Home » Drug Information » FDA Approved Drugs » 2004
Medical Areas: Nephrology
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Vesicare (solifenacin succinate)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Company: Yamanouchi, GlaxoSmithKline
Approval Status: Approved November, 2004
Treatment Area: Overactive bladder
Vesicare oral tablets contain solifenacin, a competitive
muscarinic receptor antagonist. Muscarinic receptors play an
important role in several major cholinergically mediated functions,
including contractions of urinary bladder smooth muscle. Antagonism
at these receptors has been shown to reduce tonus (elastic tension)
of the urinary bladder and slow parasympathetic contractions.
It is specifically indicated for the treatment of
overactive bladder with symptoms of urge
urinary incontinence, urgency, and urinary frequency.
Vesicare is administered via an oral tablet of 5 mg once daily,
with a possible increase in dosage, to 10 mg once daily, in
subjects experiencing good tollerance. Dosing should occur with
liquids, and tablets should not be crushed or broken prior to
FDA approval of Vesicare was based upon four 12-week
multi-center, double-blind, placebo-controlled, parallel-group
studies. The studies enrolled a total of 3027 subjects with at
least a 3 month history of increased urinary frequency, urinary
urgency, and/or urge or mixed (predominantly urge) incontinence.
Subjects in two of the trials received either 5 or 10 mg Vesicare
or placebo once daily, and subjects in the other two received
exclusively 10 mg or placebo once daily. All patients completing
the 12-week studies were eligible to enter an open label long-term
extension. All four trials found that Vesicare offered
significantly better efficacy than placebo in both primary (mean
change from baseline to 12 weeks in number of micturitions/24
hours) and secondary (including mean change from baseline to 12
weeks in number of incontinence episodes/24 hours, and mean volume
voided per micturition) endpoints.
Adverse events associated with the use of Vesicare may include,
but are not limited to, the following:
- Dry mouth
- Blurred Vission
- Urinary Retention
- Dry Eyes
In addition, three serious intestinal complications (one fecal
impaction, one colonic obstruction, and one intestinal obstruction)
and one case of angioneurotic edema occurred among patients taking
Vesicare in clinical trials. There was not a significant difference
in the incidence of serious adverse events between subjects taking
the drug for 12 weeks and 12 months.
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.
Cardozo L, Lisec M, Millard R, et al.
Randomized, double-blind placebo controlled trial of the once daily
antimuscarinic agent solifenacin succinate in patients with
overactive bladder. Journal of Urology 2004 Nov;172(5 Pt
Smulders RA, Krauwinkel WJ, Swart PJ, Huang M.
Pharmacokinetics and safety of solifenacin succinate in healthy
young men. Journal of Clinical Pharmacology 2004
Ohtake A, Ukai M, Hatanaka T,et al. In
vitro and in vivo tissue selectivity profile of solifenacin
succinate (YM905) for urinary bladder over salivary gland in rats.
European Journal of Pharmacology 2004 May
For additional information regarding Vesicare or overactive
bladder, please contact the Vesicare Web Site