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Statins

Last updated: April 28, 2021

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Statins are the lipid-lowering drugs of choice. Statins reduce hepatic cholesterol synthesis by inhibiting enzyme HMG-CoA reductase. This leads to a consequent upregulation of LDL receptors on hepatocytes, which, in turn, lowers LDL cholesterol levels and triglycerides while raising HDL cholesterol. Headache and gastrointestinal side-effects are common. Statins carry a risk of hepatic and muscle toxicity. Muscle toxicity may rarely manifest with rhabdomyolysis.

For a comparison of statins with other lipid-lowering agents, see “Overview of lipid metabolism and lipid-lowering agents.”

Overview of statin pharmacokinetics
Statin Half-life in hours CYP-450 Bioavailability [1]
Atorvastatin 15–30 CYP3A4 ∼ 10%
Simvastatin 2–3 CYP3A4, CYP3A5 ∼ 5%
Pravastatin ∼ 2 - ∼ 20%
Lovastatin 3 CYP3A4 ∼ 5%
Fluvastatin 0.5–2.5 CYP2C9 ∼20–30%
Pitavastatin 12 Limited CYP2C9 ∼ 50%
Rosuvastatin 19 Limited CYP2C9 ∼ 20%

Flo Loves Prague Since A Tour of Russia.” Lipid-lowering potency increases in the following order: Fluvastatin → Lovastatin → Pravastatin → Simvastatin → Atorvastatin → Rosuvastatin

  • General (common): headache and gastrointestinal symptoms (e.g., constipation, diarrhea, flatulence)
  • Hepatic: (up to 3% of patients) LFTs due to the involvement of cytochrome P450 systems (CYP3A4 and CYP2C9) in the breakdown of statins [3][4]
  • Muscular: Statins decrease the synthesis of coenzyme Q10 and impair energy production within the muscle.
    • Myalgia (muscle pain): continue treatment as long as creatinine phosphokinase (CK) remain normal
    • Statin-associated myopathy

Treatment must be discontinued if myopathy/rhabdomyolysis occurs.

Interaction with certain drugs can increase the risk of myopathy (see “Interactions” section below).

We list the most important adverse effects. The selection is not exhaustive.

For details, see therapy of atherosclerotic disease and guidelines for lipid-lowering therapy (ATP III guidelines)

Statins are the first-line therapy for hypercholesterolemia.

Treatment of hyperlipidemia with statins significantly reduces the risk of mortality in patients suffering from CAD.

We list the most important contraindications. The selection is not exhaustive.

Maintain a high index of suspicion for rhabdomyolysis if muscle pain occurs after administering statins.

  • Ideally administered in the evenings (especially simvastatin)
  • Combination therapy with bile acid resins has a stronger hypolipidemic effect compared to treatment with statins alone; (both groups of drugs increase LDL receptor expression)
  1. Whitfield LR, Stern RH, Sedman AJ, Abel R, Gibson DM. Effect of food on the pharmacodynamics and pharmacokinetics of atorvastatin, an inhibitor of HMG-CoA reductase.. Eur J Drug Metab Pharmacokinet.. 2000; 25 (2): p.97-101.
  2. McTaggart F, Jones P. Effects of Statins on High-Density Lipoproteins: A Potential Contribution to Cardiovascular Benefit. Cardiovasc Drugs Ther. 2008; 22 (4): p.321-338. doi: 10.1007/s10557-008-6113-z . | Open in Read by QxMD
  3. Onusko E. Statins and elevated liver tests: what's the fuss?. J Fam Pract. 2008; 57 (7): p.449-452.
  4. Chang CY, Schiano TD. Review article: drug hepatotoxicity. Aliment Pharmacol Ther. 2007; 25 (10): p.1135-1151. doi: 10.1111/j.1365-2036.2007.03307.x . | Open in Read by QxMD
  5. Statin Use for the Primary Prevention of Cardiovascular Disease in Adults: Preventive Medication. https://www.uspreventiveservicestaskforce.org/uspstf/recommendation/statin-use-in-adults-preventive-medication. Updated: November 16, 2016. Accessed: February 4, 2021.
  6. Stone NJ, Robinson JG, Lichtenstein AH et al. 2013 ACC/AHA Guideline on the Treatment of Blood Cholesterol to Reduce Atherosclerotic Cardiovascular Risk in Adults. Journal of the American College of Cardiology. 2014; 63 (25). doi: 10.1016/j.jacc.2013.11.002 . | Open in Read by QxMD
  7. Herold G. Internal Medicine. Herold G ; 2014
  8. Kasper DL, Fauci AS, Hauser SL, Longo DL, Lameson JL, Loscalzo J. Harrison's Principles of Internal Medicine. McGraw-Hill Education ; 2015