Colesevelam

Colesevelam is a bile acid sequestrant, used in adults along with diet, weight loss, and exercise to lower cholesterol levels and fatty substances in the blood alone or in combination with other cholesterol-lowering medications known as statins. Colesevelam is also used to treat with familial heterozygous hypercholesterolemia alone or with statins in some boys and in girls, between the ages of 10 to 17. This is an inherited condition body is unable to naturally reduce cholesterol levels and other fatty substances in the blood. Colesevelam is also used to control blood sugar levels in adults with type 2 diabetes. Colesevelam actions bind bile acids in intestines to form a product that is removed from the body. Colesevelam is sold under the brand name Welchol, Genzyme, Cholestagel among others. GelTex Pharmaceuticals first developed Colesevelam compounds in early 2000. Genzyme acquired GelTex Pharmaceuticals, there by getting the ownership of the patent. Genzyme in turn was bought by sanofi-aventis in 2011.

Dosage and information

Colesevelam is available as a tablet, in a chewable bar, and as a powder to be mixed with a liquid, all three are administered orally. The usual recommended dose of tablets is taken once or twice a day. The dose of chewable bars and the powder is once a day. Colesevelam should be taken exactly as directed. Users are warned not never take more or less of it or take it more often than prescribed by the Doctor. The dose when taking the powder for oral suspension, is one entire packet into a glass. It has to be mixed with 8 ounces of water, fruit juice or soft drinks. This medicine should not be taken as powder in its dry form. The dose for chewable bars contain 80 calories per bar.

The cost of Colesevelam

In the USA, the consumer pay an average retail price of $191.49 for 60 tablets of 625mg.

How does Colesevelam Work?

Colesevelam belongs to class of medicines known as bile acid sequestrants. Colesevelam hydrochloride has several mechanism of action. In the treatment of Primary Hyperlipidemia, this lipid-lowering polymer binds bile acids in the intestine, impeding their reabsorption. With the reduction of the bile acid pool, the hepatic enzyme called cholesterol 7-α-hydroxylase, increases the cholesterol conversion into bile acids. The overall effect of this is an increased demand for cholesterol in the liver cells. This in turn results in the two benefits, first it increases transcription and activity of the cholesterol biosynthetic enzyme, HMG-CoA reductase, and second, in increasing the hepatic LDL receptors. The overall compensatory effects are felt in increased clearing of LDL-C from the blood. This finally results in lowering the serum LDL-C levels in blood. However, usage of this medicine may increase or maintain Serum TG levels. Its mechanism of action in treating Type 2 Diabetes Mellitus improves glycemic control but its exact actions are not known.

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