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Bile Binding Resin

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2. Bile Binding Resin

Bile Binding Resin Bile Binding Resin Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Bile Binding Resin Bile Binding Resin Aka: Bile (...) Binding Resin , Bile Acid-Binding Resin , Cholestyramine , Colestipol , Colesevelam , Welchol From Related Chapters II. Effects decreased (15-30%) increased (3-5%) s increased III. Efficacy Lowers cardiovascular mortality by 30% Reduces risk IV. Adverse effects Gastrointestinal Effects Reduce Adverse GI side effects Use moderate doses: 8-10 g per day Increase or supplement with Colesevelam may have less GI intolerance Interferes with fat soluble bsorption Take 2 hours before or 4 hours after Resin

2018 FP Notebook

3. Glucose-lowering effects and mechanisms of the bile acid-sequestering resin sevelamer. (Abstract)

Glucose-lowering effects and mechanisms of the bile acid-sequestering resin sevelamer. Sevelamer, a non-absorbable amine-based resin used for treatment of hyperphosphataemia, has been demonstrated to have a marked bile acid-binding potential alongside beneficial effects on lipid and glucose metabolism. The aim of this study was to investigate the glucose-lowering effect and mechanism(s) of sevelamer in patients with type 2 diabetes.In this double-blinded randomized controlled trial, we (...) randomized 30 patients with type 2 diabetes to sevelamer (n = 20) or placebo (n = 10). Participants were subjected to standardized 4-hour liquid meal tests at baseline and after 7 days of treatment. The main outcome measure was plasma glucagon-like peptide-1 excursions as measured by area under the curve. In addition, blood was sampled for measurements of glucose, lipids, glucose-dependent insulinotropic polypeptide, C-peptide, glucagon, fibroblast growth factor-19, cholecystokinin and bile acids

2018 obesity & metabolism Controlled trial quality: uncertain

4. Canadian Association of Gastroenterology Clinical Practice Guideline on the Management of Bile Acid Diarrhea

discontinuation rates with BAST, alternative treatments often are needed. HPC may im- prove diarrhea in patients with BAD through its bulking effects and its ability to bind bile acids (63–66). In addition, some patients may benefit from loperamide; given its low cost and rel - atively good safety profile (although no cost-effectiveness data are available), a treatment trial may be warranted. Statement 13. In patients with BAD who re- spond to BAST, we suggest that intermittent, on-demand dosing be tried (...) Canadian Association of Gastroenterology Clinical Practice Guideline on the Management of Bile Acid Diarrhea e10 © 2019 by the Canadian Association of Gastroenterology and the AGA Institute This article is being published jointly in Journal of the Canadian Association of Gastroenterology and Clinical Gastroenterology and Hepatology. This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http:// creativecommons.org/licenses/by-nc

2020 Canadian Association of Gastroenterology

5. Bile Binding Resin

Bile Binding Resin Bile Binding Resin Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Bile Binding Resin Bile Binding Resin Aka: Bile (...) Binding Resin , Bile Acid-Binding Resin , Cholestyramine , Colestipol , Colesevelam , Welchol From Related Chapters II. Effects decreased (15-30%) increased (3-5%) s increased III. Efficacy Lowers cardiovascular mortality by 30% Reduces risk IV. Adverse effects Gastrointestinal Effects Reduce Adverse GI side effects Use moderate doses: 8-10 g per day Increase or supplement with Colesevelam may have less GI intolerance Interferes with fat soluble bsorption Take 2 hours before or 4 hours after Resin

2015 FP Notebook

6. Effects of bile-acid-binding resin (colestimide) on blood glucose and visceral fat in Japanese patients with type 2 diabetes mellitus and hypercholesterolemia: an open-label, randomized, case-control, crossover study. (Abstract)

Effects of bile-acid-binding resin (colestimide) on blood glucose and visceral fat in Japanese patients with type 2 diabetes mellitus and hypercholesterolemia: an open-label, randomized, case-control, crossover study. The objective was to examine the effects of colestimide on blood glucose, visceral fat, adipocytokines, and bile acid conjugate fractions in Japanese patients.This study was an open-label, randomized, case-control, crossover study of colestimide 3 g/day in 40 Japanese patients

2012 Journal of diabetes and its complications Controlled trial quality: uncertain

7. Drug-Resin Drug Interactions in Patients with Delayed Gastric Emptying: What is optimal time window for drug administration? Full Text available with Trip Pro

Drug-Resin Drug Interactions in Patients with Delayed Gastric Emptying: What is optimal time window for drug administration? Most drug-drug interactions involve overlap or competition in drug metabolic pathways. However, there are medications, typically resins, whose function is to bind injurious substances such as bile acids or potassium within the digestive tract. The objective of this article is to review the functions of the stomach and the kinetics of emptying of different food forms (...) or formulations to make recommendations on timing of medication administration in order to avoid intragastric drug interactions. Based on the profiles and kinetics of emptying of liquid nutrients and homogenized solids, a window of 3 h between administration of a resin drug and another 'target' medication would be expected to allow a median of 80% of medications with particle size <1 mm to empty from the stomach and, hence, avoid potential interaction such as binding of the 'target' medication within

2016 Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society

8. Intestinal Bile Acid Composition Modulates Prohormone Convertase 1/3 (PC1/3) Expression and Consequent GLP-1 Production in male mice. Full Text available with Trip Pro

Intestinal Bile Acid Composition Modulates Prohormone Convertase 1/3 (PC1/3) Expression and Consequent GLP-1 Production in male mice. Besides an established medication for hypercholesterolemia, bile acid binding resins (BABRs) present antidiabetic effects. Although the mechanisms underlying these effects are still enigmatic, glucagon-like peptide-1 (GLP-1) appears to be involved. In addition to a few reported mechanisms, we propose prohormone convertase 1/3 (PC1/3), an essential enzyme of GLP-1 (...) production, as a potent molecule in the GLP-1 release induced by BABRs. In our study, the BABR colestimide leads to a bile acid-specific G protein-coupled receptor TGR5-dependent induction of PC1/3 gene expression. Here, we focused on the alteration of intestinal bile acid composition and consequent increase of total TGR5 agonistic activity to explain the TGR5 activation. Furthermore, we demonstrate that nuclear factor of activated T cells mediates the TGR5-triggered PC1/3 gene expression. Altogether

2016 Endocrinology

9. Effect of Bile Acid Secretion and Sequestration on GLP-1 Secretion

is a human interventional randomized controlled cross-over study including four study days for each participant. As a tool to sequester bile acids we will use sevelamer, a phosphate binding resin used in the treatment of hyperphosphataemia in adult patients with chronic kidney disease. Surprisingly, sevelamer has been shown to improve glycaemic control in patients with chronic kidney disease and type 2 diabetes. Intravenous infusion of cholecystokinin will be used to elicit gallbladder contraction (...) Effect of Bile Acid Secretion and Sequestration on GLP-1 Secretion Effect of Bile Acid Secretion and Sequestration on GLP-1 Secretion - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search for terms x × Study Record Detail Saved Studies Save this study Warning You have reached the maximum number of saved studies (100). Please remove one or more studies before adding more. Effect of Bile Acid

2015 Clinical Trials

10. Effect of Bile Acid Sequestration on Postprandial GLP-1 Secretion, Glucose Homeostasis and Gut Microbiota

, gut microbiota and glucose homeostasis in patients with type 2 diabetes and healthy individuals. As a tool to sequester bile acids we will use sevelamer, a phosphate binding resin used in the treatment of hyperphosphataemia in adult patients with chronic kidney disease. Surprisingly, sevelamer was recently shown to improve glycaemic control in patients with chronic kidney disease and type 2 diabetes. The investigators hypothesize that higher luminal concentrations of bile acids in the distal gut (...) Effect of Bile Acid Sequestration on Postprandial GLP-1 Secretion, Glucose Homeostasis and Gut Microbiota Effect of Bile Acid Sequestration on Postprandial GLP-1 Secretion, Glucose Homeostasis and Gut Microbiota - Full Text View - ClinicalTrials.gov Hide glossary Glossary Study record managers: refer to the if submitting registration or results information. Search for terms x × Study Record Detail Saved Studies Save this study Warning You have reached the maximum number of saved studies (100

2014 Clinical Trials

11. Management of Dyslipidaemias Full Text available with Trip Pro

diabetes mellitus 29 8.1.4.4 Increased risk of haemorrhagic stroke 29 8.1.4.5 Adverse effects on kidney function 29 8.1.4.6 Interactions 29 8.2 Cholesterol absorption inhibitors 30 8.2.1 Mechanism of action 30 8.2.2 Effects on lipids 30 8.2.3 Effect on cardiovascular morbidity and mortality 30 8.2.4 Adverse effects and interactions 30 8.3 Bile acid sequestrants 30 8.3.1 Mechanism of action 30 8.3.2 Effects on lipids 30 8.3.3 Effect on cardiovascular morbidity and mortality 30 8.3.4 Adverse effects (...) Trialists CV Cardiovascular CVD Cardiovascular disease CYP Cytochrome P450 4D Die Deutsche Diabetes Dialyse Studie dal-OUTCOMES Effects of Dalcetrapib in Patients with a Recent Acute Coronary Syndrome DASH Dietary Approaches to Stop Hypertension DGAT-2 Diacylglycerol acyltransferase-2 DHA Docosahexaenoic acid DM Diabetes mellitus EAPC European Association of Preventive Cardiology EAS European Atherosclerosis Society EBBINGHAUS Evaluating PCSK9 Binding Antibody Influence on Cognitive Health in High

2019 European Society of Cardiology

12. British Association of Dermatologists? guidelines for the investigation and management of generalized pruritus in adults without an underlying dermatosis

British Association of Dermatologists British Journal of Dermatology (2018) 178, pp34–60 BAD guidelines for generalized pruritus, 2018, G.W.M. Millington et al. 41For pruritus associated with parenchymal liver disease, cholestyramine is often given as ?rst-line therapy, although there is limited evidence. Cholestyramine, colestipol and cole- sevelam (anion exchange binding resins) bind bile salts in the gut lumen, thus preventing absorption of bile acids in the ter- minal ileum. 144,145 A meta (...) patients with chronic GPWOR. Note that ferritin is an acute-phase pro- teinandmaybeelevatedinasituationofironde?ciency. Where iron de?ciency is suspected, and ferritin is appar- ently ‘normal’, it may be necessary to check serum iron and total iron binding capacity as well. A trial of iron replacement should be given if the ferritin is below the lower limit of the reference range (between 15 and 25 lgL 1 in most U.K. lab- oratories) or if there is anaemia or microcytosis not attributa- ble to any other

2018 British Association of Dermatologists

13. Obeticholic acid (Ocaliva) - Liver Cirrhosis, Biliary

concentrations and efficacy of OCA in clinical studies and attenuate its efficacy. Therefore OCA should be taken at least 4-6 hours before or 4-6 hours after (or at as great an interval as possible) taking bile acid resin as outlined in the SmPC. No further clinically significant DDIs are expected based upon metabolic profiles of the most widely used concomitant medications in PBC patients. From a clinical point of view, the information regarding OCA´s PD, in particular on the mechanistic of the anti (...) Code): bile therapy, bile acid preparations (A05AA04) Therapeutic indication(s): OCALIVA is indicated for the treatment of primary biliary cholangitis (also known as primary biliary cirrhosis) in combination with ursodeoxycholic acid (UDCA) in adults with an inadequate response to UDCA or as monotherapy in adults unable to tolerate UDCA. Pharmaceutical form(s): Film-coated tablet Strength(s): 5 mg and 10 mg Route(s) of administration: Oral use Packaging: bottle (HDPE) Package size(s): 30 tablets

2017 European Medicines Agency - EPARs

14. Primary Biliary Cholangitis

axis, including the farnesoid X receptor (FXR)/?broblast growth factor (FGF)-19 signalling pathway. FXR is a central transcriptional sensor of bile acid metabolism, and one of its key target genes in the gut is FGF-19, which encodes an enterokine released into portal blood, following bile acid binding to FXR. PBC impacts patients both through progression to end-stage liver disease (i.e. cirrhosis and the need for liver transplantation), and symptomatically. The symptoms associated with PBC impact (...) that predominantlyaffectswomen.It isa globallyrecognised autoim- mune cholestatic liver disease [2–5] with several characteristics, including: cholestasis, serologic reactivity to antimitochondrial antibodies (AMA) or speci?c antinuclear antibody (ANA) reactivity, with accompanying histologic evidence of chronic non-suppurative, granulomatous, lymphocytic small bile duct cholangitis. The disease is chronic and often progressive, result- ing in end-stage liver disease and its associated complications [6–8]. The youngest

2017 European Association for the Study of the Liver

15. Guidance on Primary Biliary Cholangitis

or a higher dose of 23 to 25 mg/kg/day in biochemical responses and cost. (145) The studies that show an improvement in survival have all used this dose of 13 to 15 mg/kg/ day. A direct comparison of different drug formula- tions has not been studied in patients with PBC. A short-term pharmacokinetic study of normal volun- teers suggested substantial differences in bioavailabil- ity on the basis of preparation. (146) Cholestyramine and other bile acid-binding sequestrants as well as some antacids may (...) - logic signature, antimitochondrial antibody (AMA), and specific bile duct pathology. (1-4) The etiology of PBC is thought to be due to a combination of genetic risk factors and environmental triggers. (5-7) AMA is a highly disease-specific autoantibody (8) that targets the lipoic acid present on the 2-oxo-acid Abbreviations: AASLD, American Association for the Study of Liver Diseases; AIH, autoimmune hepatitis; ALP, alkaline phosphatase; AMA, antimitochondrial antibody; FDR, first-degree relative

2018 American Association for the Study of Liver Diseases

16. Etelcalcetide (Parsabiv) - reduce the levels of parathyroid hormone in adults who have high levels of this hormone because of their long-term kidney disease (secondary hyperparathyroidism)

2.9.1. User consultation 87 2.9.2. Additional monitoring 87 3. Benefit-Risk Balance 87 Discussion on the benefit-risk assessment 95 4. Recommendations 97 Assessment report EMA/664198/2016 Page 4/98 List of abbreviations ADME absorption, distribution, metabolism, excretion AMG 416 Etelcalcetide AUC area under the concentration-time curve BDC bile duct cannulated BSAP bone specific alkaline phosphatase CaSR calcium-sensing receptor cCA corrected calcium cCa x P corrected calcium-phosphorus product CI (...) to an L-cysteine via a disulfide bond that acts as an allosteric activator of the CaSR. It binds directly to the extracellular domain and activates the receptor at a site which is distinct from the calcium activating site. This suppresses secretion of PTH due to an increased sensitivity of the CaSR receptor to calcium, leading to a decrease in calcium levels. Dose recommendation Etelcalcetide (AMG 416) is the only calcimimetic formulated for i.v. administration. The recommended initial dose

2016 European Medicines Agency - EPARs

18. Hetlioz - tasimelteon

regulator that resets the master body clock in the suprachiasmatic nucleus (SCN). Tasimelteon is a Dual Melatonin Receptor Agonist (DMRA) with selective agonist activity at the MT1 and MT2 receptors believed to act in the SCN. All of tasimelteon’s main metabolites (M3, M9, M11, M12, M13, and M14) bind to the melatonin receptors but with less affinity than the parent. 2.4. Quality aspects 2.4.1. Introduction The finished product is presented as hard capsules containing 20 mg of tasimelteon as active (...) capsules with polypropylene child-resistant closures containing polypropylene resin induction seals. Each bottle also contains a 1.5-g silica gel desiccant canister and polyester dunnage. Single HDPE bottle is provided in paperboard carton. 2.4.2. Active Substance General information The chemical name of tasimelteon is (1R, 2R)-N-[2-(2,3-dihydrobenzofuran-4-yl)cyclopropylmethyl] propanamide and has the following structure: EMA/CHMP/601383/2014 Page 11/79 The chemical structure of tasimelteon has been

2015 European Medicines Agency - EPARs

19. BindRen (colestilan)

, L.Sativa, L.Esculentum Earthworm, Acute Toxicity Tests OECD 207 NOEC 1000 mg/ kg Eisenia Fetida It can be concluded that the proposed use of colestilan is not expected to pose a risk to the environment. 2.3.6. Discussion on non-clinical aspects MCI-196 is an anion exchange resin and the primary pharmacodynamic effect of MCI 196 in the treatment of hyperphosphataemia is due exclusively to its binding and excretion of phosphate. The same mechanism of action (i.e. the ability of MCI-196 to bind anions (...) ) is also the basis for the secondary pharmacodynamic effect of MCI-196, the binding and excretion of bile acids. Phosphate binding characteristics of MCI-196 have been studied in vitro and the results obtained indicate that MCI-196 would be expected to bind phosphates within the GI tract after oral administration. In phosphate solution a lower affinity for phosphate was seen in artificial intestinal fluid and in presence of cholate. Results of in vivo phosphorus mass balance studies in normal rats

2015 European Medicines Agency - EPARs

20. Screening and Management of Lipids

of myopathy and rhabdomyolysis. Bile acid resins. Cholestyramine, colestipol, and colesevelam are generally considered second line because of poor patient tolerability to side effects and difficult dosing/administration time. These drugs have been shown to reduce LDL-C cholesterol 15-30%, depending on dose. They are available in powder and tablet form. Resins work by binding cholesterol in the gut and interfering with absorption. They may increase triglycerides and should not be initiated in individuals (...) . Pharmacologic Treatment: Statins Statins the first-line agents. Statins are the first-line agents for lipid management. Statins have the advantage of potency, tolerability, safety, and strong clinical trial data supporting benefit. Bile acid resins are generally more expensive per LDL-C reduction, and have much higher rates of side effects. Fibrates are well tolerated, but have minimal impact on LDL-C and have not shown dramatic results in terms of event reduction. Niacin is effective at improving metabolic

2016 University of Michigan Health System

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