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.