Which statins are most affected by grapefruit?

Which statins are most affected by grapefruit?

• A. Rosuvastatin only
• B. All statins equally
• C. Atorvastatin, simvastatin, and lovastatin
• D. Pravastatin and fluvastatin

Answer: (C)

Grapefruit juice can inhibit intestinal CYP3A4, the enzyme that metabolizes many statins. When this enzyme is blocked, the drugs that rely on CYP3A4 for their breakdown build up in the blood. Among statins, atorvastatin, simvastatin, and lovastatin are mainly processed by CYP3A4, so grapefruit can significantly raise their levels and increase the risk of muscle side effects like myopathy or rhabdomyolysis, especially at higher doses or with other risk factors. The other statins are less affected because they’re cleared mainly by other enzymes or pathways (pravastatin and fluvastatin by CYP2C9 and other routes, rosuvastatin largely by non-CYP pathways). So the statins most influenced by grapefruit are atorvastatin, simvastatin, and lovastatin. Clinical take-home: avoid grapefruit while taking these meds or monitor for symptoms if you choose to consume it.

Grapefruit juice can inhibit intestinal CYP3A4, the enzyme that metabolizes many statins. When this enzyme is blocked, the drugs that rely on CYP3A4 for their breakdown build up in the blood. Among statins, atorvastatin, simvastatin, and lovastatin are mainly processed by CYP3A4, so grapefruit can significantly raise their levels and increase the risk of muscle side effects like myopathy or rhabdomyolysis, especially at higher doses or with other risk factors. The other statins are less affected because they’re cleared mainly by other enzymes or pathways (pravastatin and fluvastatin by CYP2C9 and other routes, rosuvastatin largely by non-CYP pathways). So the statins most influenced by grapefruit are atorvastatin, simvastatin, and lovastatin. Clinical take-home: avoid grapefruit while taking these meds or monitor for symptoms if you choose to consume it.