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JAMP DARIFENACIN is a brand name for Darifenacin, supplied as a tablet (extended-release). The medicine, its uses, side effects and dosage are the same regardless of brand.
Used for: AND CLINICAL USE.................................................................................3 CONTRAINDICATIONS.....................................................................................................3 WARNINGS AND PRECAUTIONS…
Verbatim from this product's HC label. Tap a section to expand.
Dosing Considerations Use in Children The safety and effectiveness of darifenacin hydrobromide in pediatric patients with overactive bladder or any other condition have not been investigated. Use in Elderly There are no special dosing requirements for the elderly.
Gender No special dosing requirements are necessary based on gender. Renal Insufficiency There are no special dosing requirements for patients with renal impairment. Hepatic Impairment There is a risk of increased exposure in this population, however, no dose adjustment is required in patients with mild hepatic impairment (Child Pugh A).
g. 5 mg. Jamp Darifenacin is not recommended for use in patients with severe hepatic impairment (Child Pugh C) (see CLINICAL PHARMACOLOGY Special Population Considerations). 5 mg once daily. 5 mg daily and requiring greater symptom relief, the dose may be increased to 15 mg daily as early as two weeks after starting therapy, based on individual response.
Jamp Darifenacin (darifenacin extended release tablets) should be taken once daily. They may be taken with or without food, and should be swallowed whole and not chewed, divided or crushed. OVERDOSAGE No cases of overdose were recorded in the darifenacin clinical development program that included doses as high as 60 mg daily (4 times the recommended maximum daily dose).
Moreover, in a study evaluating the interaction between ketoconazole and daily doses of 30 mg darifenacin, the systemic plasma exposure exceeded the systemic exposure observed after a 60 mg dose by a factor of two, with no reported SAEs.
” For management of a suspected drug overdose, contact your regional Poison Control Centre immediately. Page 11 of 27 Overdosage with antimuscarinic agents can potentially result in severe antimuscarinic effects. Treatment should be symptomatic and supportive when necessary.
Treatment should be aimed at reversing the antimuscarinic symptoms under careful medical supervision. ACTION AND CLINICAL PHARMACOLOGY Mechanism of Action Darifenacin is a potent muscarinic M3 selective receptor antagonist that exhibits, in vitro, a nine to 59-fold selectivity for the human M3 receptor over human M1, M2, M4 and M5 receptors.
The M3 receptor is the major subtype that modulates urinary bladder muscle contraction. Darifenacin has a clinically significant effect on bladder function. Pharmacodynamics Individuals with full CYP 2D6 activity are referred to as extensive metabolizers (EMs).
Not medical advice. Always read the patient information leaflet and follow your prescriber or pharmacist.
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5 and 15 mg extended release tablets, respectively. Pharmacokinetics Following administration of the extended release tablets maximum plasma levels are reached approximately 7 h after dosing and steady-state plasma levels are achieved by the sixth day of dosing.
76 for 15 mg) (Figure 1), thereby maintaining therapeutic plasma levels over the dosing interval. 7 hours. 5mg od 15mg od 6 5 4 3 2 1 0 0 2 4 6 8 10 12 14 16 18 20 22 24 Time post-dose (h) Darifenacin concentration (ng/ml) Page 12 of 27 Absorption In healthy volunteers, darifenacin is rapidly and completely (>98%) absorbed after oral administration, although oral bioavailability is limited by first pass metabolism (see Metabolism).
Distribution Darifenacin is a lipophilic base and is 98% bound to plasma proteins (primarily to alpha- 1- acid- glycoprotein). The steady-state volume of distribution (Vss) is estimated to be 163 L. Based on free drug levels in animal cerebrospinal fluid and plasma, darifenacin shows negligible concentrations in the CSF, suggesting low penetration of the blood brain barrier.
Metabolism Darifenacin is extensively metabolized by the liver following oral dosing. Metabolism is mediated by cytochrome P450 enzymes CYP 2D6 and CYP 3A4. The three main metabolic routes are as follows: (i) monohydroxylation in the dihydrobenzofuran ring; (ii) dihydrobenzofuran ring opening; (iii) N-dealkylation of the pyrrolidine nitrogen.
The initial products of the hydroxylation and N-dealkylation pathways are major circulating metabolites but none contributes significantly to the overall clinical effect of darifenacin. One of the hydroxylated derivatives has some anti-M3 muscarinic receptor activity.
This metabolite’s contribution to overall activity is negligible. e. approximately 7% of the Caucasian population). Therefore, the metabolism of darifenacin in these poor metabolizers (PMs) will be principally mediated via CYP 3A4. 7, respectively.
Population pharmacokinetic analyses of Phase 3 data indicated that on average PMs have 55% higher steady-state exposure than EMs. However, there is considerable overlap between the ranges of exposures seen in EM and PM populations and clinical experience confirms that there are no special dosing requirements for PMs.
Excretion Following administration of an oral dose of […]