Goepel M, Steinwachs K-C
Klinik für Urologie, Kinderurologie, Urologische Onkologie, Klinikum Niederberg-Velbert, Kontinenzzentrum der DKG, Akademisches Lehrkrankenhaus, Universität Duisburg-Essen, 42549, Velbert.
Urologe A. 2007 Apr;46(4):387-8, 390-2. doi: 10.1007/s00120-007-1326-5.
Anticholinergic agents are used for treatment of overactive bladder syndrome (OAB) by competitive blockade of acetylcholine at the muscarinic receptor. At present five different subtypes of M-receptors can be differentiated. Primary detrusor effects are mediated by M3-receptors as are side effects like dry mouth and constipation. Cardiac and central nervous system side effects appear to be M2 or M1 related. OAB symptom relief by the unselective drugs tolterodine, oxybutynin or trospium chloride and by M3-selective agents like darifenacin or solifenacin seems to be rather similar. Central side effects are different depending on gastrointestinal reabsorption, serum metabolism and penetration of the blood-brain barrier. Slow release formulations may be better tolerated. Anticholinergics that penetrate the blood-brain barrier may cause cognitive imbalance in older patients, as recent studies have shown for oxybutynin. Here M3-selective agents may offer an advantage.
抗胆碱能药物通过在毒蕈碱受体处竞争性阻断乙酰胆碱来治疗膀胱过度活动症（OAB）。目前可以区分出五种不同亚型的M受体。主要的逼尿肌效应由M3受体介导，口干和便秘等副作用也是如此。心脏和中枢神经系统副作用似乎与M2或M1有关。非选择性药物托特罗定、奥昔布宁或氯化曲司氯铵以及M3选择性药物如达非那新或索利那新对OAB症状的缓解似乎相当相似。中枢副作用因胃肠道重吸收、血清代谢和血脑屏障的穿透情况而异。缓释制剂的耐受性可能更好。穿透血脑屏障的抗胆碱能药物可能会导致老年患者出现认知失衡，正如最近关于奥昔布宁的研究所表明的那样。在此方面，M3选择性药物可能具有优势。
