Darifenacin

Indications
 Oral
Overactive bladder
Adult: For symptomatic treatment of urge incontinence, urinary frequency and urgency. Initial: 7.5 mg once daily; may increase dose to 15 mg once daily if no adequate response after 2 wk of therapy.
Hepatic impairment: Moderate hepatic impairment (Child Pugh B): Maximum daily dose is 7.5 mg. Severe hepatic impairment (Child Pugh C): Not recommended.
Contraindications
 Patient with urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, and in patients who are at risk for these conditions.
Warnings / Precautions
 Anticholinergic agents including Darifenacin, may cause urinary retention and decreased GI motility. Caution when used in patients with clinically significant bladder outflow obstruction, GI obstructive disorder (e.g. pyloric stenosis), severe constipation, ulcerative colitis, and myasthenia gravis. For patients being treated for narrow-angle glaucoma, caution and only use where potential benefits outweigh the risks. May cause heat prostration when used in a hot environment. May cause dizziness and blurred vision; caution when operating machinery or driving vehicle. Not recommended in severe hepatic impairment. Safety and efficacy have not been established in paediatric patients. Pregnancy and lactation.
Adverse Reactions
 Dry mouth, nausea, abdominal pain, constipation, diarrhoea, dyspepsia, dizziness, headache, asthaenia, pain, weight gain, dry skin, rash, pruritus, dry eyes, abnormal vision, arthralgia, bronchitis, pharyngitis, rhinitis, sinusitis, flu-like syndrome, UTI, vaginitis, acute urinary retention, hypertension and peripheral oedema.
Potentially Fatal: Hypersensitivity reactions, including angioedema.
Overdose Reactions
 Symptoms: May cause severe antimuscarinic effects; abnormal vision has been reported. Treatment: Monitor ECG and provide symptomatic and supportive treatment.
Drug Interactions
 Concurrent use of CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, clarithromycin, nefazodone, troleandomycin, ritonavir, nelfinavir) or CYP2D6 inhibitors (e.g. quinidine, paroxetine) may increase serum levels of Darifenacin. CYP3A4 inducers (e.g. barbiturates, phenytoin, rifampicin) may likely decrease Darifenacin serum concentrations. Darifenacin may act as a moderate inhibitor of CYP2D6, caution when used concomitantly with CYP2D6 substrates that have narrow therapeutic index (e.g. flecainide, thioridazine, imipramine). Concurrent use of another agent with antimuscarinic properties may potentiate the side effects of Darifenacin.
See Below for More darifenacin Drug Interactions
Food Interactions
 Avoid grape fruit juice, may increase levels of Darifenacin. St John's wort may decrease Darifenacin levels.
Mechanism of Actions
 Darifenacin is a potent, competitive and selective muscarinic receptor antagonist which has greater binding affinity for muscarinic M3 receptors. M3 receptors are involved in the contraction of the detrusor muscle of the bladder, GI smooth muscle, saliva production, and iris sphincter function. Darifenacin may increase volume threshold in patients with involuntary detrusor contraction, thus increase bladder capacity.
Absorption: Tmax: About 7hr. Steady-state plasma concentrations reached within 6th day of dosing. Bioavailability: About 15% (for 7.5 mg tab) and 19% (for 15 mg tab).
Distribution: Protein binding: About 98% (mainly to α1-acid glycoproteins). Vd: About 163 L.
Metabolism: Extensive hepatic metabolism mainly by CYP3A4 and CYP2D6. Metabolism in individuals who are poor metaboliser (PMs) of CYP2D6 will be principally mediated by CYP3A4.
Excretion: Urine (about 60%) and faeces (about 40%). Elimination half-life: About 13-19 hr.
Administration
 May be taken with or without food. (Swallow whole, do not chew/crush/divide.)
Storage Conditions
 Oral: Store at 25°C (77°F); excursions permitted 15-30°C (59-86°F). Protect from light.
ATC Classification
 G04BD10 - darifenacin ; Belongs to the class of urinary antispasmodics.
Storage
 Oral: Store at 25°C (77°F); excursions permitted 15-30°C (59-86°F). Protect from light.
Available As
  • Darifenacin 15 mg
  • Darifenacin 7.5 mg

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