Colesevelam

C10AC04

Lipid-lowering agents, bile acid sequestrants

Absorption of bile acids

Colesevelam (trade name Cholestagel ®) is a bile acid binder and thus an absorption inhibitors for cholesterol Genzyme. It is used in hypercholesterolemia, either as the sole active ingredient or in combination with a statin or in combination with ezetimibe, with or without a statin. As an alternative to statin therapy - for example, with statin intolerance - are both ezetimibe and colesevelam in question.

Pharmacology

Pharmacokinetics

Colesevelam is not absorbed from the gastrointestinal tract.

Pharmacodynamics

Colesevelam binds bile acids, among others, Glycocholic, the major bile acid in humans. Cholesterol is the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestine. A major portion of bile acids is then absorbed from the intestinal tract and transported back to the liver via the enterohepatic circulation.

Dosage form

Film-coated tablet ( tablet). Off-white capsule-shaped, film-coated tablets printed on one side with " Cholestagel ".

Areas of application

Colesevelam in combination with an HMG -CoA reductase inhibitor ( statin ) adjuvant indexed to diet in order to achieve an additional reduction of LDL - cholesterol in patients with primary hypercholesterolemia in those with a statin alone do not adequately controlled.

Colesevelam as monotherapy is indicated for patients with isolated primary hypercholesterolaemia for the reduction of elevated total and LDL cholesterol levels adjuvant to diet, when a statin is considered inappropriate or not tolerated.

Colesevelam is newly approved for use in combination with ezetimibe, with or without a statin, in adult patients with primary hypercholesterolaemia, including patients with familial hypercholesterolemia.

Contraindications

Hypersensitivity to the active substance or to any of the excipients; Bowel or biliary obstruction.

Side effects

In controlled clinical trials involving approximately 1400 patients, the following adverse reactions were reported in patients treated with colesevelam. When reporting is by very common ( ≥ 1/10 ), common ( ≥ 1/100, 51/ 10), uncommon ( ≥ 1/1000, 51/ 100), rare ( ≥ 1/10.000, 51/ 1000) and very rare ( 51/10.000 ) including isolated cases are distinguished:

Investigations Common: triglycerides in the blood serum increased; Uncommon: increased transaminases in blood serum

Nervous system disorders Common: headache

Gastrointestinal disorders Very common: flatulence, constipation; Common: Vomiting, diarrhea, dyspepsia, abdominal pain, stool abnormalities, nausea

Musculoskeletal and connective tissue disorders Uncommon: Myalgia

The background incidence of flatulence and diarrhea was higher in patients who received placebo in the same controlled clinical trials, higher. Only constipation and dyspepsia were of a higher percentage of patients receiving Cholestagel reported compared to placebo. The side effects were generally mild or moderate.

In the application of colesevelam in combination with statins, it came to treatment with statins alone is not unexpected frequent side effects.

Trade names

Cholestagel ( In the U.S.: WelChol )