title: Pharmacodynamic activity of lipoprotein lipase and hepatic lipase, and pharmacokinetic parameters measured in normolipidaemic subjects receiving ciprofibrate (100 or 200 mg/day) or micronised fenofibrate (200 mg/day) therapy for 23 days.
abstract: The activities of lipoprotein lipase (LPL) and hepatic lipase (HL) were investigated after 23 days of ciprofibrate (100 mg or 200 mg) therapy or fenofibrate (200 mg) therapy. In a double-blind, double-placebo, cross-over study, three groups of six healthy volunteers received either 100 mg ciprofibrate/day followed by 200 mg fenofibrate 'high bioavailability' (HB)/day, or vice versa (group A), 200 mg ciprofibrate HB/day followed by 200 mg fenofibrate HB/day, or vice versa (group B), or 100 mg ciprofibrate/day followed by 200 mg ciprofibrate/day, or vice versa (group C). Fasting plasma lipid levels and safety parameters were evaluated before and after treatment. One hundred milligrams ciprofibrate/day therapy was found to be approximately as effective as 200 mg fenofibrate HB/day therapy in altering the lipid profile. The highest activation of LPL was obtained after treatment with 200 mg ciprofibrate/day. A modest, but statistically significant, increase in HL activity was found after 100 or 200 mg ciprofibrate treatment. Investigation of the pharmacokinetics of ciprofibrate and fenofibric acid revealed a shorter time to reach peak plasma levels, but a longer elimination half life for the ciprofibrate preparations in comparison with fenofibrate. A dose of 200 mg ciprofibrate/day is more effective than 100 mg ciprofibrate/day at increasing LPL and HL activity; however, 200 mg ciprofibrate/day is also associated with a potential detrimental change in safety parameters. Two hundred milligrams fenofibrate HB/day therapy may represent an alternative therapy to 100 mg ciprofibrate/day for hyperlipidaemic patients.
authors.affiliation: Pharmacotherapy Laboratory, Catholic University of Louvain, Brussels, Belgium.
authors.forename: J P
authors.initials: JP
authors.lastname: Desager
authors.forename: Y
authors.initials: Y
authors.lastname: Horsmans
authors.forename: C
authors.initials: C
authors.lastname: Vandenplas
authors.forename: C
authors.initials: C
authors.lastname: Harvengt
mesh_terms: D000328:Adult; D002851:Chromatography, High Pressure Liquid; D002995:Clofibric Acid / Q000031:analogs & derivatives / Q000493:pharmacokinetics / Q000494:pharmacology; D018592:Cross-Over Studies; D004311:Double-Blind Method; D004797:Enzyme-Linked Immunosorbent Assay; D011345:Fenofibrate / Q000493:pharmacokinetics / Q000494:pharmacology; D058607:Fibric Acids; D006207:Half-Life; D006801:Humans; D000960:Hypolipidemic Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D008049:Lipase / Q000097:blood*; D008071:Lipoprotein Lipase / Q000097:blood*; D008099:Liver / Q000201:enzymology*; D008297:Male; D009391:Nephelometry and Turbidimetry; D012016:Reference Values
chemical_list: D058607:Fibric Acids; D000960:Hypolipidemic Agents; D002995:Clofibric Acid; D008049:Lipase; D008071:Lipoprotein Lipase; C019304:ciprofibrate; D011345:Fenofibrate