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Intrahepatic Cholestasis of Pregnancy
Published in Vincenzo Berghella, Maternal-Fetal Evidence Based Guidelines, 2022
Cholestyramine. Cholestyramine is an anion exchange resin that binds to bile acids and decreases their absorption in the ileum. Compared to UDCA, cholestyramine had a lower effect on pruritus and liver function. No significant differences were observed in fetal outcomes and caesarean section rates. Cholestyramine use was found to have a greater number of adverse effects [22]. Cholestyramine should not be taken with other medications because of potential interference with their absorption. Safety: FDA pregnancy category C. Dose: 8 g orally once a day. Significant side effects include a decrease in intestinal absorption of fat-soluble vitamins A, D, E, and K, increased intestinal gas, diarrhea and poor palatability. No studies support the use of vitamin K supplementation to decrease risks associated with deficiency [29].
Rational Medical Therapy of Functional GI Disorders
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
Richard M. Sperling, Kenneth R. McQuaid
Bile-salt binding agents—the role of bile-salt malabsorption in diarrhea-predominant IBS remains controversial (see above). The bile-salt binding agent cholestyramine may be effective in reducing diarrhea in patients with documented bile-salt malabsorption, such as those with partial ileal resections. In addition, cholestyramine may cause constipation in normal subjects, suggesting that it has nonspecific constipating actions. Experience with cholestyramine in IBS has been extremely limited. In a study of 17 patients with idiopathic diarrhea (14 of whom had some evidence of increased bile malabsorption), cholestyramine had no significant effect on stool weight (242). In another study (243), cholestyramine resulted in “improvement” in four of six patients with diarrhea-predominant IBS and evidence of bile-salt malabsorption on nuclear testing. There may be rare IBS patients who experience symptomatic improvement with cholestyramine, but most patients find the agent unpalatable.
Atherosclerosis
Published in George Feuer, Felix A. de la Iglesia, Molecular Biochemistry of Human Disease, 2020
George Feuer, Felix A. de la Iglesia
Absorption of cholesterol only occurs in the presence of bile acids. If bile acid uptake is blocked, this effect will result in reduced cholesterol absorption.238,240,268,300,447,485,673,691Various anion exchange resins have been used to decrease cholesterol intake from the intestine. Cholestyramine or DDAE Sephadex exert hypocholesterolemic action by removing bile acids in the form of insoluble complexes which are then excreted in the stool.638 Cholestyramine increases the turnover of bile acids at the expense of cholesterol (Figure 38). The major disadvantage of this therapy is not only the bulk, but resins are not specific absorbents for bile acids preventing at the same time other compounds from being taken up. Observed side effects with resins mainly include constipation. Linoleamides are also inhibitors of cholesterol absorption. One of the most potent representatives of these drugs, moctamide, inhibits dietary induced hypercholesterolemia.636
Alterations in microbiota and their metabolites are associated with beneficial effects of bile acid sequestrant on icteric primary biliary Cholangitis
Published in Gut Microbes, 2021
Bo Li, Jun Zhang, Yong Chen, Qixia Wang, Li Yan, Rui Wang, Yiran Wei, Zhengrui You, Yikang Li, Qi Miao, Xiao Xiao, Min Lian, Weihua Chen, Dekai Qiu, Jingyuan Fang, M. Eric Gershwin, Ruqi Tang, Xiong Ma
Cholestyramine is one of the bile acid sequestrants capable of binding to intestinal lumen bile acids and has been used to treat cholestatic pruritus with a good safety profile and accessibility.11 In the Mdr2 knockout mouse model, bile acid sequestrants alleviate cholestatic liver and bile duct injury12 and, in humans with primary sclerosing cholangitis (PSC), there are case reports of improvement of cholestasis by cholestyramine.13 Here, we performed a 16-week longitudinal study in icteric PBC subjects using cholestyramine to characterize the compositional and functional responses of gut microbiota to alterations in endogenous bile acid levels. Multi-omic analysis including shotgun metagenomic sequencing and targeted metabolomic profiling was utilized. We further investigated whether these changes in bile acids and microbiota could explain the beneficial effects of cholestyramine on cholestasis.
Knowing when to use steroids, immunosuppressants or biologics for the treatment of sarcoidosis
Published in Expert Review of Respiratory Medicine, 2020
We then reported on our experience with LEF in 76 patients with pulmonary and extra-pulmonary sarcoidosis [71]. Fifty-four of these had adequate follow-up, and assessment of efficacy. The ones who were on systemic corticosteroids were able to wean their dose significantly or come off completely. We demonstrated that the gently declining FVC trajectory of patients with pulmonary disease could be reversed at the 6 months follow-up mark. It was also quite effective for extra-pulmonary sarcoidosis, leading to a complete response in half the affected organs and partial response in a third. We recommend treating patients with a daily dose of 20 mg. A significant proportion of our patients (20%) discontinued treatment because of side effects, mostly diarrhea and minor transaminitis. Length dependent peripheral neuropathy is a unique complication of LEF use [72]. Just two patients in our series developed a mild form of neuropathy, although we encounter this more frequently in clinical practice. Eight of our patients developed pulmonary infiltrates. Most of these responded to outpatient antibiotic therapy and were continued on the medication. LEF is also known to cause hypersensitivity pneumonitis, reversible upon drug discontinuation [73]. This may well have occurred in a couple of these patients, who required hospitalization and drug discontinuation. Cholestyramine [74,75] can be administered to patients with serious complications, to actively remove drug metabolites.
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.