Darifenacin
Brand names,
Darifenacin
Analogs
Darifenacin
Brand Names Mixture
- Cystosol W 3% Hexitols (Mannitol + Sorbitol)
- Sorbitol Mannitol Irrigation (Mannitol + Sorbitol)
Darifenacin
Chemical_Formula
C28H30N2O2
Darifenacin
RX_link
http://www.rxlist.com/cgi/generic3/enablex.htm
Darifenacin
fda sheet
Darifenacin
msds (material safety sheet)
Darifenacin
Synthesis Reference
No information avaliable
Darifenacin
Molecular Weight
426.55 g/mol
Darifenacin
Melting Point
No information avaliable
Darifenacin
H2O Solubility
No information avaliable
Darifenacin
State
Solid
Darifenacin
LogP
4.832
Darifenacin
Dosage Forms
Extended-release tablets (containing 7.5 mg or 15 mg darifenacin as hydrobromide salt)
Darifenacin
Indication
For the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
Darifenacin
Pharmacology
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.
Darifenacin
Absorption
The mean oral bioavailability at steady state is estimated to be 15% and 19% for 7.5 mg and 15 mg tablets, respectively.
Darifenacin
side effects and Toxicity
Overdosage can potentially result in severe central anticholinergic effects.
Darifenacin
Patient Information
Darifenacin
Organisms Affected
Humans and other mammals