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Mariko Iwase, Yuki Nishimura, Norimitsu Kurata, Hokuto Namba, Takahito Hirai, Yuji Kiuchi
OTC drugs have an important role in self-medication. However, the pharmacokinetic properties of some OTC drugs have not been fully investigated and reports concerning their drug interactions are insufficient. Several gastrointestinal drugs are available as OTC drugs. Because of their pharmacological properties, these drugs are often used concomitantly with other drugs. Therefore, it is important to predict the possible drug interactions among these drugs. In the current study, we investigated the inhibitory effects of five gastrointestinal drugs, namely loperamide, oxethazaine, papaverine, pirenzepine, and trimebutine, on CYP activities in human liver microsomes...
2017: Biological & Pharmaceutical Bulletin
Junping Xu, Chengliang Hu, Qiong Jiang, Hongchao Pan, Huifan Shen, Melitta Schachner
Curing spinal cord injury (SCI) in mammals is a daunting task because of the lack of permissive mechanisms and strong inhibitory responses at and around the lesion. The neural cell adhesion molecule L1CAM (L1) has been shown to favor axonal regrowth and enhance neuronal survival and synaptic plasticity but delivery of full-length L1 or its extracellular domain could encounter difficulties in translation to therapy in humans. We have, therefore, identified several small organic compounds that bind to L1 and stimulate neuronal survival, neuronal migration and neurite outgrowth in an L1-dependent manner...
September 1, 2017: Disease Models & Mechanisms
Young Joo Yang, Chang Seok Bang, Gwang Ho Baik, Tae Young Park, Suk Pyo Shin, Ki Tae Suk, Dong Joon Kim
BACKGROUND: Controversies persist regarding the effect of prokinetics for the treatment of functional dyspepsia (FD). This study aimed to assess the comparative efficacy of prokinetic agents for the treatment of FD. METHODS: Randomized controlled trials (RCTs) of prokinetics for the treatment of FD were identified from core databases. Symptom response rates were extracted and analyzed using odds ratios (ORs). A Bayesian network meta-analysis was performed using the Markov chain Monte Carlo method in WinBUGS and NetMetaXL...
June 26, 2017: BMC Gastroenterology
Miguel Saps, Adrian Miranda
There is little evidence for most of the medications currently used to treat functional abdominal pain disorders (FAPDs) in children. Not only are there very few clinical trials, but also most have significant variability in the methods used and outcomes measured. Thus, the decision on the most appropriate pharmacological treatment is frequently based on adult studies or empirical data. In children, peppermint oil, trimebutine, and drotaverine have shown significant benefit compared with placebo, each of them in a single randomized clinical trial...
2017: Handbook of Experimental Pharmacology
Eleonora Giannetti, Marco Maglione, Elisa Sciorio, Vincenzo Coppola, Erasmo Miele, Annamaria Staiano
OBJECTIVE: Few data exist on natural history of irritable bowel syndrome (IBS) in children; therefore we investigated symptoms evolution over time in a cohort of children with IBS. STUDY DESIGN: In this observational, single-center study, we prospectively enrolled newly diagnosed children with IBS and reassessed them after 24 months. At both time points, patients completed a symptoms questionnaire, and a score of stool consistency was obtained. The therapeutic strategy adopted was also recorded...
April 2017: Journal of Pediatrics
Doina Georgescu, Oana Elena Ancusa, Liviu Andrei Georgescu, Ioana Ionita, Daniela Reisz
Despite the fact that nonmotor symptoms (NMS) like gastrointestinal (GI) complaints are frequently reported in Parkinson's disease (PD), no therapeutic guidelines are available. This study aimed to manage some lower GI-NMS in a group of patients with PD. A total of 40 patients (17 males, 23 females; mean age 76.05±2.09 years) were randomly selected for this study. Patients were confirmed to have PD (modified Hoehn-Yars scale: 2.075±0.4) who had undergone levodopa or dopamine agonist treatment. In the non-motor symptoms questionnaire (NMS-Quest), regarding GI complaints, the following were recorded: abdominal pain, bloating, and constipation of mild-to-moderate severity...
2016: Clinical Interventions in Aging
Sibel Naska, Scott A Yuzwa, Adam P W Johnston, Smitha Paul, Kristen M Smith, Maryline Paris, Michael V Sefton, Alessandro Datti, Freda D Miller, David R Kaplan
Here, we asked whether we could identify pharmacological agents that enhance endogenous stem cell function to promote skin repair, focusing on skin-derived precursors (SKPs), a dermal precursor cell population. Libraries of compounds already used in humans were screened for their ability to enhance the self-renewal of human and rodent SKPs. We identified and validated five such compounds, and showed that two of them, alprostadil and trimebutine maleate, enhanced the repair of full thickness skin wounds in middle-aged mice...
January 12, 2016: Stem Cell Reports
N Cenac, M Castro, C Desormeaux, P Colin, M Sie, M Ranger, N Vergnolle
BACKGROUND: Trimebutine maleate, a noncompetitive spasmolytic agent with some affinity for peripheral μ- and κ-opioid receptors has been evaluated as a treatment in a limited number of patients undergoing sedation-free full colonoscopy. The efficiency of such treatment was comparable to sedation-based colonoscopies to relieve from pain and discomfort. METHODS: A new and improved trimebutine salt capable of releasing in vivo hydrogen sulphide (H2S), a gaseous mediator known to reduce nociception, has been developed...
May 2016: European Journal of Pain: EJP
Islam Amine Larabi, Charlotte Duverneuil-Mayer, Emuri Abe, Frédéric Baud, Jean-Claude Alvarez
A liquid chromatography-MS-MS turbulent flow on-line extraction method was developed for the determination of trimebutine (TMB) and its main active metabolite N-mono-desmethyltrimebutine (nortrimebutine or nor-TMB) in human plasma. After protein precipitation and internal standard (IS, haloperidol-d4) addition, 50 µL of the supernatant were transferred onto a Cyclone-Turbo-Flow extraction column followed by an Hypersil PFP Gold analytical column. Detection was carried out on a triple quadrupole tandem mass spectrometer using positive electrospray ionization...
November 2015: Journal of Analytical Toxicology
F Rusu, D L Dumitraşcu
UNLABELLED: There is little data on the long term evolution of patients with irritable bowel syndrome (IBS) and of associated conditions. We therefore studied the evolution of IBS patients in a single tertiary center during a long interval of time. METHODS: We carried out a retrospective study based on the survey of patients records. We analyzed the records of symptoms, therapy, associated diseases, as consigned at follow-up visits for an interval of 4 years in average (2008-2011)...
January 2015: Romanian Journal of Internal Medicine, Revue Roumaine de Médecine Interne
Hélène Montpetit, Maxime Ranger, Patrick Colin, Milton Furtado, Fabio Garofolo
BACKGROUND: A failure in incurred sample reanalysis (ISR) for N-desmethyltrimebutine (NDMT), during the analysis of a trimebutine-containing drug GIC-1001 Phase I study, led to the discovery of a never-before reported metabolite of trimebutine. RESULTS: A positive bias for NDMT during the ISR and post-reconstitution stability evaluations indicated the presence of an unstable metabolite of NDMT. Precursor ion scans performed on freshly extracted samples enabled the identification of this metabolite to be the NDMT glucuronide conjugate and its fragmentation pattern suggested that the glucuronide moiety was attached at the N-terminal of NDMT...
2015: Bioanalysis
Ikram Jemel-Oualha, Jihene Elloumi-Mseddi, Abdelhamid Beji, Bochra Hakim, Sami Aifa
UNLABELLED: The use of some classic antibiotics was recently shown to inhibit growth and to induce apoptosis in human LOVO colon cancer cells. In this study, we describe that ciprofloxacin (CI), trimebutine maleate (COL) and tiemonium methylsulfate (VIS) greatly inhibit cell proliferation in vitro. Proliferation inhibition reached its maximum at 10(-4 )M, 10(-3 )M and 10(-2 )M, respectively, for COL, CI and VIS. Moreover, phospho-extracellular-regulated kinase was totally abrogated in non-apoptotic cytotoxicity of VIS but decreases or increases in the apoptotic inhibition, respectively, of COL and CI treatments...
2016: Journal of Receptor and Signal Transduction Research
Jean-Michel Paquette, Marianne Rufiange, Mirela Iovu Niculita, Julie Massicotte, Marc Lefebvre, Patrick Colin, Ariles Telmat, Maxime Ranger
PURPOSE: Trimebutine 3-thiocarbamoylbenzenesulfonate (GIC-1001) is a new drug intended to be used for the management of visceral pain in patients undergoing sedation-free, full colonoscopy. The objectives of this Phase I, single-center, randomized, double-blinded, placebo-controlled, integrated study were to evaluate the safety and pharmacokinetics of GIC-1001 after single ascending doses (SAD) and multiple ascending doses (MAD) and to evaluate the influence of food on the pharmacokinetics in healthy volunteers...
November 1, 2014: Clinical Therapeutics
I S Lembrik
In the article results of supervision of the patients with chronic pancreatitis and dysfunction of Oddi's sphincter, pancreatic type, in polyclinic were presented. Among them: 50 children received in clinic therapeutic complex offered by us which included: phytoenzyme, spasmolytic and antioxidant. 50 children were treated in traditional way. Screening of functional condition of the pancreas revealed decreasing percentage of moderate exocrine insufficiency of pancreas (10% of incidences) in children with recurrent course of pancreatitis...
June 2013: Likars'ka Sprava
Hoda M Elqudaby, Gehad G Mohamed, Ghada M G El-Din
Charge transfer complexes of loperamide hydrochloride (LOP.HCl) and trimebutine (TB) drugs as electron donor with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ), tetracyanoethylene (TCNE) and 7,7,8,8-tetracyanoquinodimethane (TCNQ) as π-acceptors in acetonitrile were investigated spectrophotometrically to determine the cited drugs in pure and dosage forms. The reaction gives highly coloured complex species which are measured spectrophotometrically at 460, 415 and 842nm in case of LOP.HCl and at 455, 414 and 842nm in case of TB using DDQ, TCNE and TCNQ reagents, respectively...
August 14, 2014: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
M Z Rahman, D S Ahmed, M Mahmuduzzaman, M A Rahman, M S Chowdhury, R Barua, S M Ishaque
Irritable bowel syndrome (IBS) is a functional disorder characterized by chronic or recurrent abdominal pain or discomfort with bowel disturbances. This prospective, randomized clinical trial has been conducted on IBS patients, using trimebutine and Mebeverine in separate group in parallel design to compare the efficacy and safety of Trimebutine 100mg twice daily with mebeverine 135mg twice daily. Patients of 15 to 60 years old and both sexes were included from the out patient department (OPD) of gastroenterology, Bangabandhu Sheikh Mujib Medical University (BSMMU) from June 2010 to December 2011...
January 2014: Mymensingh Medical Journal: MMJ
(no author information available yet)
Trimebutine, an antispasmodic drug, is used to relieve pain associated with irritable bowel syndrome, despite a lack of proven efficacy. Trimebutine has been shown to act on peripheral opioid receptors. Cases of trimebutine abuse and addiction have been reported in young adults, especially with the injectable form. Cases of serious accidental or intentional trimebutine overdose have been reported in infants and young adults, leading to neurological disorders (loss of consciousness, coma, drowsiness and convulsions) and cardiac disorders (bradycardia, ventricular tachycardia, arterial hypertension)...
October 2013: Prescrire International
Seong Hee Kang, Yoon Tae Jeen, Ja Seol Koo, Yang Seo Koo, Kyoung Oh Kim, You Sun Kim, Seung Yeong Kim, Jeong Seop Moon, Jong Jae Park, Il Hyun Baek, Sung Chul Park, Sung Joon Lee, Jong Hun Lee, Rok Seon Choung, Suck Chei Choi
BACKGROUND/AIMS: Antispasmodic agents have been used in the management of irritable bowel syndrome. However, systematic reviews have come to different conclusions about the efficacy in irritable bowel syndrome. Fenoverine acts as a synchronizer of smooth muscle in modulating the intracellular influx of calcium. We compared fenoverine with trimebutine for the treatment of patients with IBS. METHODS: A multicenter, randomized, double-blind, non-inferiority clinical study was conducted to compared fenoverine with trimebutine...
November 2013: Korean Journal of Gastroenterology, Taehan Sohwagi Hakhoe Chi
J Kountouras, D Sofianou, E Gavalas, E Sianou, C Zavos, G Meletis, E Tsiaousi
AIM: The aim of this preliminary study was to investigate the in vitro effect of "non-antibiotic" trimebutine against reference strains Staphylococcus aureus ATCC 29213, ATCC 25923, Escherichia coli ATCC 25922, ATCC 35218, Pseudomonas aeruginosa ATCC 27853 and Enterococcus faecalis ATCC 29212; microbiota that are potentially involved in the pathophysiology of post-infectious functional gastrointestinal disorders. METHODS: Trimebutine activity was assessed by the broth microdilution method according to Clinical and Laboratory Standards Institute recommendations against reference strains S...
October 2012: Hippokratia
Gülcan S Karabulut, Omer F Beşer, Ethem Erginöz, Tufan Kutlu, Fügen Ç Cokuğraş, Tülay Erkan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS) is one of the most common functional gastrointestinal disorders and when compared to the vast knowledge pertaining to adults with IBS, very little is known about IBS in children and adolescents. We aimed to explore the prevalence of IBS, identify symptoms and contributing factors and also to examine the efficacy of trimebutine maleate in children and adolescents. METHODS: The study involved 345 children and adolescents (4-18 years) and parents were requested to fill in a questionnaire, Rome III criteria was used to diagnose IBS...
January 2013: Journal of Neurogastroenterology and Motility
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