Darifenacin

• Urinary antispasmodics
• ATC:G04BD10

• Enablex

• Cystosol W 3% Hexitols (Mannitol + Sorbitol)
• Sorbitol Mannitol Irrigation (Mannitol + Sorbitol)

C₂₈H₃₀N₂O₂

http://www.rxlist.com/cgi/generic3/enablex.htm

Darifenacin FDA

No information avaliable

426.55 g/mol

No information avaliable

No information avaliable

Solid

4.832

Extended-release tablets (containing 7.5 mg or 15 mg darifenacin as hydrobromide salt)

For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.

Darifenacin is a competitive muscarinic receptor antagonist. In vitro studies using human recombinant muscarinic receptor subtypes show that darifenacin has greater affinity for the M3 receptor than for the other known muscarinic receptors (9 and 12-fold greater affinity for M3 compared to M1 and M5, respectively, and 59-fold greater affinity for M3 compared to both M2 and M4). Muscarinic receptors play an important role in several major cholinergically mediated functions, including contractions of the urinary bladder smooth muscle and stimulation of salivary secretion. Adverse drug effects such as dry mouth, constipation and abnormal vision may be mediated through effects on M3 receptors in these organs.

The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.

Overdosage can potentially result in severe central anticholinergic effects.

Humans and other mammals