Solifenacin_Succinate: profile and news

Astellas Pharma Obtains Approval for Funguard and Vesicare Apr 21, 2006
Vesicare Tablet (solifenacin succinate), which is currently available in about 20 countries worldwide, is the first approved agent for treating OAB. ... - Japan Corporate News (press release),

Other information

Indication
For the treatment of micturition frequency/polyuria

Pharmacology
Solifenacin Succinate is a competitive muscarinic receptor antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Muscarinic receptors play an important role in several major cholin-ergically mediated functions, including contractions of urinary bladder smooth muscle and stimulation of salivary secretion.

Mechanism Of Action
Solifenacin acts as a direct antagonist at muscarinic acetylcholine receptors in cholinergically innervated organs. Its anticholinergic-parasympatholytic action reduces the tonus of smooth muscle in the bladder, effectively reducing the number of required voids, urge incontinence episodes, urge severity and improving retention, facilitating increased volume per void.

Drug Category
Antispasmodics; Anti-Incontinence Agents; ATC:G04BD08

Brand Names/Synonyms
Butanedioic Acid; Solifenacin Succinate [Usan]; Vesicare

Dosage Forms
Not Available

Absorption
Not Available

Interactions
Interactions for Solifenacin Succinate: Drugs Metabolized by Cytochrome P450: At therapeutic concentrations, solifenacin does not inhibit CYP1A1/2, 2C9, 2C19, 2D6, or 3A4 derived from human liver microsomes. CYP3A4 Inhibitors: In vitro drug metabolism studies have shown that solifenacin is a substrate of CYP3A4. Inducers or inhibitors of CYP3A4 may alter solifenacin pharmacokinetics. Ketoconazole Interaction Study: Following the administration of 10 mg of Solifenacin in the presence of 400 mg of ketoconazole, a potent inhibitor of CYP3A4, the mean Cmax and AUC of solifenacin increased by 1.5 and 2.7-fold, respectively. Therefore, it is recommended not to exceed a 5 mg daily dose of Solifenacin when administered with therapeutic doses of ketoconazole or other potent CYP3A4 inhibitors. Oral Contraceptives: In the presence of solifenacin there are no significant changes in the plasma concentrations of combined oral contraceptives (ethinyl estradiol/levogestrel). Warfarin: Solifenacin has no significant effect on the pharmacokinetics of R-warfarin or S-warfarin. Digoxin: Solifenacin had no significant effect on the pharmacokinetics of digoxin (0.125 mg/day) in healthy subjects.

Chemical IUPAC Name
4-azabicyclo[2.2.2]oct-7-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate

Chemical Formula
C27H32N2O6

Half Life
45 - 68 hours

Drug Type
Approved Drug

# Accession No
APRD00168

CAS Registry Number
242478-38-2