Effect of Statin Treatment on Plasma 4β‐Hydroxycholesterol Concentrations. Issue 6 (14th January 2016)

• Record Type: Journal Article
• Authors: Björkhem‐Bergman, Linda; Nylén, Hanna; Eriksson, Mats; Parini, Paolo; Diczfalusy, Ulf
• Is Part Of: Basic & clinical pharmacology & toxicology. Volume 118:Issue 6(2016)
• Page Start: 499
• Page End: 502
• Publication Date: 2016-01-14
• Subjects: Pharmacology -- Periodicals; Toxicology -- Periodicals; Pharmacology -- Periodicals; Toxicology -- Periodicals; Pharmacology, Clinical -- Periodicals; Computer network resources; Electronic journals; 615.1
• DOI: 10.1111/bcpt.12537
• Languages: English
• ISSNs: 1742-7835

Abstract

Abstract: The endogenous oxysterol 4β‐hydroxycholesterol may be used as a marker for the drug‐metabolizing enzymes cytochrome P450 3A (CYP3A). 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 CYP3A 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.