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Bowel disorders
Published in Henry J. Woodford, Essential Geriatrics, 2022
Prucalopride is a pro-kinetic agent acting at gut serotonin (5-HT4) receptors. Lubiprostone activates chloride channels in the intestinal wall to increase fluid and electrolyte secretion into the bowel. Linaclotide is a guanylate cyclise-C receptor agonist that promotes intestinal fluid secretion. There are few data to support either efficacy or safety of these drugs in frail older people.20,21
Using Medication Wisely
Published in Melissa G. Hunt, Aaron T. Beck, Reclaim Your Life From IBS, 2022
Melissa G. Hunt, Aaron T. Beck
Lubiprostone (Amitiza) is another prescription medication. Weirdly, it is only approved for use by adult women with IBS-C, not men. It also works biochemically (as a chloride channel activator) to increase the amount of water in your stool. Like Linzess, it can exacerbate bowel obstructions. It can also cause temporary chest tightness or shortness of breath within an hour of taking it, which can be very anxiety-provoking and uncomfortable. Other common side effects include diarrhea, gas, bloating, headache, and nausea.
Severe functional constipation: Surgery and gastroenterologic collaboration
Published in Alejandra Vilanova-Sánchez, Marc A. Levitt, Pediatric Colorectal and Pelvic Reconstructive Surgery, 2020
Peter L. Lu, Desalegn Yacob, Carlo Di Lorenzo
Traditional pharmacological treatment for children with constipation has included osmotic laxatives, stimulant laxatives, and lubricants [17]. However, newer pharmacological treatments used in adults with constipation and IBS with constipation show promise for children with similar conditions, particularly when abdominal pain limits stimulant laxative use. Lubiprostone is a prostaglandin E1 derivative that promotes intestinal fluid secretion, softening stool and promoting intestinal motility through luminal distention [18]. Several randomized-controlled studies have demonstrated the efficacy and safety of lubiprostone in adults with constipation [19–21]. An open-label study of lubiprostone in children with functional constipation found it to be well tolerated and effective in improving bowel movement frequency, but improvements in abdominal pain were not significant [22]. Linaclotide is a peptide agonist of the intestinal guanylate cyclase-C receptor, which also promotes intestinal fluid secretion. Linaclotide not only softens stool and accelerates intestinal transit, but can also decrease visceral sensitivity in animal models [18,23]. Several randomized-controlled studies in adults have demonstrated improvements in constipation symptoms and abdominal pain [23–25]. Although research is ongoing, no studies have been published yet on the use of linaclotide for children with constipation-predominant IBS, and its use is contraindicated in children younger than 6 years of age because of the risk of severe dehydration.
An update on the use of pharmacotherapy for opioid-induced bowel dysfunction
Published in Expert Opinion on Pharmacotherapy, 2023
Taraneh Mousavi, Shekoufeh Nikfar, Mohammad Abdollahi
Results from a pool analysis study of three phases III, randomized, double-blind, placebo-controlled, multicenter clinical trials comparing the efficacy of lubiprostone (24 mcg, twice a day) and placebo for 12 weeks for OIC were as follows. In those taking phenanthrene or phenylpiperidine opioids for chronic noncancer-related pain, lubiprostone was superior to placebo in alleviating OIC symptoms and enhancing SBM frequency from baseline [66]. In contrast, lubiprostone was ineffective in reversing diphenylheptane (e.g. methadone) OIC. This was also considered the ‘limitation of use’ in the monograph of this agent [64]. The most common adverse effects reported in these studies were nausea, diarrhea, flatulence, vomiting, abdominal pain and distension, peripheral edema, increased blood triglycerides, and bronchitis. In another randomized, placebo-controlled clinical study on 418 patients, treatment with lubiprostone led to better SBMs compared to baseline at eight weeks post-treatment. However, this efficacy was not achieved at 12 weeks [3]. A very recent meta-analysis on 1284 patients with OIC also confirmed the significant impact of lubiprostone in improving 24 h and weekly SBM frequency compared to the placebo groups [67].
Development and validation of a highly sensitive and selective LC-MS/MS method for the determination of 15-hydroxylubiprostone in human plasma: application to a pharmacokinetic study in healthy Chinese volunteers
Published in Xenobiotica, 2022
Xianjing Li, Haitao Yu, Wenjing Guo, Minlu Cheng, Qinxin Song, Li Ding
Lubiprostone, developed by Sucampo Pharmaceutical, Inc. and marketed in 2006, is the first chemical-type constipation treatment approved by FDA. Several studies have demonstrated the efficacy of lubiprostone for improving constipation-predominant Irritable bowel syndrome, chronic idiopathic constipation and opioid-induced constipation (Drossman et al. 2009; Lembo et al. 2011; Jamal et al. 2015; Black and Ford 2018; Alammar and Stein 2019; Viscusi 2019). As a derivative of prostaglandin E1 (PGE1), lubiprostone is a chloride channel agonist, which is proposed to act by selectively activating voltage-dependent type-2 chloride channels in the small intestine, stimulating intestinal chloride secretion and triggering sodium and fluid diffuse to the intestine (Cuppoletti et al. 2004). However, this pharmacological mechanism is still disputed. Recently, M. A. Catalan et al have proposed the CFTR-mediated effect of lubiprostone that might be mediated via prostaglandin receptors (Mei et al. 2011; Norimatsu et al. 2012; Catalan et al. 2020). CFTR is another phosphorylation-dependent chloride channel.
Safety of elobixibat and lubiprostone in Japanese patients with chronic constipation: a retrospective cohort study
Published in Expert Opinion on Drug Safety, 2021
Nobuhiro Ooba, Yoshinori Takahashi, Marina Nagamura, Masao Takahashi, Makoto Ushida, Eiji Kawakami, Masaomi Kimura, Tsugumichi Sato, Junichi Tokuyoshi, Choichiro Miyazaki, Mitsuaki Shimada
The incidence proportion of highly reported events among elobixibat and lubiprostone users is shown in Table 2. Some events, including diarrhea, abdominal pain, and laxative and anti-hypertensive use, were common in both groups. For elobixibat, the proportion of any adverse reaction was 12.4%, with diarrhea (2.9%), abdominal pain (1.4%), and constipation (0.8%) being the most frequent adverse events. Other drugs were added for 19.7% of elobixibat users; of these, the most reported were laxatives without lubiprostone (11.3%), anti-hypertensives (1.8%), and lubiprostone (1.4%), in that order. The occurrence of any adverse reaction was 15.7% for lubiprostone, with diarrhea (4.0%), constipation (1.5%), and abdominal pain (1.1%) being the most reported adverse events. Other drugs were added to 21.2% of lubiprostone users, and the most reported were laxatives without elobixibat (11.7%), anti-hypertensives (1.7%), and elobixibat (1.3%) in that order. The top three adverse events (diarrhea, abdominal pain, and constipation) and added drugs (laxatives, anti-hypertensives, and study drugs) after the initiation of the study drugs were similar. The pre-identified risk of nausea was 0.72% (n = 6) for lubiprostone and 0.1% (n = 1) for elobixibat. Details of events related to hospitalization in both drug groups were unknown.