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HMG-CoA Reductase Inhibitors (Statins) and their Drug Interactions Involving CYP Enzymes, P-glycoprotein and OATP Transporters-An Overview

[ Vol. 22 , Issue. 5 ]


Rajkapoor Balasubramanian* and Naina M.P. Maideen   Pages 328 - 341 ( 14 )


Background: Hydroxymethyl glutaryl-CoA (HMG-CoA) reductase inhibitors (Statins) are used to treat dyslipidemia. Generally, the statins are the substrates of CYP enzymes, P-glycoprotein (P-gp), and organic anion transporting polypeptides transporters (OATP1B1).

Objective: This review article focuses on the clinical significance of statins, and their interactions in real practice.

Methods: The databases like Medline/PubMed Central/PubMed, Google Scholar, Science Direct, Cochrane Library, Directory of open access journals (DOAJ), and reference lists were searched to identify relevant articles.

Results: Most of the drug interactions of statins result in elevated plasma concentrations and toxicity of statins due to the inhibition of CYP3A4, P-gp and/or OATP1B1 transporters. The toxicity of statins includes myopathy, rhabdomyolysis, elevated liver enzymes, acute kidney injury, and diabetes. The statins like simvastatin, lovastatin, and atorvastatin are substrates of CYP3A4 enzyme and P-glycoprotein and their concomitant use with the drugs inhibiting or inducing them would result in changes in plasma concentrations and toxicity/efficacy. However, the statins like pravastatin, rosuvastatin and pitavastatin are not substrates of CYP enzymes and hence the concomitant use of CYP inhibitors or inducers does not affect them. Almost all the statins are the substrates of OATP1B1 transporter, and the co-prescription of inhibitors of OATP1B1 elevates the plasma concentrations and muscle toxicity of statins.

Conclusion: Understanding the interacting potential of each statin will enable the prescribers, pharmacists, and other health care professionals to use statins effectively without compromising patient safety.


Drug interactions, statin, HMG-CoA reductase inhibitors, CYP3A4, P-glycoprotein, OATP1B1 transporter.


Department of Pharmacology, J.K.K. Nattraja College of Pharmacy, Komarapalayam 638 183, Dubai Health Authority, P.O. Box: 4545, Dubai

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