Colesevelam hydrochloride

Colesevelam hydrochloride, 5 145 Colestid, molecular formula and structure, 5 14 It... 

Currently available BAS include cholestyramine, colestipol and colesevelam hydrochloride (colestimide). Cholestyramine comprises a long-chain polymer of styrene with divinylbenzene trimethylbenzylammonium groups, whereas colestipol is a long-chain polymer of l-chloro-2,3-epoxypropane with diethylenetriamine. Colesevelam HCl is poly(allylamine hydrochloride) cross-linked with epichlorohydrin and alkylated with 1-bromodecane and 6-bromo-hexyl-trimethylammonium bromide. Bile-acid binding is enhanced and stabilised in the latter compound by long hydrophobic sidechains, increased density of primary amines, and quaternary amine sidechains. For this reason, colesevelam HCl exhibits increased affinity, specificity and capacity to bind bile acids compared with the other BAS. Colesevelam HCl also binds dihydroxy and trihydroxy bile acids with equal affinity, contrasting with cholestyramine and colestipol that preferentially bind dihydroxy bile acids (CDCA and deoxycholic acid). The latter BAS can lead to an imbalance towards trihydroxy bile acids and a more hydrophilic bile-acid pool. 

Aldridge MA, Ito MK. Colesevelam hydrochloride a novel bile acid-binding resin. Ann Pharmacother 2001 Jul-Aug 35(7-8) 898-907. 

Colesevelam hydrochloride ( welchol) is available as a solid tablet containing 0.625 g of colesevelam. The starting dose is either three tablets taken twice daily with meals or all six tablets taken with a meal. The tablets should be taken with a liquid. The maximum daily dose is 7 tablets (4.375 g). 

Donovan JM, Stypinski D, Stiles MI Olson TA Burke SK. Drug interactions with colesevelam hydrochloride, a novel, potent lipid-lowering agent. Cardiovasc Drugs Ther (2000) 14, 681-90. 

Liimebur SA, Capell WH, Saseen JJ, Wolfe P, Eckel RH (2007) Plant sterols added to combination statin and colesevelam hydrochloride therapy failed to lower low-density lipoprotein cholesterol concentrations. J Clin Lipidol l(6) 626-633. doi 10.1016/j. jacl.2007.10.004... 

Product information. Welchol (Colesevelam hydrochloride) Parsippany. New Jersey Daiichl Sankyo Inc 2009. 

Davidson MH, Dfllon MA, Gordon B, Jones P, Samuels J, Weiss S, et al. Colesevelam hydrochloride (Cholestagel) a new, potent bile acid sequestrant associated with a low incidence of gastrointestinal side effects. Arch Intern Med 1999 159 1893-900. 

Davidson MH, EHckhn MR, Maki KC, Kleinpeh RM. Colesevelam hydrochloride a non-absorbed, polymeric cholesterol-lowering agent. Expert Opin Investig Drugs 2000 9 2663-71. 

Tuteja S, Pyrsopoulos NT, Wolowich WR, Khanmoradi K, Levi DM, Selvaggi G, et al. Simvastatin-ezetrmibe-induced hepatic failure necessitating liver transplantation. Pharmacotherapy 2008 28 1188-93. Product information. Welchol (Colesevelam hydrochloride) Parsippany. New Jersey Daiichi Sankyo Inc, 2009. 

Weitzman, S. P. Ginsburg, K. C. et al. (2009). "Colesevelam hydrochloride and lanthanum carbonate interfere with the absorption of levothyroxine." Thyroid, 19(1), 77-9. 

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