The effects of colestipol tablets compared with colestipol granules on plasma cholesterol and other lipids in moderately hypercholesterolemic patients

Insull, William; Davidson, Michael; Demke, Donald M.; Dujovne, Carlos A.; Eckert, Susan M.; Ginsberg, David A.; Goldberg, Anne C.; Hodis, Howard N.; Hughes, Thomas A.; Kane, John P.; Oliphant, Thomas H.; Pitt, William A.; Schrott, Helmut G.; Sprecher, Dennis L.; Zavoral, James H.

doi:10.1016/0021-9150(94)05418-i

Cited by 12 publications

(4 citation statements)

References 26 publications

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“…These reductions were accompanied by a 19% reduction in the incidence of coronary heart disease [3, 4]. Similarly, treatment with colestipol (2 or 8 g twice daily) reduced LDLC levels in patients with mild hypercholesterolemia by 12% or 24%, respectively ( P ≤ 0.05) [5]. Monotherapy with colesevelam resulted in mean reductions in LDLC of 15% to 19% in adults with hypercholesterolemia [6, 7].…”

Section: Clinical Effects Of Bile Acid Sequestrantsmentioning

confidence: 99%

Bile Acid Sequestrants for Lipid and Glucose Control

2010

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Bile acids are generated in the liver and are traditionally recognized for their regulatory role in multiple metabolic processes including bile acid homeostasis, nutrient absorption, and cholesterol homeostasis. Recently, bile acids emerged as signaling molecules that, as ligands for the bile acid receptors farnesoid X receptor (FXR) and TGR5, activate and integrate multiple complex signaling pathways involved in lipid and glucose metabolism. Bile acid sequestrants are pharmacologic molecules that bind to bile acids in the intestine resulting in the interruption of bile acid homeostasis and, consequently, reduction in low-density lipoprotein cholesterol levels in hypercholesterolemia. Bile acid sequestrants also reduce glucose levels and improve glycemic control in persons with type 2 diabetes mellitus (T2DM). This article examines the mechanisms by which bile acid–mediated activation of FXR and TGR5 signaling pathways regulate lipid and glucose metabolism and the potential implications for bile acid sequestrant–mediated regulation of lipid and glucose levels in T2DM.

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Section: Clinical Effects Of Bile Acid Sequestrantsmentioning

confidence: 99%

Bile Acid Sequestrants for Lipid and Glucose Control

2010

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“…However, in the National Heart, Lung and Blood Institute (NHLBI) Type II Coronary Intervention study colestyramine resulted in a 28% increase in TG levels [39,63]. There is also evidence that the TG increase is dosedependent, at least for colestipol [64,65]. The increase of TG levels seen in studies with DM patients is a concern since TG concentrations is usually raised in these patients [66].…”

Section: Iii) Tgmentioning

confidence: 93%

“…BAS decreased apo B by 6 to 23% in several studies, in a dose-dependent manner [26,34,37,64,[76][77][78][79][80][81][82]. BAS treatment has been reported to induce the hepatic synthesis of apo AI, the major lipoprotein constituent of HDL, but not significantly so in all studies [28,76,83,84].…”

Section: Iv) Lipoproteins and Apolipoproteinsmentioning

confidence: 99%

Lipid-Lowering Drugs Acting at the Level of the Gastrointestinal Tract

Filippatos

Mikhailidis²

2009

CPD

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This review considers the hypolipidaemic drugs that act on the gastrointestinal (GI) tract. We searched PubMed up to April 2008 and included randomized controlled trials, original papers, review articles and case reports. Bile acid sequestrants (BAS) have a well-established low density lipoprotein cholesterol (LDL-C) lowering effect, but may increase triglyceride (TG) levels. BAS have no systematic adverse effects, but are associated with increased GI adverse effects and interactions with the absorption of other drugs. Ezetimibe improves LDL-C, high density lipoprotein cholesterol and TG levels, as monotherapy or especially when given with a statin. Ezetimibe has not been associated with serious adverse effects. Ezetimibe has not been evaluated in large clinical trials with cardiovascular disease (CVD) endpoints. Phytosterols are not licensed drugs; they have a well-established LDL-C lowering effect, but there are no large long-term randomized clinical trials investigating their effects on CVD events. Orlistat is an antiobesity drug with a small additional LDL-C lowering effect independent of weight loss. Orlistat-assisted weight loss improves the overall lipid profile, carbohydrate metabolism and transaminase activities. However, its use should be limited to weight reduction. This drug is associated with increased GI adverse effects.

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“…However, we have found that selected generic formulations of cholestyramine have poor palatability, which may impact patient adherence. 33,34 Colesevelam is formulated as a filmcoated tablet, and palatability will likely not be an issue. On the other hand, when comparing colesevelam with the packet form of brand products of the older bile acid-binding resins, colesevelam results in a 20-32% cost savings per percent reduction in LDL cholesterol.…”

Section: Therapeutic and Economic Issuesmentioning

confidence: 99%