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Effect of Statin Treatment on Plasma 4β‐Hydroxycholesterol Concentrations
Author(s) -
BjörkhemBergman Linda,
Nylén Hanna,
Eriksson Mats,
Parini Paolo,
Diczfalusy Ulf
Publication year - 2016
Publication title -
basic and clinical pharmacology and toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.805
H-Index - 90
eISSN - 1742-7843
pISSN - 1742-7835
DOI - 10.1111/bcpt.12537
Subject(s) - fluvastatin , atorvastatin , placebo , medicine , oxysterol , cholesterol , statin , endocrinology , hmg coa reductase , pharmacology , cytochrome p450 , endogeny , chemistry , metabolism , enzyme , reductase , biochemistry , alternative medicine , pathology , simvastatin
The endogenous oxysterol 4β‐hydroxycholesterol may be used as a marker for the drug‐metabolizing enzymes cytochrome P450 3A ( CYP 3A). The primary aim of this study was to investigate the effect of statin treatment on plasma 4β‐hydroxycholesterol concentrations. Plasma samples from a previously performed clinical study where gallstone patients had been treated with placebo (n = 6), 20 mg fluvastatin (n = 9) or 80 mg atorvastatin (n = 9) daily for 4 weeks were analysed. Hepatic CYP 3A mRNA levels had previously been shown to be unchanged in all three treatment groups. Plasma 4β‐hydroxycholesterol did not change significantly ( p = 0.92) in the placebo group, but treatment with low‐dose fluvastatin or high‐dose atorvastatin resulted in reductions in plasma concentration of 10.7% ( p < 0.05) and 36.5% ( p < 0.01), respectively. However, the 4β‐hydroxycholesterol/cholesterol ratio did not change significantly for the patients receiving placebo or patients receiving low‐dose fluvastatin. The ratio for patients receiving high‐dose atorvastatin increased by 12% ( p < 0.05). In conclusion, the total plasma cholesterol level is an important determinant for the plasma 4β‐hydroxycholesterol level.