Darifenacin

Darifenacin is a competitive muscarinic receptor antagonist. Muscarinic receptors play a role in cholinergically mediated functions, including contractions of the urinary bladder smooth muscle.

• Darifenacin extended-release tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.ICD-10: N32.81

• Darifenacin extended-release tablets are contraindicated in patients with, or at risk for, the following conditions: urinary retention gastric retention, or uncontrolled narrow-angle glaucoma. Darifenacin extended-release tablets are contraindicated in patients with, or at risk for, the following conditions ( 4 ): urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma.contraindicated

The recommended starting dose of darifenacin extended-release tablets is 7.5 mg orally once daily. Based upon individual response, the dose may be increased to 15 mg once daily, as early as two weeks after starting therapy. Darifenacin extended-release tablets should be taken orally once daily with water. Darifenacin extended-release tablets may be taken with or without food, and should be swallowed whole and not chewed, divided or crushed. For patients with moderate hepatic impairment (Child-Pugh B) or when co-administered with potent CYP3A4 inhibitors (for example, ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin and nefazadone), the daily dose of darifenacin extended-release tablets should not exceed 7.5 mg. Darifenacin extended-release tablets are not recommended for use in patients with severe hepatic impairment (Child-Pugh C) [see Warnings and Precautions (5.6), Drug Interactions (7.1) , Use in Specific Populations (8.6) and Clinical Pharmacology (12.3) ] . The recommended starting dose of darifenacin extended-release tablets is 7.5 mg once daily.

Darifenacin extended-release tablets should be administered with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention ( 5.1 ) Darifenacin extended-release tablets should be administered with caution to patients with gastrointestinal obstructive disorders because of the risk of gastric retention ( 5.2 ) Darifenacin extended-release tablets should be used with caution in patients being treated for narrow-angle glaucoma and only where the potential benefits outweigh the risks ( 5.3 ) Central Nervous System Effects: Somnolence has been reported with darifenacin extended-release tablets. Advise patients not to drive or operate heavy machinery until they know how darifenacin extended-release tablets affect them ( 5.5 ) 5.1 Risk of Urinary Retention Darifenacin extended-release tablets should be administered with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention. 5.2 Decreased Gastrointestinal Motility Darifenacin extended-release tablets should be administered with caution to patients with gastrointestinal obstructive disorders because of the risk of gastric retention. Darifenacin extended-release tablets, like other anticholinergic drugs, may decrease gastrointestinal motility and should be used with caution in patients with conditions such as severe constipation, ulcerative colitis, and myasthenia gravis.

The most frequently reported adverse reactions (greater than 3%) for darifenacin extended-release tablets are: constipation, dry mouth, headache, dyspepsia, nausea, urinary tract infection, accidental injury, and flu symptoms ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Aurobindo Pharma USA, Inc. at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of darifenacin extended-release tablets was evaluated in controlled clinical trials in a total of 8,830 patients, 6,001 of whom were treated with darifenacin extended-release tablets. Of this total, 1,069 patients participated in three, 12-week, randomized, placebo-controlled, fixed-dose efficacy and safety studies (Studies 1, 2 and 3). Of this total, 337 and 334 patients received darifenacin extended-release tablets 7.5 mg daily and 15 mg daily, respectively. In all long-term trials combined, 1,216 and 672 patients received treatment with darifenacin extended-release tablets for at least 24 and 52 weeks, respectively. In Studies 1, 2 and 3 combined, the serious adverse reactions to darifenacin extended-release tablets were urinary retention and constipation.

Pregnancy: Darifenacin extended-release tablets should be used during pregnancy only if the benefit to the mother outweighs the potential risk to the fetus ( 8.1 ) Nursing Mothers: It is not known whether darifenacin is excreted into human milk and therefore caution should be exercised before darifenacin extended-release tablets are administered to a nursing woman (8.3) Pediatric Use: The safety and effectiveness of darifenacin extended-release tablets in pediatric patients have not been established ( 8.4 ) 8.1 Pregnancy Risk Summary There are no available data on darifenacin extended-release tablets use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal studies, darifenacin was not teratogenic in rats and rabbits at plasma exposures of free drug (via AUC) up to 59 and 28 times the maximum recommended human dose (MRHD) of 15 mg, respectively. Effects on embryofetal development were observed following administration of darifenacin during pregnancy (dilated ureter and/or kidney pelvis in rabbits at about 9 times the MRHD, post-implantation loss in rabbits at about 28 times, and delayed ossification in rats at about 59 times) and during pregnancy and lactation (developmental delays in rats at about 17 times the MRHD), which was associated with maternal toxicity (see Data).

Metabolism

Absorption After oral administration of darifenacin extended-release tablets to healthy volunteers, peak plasma concentrations of darifenacin are reached approximately seven hours after multiple dosing and steady-state plasma concentrations are achieved by the sixth day of dosing. The mean (SD) steady-state time course of darifenacin extended-release tablets 7.5 mg and 15 mg is depicted in Figure 1.

Overdosage with antimuscarinic agents, including darifenacin extended-release tablets, can result in severe antimuscarinic effects. Treatment should be symptomatic and supportive. In the event of overdosage, ECG monitoring is recommended. Darifenacin extended-release tablets have been administered in clinical trials at doses up to 75 mg (five times the maximum therapeutic dose) and signs of overdose were limited to abnormal vision.

• Sep 1, 2016ANDAANDA207664Cipla
• Sep 19, 2016ANDAANDA206743Aurobindo Pharma
• Nov 17, 2016ANDAANDA205209Torrent
• Jul 28, 2017ANDAANDA207302Macleods Pharms Ltd
• Dec 8, 2017ANDAANDA207681Alembic
• Jan 6, 2020ANDAANDA211045Puracap Labs Blu

1. 1Drug Ineffective18321%
2. 2Herpes Zoster13616%
3. 3Peripheral Swelling13516%
4. 4Pneumonia Viral11714%
5. 5Arthralgia11313%
6. 6Synovitis10713%
7. 7Anaemia10212%
8. 8Fibromyalgia10012%
9. 9Arthritis9811%
10. 10Joint Swelling9711%
11. 11Blood Cholesterol Increased9611%
12. 12Leukopenia9611%
13. 13Liver Function Test Abnormal8910%
14. 14Infection8710%
15. 15Oral Pain809.4%

The 10 most recently updated of 30 ClinicalTrials.gov registrations naming Darifenacin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Efficacy of Low-Intensity Shockwave Therapy in Treating Radiation Cystitis
  Completed · Early phase 1 · Interventional · 25 enrolled · Thanakrit Visuthikosol
  NCT07016451updated 2026-05-15
• Efficacy and Tolerability of Tadalafil Versus Darifenacin in Management of Ureteric Stent-Related LUTS
  Completed · Phase 1 · Phase 2 · Interventional · 150 enrolled · Ain Shams University
  NCT07206706updated 2026-01-16
• A Study to Assess the Safety, Tolerability, and Pharmacology of Darifenacin in Patients With ALS
  Recruiting · Phase 2 · Interventional · 30 enrolled · Oliver Blanchard
  NCT06249867updated 2025-09-05
• A Prospective, Observational, Multicenter Study of Patients Following Initiation of a New Course of Treatment for Overactive Bladder (OAB)
  Completed · Observational · 1,524 enrolled · Astellas Scientific & Medical Affairs, Inc.
  NCT02386072updated 2024-10-16
• Treatment Persistence Among Patients With Overactive Bladder: A Retrospective Secondary Data Analysis in Asia Oceania
  Completed · Observational · 5,589 enrolled · Astellas Pharma Singapore Pte. Ltd.
  NCT03602508updated 2024-10-16
• Darifenacin x Parasacral Transcutaneous Electric Nerve Stimulation for OAB in Patients Infected With Human T-Lymphotropic Virus 1
  Completed · Phase 4 · Interventional · 42 enrolled · Hospital Universitário Professor Edgard Santos
  NCT06616675updated 2024-10-01
• A Two-week Open-label Pharmacodynamic and Pharmacokinetic Study of Multiple Doses of a Darifenacin Liquid Oral Suspension in Children (2 - 15 Years) With Neurogenic Detrusor Overactivity
  Terminated · Phase 2 · Interventional · 35 enrolled · Warner Chilcott
  NCT00712322updated 2022-06-09
• A Registry Study of Patients Initiating a Course of Drug Therapy for Overactive Bladder in Taiwan, Korea and China
  Completed · Observational · 805 enrolled · Astellas Pharma Singapore Pte. Ltd.
  NCT03572231updated 2020-04-22
• Bladder Antimuscarinic Medication and Accidental Bowel Leakage
  Completed · Observational · 32 enrolled · University of Alabama at Birmingham
  NCT03543566updated 2019-01-22
• Behavioural Therapy With Checklist for Overactive Bladder
  Completed · Interventional · 120 enrolled · Ankara Training and Research Hospital
  NCT03662893updated 2018-09-10

CPIC-curated drug–gene pairs for Darifenacin. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2D6CPIC C (provisional)FDA label: Informative PGx

Frequently asked questions

How does Darifenacin work?

Darifenacin is a competitive muscarinic receptor antagonist. Muscarinic receptors play a role in cholinergically mediated functions, including contractions of the urinary bladder smooth muscle.

What is Darifenacin used for?

According to FDA labeling, Darifenacin carries indications including: Darifenacin extended-release tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Darifenacin?

Darifenacin is classified as Drugs for urinary frequency and incontinence, Cholinergic Muscarinic Antagonist, Cholinergic Muscarinic Antagonists.

What are the brand names for Darifenacin?

Darifenacin is marketed under brand names including Enablex.

What are the contraindications for Darifenacin?

Darifenacin labeling lists contraindications including: Darifenacin extended-release tablets are contraindicated in patients with, or at risk for, the following conditions: urinary retention gastric retention, or uncontrolled narrow-angle glaucoma. Darifenacin extended-release tablets are contraindicated in patients with, or at risk for, the following conditions ( 4 ): urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma.. Always consult the full prescribing information and a clinician.