Search results for "Bisacodyl"
showing 7 items of 7 documents
Fishing anti-inflammatories from known drugs: In silico repurposing, design, synthesis and biological evaluation of bisacodyl analogues
2017
Herein is described in silico repositioning, design, synthesis, biological evaluation and structure-activity relationship (SAR) of an original class of anti-inflammatory agents based on a polyaromatic pharmacophore structurally related to bisacodyl (BSL) drug used in therapeutic as laxative. We describe the potential of TOMOCOMD-CARDD methods to find out new anti-inflammatory drug-like agents from a diverse series of compounds using the total and local atom based bilinear indices as molecular descriptors. The models obtained were validated by biological studies, identifying BSL as the first anti-inflammatory lead-like using in silico repurposing from commercially available drugs. Several bi…
A novel device for intracolonoscopy cleansing of inadequately prepared colonoscopy patients: a feasibility study.
2019
Abstract Background The importance of high quality preprocedural bowel preparation is widely acknowledged, but suboptimal bowel cleansing still occurs in up to 20 % of all colonoscopy patients. The aim of this study was to evaluate the performance of a novel intraprocedural cleaning device for cleaning poorly prepared colons. Methods This multicenter feasibility study included patients aged 18 – 75 years who were referred for colonoscopy. Intraprocedural cleaning was performed in patients after a limited preprocedural bowel preparation regimen (2 days of dietary restrictions and 2 × 10 mg bisacodyl). The primary outcome was the proportion of adequately prepared patients (Boston Bowel Prepar…
The effect of cathartic agents on transmucosal electrical potential difference in the human rectum.
1980
Active ion transport in the colon is generating a transmucosal electrical potential difference (PD) of about 40 mV. Cathartic agents inhibit electrolyte and water net-absorption or cause net-secretion which should be reflected in a change of PD. In 83 normal subjects the effect of an isotonic eletrolyte solution (control) and different cathartic agents on rectal PD was tested: Laxatives (bisacodyl, rhein), bile acids (cholic and deoxycholic acid), fatty acids (oleic and ricinoleic acid) and cardiac glycosides (meproscillarin, digitoxin, digoxin). Bisacodyl, deoxycholic acid in high concentration, meproscillarin and digitoxin significantly decreased PD, while the other substances did not. Ca…
Effect of Bisacodyl on Intestinal Electrolyte and Water Net Transport and Transit
1987
The effect of bisacodyl on intestinal electrolyte, glucose, and water transport, and transit was studied in 6 healthy volunteers by intestinal perfusion. A 5-lumen tube with an occluding balloon allowed constant perfusion (10 ml/min) of 30 cm of the upper jejunum and a rapid collection of the perfusate free of contaminants. A phenol red bolus was injected into the tube and its passage through the test segment was calculated by dye dilution formula. A 1-hour control period was followed by a test period with 6 mg/h bisacodyl and followed by 2 other 1-hour control periods. Net absorption of Na+ (0.35 +/- 0.08 mmol/min) and water (1.7 +/- 0.6 ml/min) changed to net secretion (Na+ -0.93 +/- 0.3 …
Einflu� eines diphenolischen Laxans (Bisacodyl) auf den Wasser- und Elektrolyttransport im menschlichen Colon
1974
Bei 5 Versuchspersonen wurde die Wirkung von Bisacodyl auf die Wasser- und Elektrolytbewegungen im menschlichen Colon untersucht. Das Colon wurde durch eine Sonde perfundiert, die in das Coecum plaziert wurde. Die Perfusionslosung enthielt NaCl (140 maq/l) als Chlorid und Bicarbonat und K (2,8 maq/l) als Chlorid sowie14C-Polyathylenglykol als Marker. Sie wurde mit einer Rate von 10 ml/min perfundiert und uber ein Darmrohr im Rectum wieder aufgefangen.
Effect of lactose, lactulose and bisacodyl on gastrointestinal transit studied by metal detector.
2007
SUMMARY Aim and methods: To study the effect of 45 g lactose, 30 g lactulose and 10 mg bisacodyl on gastrointestinal transit in 30 healthy volunteers by metal detector and Hinton marker method. The first set of measurements were performed under standard conditions. In a second stage, transit was slowed to twice the original value by loperamide to simulate constipation conditions. Results: Bisacodyl drastically accelerated small and large intestinal transit. Colonic transit was shortened to 23 % and to 31% of control values, without and with loperamide. Bisacodyl increased stool weight and decreased stool consistency in all persons. Lactulose marginally shortened small intestinal transit (P=…
<strong>In Silico Repurposing, Design, Synthesis and Biological Evaluation of Bisacodyl Analogues</strong>
2018
In a recent article was described in silico repositioning, design, synthesis, biological evaluation and structure-activity relationship (SAR) of an original class of anti-inflammatory agents based on a polyaromatic pharmacophore structurally related to bisacodyl (BSL) drug used in therapeutic as laxative.