likely associated with the suppression of the active transport of prukaloprid in the kidneys by P-glycoprotein. The same interaction as with ketoconazole can be observed with other active inhibitors of β-glycoprotein, for example, verapamil, cyclosporin A and quinidine. Prucalopride is also likely transported by kidney and other vectors. Theoretically, the suppression of the activity of all carriers involved in the active secretion of prucaloprid in the kidneys (including P-glycoprotein) can increase the level of its systemic effect by 75%. With simultaneous use of prucalopride and erythromycin, the latter concentration 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 the result of the high variability of the pharmacokinetics of erythromycin itself.; Use caution along with drugs that can lengthen the QTc interval .; Atropin-like substances can weaken the effects of prucalopride mediated through serotonic 5-HT4 receptors.
special instructions
To use with caution in patients with severe and clinically unstable concomitant diseases (liver, lung, cardiovascular, neurological, endocrine diseases, mental disorders, oncological diseases, AIDS) have not been studied, with particular caution in patients with heart rhythm disorders or ischemic heart disease in 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 increase the effect.If taking prucaloprid 1 time / day for 4 weeks does not work, you should re-examine the patient and determine the appropriateness of continuing treatment. In severe diarrhea, the effectiveness of oral contraceptives may decrease, and additional methods of contraception are recommended to prevent the effectiveness of oral contraceptives. in pediatrics; Not recommended for use in children and adolescents under the age of 18.; Effects on the ability to drive vehicles and control mechanisms; in cases with the use of prucalopride, development of dizziness and weakness was associated, especially in the first days of treatment, which may affect the ability to drive vehicles and moving mechanisms.