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Korean J Urol. 2013 Dec;54(12):806-15. doi: 10.4111/kju.2013.54.12.806. Epub 2013 Dec 10.

Rationale for the use of anticholinergic agents in overactive bladder with regard to central nervous system and cardiovascular system side effects.

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1
Department of Urology, Cerrahpasa School of Medicine Faculty, Istanbul University, Istanbul, Turkey.

Abstract

PURPOSE:

Central nervous system (CNS) and cardiovascular system (CVS) side effects of anticholinergic agents used to treat overactive bladder (OAB) are underreported. Hence, this review aimed to focus on the mechanisms of CNS and CVS side effects of anticholinergic drugs used in OAB treatment, which may help urologists in planning the rationale for OAB treatment.

MATERIALS AND METHODS:

PubMed/MEDLINE was searched for the key words "OAB," "anticholinergics," "muscarinic receptor selectivity," "blood-brain barrier," "CNS," and "CVS side effects." Additional relevant literature was determined by examining the reference lists of articles identified through the search.

RESULTS:

CNS and CVS side effects, pharmacodynamic and pharmacokinetic properties, the metabolism of these drugs, and the clinical implications for their use in OAB are presented and discussed in this review.

CONCLUSIONS:

Trospium, 5-hydroxymethyl tolterodine, darifenacin, and solifenacin seem to have favorable pharmacodynamic and pharmacokinetic properties with regard to CNS side effects, whereas the pharmacodynamic features of darifenacin, solifenacin, and oxybutynin appear to have an advantage over the other anticholinergic agents (tolterodine, fesoterodine, propiverine, and trospium) with regard to CVS side effects. To determine the real-life situation, head-to-head studies focusing especially on CNS and CVS side effects of OAB anticholinergic agents are urgently needed.

KEYWORDS:

Anticholinergics; Cardiovascular system; Central nervous system; Muscarinic receptors; Overactive bladder

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