title: 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: Division of Cardiovascular Medicine, Kanazawa University Graduate School of Medicine, Kanazawa University, Kanazawa, Japan. mk@med.kanazawa-u.ac.jp
authors: Masa-Aki
authors: MA
authors: Kawashiri
authors: Atsushi
authors: A
authors: Nohara
authors: Tohru
authors: T
authors: Noguchi
authors: Hayato
authors: H
authors: Tada
authors: Chiaki
authors: C
authors: Nakanishi
authors: Mika
authors: M
authors: Mori
authors: Tetsuo
authors: T
authors: Konno
authors: Kenshi
authors: K
authors: Hayashi
authors: Noboru
authors: N
authors: Fujino
authors: Akihiro
authors: A
authors: Inazu
authors: Junji
authors: J
authors: Kobayashi
authors: Hiroshi
authors: H
authors: Mabuchi
authors: Masakazu
authors: M
authors: Yamagishi
mesh_terms: D000368:Aged; D000369:Aged, 80 and over; D000837:Anion Exchange Resins; D000924:Anticholesteremic Agents / Q000008:administration & dosage; D001384:Azetidines / Q000008:administration & dosage*; D008078:Cholesterol, LDL / Q000097:blood* / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004359:Drug Therapy, Combination; D004811:Epichlorohydrin / Q000008:administration & dosage*; D000069438:Ezetimibe; D005260:Female; D005464:Fluorobenzenes / Q000008:administration & dosage*; D005500:Follow-Up Studies; D006579:Heterozygote; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000008:administration & dosage; D006938:Hyperlipoproteinemia Type II / Q000097:blood / Q000188:drug therapy* / Q000235:genetics; D007093:Imidazoles / Q000008:administration & dosage*; D008297:Male; D008875:Middle Aged; D011446:Prospective Studies; D011743:Pyrimidines / Q000008:administration & dosage*; D012117:Resins, Synthetic / Q000008:administration & dosage*; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides / Q000008:administration & dosage*; D016896:Treatment Outcome
chemical_list: D000837:Anion Exchange Resins; D000924:Anticholesteremic Agents; D001384:Azetidines; D008078:Cholesterol, LDL; D005464:Fluorobenzenes; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D007093:Imidazoles; D011743:Pyrimidines; D012117:Resins, Synthetic; D013449:Sulfonamides; C417427:colestimide; D004811:Epichlorohydrin; D000068718:Rosuvastatin Calcium; D000069438:Ezetimibe