Grapefruit Juice and Statins

Am J Med. 2016 Jan;129(1):26-9. doi: 10.1016/j.amjmed.2015.07.036. Epub 2015 Aug 20.

Abstract

We determined the validity of current medical advice to avoid grapefruit juice consumption while taking 3 widely used statins. A daily glass of grapefruit juice increases blood levels of simvastatin and lovastatin by about 260% if taken at the same time (about 90% if taken 12 hours apart), and atorvastatin by about 80% (whenever taken). Simvastatin 40 mg, lovastatin 40 mg, and atorvastatin 10 mg daily reduce low-density lipoprotein (LDL) cholesterol levels in a 60-year-old man with an LDL cholesterol of 4.8 mmol/L by 37%, reducing ischemic heart disease risk by 61%. When simvastatin or lovastatin are taken at the same time as grapefruit juice, the estimated reduction in LDL cholesterol is 48%, and in heart disease is 70%. If the juice is taken 12 hours before these statins, the reductions are, respectively, 43% and 66%, and for atorvastatin, 42% and 66%. The increased rhabdomyolysis risk from grapefruit juice consumption due to the increased effective statin dose is minimal compared with the greater effect in preventing heart disease. Grapefruit juice should not be contraindicated in people taking statins.

Keywords: Drug interaction; Effect enhancer; Grapefruit juice; Ischemic heart disease; LDL cholesterol; Statins.

Publication types

  • Review

MeSH terms

  • Anticholesteremic Agents* / pharmacokinetics
  • Anticholesteremic Agents* / therapeutic use
  • Beverages / adverse effects*
  • Cholesterol, LDL / blood
  • Citrus paradisi*
  • Contraindications
  • Drug Interactions
  • Heart Diseases / blood
  • Heart Diseases / prevention & control
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors* / pharmacokinetics
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors* / therapeutic use
  • Rhabdomyolysis / etiology
  • Risk Factors

Substances

  • Anticholesteremic Agents
  • Cholesterol, LDL
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors