Library
Gráifruit
Bergamottin and 6',7'-dihydroxybergamottin in grapefruit irreversibly inactivate intestinal CYP3A4 via mechanism-based covalent binding, reducing enzyme abundance by 50-70% after a single 200 ml serving. Full resynthesis takes 24-72 hours, meaning timing separation of grapefruit and medication does not prevent interactions. Parallel inhibition of intestinal P-glycoprotein raises systemic exposure to many substrates, while OATP1A2 blockade can paradoxically lower absorption of drugs like fexofenadine. Interaction magnitude varies with cultivar (white > ruby red), processing method, and individual CYP3A4 expression. Seville orange, tangelo and pomelo contain identical furanocoumarins and pose similar risks.
Also known as: Pomelo, Forbidden fruit
Classification
- Chemical: Medicine
- Tag: Fruit juice
- Tag: Furanocoumarin-containing natural product
- Tag: Not psychoactive
- Tag: Potentiator
- Tag: Supplement
Effects
- Mild Digestive Stimulation
- Bittersweet Citrus Flavor
Routes of Administration
Oral
Dosage
- Threshold: 50 ml
- Light: 100-200 ml
- Common: 200-400 ml
- Strong: 400-600 ml
- Heavy: 600 ml
Duration
- Onset: 0.25-0.5 h
- Comeup: 0.5-1 h
- Peak: 0.5 h
- Offset: 24 h
- After Effects: 24-72 h
Harm Reduction
Check interactions before mixing substances, pay attention to dose spacing and hydration, and treat all dosage guidance as approximate rather than guaranteed safe.
Sources
Substance data is aggregated from the following public harm-reduction and reference sources.
Links
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