Data from 12-week , r and omised , double-blind , placebo-controlled trials of tolterodine extended release ( ER ) , oxybutynin and solifenacin show that combined antimuscarinic+α-blocker treatment is generally more effective than monotherapy or placebo in men with OAB symptoms .
The efficacy and safety  of tolterodine ER+α-blocker treatment was not affected by prostate size or prostate-specific antigen ( PSA ) level .
In men meeting entry criteria for OAB and benign prostatic obstruction trials  , tolterodine ER alone was effective selectively in men with prostate size or PSA level below study medians .
Post hoc analyses from double-blind , placebo-controlled trials and prospect i ve studies of fesoterodine , oxybutynin , propiverine , solifenacin and tolterodine also suggest that antimuscarinics are generally safe and efficacious in men .
A retrospective data base study found that risk of AUR in men was the highest in the first month of treatment and decreased considerably thereafter .
Antimuscarinics , alone or with an α-blocker , appear to be efficacious and safe in many men with predominant OAB symptoms or persistent OAB symptoms despite α-blocker or 5-α-reductase inhibitor treatment .
Despite potential benefits , primary care clinicians may avoid using antimuscarinics in men with overactive bladder ( OAB ) symptoms because of safety concerns .
Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine.
OBJECTIVE Fesoterodine , a new antimuscarinic agent for overactive bladder , undergoes immediate and extensive hydrolysis by nonspecific esterases to 5-hydroxymethyl tolterodine ( 5-HMT ) , the metabolite principally responsible for its antimuscarinic activity . Formation of 5-HMT does not require cytochrome P450 (CYP)-mediated metabolism , but its further metabolism and inactivation involves CYP3A4 and CYP2D6 isoenzymes . Subject age , gender , and race can play a key role in inter-subject variability in pharmacokinetics and thus efficacy and safety of drugs . This article examines the effects of age , gender , and race on the pharmacokinetics and pharmacodynamics of fesoterodine . METHODS Data from two r and omized , double-blind , placebo-controlled , parallel-group trials in healthy subjects are presented : Study 1 investigated the effects of race ( white vs. black men ) and Study 2 investigated the effects of age ( young vs. old men ) and gender ( elderly men vs. elderly women ) on the pharmacokinetics and pharmacodynamics of single doses of fesoterodine 8 mg . In both studies , the primary endpoints were area under the concentration-time curve up to the last sample ( AUC0-tz ) and maximum concentration ( Cmax ) of 5-HMT in plasma . Pharmacodynamic variables included spontaneous salivary secretion ( Studies 1 and 2 ) and residual urine volume ( Study 2 only ) . The two studies included 5 groups of 16 subjects each ( r and omized 3 : 1 to fesoterodine or placebo ) : white men aged 18 - 45 years , black men aged 18 - 45 years ( Study 1 ) ; young white men aged 18 - 40 years , elderly white men aged > 65 years , and elderly white women aged > 65 years ( Study 2 ) . RESULTS There were no clinical ly meaningful differences in the primary endpoints between white and black subjects or between young white men , elderly white men , and elderly white women . Mean AUC0-tz was 70.7 ng/ml x h in whites and 64.1 ng/ml x h in blacks ; mean Cmax was 6.1 and 5.5 ng/ml in whites and blacks , respectively . Mean AUC0-tz in young white men , elderly white men , and elderly white women was 49 , 48 , and 54 ng/ml x h , respectively ; mean Cmax in young white men , elderly white men , and elderly white women was 4.1 , 3.8 , and 4.6 ng/ml , respectively . Consistent with the anticholinergic pharmacology of fesoterodine , declines in salivary volume were observed in both studies , and elevations in residual urinary volume were observed , especially in elderly subjects , in Study 2 . Fesoterodine was well tolerated , with common adverse events such as headache and dry mouth recognized as antimuscarinic class effects . CONCLUSIONS Subject demographics , such as age , gender , and race , do not have a clinical ly meaningful effect on 5-HMT pharmacokinetics or pharmacodynamics after single-dose administration of fesoterodine 8 mg ; thus , no dosage adjustment is required for fesoterodine based on age , gender , or race
Data from 12-week , r and omised , double-blind , placebo-controlled trials of tolterodine extended release ( ER ) , oxybutynin and solifenacin show that combined antimuscarinic+α-blocker treatment is generally more effective than monotherapy or placebo in men with OAB symptoms .
The efficacy and safety  of tolterodine ER+α-blocker treatment was not affected by prostate size or prostate-specific antigen ( PSA ) level .
In men meeting entry criteria for OAB and benign prostatic obstruction trials  , tolterodine ER alone was effective selectively in men with prostate size or PSA level below study medians .
Post hoc analyses from double-blind , placebo-controlled trials and prospect i ve studies of fesoterodine , oxybutynin , propiverine , solifenacin and tolterodine also suggest that antimuscarinics are generally safe and efficacious in men .
A retrospective data base study found that risk of AUR in men was the highest in the first month of treatment and decreased considerably thereafter .
Antimuscarinics , alone or with an α-blocker , appear to be efficacious and safe in many men with predominant OAB symptoms or persistent OAB symptoms despite α-blocker or 5-α-reductase inhibitor treatment .
Despite potential benefits , primary care clinicians may avoid using antimuscarinics in men with overactive bladder ( OAB ) symptoms because of safety concerns .