Colesevelam
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| Colesevelam substructures | |||||||||
| General | |||||||||
| Surname | Colesevelam | ||||||||
| CAS number | 182815-43-6 | ||||||||
| Monomers / partial structures | Allylamine , epichlorohydrin , N -allyldecylamine , N , N , N -trimethyl-6- (2-propenylamino) -1-hexanaminium chloride | ||||||||
| ATC code | |||||||||
| DrugBank | DB00930 | ||||||||
| Drug information | |||||||||
| Drug class |
Lipid lowering agents , bile acids - complexing agents |
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| Mechanism of action |
Absorption of bile acids |
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| properties | |||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||
Colesevelam (trade name Cholestagel ) is an ion exchanger from Genzyme that forms salts with the anions of bile acids, thus acting as a bile acid binder and thus also inhibiting the absorption of cholesterol . Colesevelam is used for hypercholesterolemia ; for which indication it has been approved for adults in the EU since March 2004; it is used either as the only active ingredient or together with a statin or in combination with ezetimibe , with or without a statin. As an alternative to statin therapy - e.g. B. in statin intolerance - both ezetimibe and colesevelam are possible.
pharmacology
Pharmacokinetics
Colesevelam is not absorbed from the gastrointestinal tract .
Pharmacodynamics
Colesevelam binds bile acids, u. a. Glycocholic acid, the most important bile acid in humans. Cholesterol is the only precursor to bile acids. During normal digestion , bile acids are secreted into the intestines. A large part of the bile acids is then reabsorbed by 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, imprinted with “Cholestagel” on one side.
application areas
Colesevelam, in combination with an HMG-CoA reductase inhibitor ( statin ), is indicated as an adjuvant to diet in order to achieve an additional reduction in LDL cholesterol levels in patients with primary hypercholesterolemia for whom a statin alone cannot adequately control.
Colesevelam as monotherapy is indicated in patients with isolated primary hypercholesterolemia for the lowering of elevated total and LDL cholesterol levels as an adjuvant to diet when a statin is considered inappropriate or not well tolerated.
Colesevelam is newly approved for use in combination with ezetimibe, with or without a statin, in adult patients with primary hypercholesterolemia, including patients with familial hypercholesterolemia.
Contraindications
Hypersensitivity to the active ingredient or to any of the other ingredients; Intestinal obstruction or obstruction of the bile duct.
Side effects
In controlled clinical studies involving approximately 1,400 patients, the following adverse drug reactions were reported in patients treated with colesevelam. The reporting is based on very common (≥ 1/10), common (≥ 1/100, 51/10), uncommon (≥ 1/1000, 51/100), rare (≥ 1 / 10,000, 51/1000) and very rarely (51 / 10,000) differentiated including individual cases:
Investigations Common: triglycerides in the blood serum increases; Uncommon: increased serum transaminases
Nervous system disorders Common: headache
Gastrointestinal disorders Very common: flatulence , constipation ; Common: vomiting , diarrhea , dyspepsia , abdominal pain , stool abnormalities, nausea
Musculoskeletal, connective tissue and bone disorders Uncommon: myalgia
The background incidence of flatulence and diarrhea was higher in patients receiving placebo in the same controlled clinical trials . Only constipation and dyspepsia were reported by a higher percentage of patients who received Cholestagel compared to placebo. The side effects were usually mild or moderate.
When colesevelam was used in combination with statins, there were no unexpected common side effects compared to statins alone.
Trade names
Cholestagel (In the US: WelChol)
Web links
- Entries in the NIH study register
- Public Assessment Report (EPAR) from the European Medicines Agency (EMA) on: Colesevelam
Individual evidence
- ↑ Thomas L. Lemke, David A. Williams: Foye's Principles of Medicinal Chemistry . Lippincott Williams & Wilkins, 2012, ISBN 1-60913-345-5 , pp. 824 ( limited preview in Google Book search).
- ↑ a b Entry on Colesevelam. In: Römpp Online . Georg Thieme Verlag, accessed on June 29, 2019.
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ Klose G. Statin intolerance: diagnosis, significance and consequences Perfusion 2009,3: 104-105
- ↑ a b c d e f g Summary of the characteristics of the drug Cholestagel (PDF; 82 kB) genzyme.de. Retrieved on July 5, 2012. ( Memento of March 6, 2012 in the Internet Archive )
- ↑ Drugs Commission of the German Medical Association (AkdÄ) (PDF; 61 kB).
