曲司氯铵——治疗伴有急迫性尿失禁症状的膀胱过度活动症的新药

曲司氯铵为新近上市的用于治疗伴有急迫性尿失禁症状的膀胱过度活动症的抗胆碱药物,具有抗胆碱能神经末梢M_1,M_2,M_3受体的作用,从而拮抗乙酰胆碱对人膀胱平滑肌的收缩效应。可有效降低膀胱平滑肌的紧张度、解除痉挛状态,显著增加最大膀胱容量、第1次逼尿肌收缩时膀胱容量,提高膀胱顺应性,降低最大逼尿肌压力,有效减轻尿频、尿急以及尿失禁症状。临床效能与奥昔布宁相当,而优于托特罗定。本品起效快、长期疗效优良,此外,本品仅具有抗胆碱药物的外周常见不良反应,如口干、便秘等,但不进入中枢神经系统,没有中枢神经系统毒性。本文对其药理学及临床研究进行综述。

Trospium chloride:a new drug for treating overactive bladder with urge incontinence

Trospium chloride is a new available marketing anticholinergic drug to treat the overactive bladder with urge incontinence, which directly and competitively blocks the contractile effect of acetylcholine on the smooth musculature of human urinary bladder through binding linkage to the muscarinic M1, M2, and M3 receptor subtypes. Trospium chloride effectively suppresses the tension of bladder smooth muscles, with elimination of the spastic state, obviously augments the maximum cystometric capacity with the volume at first detrusor contraction, increases the bladder compliance, reduces the maximum detrusor pressure, and effectively attenuates and reduces the symptoms of urinary frequency, urgency, and urge incontinence. The clinical efficacy of trospium chloride on clinical is as well as oxybutynin, but better than that of tolterodin. Trospium chloride effects rapidly with a long term maintenance, In addition, it only possesses the common peripheral adverse reactions such as dry mouth and constipation, but no toxicity to the central nervous system because of its poor central nervous system penetration, just like the peripheral antieholinergie agents. The present paper summarizes the pharmacology and clinical research of trospium chloride.