Presentation and Status in Health Basket
Film Coated Tablets
28 X 1 mg
Film Coated Tablets
28 X 2 mg
Women: 2 mg once daily.
Men: The safety and efficacy of Resolor for use in men has not been established in controlled clinical trials therefore Resolor is not recommended for use in men until further data becomes available.
Elderly (>65 years): Start with one 1 mg once daily; if needed the dose can be increased to 2 mg once daily.
Children and adolescents: Resolor is not recommended in children and adolescents younger than 18 years until further data become available.
Patients with renal impairment: The dose for patients with severe renal impairment (GFR < 30 ml/min/1.73 m2) is 1 mg once daily. No dose adjustment is required for patients with mild to moderate renal impairment.
Patients with hepatic impairment: Patients with severe hepatic impairment (Child-Pugh class C) start with 1 mg once daily which may be increased to 2 mg if required to improve efficacy and if the 1 mg dose is well tolerated. No dose adjustment is required for patients with mild to moderate hepatic impairment.
Resolor is indicated for symptomatic treatment of chronic constipation in women in whom laxatives fail to provide adequate relief.
Hypersensitivity to the active substance or to any of the excipients Renal impairment requiring dialysis. Intestinal perforation or obstruction due to structural or functional disorder of the gut wall, obstructive ileus, severe inflammatory conditions of the intestinal tract, such as Crohn’s disease, and ulcerative colitis and toxic megacolon/megarectum.
Renal excretion is the main route of elimination of prucalopride. A dose of 1 mg is recommended in subjects with severe renal impairment. Caution should be exercised when prescribing Resolor to patients with severe hepatic impairment (Child-Pugh class C) due to limited data in patients with severe hepatic impairment. The safety and efficacy of Resolor for use in patients with severe and clinically unstable concomitant disease (e.g. cardiovascular or lung disease, neurological or psychiatric disorders, cancer or AIDS and other endocrine disorders) have not been established in controlled clinical studied. Caution should be exercised when prescribing Resolor to patients with these conditions especially when used in patients with a history of arrhythmias or ischaemic cardiovascular disease. In case of severe diarrhoea, the efficacy of oral contraceptives may be reduced and the use of an additional contraceptive method is recommended to prevent possible failure of oral contraception.
Men: The safety and efficacy of Resolor for use in men has not been established in controlled clinical trials, therefore, Resolor is not recommended for use in men until further data becomes available. The tablets contain lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.
Headache, abdominal pain, nausea or diarrhea, dizziness, vomiting, dyspepsia, rectal haemorrhage, flatulence, abnormal bowel sounds, pollakiuria, fatigue. See prescribing information for full details.
Prucalopride has a low pharmacokinetic interaction potential. It is extensively excreted unchanged in urine (approximately 60% of the dose) and in vitro metabolism is very slow. Although 8 different metabolites are known, the most abundant of these, the carboxylic acid product of side-chain oxidative O-demethylation, represents less than 4% of the dose. Prucalopride did not inhibit specific CYP450 activities in in vitro studies in human liver microsomes at therapeutically relevant concentrations. Although prucalopride may be a weak substrate for P-glycoprotein (P-gp), it is not an inhibitor of P-gp at clinically relevant concentrations.
Effects of prucalopride on pharmacokinetics of other drugs: A 30% increase in plasma concentrations of erythromycin was found during prucalopride coadministration. The mechanism for this interaction is not clear. Prucalopride had no clinically relevant effects on the pharmacokinetics of warfarin, digoxin, alcohol, paroxetine or oral contraceptives.
Effects of other drugs on pharmacokinetics of prucalopride: Ketoconazole (200 mg twice daily), a potent inhibitor of CYP3A4 and of P-gp, increased the systemic exposure to prucalopride by approximately 40%. This effect is too small to be clinically relevant. Interactions of similar magnitude may be expected with other potent inhibitors of P-gp such as verapamil, cyclosporine A and quinidine. Therapeutic doses of probenecid, cimetidine, erythromycin and paroxetine did not affect the pharmacokinetics of prucalopride.
Pregnancy and Lactation
Pregnancy: Experience with prucalopride during pregnancy is limited. Cases of spontaneous abortion have been observed during clinical studies, although, in the presence of other risk factors, the relationship to prucalopride is unknown. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Resolor is not recommended during pregnancy. Women of childbearing potential should use effective contraception during treatment with prucalopride.
Breast-feeding: Prucalopride is excreted in breast milk. However, at therapeutic doses of Resolor no effects on breastfed newborns/infants are anticipated. In the absence of human data, it is not recommended to use Resolor during breast-feeding.
Fertility: Animal studies indicate that there is no effect on male or female fertility.
In a study in healthy volunteers treatment with prucalopride was well tolerated when given in an up-titrating scheme up to 20 mg once daily (10 times the recommended therapeutic dose). An overdose may result in symptoms resulting from an exaggeration of the medicinal product’s known pharmacodynamic effects and include headache, nausea and diarrhoea. Specific treatment is not available for Resolor overdose. Should an overdose occur, the patient should be treated symptomatically and supportive measures instituted, as required. Extensive fluid loss by diarrhoea or vomiting may require correction of electrolyte disturbances.