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Bile Acid Sequestrants
Published in Charles Theisler, Adjuvant Medical Care, 2023
Prescription bile acid sequestrants such as cholestyramine (Cholybar, Questran) and cholestipol (Colestid) are used to reduce low-density lipoprotein (LDL) cholesterol levels. After oral administration, the sequestrants are not absorbed but instead bind to bile acids (which contain cholesterol) in the intestine and prevent their reabsorption into the body.1 Drugs that sequester bile acids can result in deficiencies of iron, folic acid, and fat-soluble vitamins (A, D, E, and K).1
Dyslipidemia
Published in Jahangir Moini, Matthew Adams, Anthony LoGalbo, Complications of Diabetes Mellitus, 2022
Jahangir Moini, Matthew Adams, Anthony LoGalbo
The bile acid sequestrants block reabsorption of intestinal bile acid. This forces the up-regulation of liver LDL receptors to recruit the circulating cholesterol and synthesize bile. These sequestrants reduce cardiovascular-related deaths. They are usually used along with statins or nicotinic acid. The sequestrants are the medications of choice for women planning to become pregnant, or who are already pregnant. Though safe, the sequestrants cause bloating, constipation, cramping, and nausea. They can also increase triglycerides, so they cannot be used if hypertriglyceridemia is present. The drugs called cholestyramine and colestipol interfere with absorption of thiazides, beta-blockers, digoxin, thyroxine, and warfarin. Colesevelam also interferes with these, but not as much. The interference between the drugs can be reduced by administration that is 4 or more hours before or 1 hour after. Bile acid sequestrants are more effective if they are taken during a meal.
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.
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
The presence of cholesterol in the colon stimulates bacterial growth causing gastrointestinal adverse effects [20,27]. As a result, BAS therapy (including colesevelam) is not recommended in patients at risk of bowel obstruction or inflammatory bowel disease. Cholestyramine and colestipol have been used for years but have been limited by poorer tolerability and low compliance compared to newer agents such as colesevelam [13]. Diarrhea remains common as an adverse effect with 10% (3/30) patients reporting this even with low dose colesevelam therapy (2.25 g/day) [27,28] . Compliance in licensing trials with colesevelam was 93% at 6 weeks and 88–91% over 6 months and did not differ from the placebo group (92%). In a retrospective claims database study of 42,000 patients adherence to colesevelam treatment was 33% (>50% doses taken) [29] and in another retrospective study persistence defined as less than 30 days missed over 1 year was 49% in 483 patients [30]. In combination therapy studies with statins, constipation was reported by 10 vs. 8% (number needed to harm (NNH) 40) on combination therapy with colesevelam and statins compared to statin alone [31–33]. Furthermore, myalgia was present in 6% in combination therapy compared with 4% on statin, 2% on colesevelam alone (2.1%) and 0.4% on placebo [31]. Among unexpected effects a dose-independent increase in alkaline phosphatase (ALP) [27] was seen with colesevelam. Interestingly fibrates reduce ALP.
The safety of current and emerging therapies for multiple myeloma
Published in Expert Opinion on Drug Safety, 2020
Omar Nadeem, Kenneth C. Anderson
Lenalidomide is well tolerated, with usual doses ranging from as low as 2.5 mg and up to 25 mg daily every 14 or 21 day of each monthly cycle. Lenalidomide is renally excreted and therefore requires dose adjustment based on creatinine clearance. Side effect profile of lenalidomide includes hematologic toxicity at varying degrees, depending on the combination. Rates of grade 3 or higher hematologic toxicity are low when used as a single agent in maintenance fashion. Non-hematologic toxicity includes GI adverse events including diarrhea and constipation, venous thromboembolism, and rash. Diarrhea with lenalidomide is best managed with supportive care medications such as loperamide. Colestipol is a bile acid resin that is helpful in mitigating lenalidomide-associated diarrhea. Finally, there is a small but real increase incidence of secondary cancers in patients receiving lenalidomide maintenance post-transplant, but the prolongation of PFS and OS achieved outweighs this risk [41].
Choosing an ideal pharmacotherapeutic strategy for dyslipidemia in children
Published in Expert Opinion on Pharmacotherapy, 2019
Dragana Nikolic, Andreea Corina, Peter. P. Toth, Lubna Hammad, Manfredi Rizzo
Bile acid sequestrants (BAS) are another treatment option. These drugs act as lipid lowering agents by binding bile acids within the gastrointestinal tract. This induces activation of 7-alpha-hydroxylase, which diverts hepatic intracellular cholesterol toward bile acid biosynthesis. Because intracellular cholesterol levels decrease, hepatocytes respond by upregulating the LDL-receptor, which leads to increased clearance of LDL-cholesterol and reduced serum levels of this lipoprotein. These agents are not systemically absorbed [15], so they are considered safe for children. However, the classical BAS (cholestyramine and colestipol) can lead to gastrointestinal side effects such as constipation, influencing long-term compliance. It should be highlighted that BAS interfere with the absorption of folate and fat-soluble vitamins.