The muscarinic cholinergic binding kinetics of the human urinary bladder

Determination of (1) the absolute number of cholinergic receptors, (2) the cholinergic binding kinetics, and (3) the direct antimuscarinic activity of a series of uropharmacologic agents was accomplished by radioligand binding techniques in tissue derived from human urinary bladder. The competition between ³H-quinuclidinyl benzilate (³H-QNB) binding and selective antagonists provided the first quantitative assessment of cholinergic receptor characteristics in the human bladder fundus and represents a potential method for assessing the antimuscarinic binding potential of uropharmacologic agents.     

Umeclidinium for the treatment of uncontrolled asthma

Introduction: Smooth muscle cell contraction in the airways is the principal therapeutic target in asthmatic subjects and its insufficient treatment is often a cause of uncontrolled disease. For this reason, research has focused on targeting smooth muscle activity with anticholinergic agents, including umeclidinium.

Areas covered: This review highlights the potential application of umeclidinium, a long acting muscarinic antagonist, as a novel therapeutic approach for patients with severe uncontrolled asthma, despite maximal therapy.

Expert opinion: Umeclidinium, similarly to tiotropium, which has been recently included in guidelines, may act by contrasting cholinergic activation in airways, preventing or at least reducing smooth muscle cells contraction and the consequent bronchoconstriction. This is similar to what occurs in chronic obstructive pulmonary disease, for which umeclidinium has been regularly approved. However, available data is not sufficient and further studies are needed before regulatory approval can be sought, since only phase II clinical trials have been conducted at present. Both quality of life and objectifiable clinical data and parameters must be assessed, including lung function improvements, reduction of exacerbations and reduction of as required medications.     

胆碱能M受体:膀胱过度活动症治疗的关键

 膀胱过度活动症(overactive bladder,OAB)是一种以尿急症状为特征的症候群,常伴有尿频和夜尿症状,可伴或不伴有急迫性尿失禁。存在于膀胱逼尿肌的胆碱能M受体是介导OAB发生的关键。抗胆碱能药物是目前临床治疗OAB最基本的药物,在抑制膀胱逼尿肌不自主收缩、改善OAB症状方面发挥了重要作用。本文从分子结构、受体选择性、药代动力学、临床特点和药物不良反应等方面对目前常用的5种商品化的抗胆碱能药物进行综述。