Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz

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Fauler, G; Abletshauser, C; Erwa, W; Löser, R; Witschital, K; März, W.
Time-of-intake (morning versus evening) of extended-release fluvastatin in hyperlipemic patients is without influence on the pharmacodynamics (mevalonic acid excretion) and pharmacokinetics.
Int J Clin Pharmacol Ther. 2007; 45(6):328-334 Doi: 10.5414/CPP45328
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Führende Autor*innen der Med Uni Graz: Fauler Günter
Co-Autor*innen der Med Uni Graz: Erwa Wolfgang; März Winfried
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Abstract:: Statins inhibit the rate-limiting step in cholesterol biosynthesis, the conversion of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) to mevalonate by HMG-CoA reductase. Statins are usually taken in the evening as the HMG-CoA reductase activity is high during the night. This recommendation might not apply if statins are given as extended-release (ER) formulations. The present study investigated the influence of time of intake of fluvastatin 80 mg ER on cholesterol biosynthesis. Main objectives were to measure the change in 24-hour urinary mevalonic acid excretion, to determine plasma concentrations of mevalonic acid and fluvastatin and to monitor triglycerides, total cholesterol, HDL-cholesterol and LDL-cholesterol. This was a randomized, 2-period crossover study in 26 hypercholesterolemic patients who received a single daily dose of fluvastatin both in the morning and in the evening. At baseline, the amount of mevalonic acid was 204.9 +/- 68.1 microg/g creatinine. After a single dose of fluvastatin mean urine values of mevalonate were significantly reduced to 129.8 +/- 66.2 micro/g (evening) and to 118.7 +/-34.3 microg/g (morning; n.s. between groups), thus representing a reduction of about 39%. Compared to baseline, plasma mevalonate concentrations were decreased by fluvastatin resulting in similar 24-hour profiles after the morning and the evening dosage. The pharmacokinetics of fluvastatin were similar in both periods of the study, with higher plasma concentrations for several hours following the evening dosage. This study demonstrates that fluvastatin ER is equally effective in inhibiting cholesterol biosynthesis when given once daily in the morning and once daily in the evening.
Find related publications in this database (using NLM MeSH Indexing): Adult -; Biomarkers -; Cholesterol - metabolism; Cholesterol, HDL - blood; Cholesterol, LDL - blood; Cross-Over Studies -; Delayed-Action Preparations -; Fatty Acids, Monounsaturated - administration & dosage Fatty Acids, Monounsaturated - pharmacokinetics Fatty Acids, Monounsaturated - therapeutic use; Female -; Humans -; Hydroxymethylglutaryl-CoA Reductase Inhibitors - administration & dosage Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacokinetics Hydroxymethylglutaryl-CoA Reductase Inhibitors - therapeutic use; Hyperlipidemias - blood Hyperlipidemias - drug therapy Hyperlipidemias - urine; Indoles - administration & dosage Indoles - pharmacokinetics Indoles - therapeutic use; Male -; Mevalonic Acid - blood Mevalonic Acid - urine; Middle Aged -; Time Factors -; Triglycerides - blood
Find related publications in this database (Keywords): fluvastatin 80 mg extended-release formulation; morning versus evening dosing; mevalonic acid; pharmacokinetics of fluvastatin