Darifenacin (trade name Enablex in United States and Canada, Emselex in the European Union) is a

medication A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the medical field and ...

used to treat

urinary incontinence Urinary incontinence (UI), also known as involuntary urination, is any uncontrolled leakage of urine. It is a common and distressing problem, which may have a large impact on quality of life. It has been identified as an important issue in geri ...

due to an

overactive bladder Overactive bladder (OAB) is a condition where there is a frequent feeling of needing to urinate to a degree that it negatively affects a person's life. The frequent need to urinate may occur during the day, at night, or both. If there is loss ...

. It was discovered by scientists at the Pfizer research site in Sandwich, UK under the identifier UK-88,525 and used to be marketed by

Novartis Novartis AG is a Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and Cambridge, Massachusetts, United States (global research).name="novartis.com">https://www.novartis.com/research-development/research-lo ...

. In 2010, the US rights were sold to

Warner Chilcott Warner Chilcott (formerly Galen) was a company in the pharmaceutical industry based in Rockaway, New Jersey. It was primarily focused on women’s healthcare and dermatology. On October 1, 2013, the company was acquired by Actavis (now Allergan). ...

for .

Adverse effects

Darifenacin should not be used in people with

urinary retention Urinary retention is an inability to completely empty the bladder. Onset can be sudden or gradual. When of sudden onset, symptoms include an inability to urinate and lower abdominal pain. When of gradual onset, symptoms may include loss of bladd ...

. Anticholinergic agents, such as darifenacin, may also produce constipation and blurred vision.

Heat prostration Heat illness is a spectrum of disorders due to increased body temperature. It can be caused by either environmental conditions or by exertion. It includes minor conditions such as heat cramps, heat syncope, and heat exhaustion as well as the mo ...

(due to decreased sweating) can occur when anticholinergics such as darifenacin are used in a hot environment.

Medical uses

Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency in adults. It may also be recommended with an

alpha blocker Alpha (uppercase , lowercase ; grc, ἄλφα, ''álpha'', or ell, άλφα, álfa) is the first letter of the Greek alphabet. In the system of Greek numerals, it has a value of one. Alpha is derived from the Phoenician letter aleph , whic ...

to help provide symptomatic benefit for overactive bladder and obstructive symptoms such as likely associated with

benign prostatic hypertrophy Benign prostatic hyperplasia (BPH), also called prostate enlargement, is a noncancerous increase in size of the prostate gland. Symptoms may include frequent urination, trouble starting to urinate, weak stream, inability to urinate, or loss o ...

. American Urological Association (AUA) Guideline. Diagnosis and Treatment of Overactive Bladder in Adults: AUA/SUFA guideline 2012

Mechanism of action

Darifenacin works by blocking the M₃

muscarinic acetylcholine receptor Muscarinic acetylcholine receptors, or mAChRs, are acetylcholine receptors that form G protein-coupled receptor complexes in the cell membranes of certain neurons and other cells. They play several roles, including acting as the main end- ...

, which is primarily responsible for

bladder The urinary bladder, or simply bladder, is a hollow organ in humans and other vertebrates that stores urine from the kidneys before disposal by urination. In humans the bladder is a distensible organ that sits on the pelvic floor. Urine en ...

muscle contraction Muscle contraction is the activation of tension-generating sites within muscle cells. In physiology, muscle contraction does not necessarily mean muscle shortening because muscle tension can be produced without changes in muscle length, such a ...

s. It thereby decreases the urgency to

urinate Urination, also known as micturition, is the release of urine from the urinary bladder through the urethra to the outside of the body. It is the urinary system's form of excretion. It is also known medically as micturition, voiding, uresis, ...

. It is not known whether this selectivity for the M₃ receptor translates into any clinical advantage when treating symptoms of

syndrome.

References

External links

* * {{Portal bar , Medicine Muscarinic antagonists 5-Benzofuranethanamines Carboxamides CYP2D6 inhibitors AbbVie brands Novartis brands Pyrrolidines Benzhydryl compounds