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Colesevelam hydrochloride: reducing atherosclerotic coronary heart disease risk factors.

Bays H, Jones PH - Vasc Health Risk Manag (2007)

Bottom Line: Colesevelam HCl is a bile acid sequestrant (BAS) which has been specifically designed with a unique structure for the purpose of improving tolerability and reducing potential drug interactions compared to older BAS, such as cholestyramine and colestipol.Colesevelam HCl has specifically been shown to reduce total and low-density lipoprotein (LDL) cholesterol levels, and has been approved as a cholesterol-lowering drug since year 2000.This discussion reviews mechanisms by which BAS lower cholesterol, and potential mechanisms by which BAS lower glucose levels in patients with type 2 diabetes mellitus.

View Article: PubMed Central - PubMed

Affiliation: L-MARC Research Center, 3288 Illinois Avenue, Louisville, KY 40213, USA. hbaysmd@aol.com

ABSTRACT
Colesevelam HCl is a bile acid sequestrant (BAS) which has been specifically designed with a unique structure for the purpose of improving tolerability and reducing potential drug interactions compared to older BAS, such as cholestyramine and colestipol. As a class, BAS are known to reduce cholesterol and glucose levels, and to reduce atherosclerotic coronary heart disease (CHD) risk as monotherapy, and in combination with other lipid-altering drug therapies. Colesevelam HCl has specifically been shown to reduce total and low-density lipoprotein (LDL) cholesterol levels, and has been approved as a cholesterol-lowering drug since year 2000. It has also been shown to reduce glucose levels. This discussion reviews mechanisms by which BAS lower cholesterol, and potential mechanisms by which BAS lower glucose levels in patients with type 2 diabetes mellitus. Finally this paper specifically reviews colesevelam HCl's pharmacology, lipid and glucose efficacy, safety/tolerability, and clinical use.

Show MeSH

Related in: MedlinePlus

Bile acid composition in bile and intestine.
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fig1: Bile acid composition in bile and intestine.

Mentions: The hepatic conversion of cholesterol to bile acids occurs through the rate-limiting enzyme, cholesterol cytochrome P450 7 alpha hydroxylase (CYP7A1) (Figure 1). Once conjugated with glycine or taurine, primary bile acids are then stored in the gall bladder and/or secreted into the intestine through the bile. Once in the intestine, bacterial 7-dehydroxylation results in the formation of secondary bile acids such as lithocholic and deoxycholic acid. The monohydroxy lithocholic acid can undergo 7 beta-hydroxylation, resulting in the formation of the tertiary, dihydroxy bile acid ursodeoxycholic acid. Ursodeoxycholic acid can undergo 7-dehydroxylation to form lithocholic acid. Although found in small amounts in humans, ursodeoxycholic acid is the principal bile acid produced in bears. It may decrease the intestinal absorption of cholesterol. And because an imbalance in cholesterol versus bile acids may contribute to gallstone formation, ursodeoxycholic acid is therapeutically used to prevent and treat cholesterol gallstone formation by blocking hepatic cholesterol production, decreasing biliary cholesterol, and promoting the dissolution of gallstones.


Colesevelam hydrochloride: reducing atherosclerotic coronary heart disease risk factors.

Bays H, Jones PH - Vasc Health Risk Manag (2007)

Bile acid composition in bile and intestine.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2291317&req=5

fig1: Bile acid composition in bile and intestine.
Mentions: The hepatic conversion of cholesterol to bile acids occurs through the rate-limiting enzyme, cholesterol cytochrome P450 7 alpha hydroxylase (CYP7A1) (Figure 1). Once conjugated with glycine or taurine, primary bile acids are then stored in the gall bladder and/or secreted into the intestine through the bile. Once in the intestine, bacterial 7-dehydroxylation results in the formation of secondary bile acids such as lithocholic and deoxycholic acid. The monohydroxy lithocholic acid can undergo 7 beta-hydroxylation, resulting in the formation of the tertiary, dihydroxy bile acid ursodeoxycholic acid. Ursodeoxycholic acid can undergo 7-dehydroxylation to form lithocholic acid. Although found in small amounts in humans, ursodeoxycholic acid is the principal bile acid produced in bears. It may decrease the intestinal absorption of cholesterol. And because an imbalance in cholesterol versus bile acids may contribute to gallstone formation, ursodeoxycholic acid is therapeutically used to prevent and treat cholesterol gallstone formation by blocking hepatic cholesterol production, decreasing biliary cholesterol, and promoting the dissolution of gallstones.

Bottom Line: Colesevelam HCl is a bile acid sequestrant (BAS) which has been specifically designed with a unique structure for the purpose of improving tolerability and reducing potential drug interactions compared to older BAS, such as cholestyramine and colestipol.Colesevelam HCl has specifically been shown to reduce total and low-density lipoprotein (LDL) cholesterol levels, and has been approved as a cholesterol-lowering drug since year 2000.This discussion reviews mechanisms by which BAS lower cholesterol, and potential mechanisms by which BAS lower glucose levels in patients with type 2 diabetes mellitus.

View Article: PubMed Central - PubMed

Affiliation: L-MARC Research Center, 3288 Illinois Avenue, Louisville, KY 40213, USA. hbaysmd@aol.com

ABSTRACT
Colesevelam HCl is a bile acid sequestrant (BAS) which has been specifically designed with a unique structure for the purpose of improving tolerability and reducing potential drug interactions compared to older BAS, such as cholestyramine and colestipol. As a class, BAS are known to reduce cholesterol and glucose levels, and to reduce atherosclerotic coronary heart disease (CHD) risk as monotherapy, and in combination with other lipid-altering drug therapies. Colesevelam HCl has specifically been shown to reduce total and low-density lipoprotein (LDL) cholesterol levels, and has been approved as a cholesterol-lowering drug since year 2000. It has also been shown to reduce glucose levels. This discussion reviews mechanisms by which BAS lower cholesterol, and potential mechanisms by which BAS lower glucose levels in patients with type 2 diabetes mellitus. Finally this paper specifically reviews colesevelam HCl's pharmacology, lipid and glucose efficacy, safety/tolerability, and clinical use.

Show MeSH
Related in: MedlinePlus