Resolor Filmomhulde Tabletten,

Uses

Resolor Filmomhulde Tabletten, is used for symptomatic treatment of chronic constipation in adults in whom laxatives fail to provide adequate relief.
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.

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 Filmomhulde Tabletten, is also used to associated treatment for these conditions: Opioid Induced Constipation (OIC), Chronic idiopathic constipation (CIC), Refractory Chronic idiopathic constipation

How Resolor Filmomhulde Tabletten, works

Resolor Filmomhulde Tabletten, acts as a selective stimulator of the 5-HT4 receptors while having no interaction with hERG channel or 5-HT1 receptors which reduces significantly the cardiovascular risk found in other similar drugs.

5-HT4 receptors can be found throughout the gastrointestinal tract primarily in smooth muscle cells, enterochromaffin cells, and myenteric plexus. Its activation produces the release of acetylcholine which is the major excitatory neurotransmitter in the GI tract.

Hence, prucalopride stimulates motility by interacting specifically with 5-HT4 receptors in the GI tract which causes a release of acetylcholine and further contraction of the muscle layer of the colon and relaxation of the circular muscle layer leading to the propulsion of luminal content.

Dosage

Resolor Filmomhulde Tabletten, dosage

Adults: 2 mg once daily with or without food, at any time of the day. Due to the specific mode of action of prucalopride (stimulation of propulsive motility), exceeding the daily dose of 2 mg is not expected to increase efficacy.

Older people: Start with 1 mg once daily; if needed the dose can be increased to 2 mg once daily.

Children: Resolor Filmomhulde Tabletten, should not be used in children and adolescents younger than 18 years

Side Effects

The most frequently reported adverse reactions associated with Resolor Filmomhulde Tabletten, therapy are headache (17.8%) and gastrointestinal symptoms (abdominal pain), nausea and diarrhoea. The adverse reactions occur predominantly at the start of therapy and usually disappear within a few days with continued treatment. Other adverse reactions have been reported occasionally. The majority of adverse events were mild to moderate in intensity.

Toxicity

Resolor Filmomhulde Tabletten, is well tolerated in doses reaching 10 times the recommended therapeutic dose and signs of overdose are thought to be stared by the presence of headaches, nausea and diarrhea. Carcinogenicity studies in mice indicated an increased incidence of mammary gland adenocarcinoma at a dose of 80 mg/kg/day. In rats, high doses were linked to increased incidence of benign adrenal pheochromocytoma, pituitary adenoma, pancreatic adenoma, hepatocellular adenoma and thyroid follicular tumors.

For genotoxicity, prucalopride showed only one weak positive result in one of the five bacterial strain reverse mutation test at high concentrations. As well, there is no evidence of adverse effects on fertility, even in high doses.

Precaution

• 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 Filmomhulde Tabletten, to patients with severe hepatic impairment (Child-Pugh class C) due to limited data in patients with severe hepatic impairment.
• 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.
• 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.

Interaction

In-vitro data indicate that, Resolor Filmomhulde Tabletten, has a low interaction potential and therapeutic concentrations of Resolor Filmomhulde Tabletten, are not expected to affect the CYP-mediated metabolism of co medicated medicinal products. Although Resolor Filmomhulde Tabletten, may be a weak substrate for P-glycoprotein (P-gp), it is not an inhibitor of P-gp at clinically relevant concentrations.

Ketoconazole (200 mg b.i.d.), 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.

Studies in healthy subjects showed that, there were no clinically relevant effects of Resolor Filmomhulde Tabletten, on the pharmacokinetics of warfarin, digoxin, alcohol, paroxetine or oral contraceptives.

Food Interaction

• Take with or without food.

Resolor Filmomhulde Tabletten, Drug Interaction

Moderate: ipratropium, diphenhydramineUnknown: lactobacillus acidophilus, lubiprostone, multivitamin with minerals, ciprofloxacin, pancrelipase, duloxetine, lvp solution, apixaban, linaclotide, pregabalin, metoprolol, polyethylene glycol 3350, acetaminophen, montelukast, multivitamin, cyanocobalamin, ascorbic acid, cholecalciferol

Resolor Filmomhulde Tabletten, Disease Interaction

Major: intestinal inflammation, intestinal perforation, renal dysfunctionModerate: depression

Volume of Distribution

The mean volume of distribution of prucalopride is registered to be 623 L.

Elimination Route

Resolor Filmomhulde Tabletten, is well absorbed and it reaches maximum plasma concentration of 3.79ng/ml with a tmax of 2.77 hours after initial administration. It presents an AUC of 96.5 mn.h/ml. The bioavailability of prucalopride is of over 90% and this bioavailability does not get influenced by the ingestion of food.

Half Life

The reported half-life of prucalopride is of around 18-20 hours.

Clearance

Resolor Filmomhulde Tabletten, renal clearance is reported to be of 17 L/h which actually exceeds the glomerular filtration rate of the kidney.

Elimination Route

After maximum plasma concentration, prucalopride concentration decline in a biphasic manner. Resolor Filmomhulde Tabletten, is mainly excreted by the urine, representing 84% of the administered dose while only 13% of the dose is recovered in feces.

Pregnancy & Breastfeeding use

Resolor Filmomhulde Tabletten, is not recommended during pregnancy and women of childbearing potential should use effective contraception during treatment. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition, or postnatal development. In the absence of human data, it is not recommended to use Resolor Filmomhulde Tabletten, during breastfeeding

Contraindication

Resolor Filmomhulde Tabletten, is contraindicated in those people who are hypersensitive to the active substance or to any of the excipients and people with renal impairment requiring dialysis.

Acute Overdose

An overdose may result in symptoms resulting from an exaggeration of prucalopride's known pharmacodynamic effects and include headache, nausea and diarrhoea. Specific treatment is not available for Resolor Filmomhulde Tabletten, 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.

Storage Condition

Store at room temperature, below 30°C. Do not remove desiccant. Dispense in original bottle.

Innovators Monograph

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