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Do I Have IBS?
Published in Melissa G. Hunt, Aaron T. Beck, Reclaim Your Life From IBS, 2022
Melissa G. Hunt, Aaron T. Beck
The good news is that there is a very effective treatment for bile acid diarrhea. You take a medication called a bile acid sequestrant (cholestyramine, colestipol, or colesevelam). The medicine binds to the bile acid and keeps it from pulling so much water into the large intestine. A positive response to a bile acid sequestrant is usually a pretty good sign that excess bile acid was causing diarrhea, to begin with. Unfortunately, there are two downsides to the treatment. First, the medicine is a little hard to take. The medications come in two forms – resinous powder that needs to be mixed with food (like apple sauce or yogurt) or pills. The powder doesn’t taste great and it’s got a weird gritty texture that most people find pretty unappealing. The pills are quite large and hard to swallow, and you usually have to take at least 4 of them a day to get any benefit. (If you try them, be sure to ask the pharmacist to give you the brand name drug, not the generic. The generic pills are even harder to swallow.) The other downside is that the medications interfere with the absorption of lots of other medications, so you have to take it two hours after or four hours before you take anything else. That can make it hard to time them and hard to remember to take them. On the other hand, if your symptoms are really the result of bile acid diarrhea, and not IBS, then taking one of these medications may solve your symptoms completely.
Cardiovascular Drugs
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: The reproduction studies in animals have shown no evidence of fetal harm or impaired fertility. The pregnancy experience in humans is limited. Colesevelam should have no direct effect on the fetus because it is not absorbed systemically. However, it is well known that Colesevelam reduces the absorption of fat-soluble vitamins (A, K, E, and D).
Enzyme Kinetics and Drugs as Enzyme Inhibitors
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Bile acid sequestrants (colesevelam, cholestyramine, colestipol) are polymeric resigns that reduce LDL cholesterol levels. When administered orally, they are not absorbed but bind to cholesterol-containing bile acids in the intestine via ion exchange and prevent their reabsorption into the body. As a consequence of decreased concentration in bile acid hepatic synthesis of bile acids from cholesterol is increased which in turn increases LDL receptor activity resulting in an increased removal of LDL cholesterol from the blood. These drugs have been used for the treatment of hypercholesterolemia and dyslipidemia but are meanwhile displaced by other hypolipidemic agents, in particular by statins. Hansen et al. (2017) reported that treatment with bile acid sequestrants improves glycemic control suggesting their inclusion in current diabetes management strategies.
Colesevelam – a bile acid sequestrant for treating hypercholesterolemia and improving hyperglycemia
Published in Expert Opinion on Pharmacotherapy, 2022
Oluwayemisi Esan, Adie Viljoen, Anthony S. Wierzbicki
Colesevelam can be used to achieve a reduction in LDL–C in cases of statin intolerance or in combination with other lipid-lowering medications in these individuals [6,20]. Colesevelam is an effective alternative to other BAS due to its improved tolerability, dosage convenience and moderately more favorable pharmacokinetic interaction [13]. No studies have compared colesevelam with the traditional BASs using surrogate or CVD end points. Though it shows clear benefits in reducing LDL-C, C-reactive protein and HbA1c it does have significant disadvantages [6,20]. The side-effect profile of colesevelam is better than other BAS [13] but not as good as alternative agents. It has potential advantages in the treatment of the metabolic syndrome and diabetes given its action in reducing HbA1c and affects the absorption of hydrophobic drug therapies. However, its action in increasing TGs means its use is not recommended in patients with initial TG>3.5 mmol/L and it is also limited by its drug burden in terms of capsule numbers [35].
Efficacy and safety of add on therapies in patients with hypercholesterolemia undergoing statin therapy
Published in Expert Opinion on Pharmacotherapy, 2020
Brian Tomlinson, Paul Chan, Yuzhen Zhang, Christopher Wai Kei Lam
Colesevelam has demonstrated efficacy in lowering HbA1c in addition to LDL-C, although clinical outcomes data are lacking. Several mechanisms for the effect of colesevelam in patients with type 2 diabetes mellitus (T2DM) have been proposed, including effects on insulin sensitivity and secretion, incretin effects, changes in bile acid composition, and splanchnic sequestration of mealtime glucose [27]. Colesevelam is associated with absolute reductions in HbA1c in T2DM patients ranging from 0.32 to 1.1%. Colesevelam is generally well-tolerated, and indirect comparisons with cholestyramine suggest that it is associated with fewer gastrointestinal symptoms [27].
Preclinical discovery and development of colesevelam for the treatment of type 2 diabetes
Published in Expert Opinion on Drug Discovery, 2018
Henriette Holst Nerild, Mikkel Bring Christensen, Filip Krag Knop, Andreas Brønden
Across the four phase III clinical trials described above, the addition of colesevelam to various combinations of oral glucose-lowering drugs and/or insulin resulted in consistent placebo-corrected reductions in HbA1c of about 5 mmol/mol (0.5%) [18–21]. These findings have been confirmed by subsequent meta-analyses [54,55]. Furthermore, colesevelam has been demonstrated to cause statistically and clinically significant reductions in LDL cholesterol and total cholesterol, whereas some studies have demonstrated increased serum triglyceride concentrations following treatment with colesevelam.