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Cholesterol absorption inhibitors are a class of compounds that prevent the uptake of cholesterol from the small intestine into the circulatory system. Most of these molecules are monobactams but show no antibiotic activity. An example is ezetimibe (SCH 58235)[1][2][3][4] Another example is Sch-48461.[5] The "Sch" is for Schering-Plough, where these compounds were developed.
Phytosterols are also cholesterol absorption inhibitors.
Viscous soluble fiber is available in foods or fiber supplements and can reduce LDL-C. It is hypothesized that this effect is by binding to bile acids and preventing their resorption.[6] Psyllium reduces LDL-C by 0.33 mmol/l (12.5 mg/dl) and also reduces apolipoprotein B, leading one systematic review to conclude that it "effectively improves conventional and alternative lipids markers, potentially delaying the process of atherosclerosis-associated CVD risk in those with or without hypercholesterolemia".[7] Another soluble fiber, konjac glucomannan, reduces LDL by 10 percent.[8]
^Patrick JE, Kosoglou T, Stauber KL, et al. (April 2002). "Disposition of the selective cholesterol absorption inhibitor ezetimibe in healthy male subjects" (PDF). Drug Metab. Dispos. 30 (4): 430–7. doi:10.1124/dmd.30.4.430. PMID 11901097. S2CID 30862556. Archived from the original (PDF) on 2019-03-04.
^Dujovne CA, Ettinger MP, McNeer JF, et al. (November 2002). "Efficacy and safety of a potent new selective cholesterol absorption inhibitor, ezetimibe, in patients with primary hypercholesterolemia". Am. J. Cardiol. 90 (10): 1092–7. doi:10.1016/S0002-9149(02)02798-4. PMID 12423709.
^Rosenblum SB, Huynh T, Afonso A, et al. (March 1998). "Discovery of 1-(4-fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4 -hydroxyphenyl)-2-azetidinone (SCH 58235): a designed, potent, orally active inhibitor of cholesterol absorption". J. Med. Chem. 41 (6): 973–80. doi:10.1021/jm970701f. PMID 9526571.
^Jeu L, Cheng JW (September 2003). "Pharmacology and therapeutics of ezetimibe (SCH 58235), a cholesterol-absorption inhibitor". Clin Ther. 25 (9): 2352–87. doi:10.1016/S0149-2918(03)80281-3. PMID 14604738.
^Salisbury BG, Davis HR, Burrier RE, et al. (May 1995). "Hypocholesterolemic activity of a novel inhibitor of cholesterol absorption, SCH 48461". Atherosclerosis. 115 (1): 45–63. doi:10.1016/0021-9150(94)05499-9. PMID 7669087.
^Moreyra, Abel E. (23 May 2005). "Effect of Combining Psyllium Fiber With Simvastatin in Lowering Cholesterol". Archives of Internal Medicine. 165 (10): 1161. doi:10.1001/archinte.165.10.1161.
^Jovanovski, Elena; Yashpal, Shahen; Komishon, Allison; Zurbau, Andreea; Blanco Mejia, Sonia; Ho, Hoang Vi Thanh; Li, Dandan; Sievenpiper, John; Duvnjak, Lea; Vuksan, Vladimir (1 November 2018). "Effect of psyllium (Plantago ovata) fiber on LDL cholesterol and alternative lipid targets, non-HDL cholesterol and apolipoprotein B: a systematic review and meta-analysis of randomized controlled trials". The American Journal of Clinical Nutrition. 108 (5): 922–932. doi:10.1093/ajcn/nqy115. ISSN 1938-3207. PMID 30239559.
^Ho, Hoang Vi Thanh; Jovanovski, Elena; Zurbau, Andreea; Blanco Mejia, Sonia; Sievenpiper, John L.; Au-Yeung, Fei; Jenkins, Alexandra L.; Duvnjak, Lea; Leiter, Lawrence; Vuksan, Vladimir (May 2017). "A systematic review and meta-analysis of randomized controlled trials of the effect of konjac glucomannan, a viscous soluble fiber, on LDL cholesterol and the new lipid targets non-HDL cholesterol and apolipoprotein B". The American Journal of Clinical Nutrition. 105 (5): 1239–1247. doi:10.3945/ajcn.116.142158. ISSN 1938-3207. PMID 28356275.
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Cholesterolabsorptioninhibitors are a class of compounds that prevent the uptake of cholesterol from the small intestine into the circulatory system...
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and fatigue. Ezetimibe inhibits the absorption of cholesterol from the small intestine and decreases the amount of cholesterol normally available to liver...
treatment of high cholesterol (e.g., statins, cholesterolabsorptioninhibitors), medications to treat high blood pressure (e.g., ACE inhibitors, angiotensin...
atorvastatin works by inhibiting HMG-CoA reductase, an enzyme found in the liver that plays a role in producing cholesterol. Atorvastatin was patented...
for decreasing LDL cholesterol. The most common side effects include bloating and diarrhea. Inhibitors of intestinal sterol absorption, such as ezetimibe...
lipids found in the human body from ingesting food are triglycerides and cholesterol. Other types of lipids found in the body are fatty acids and membrane...
cholestyramine, colestipol) could be considered. In October 2002, a new cholesterolabsorptioninhibitor, ezetimibe, received US Food and Drug Administration (FDA)...
were used to reduce LDL cholesterol levels. More controversial is the addition of ezetimibe, which inhibitscholesterolabsorption in the gut. While it reduces...
attenuate the absorption of sugar, reduce sugar response after eating, and reduce lipid absorption (notably shown with cholesterolabsorption). Their use...
Hyzetimibe is a pharmaceutical drug that inhibitscholesterolabsorption. It targets the NPC1-like intracellular cholesterol transporter 1. In China, it is used...
brush border membrane, which results in fat absorption. Synthesis of bile acids is a major route of cholesterol metabolism in most species other than humans...
anticonvulsant and a steroidogenesis inhibitor. In terms of the latter property, it inhibits enzymes such as cholesterol side-chain cleavage enzyme (CYP11A1...
the ability of berberine to lower serum cholesterol. Annexin A2, an endogenous protein, is a natural inhibitor of PCSK9 activity. GRCh38: Ensembl release...
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clearance. a Moderate inhibitor causes at least a 2-fold increase in the plasma AUC values, or 50–80% decrease in clearance. a Weak inhibitor causes at least...
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