Statins (Dosage and risk of myopathy)

Statins are the most widely used drugs for the treatment of hypercholesterolemia. Myopathy is a side effect associated with the use of these drugs and its occurrence has been related to polymorphic variants of the SLCO1B1 gene, a gene that codes for a hepatic transporter of certain drugs.

Simvastatin (Zocor®) belongs to a class of cholesterol-lowering medicines called statins that when used together with a heart healthy .diet and exercise, reduce the risk of heart attack, stroke and death from heart diseases. Simvastatin is one of the most commonly prescribed statins. Although statins are effective and generally safe, some persons who take them experience myopathy, a condition that causes muscular weakness, pain and cramps. Myopathy can affect 5 -10% of those who take statins.

Although all statins can cause myopathy, simvastatin, especially in high doses, is the one that most probably causes it. Many genetic and non-genetic factors can affect the myopathy generated by statins. The most studied is the genetic variant on the gene SLCO1B1 that is linked to myopathy on taking simvastatin. SLCO1B1 encodes a protein that helps the liver absorb statins. When this protein does not function adequately, the simvastatin levels in the blood and muscle tissue can become very high.

Risk factors such as age, gender, ethnicity, body mass index, other health conditions and medicines that are taken at the same time can affect how a person responds to simvastatin.


BRAND NAMES

  • Zocor®
  • Lipitor®
  • Baycol®
  • Lipobay®

Genes analyzed

SLCO1B1

Bibliography

Cooper-DeHoff RM, Niemi M, Ramsey LB, et al. The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 genotypes and Statin-Associated Musculoskeletal Symptoms. Clin Pharmacol Ther. 2022 May;111(5):1007-1021.

Patel J, Superko HR, Martin SS, et al. Genetic and immunologic susceptibility to statin-related myopathy. Atherosclerosis. 2015 May;240(1):260-71.

Postmus I, Trompet S, Deshmukh HA, et al. Pharmacogenetic meta-analysis of genome-wide association studies of LDL cholesterol response to statins. Nat Commun. 2014 Oct 28;5:5068.

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