选择性β3-AR拮抗剂治疗高反应性膀胱
作者：Karl-Erik Andersson, Nancy Martin, Victor Nitti 来源：Journal of Urology 日期：2013-03-12
导读
Selective β3-Adrenoceptor Agonists in the Treatment of the Overactive Bladder
Abstract
Background and Purpose
Bladder effects of isoprenaline and selective β1- and β2-adrenoceptor (AR) agonists reported in early studies suggested that bladder β-ARs are “atypical”. Since there is a lack of alternatives to antimuscarinics in the treatment of overactive bladder (OAB) symptoms, there has been an intensive search for new drug targets. The discovery of the β3-AR with high expression in the bladder, suggested that this receptor, mediating detrusor relaxation, could be a target for treatment of patients with OAB symptoms.
Methods
An overview of published literature on β-ARs and bladder (MEDLINE) was performed. The US Food and Drug Administration web site, clinicaltrials.gov, and controlled-trials.com online trial registries were searched for English-language articles containing the terms β3-ARs and β3-AR agonists. In addition, abstracts from recent international scientific meetings were searched for randomised controlled trials (RCTs) on β3-AR agonists.
Results
Stimulation of β3-ARs relaxes detrusor smooth muscle, decreases afferent signaling from the bladder, improves bladder compliance on filling, and increases bladder capacity. RCTs show that the selective β3-AR agonist, mirabegron, for which most information is available and which is approved in Japan, USA, and Europe, reduces the number of micturitions and incontinence episodes in a 24-h period compared with placebo. The most common adverse effects recorded are dry mouth (placebo level) and gastrointestinal disturbances rated as mild to moderate. Small rises in mean heart rate (1 beat /minute) and blood pressure (1 mm Hg) have been demonstrated in OAB patients.
Conclusions
Available information suggests that β3-AR agonists may be a promising alternative to antimuscarinics in the treatment of OAB. However, further clinical experiences outside clinical trials, and information on the long-term use in terms of efficacy, safety, and tolerability are warranted to optimally characterize the position of β3-AR agonists in the treatment algorithm for OAB.
http://www.jurology.com/article/S0022-5347(13)00380-7/abstract
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