Medication · Medication

Grapefruit

Not a drug — a food, but a potent and long-lasting inhibitor of the CYP3A4 enzyme in the gut, which is why it has a drug-like interaction profile.

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A medication reference built from the interaction graph. It is not prescribing information — the label and your prescriber are.

What is uncertain

Read off the same rows as above. Nothing here is added that the entry does not itself record.

  • Caution with Rapamycin (Sirolimus): CYP3A4 inhibition raises rapamycin levels substantially.
  • Caution with Statins: Grapefruit inhibits CYP3A4, raising levels of simvastatin/atorvastatin and the risk of muscle toxicity.
  • Caution with Immunosuppressants: Grapefruit sharply raises cyclosporine/tacrolimus levels — a classic dangerous food-drug interaction.
  • Caution with Benzodiazepines: Grapefruit raises levels of some benzodiazepines, deepening sedation.
  • Caution with BP meds: Grapefruit raises several calcium-channel-blocker levels, exaggerating blood-pressure drops.

Interactions

Documented pairings with supplements and medicines. A medicine on this list is a conversation for whoever prescribes it.

  • Rapamycin (Sirolimus)Caution

    CYP3A4 inhibition raises rapamycin levels substantially.

  • StatinsCaution

    Grapefruit inhibits CYP3A4, raising levels of simvastatin/atorvastatin and the risk of muscle toxicity.

  • ImmunosuppressantsCaution

    Grapefruit sharply raises cyclosporine/tacrolimus levels — a classic dangerous food-drug interaction.

  • BenzodiazepinesCaution

    Grapefruit raises levels of some benzodiazepines, deepening sedation.

  • BP medsCaution

    Grapefruit raises several calcium-channel-blocker levels, exaggerating blood-pressure drops.

The evidence in words

What it is

Not a drug — a food, but a potent and long-lasting inhibitor of the CYP3A4 enzyme in the gut, which is why it has a drug-like interaction profile.

How it works

Furanocoumarins in grapefruit irreversibly inhibit intestinal CYP3A4, so drugs normally broken down there reach much higher blood levels — an effect that lasts a day or more per serving.

What it's used for

n/a — this page exists because of its interactions.

Supplement & drug interactions

Grapefruit has 5 documented interactions mapped below and in the interactions graph. Grapefruit raises levels of dozens of medications: several statins (myopathy), some calcium-channel blockers (blood-pressure drops), certain benzodiazepines (sedation), and immunosuppressants (toxicity). If a medication label says avoid grapefruit, take it seriously — the effect is large and long.

The rule

This is a medication reference for spotting interactions, not dosing advice. Every change to a supplement stack around a prescription belongs with the person who prescribes it.

Entries that share this one's tags or conditions.

  • AlcoholEthanol — a CNS depressant and hepatotoxin with a broad interaction footprint.Evidence grade A
  • ImmunosuppressantsDrugs that suppress the immune system to prevent transplant rejection or control autoimmunity.Evidence grade A
  • Oral ContraceptivesEstrogen/progestin (or progestin-only) pills for contraception and cycle control.Evidence grade A
  • St. John's WortGenuinely works for mild-to-moderate depression — and is the single most dangerous supplement for drug interactions.Evidence grade B

Sources

This entry lists no references of its own.

Last revised . A grade is this entry's reading of the evidence, not medical advice.