Efficacy and safety of coadministration of rosuvastatin, ezetimibe, and colestimide in heterozygous familial hypercholesterolemia.

Abstract

Aggressive low-density lipoprotein (LDL) cholesterol-lowering therapy is important for high-risk patients. However, sparse data exist on the impact of combined aggressive LDL cholesterol-lowering therapy in familial hypercholesterolemia (FH), particularly on side effects to changes in plasma coenzyme Q10 and proprotein convertase subtilisin/kexin type 9 levels. We enrolled 17 Japanese patients with heterozygous FH (12 men, 63.9 ± 7.4 years old) with single LDL receptor gene mutations in a prospective open randomized study. Permitted maximum doses of rosuvastatin (20 mg/day), ezetimibe (10 mg/day), and granulated colestimide (3.62 g/day) were introduced sequentially. Serum levels of LDL cholesterol decreased significantly by -66.4% (p <0.001) and 44% of participants achieved LDL cholesterol levels <100 mg/dl. There were no serious side effects or abnormal laboratory data that would have required the protocol to have been terminated except for 1 patient with myalgia. Coadministration of ezetimibe and granulated colestimide further lowered serum LDL cholesterol more than rosuvastatin alone without changing plasma coenzyme Q10 and proprotein convertase subtilisin/kexin type 9 levels. In conclusion, adequate introduction of this aggressive cholesterol-lowering regimen can improve the lipid profile of FH.

• Authors: Masa-Aki Kawashiri, Atsushi Nohara, Tohru Noguchi, Hayato Tada, Chiaki Nakanishi, Mika Mori, Tetsuo Konno, Kenshi Hayashi, Noboru Fujino, Akihiro Inazu, Junji Kobayashi, Hiroshi Mabuchi, Masakazu Yamagishi
• Journal: The American journal of cardiology (Am J Cardiol) Vol. 109 Issue 3 Pg. 364-9 (Feb 01 2012) ISSN: 1879-1913 [Electronic] United States
• PMID: 22112743 (Publication Type: Comparative Study, Journal Article, Randomized Controlled Trial)
• Copyright: Copyright © 2012 Elsevier Inc. All rights reserved.

Chemical References

• Anion Exchange Resins
• Anticholesteremic Agents
• Azetidines
• Cholesterol, LDL
• Fluorobenzenes
• Hydroxymethylglutaryl-CoA Reductase Inhibitors
• Imidazoles
• Pyrimidines
• Resins, Synthetic
• Sulfonamides
• colestimide
• Epichlorohydrin
• Rosuvastatin Calcium
• Ezetimibe

Topics

• Aged
• Aged, 80 and over
• Anion Exchange Resins
• Anticholesteremic Agents (administration & dosage)
• Azetidines (administration & dosage)
• Cholesterol, LDL (blood, drug effects)
• Dose-Response Relationship, Drug
• Drug Therapy, Combination
• Epichlorohydrin (administration & dosage)
• Ezetimibe
• Female
• Fluorobenzenes (administration & dosage)
• Follow-Up Studies
• Heterozygote
• Humans
• Hydroxymethylglutaryl-CoA Reductase Inhibitors (administration & dosage)
• Hyperlipoproteinemia Type II (blood, drug therapy, genetics)
• Imidazoles (administration & dosage)
• Male
• Middle Aged
• Prospective Studies
• Pyrimidines (administration & dosage)
• Resins, Synthetic (administration & dosage)
• Rosuvastatin Calcium
• Sulfonamides (administration & dosage)
• Treatment Outcome