Grapefruit and Statin: interaction, severity and spacing
Grapefruit and Statin interact because grapefruit furanocoumarins irreversibly inhibit intestinal CYP3A4, which sharply raises blood levels of simvastatin and atorvastatin and increases rhabdomyolysis risk. Take them with care. Severe risk.
The interaction in detail
| Pair | Grapefruit and Statin |
|---|---|
| Type | Food interaction |
| Severity | Severe |
| Required spacing | None specified |
| Onset | At the time of dosing |
Mechanism
Grapefruit furanocoumarins irreversibly inhibit intestinal CYP3A4, which sharply raises blood levels of simvastatin and atorvastatin and increases rhabdomyolysis risk.
What to do
Avoid grapefruit and grapefruit juice with simvastatin or atorvastatin. Rosuvastatin and pravastatin are not CYP3A4 substrates.
How to fit both into one day
Cholesterol synthesis peaks overnight, so most statins are dosed in the evening. Avoid grapefruit, which raises drug levels.
Putting Grapefruit in the morning and Statin in the evening satisfies the 0-hour separation without disrupting either one's absorption window.