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Comparative Hepatic and Intestinal Metabolism and Pharmacodynamics of Statins by Anne M. Filppula; Päivi Hirvensalo; Heli Parviainen; Vilma E. Ivaska; K. Ivar Lönnberg; Feng Deng; Jenni Viinamäki; Mika Kurkela; Mikko Neuvonen; Mikko Niemi is a Medicine article available to read on EtoBox.
What is Comparative Hepatic and Intestinal Metabolism and Pharmacodynamics of Statins about?
This study aimed to comprehensively investigate the in vitro metabolism of statins. The metabolism of clinically relevant concentrations of atorvastatin, fluvastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, and their metabolites were investigated using human liver microsomes (HLMs), human intestine microsomes (HIMs), liver cytosol, and recombinant cytochrome P450 enzymes. We also determined the inhibitory effects of statin acids on their pharmacological target, 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. In HLMs, statin lactones were metabolized to a much higher extent than their acid forms. Atorvastatin lactone and simvastatin (lactone) showed extensive metabolism [intrinsic clearance (CL) values of 3700 and 7400 μl/min per milligram], whereas the metabolism of the lactones of 2-hydroxyatorvastatin, 4-hydroxyatorvastatin, and pitavastatin was slower (CL 20-840 μl/min per milligram). The acids had CL values in the range <0.1-80 μl/min per milligram. In HIMs, only atorvastatin lactone and simvastatin (lactone) exhibited notable metabolism, with CL values corresponding to 20% of those observed in HLMs. CYP3A4/5 and CYP2C9 were the main statin-metabolizing
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- Author
- Anne M. Filppula; Päivi Hirvensalo; Heli Parviainen; Vilma E. Ivaska; K. Ivar Lönnberg; Feng Deng; Jenni Viinamäki; Mika Kurkela; Mikko Neuvonen; Mikko Niemi
- Publisher
- American Society for Pharmacology & Experimental Therapeutics (ASPET)
- Published
- 2021
- Language
- EN
- Field
- Medicine (Life Sciences)