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Colesevelam

Trade name Welchol

A non-systemic agent as it is not absorbed and not metabolised.

Excreted by intestines.

A bile acid sequestrant administered orally.

Indicated as an adjunct to diet and exercise to reduce elevated low-density lipoprotein cholesterol (LDL-C) in patients with primary hyperlipidemia as monotherapy and to improve glycemic control in adults with type 2 diabetes mellitus.

Indicated as adjunct to diet and exercise to reduce elevated low density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia. (Tyoe IIa) as monotherapy or in combination ith a HMG CoA reductase inhibitor, a statin.

Indicated as monotherapy or in combination with a statin for boys and girls 10-17 with heterozygous familial hypercholesterolemia if diet therapy failed, and a positive family history of premature CV disease exists, otr the patient has 2 or more other CV risk factors.

Second line agent to statins.

Side effects bloating and constipation.

The active ingredient is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine.

As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-α-hydroxylase, is upregulated, increasing the conversion of cholesterol to bile acids.

Increased demand for cholesterol in liver cells, results in increasing transcription and activity of the cholesterol biosynthetic enzyme, HMG-CoA reductase, and increases the number of hepatic LDL receptors: resulting in increased clearance of LDL-C from the blood, and decreased serum LDL-C levels.

Serum TG levels may increase or remain unchanged.

Can lower total and LDL cholesterol levels and raising HDL.

Taking 3,800 mg to 4,500 mg of colesevelam daily can reduce LDL cholesterol by 15 to 18 percent, reduce total cholesterol by 7 to 10 percent, and raise HDL cholesterol by 3 percent.

The combination of colesevelam with a HMG-CoA reductase inhibitor can further lower cholesterol levels.

Use contraindicated in patients with history of bowel obstruction.

Use contraindicated with seum triglyceride concentrations above 500 mg/dL.

A bile acid sequestrant an can increase triglyceride levels.

May decrease absorption of fat soluble vitamins A,D,E, and K.

Reduces liver glucose production and increases incretin levels improving diabetes.

Has constipating effects and is not recommended with gastrointestial motility disorders.

Reduces gastrointestinal absorption of some drugs, and should be administered at least 4 hours prior to colesevam.

Commonly associated with constipation, dyspepsia, nausea, and asthenia.

Reduces high cholesterol levels.

It may be used alone or with other medicines.

Also used along with diet and exercise to control blood sugar in patients with type 2 diabetes.

Should not be used to treat type 1 diabetes or diabetic ketoacidosis.

A bile acid sequestrant.

Works in the bowel to help remove bile acids from the body.

The body then uses cholesterol to make more bile acids, which causes blood cholesterol levels to decrease.

How it works to treat type 2 diabetes is not known.

Birth control pills, cyclosporine, glimepiride, glipizide, glyburide, hydantoins, olmesartan, thyroid hormones or vitamins should be taken at least 4 hours before colesevelam

May cause constipation.

May decrease the absorption of certain other medicines.

Used with extreme caution in those younger than 10 years old or in girls who have not had their first menstrual period; safety and effectiveness in these children have not been confirmed.

Back pain; constipation; headache; indigestion; mild stomach pain; muscle aches or pain; nausea; sore throat; stomach upset; stuffy or runny nose; tiredness; weakness.

The recommended dose in adults, whether used as monotherapy or in combination with a statin, is 6 tablets once daily or 3 tablets twice daily.

Tablets should be taken with a meal and liquid.

The recommended dose for oral suspension, in adults and children 10 to 17 years of age, is one 3.75 gram packet once daily or one 1.875 gram packet twice daily.

The recommended dose for Type 2 Diabetes Mellitus is 6 tablets once daily or 3 tablets twice daily.

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