Included in the formulation
АТХ:A.06.A.X.05 Prukalopride
Pharmacodynamics:Selective, high affinity 5HT agonist4-serotonin receptors, enhancing intestinal motility.
Pharmacokinetics:After oral administration, it is rapidly absorbed from the digestive tract. After taking a 2 mg dose, the maximum concentration is achieved in 2-3 hours. Absolute bioavailability after oral intake exceeds 90% and does not depend on food intake. Binding to plasma proteins is approximately 30%. The equilibrium concentration is achieved after 3-4 days of admission, and when taking the drug at a dose of 2 mg once a day, the minimum and maximum concentration in the blood plasma in the equilibrium state are 2.5 and 7 ng / ml, respectively. The pharmacokinetics of prucalopride linearly depend on the dose in the range of up to 20 mg per day and when taken once a day does not depend on the duration of treatment. Biotransformation occurs in the liver. About 85% of the orally taken dose is excreted unchanged in the main kidneys. And partly through the intestines. The clearance from plasma is an average of 317 ml / min, the final half-life - approximately 24 hours.
Indications:Symptomatic therapy of chronic constipation in women with ineffective laxatives.
XI.K55-K63.K59.0 Constipation
Contraindications:Impaired renal function requiring dialysis; perforation or bowel obstruction due to anatomical or functional disorders of the intestinal wall, mechanical intestinal obstruction, severe intestinal inflammation, including Crohn's disease, ulcerative colitis and toxic megacolon or megarethktum; hypersensitivityto the preparation.
Carefully:Use with caution in patients with severe and clinically unstable concomitant diseases (liver, lung, cardiovascular diseaseneurological, endocrine diseases, mental disorders, oncological diseases, AIDS), with extreme caution - for heart rhythm disturbances or coronary artery disease in the anamnesis.
Pregnancy and lactation:It is not recommended to use during pregnancy and lactation.
Women of childbearing age in the period of treatment should use reliable methods of contraception.
Prucalopril is excreted in breast milk, but when applied in therapeutic doses, the effect on newborns and infants is unlikely. Data on the use of lactating mothers are absent.
Dosing and Administration:Accepted inside regardless of food intake, at any time of the day.
Adult patients and elderly patients (over 65 years of age): the initial dose is 1 mg once a day, if necessary, increase the dose to 2 mg once a day.
Patients with severe impairment of kidney or liver function are prescribed 1 mg 1 time per day.
It is not recommended for use in children and adolescents under 18 years of age.
Side effects:From the side digestive system: very often - nausea, diarrhea, abdominal pain; often - vomiting, indigestion, rectal bleeding, flatulence, pathological intestinal noises; infrequently - anorexia.
From the side nervous system: very often - headache; often - dizziness; infrequently - a tremor.
From the side of cardio-vascular system: infrequently - palpitations.
From the side urinary system: often - pollakiuria.
Common reactions: often - weakness; infrequently - a fever, bad state of health.
Overdose:Symptoms: increased side effects, including headache, nausea and diarrhea.
Treatment: symptomatic. With a large loss of fluid due to diarrhea or vomiting - correction of electrolyte balance disorders.
Interaction:With caution apply simultaneously with drugs that can extend the QT interval.
Atropine-like substances can weaken the effects of prucalopride mediated via serotonin 5-HT4 receptors.
Special instructions:Increasing the daily dose of more than 2 mg does not lead to an increase in action. If the drug is administered once a day for 4 weeks does not produce the desired effect, the patient should be re-examined and the expediency of continuing treatment should be determined.
With severe diarrhea, the effectiveness of oral contraceptives may decrease; recommended the use of additional methods of contraception.
There may be dizziness and weakness, especially in the early days of treatment, which can affect the ability to drive vehicles and moving mechanisms.