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Effects of colesevelam HC1 on sterol and bile acid excretion in patients with type IIa hypercholesterolemia.

Abstract
Colesevelam HC1 is a potent bile acid-binding polymer. This study's aim was to determine effects of colesevelam HCl on sterol and bile acid excretion in patients with type IIa hypercholesterolemia. Twenty-four patients (low-density lipoprotein cholesterol, 130 to 220 mg/dL) enrolled in an open-label, parallel-design study, entered an American Heart Association/National Cholesterol Education Program diet for 6 weeks and were randomized to colesevelam HCl, 2.3 or 3.8 g/day for 4 weeks. In an apparent dose-related manner, respective mean serum concentrations HCl of low-density lipoprotein cholesterol decreased by 10% (P < 0.01) and 13% (P = 0.05), mean total cholesterol levels decreased by 4.9% (P = 0.05) and 6.1% (P = 0.09), and total fecal bile acid excretion showed median changes of +324% (P < 0.05) and +316% (P < 0.05). Colesevelam HCl did not affect fecal neutral sterol or fecal fatty acid excretion; however, 24-hr urinary mevalonic acid levels significantly increased in both treatment groups (P < 0.05). The cholesterol-lowering action of colesevelam HCl appears to be mediated through increased bile acid excretion.
AuthorsJ M Donovan, K Von Bergmann, K D R Setchell, J Isaacsohn, A S Pappu, D R Illingworth, T Olson, S K Burke
JournalDigestive diseases and sciences (Dig Dis Sci) Vol. 50 Issue 7 Pg. 1232-8 (Jul 2005) ISSN: 0163-2116 [Print] United States
PMID16047465 (Publication Type: Clinical Trial, Journal Article, Randomized Controlled Trial, Research Support, Non-U.S. Gov't)
Chemical References
  • Bile Acids and Salts
  • Cholesterol, LDL
  • Sterols
  • Allylamine
  • Cholesterol
  • Colesevelam Hydrochloride
Topics
  • Allylamine (administration & dosage, adverse effects, analogs & derivatives, therapeutic use)
  • Bile Acids and Salts (metabolism)
  • Cholesterol (blood)
  • Cholesterol, LDL (blood)
  • Colesevelam Hydrochloride
  • Dose-Response Relationship, Drug
  • Feces (chemistry)
  • Female
  • Humans
  • Hypercholesterolemia (drug therapy, metabolism)
  • Male
  • Middle Aged
  • Sterols (metabolism)
  • Treatment Outcome

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