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Rational Medical Therapy of Functional GI Disorders
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
Richard M. Sperling, Kenneth R. McQuaid
In a recent meta-analysis, Poynard et al. (177) analyzed 25 randomized, double-blind, placebo-controlled trials that assessed the efficacy of eight smooth-muscle relaxants and anticholinergic agents in the treatment of IBS. A total of eight drugs were analyzed in these trials: cimetropium bromide (four trials), dicyclomine hydrochloride (two trials,) hyoscine butyl bromide (three trials), mebeverine (five trials), octylonium (two trials), pinaverium bromide (two trials), trimebutine (four trials), and peppermint oil (four trials). A statistically significant improvement in global improvement was detected in 62% of patients treated with active drug versus 32% with placebo. When analyzed separately, all drugs still demonstrated global improvement versus placebo. Pain improvement (occurred in 64% of patients treated with myorelaxants compared with 45% of placebo-treated patients—a modest 19% improvement, which was statistically significant. However, when the drugs were analyzed separately, only three demonstrated significant efficacy versus placebo: cimetropium bromide, octylonium, and dicylomine bromide. No significant differences were detected in constipation or abdominal distension in the active treatment groups compared with placebo when the drugs were analyzed collectively or separately. The statistical power of meta-analyses provides strong evidence that anticholinergics and smooth-muscle relaxants do benefit a subset of patients with IBD, namely, those with pain-predominant symptoms.
Functional abdominal disorders
Published in Michael JG Farthing, Anne B Ballinger, Drug Therapy for Gastrointestinal and Liver Diseases, 2019
Bernard Coulie, Michael Camilleri
Poynard et al.112 concluded that, as a therapeutic class, smooth muscle relaxants or anti-spasmodics were significantly better than placebo for global assessment (62% versus 35% placebo improvement) and abdominal pain (64% versus 45% placebo improvement, both significant). Five drugs showed efficacy over placebo in IBS, namely: The antimuscarinic compound cimetropium bromideThe quaternary ammonium derivative pinaverium bromideThe quatenary ammonium derivative otilinium bromideThe peripheral opiate antagonist trimebutine, andthe anticholinergic compound mebeverine.
How can we develop better antispasmodics for irritable bowel syndrome?
Published in Expert Opinion on Drug Discovery, 2019
Sheyda Ranjbar, Seyed Afshin Seyednejad, Shekoufeh Nikfar, Roja Rahimi, Mohammad Abdollahi
In order to restrict the effect of drug molecules to GI tract, plenty of design approaches exist, which are comprehensively reviewed elsewhere [11] and can be used as a guide for drug design and optimization of antispasmodics. These approaches enable the medicinal chemist to manipulate physicochemical properties of active compounds or prodrugs to obtain drug molecules with negligible absorption, thereby guarantying both increased concentration in the site of action and less adverse effects due to the low systemic exposure [12]. To achieve that, the drug’s molecular weight, lipophilicity and polarity must be taken into account. For instance, current gut-selective antispasmodics like otolinium or pinaverium bromide that exhibit poor intestinal absorption have quaternary ammonium in their molecular structure [13]. It can be suggested that the implementation of quaternary ammonium in the structure of antispasmodics is one of the ways to restrict their effect to the colon. This also shows the role of rational drug design to increase the safety of drugs used in GI conditions. However, despite limiting systemic absorptions of drugs, still some degree of uptake into GI is crucial. For example, in the case of antispasmodics, drug targets are in sublayers of GI tract [14] and penetration of an efficacious antispasmodic drug to these layers must be substantial.
Wei Chang An pill regulates gastrointestinal motility in a bidirectional manner
Published in Pharmaceutical Biology, 2021
Sitong Jia, Lijuan Chai, Jing Zhang, Min Zhang, Lin Li, Yaxin Qi, Yafen Pang, Xi Chen, Nana Fan, Lin Wang, Yujing Wang, Jixiang Song, Yingjie Sun, Yi Wang, Lin Miao, Han Zhang
WCA was supplied by Le Ren Tang Zhongxin Pharmaceutical Group Co., Ltd. (Tianjin, China). Folium senna was bought from Liankang Pharmaceutical Co., Ltd. (Hebei, China). Diphenoxylate hydrochloride (CDT) was produced by Dingchang Pharmaceutical Co., Ltd. (Henan, China). Pinaverium Bromide Tablets (PBT) were obtained from Abbott Healthcare SAS Co., Ltd. (Shanghai, China). Sennosides A was obtained from Meilun Biotechnology Co., Ltd. (Dalian, China). Enzyme-linked immunosorbent assay (ELISA) kit of NO was obtained from Nanjing Jiancheng Bioengineering Institute (Nanjing, China). ELISA kits of Substance P (SP), motilin (MTL), 5-hydroxytryptamine (5-HT) and vasoactive intestinal polypeptide (VIP) were bought from Huamei Bioengineering Co., Ltd. (Wuhan, China).