Hallén B, Massey A, Guilbaud O, Sundwall A
Department of Pharmacology, R&D, KabiVitrum AB, Stockholm, Sweden.
Arzneimittelforschung. 1988 Oct;38(10):1482-5.
Clinical trials with increased dosages, relative to the standard regimen, of the anticholinergic drug emepronium (Cetiprin Novum) resulted in a clear improvement in micturition- and urodynamic parameters in urinary incontinent patients. In the present study possible effects on the gastric emptying were tested in dogs and in human volunteers. In dogs a wide dose range of emepronium (5-100 mg/kg p.o.) was used to establish a relationship between serum concentration and effect on the gastric emptying. Gastric emptying was slightly decreased after 25 mg/kg (peak conc. of emepronium about 100 micrograms/l) and markedly decreased after 50 mg/kg (500 micrograms/l) and 100 mg/kg (5000 micrograms/l). In the volunteers no effect of emepronium on gastric emptying was observed, either after 200 mg q.i.d. or after 400 mg q.i.d. (about 3 and 6 mg/kg q.i.d.), which resulted in peak serum concentrations of 100-300 micrograms/l).
与抗胆碱能药物依美溴铵(新喜滴灵)标准治疗方案相比,增加剂量的依美溴铵临床试验使尿失禁患者的排尿和尿动力学参数得到明显改善。在本研究中,对犬类和人类志愿者测试了其对胃排空的可能影响。在犬类实验中,使用了大剂量范围的依美溴铵(口服5 - 100毫克/千克)来确定血清浓度与胃排空影响之间的关系。25毫克/千克(依美溴铵峰值浓度约为100微克/升)后胃排空略有下降,50毫克/千克(500微克/升)和100毫克/千克(5000微克/升)后胃排空明显下降。在志愿者中,无论是每日四次服用200毫克还是每日四次服用400毫克(约每日四次3和6毫克/千克),均未观察到依美溴铵对胃排空有影响,这导致血清峰值浓度为100 - 300微克/升。