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>This happens in two very different ways. In the first, the effect is from natural furanocoumarins such as bergamottin and 6',7'-dihydroxybergamottin, which occur in both grapefruit flesh and peel. Furanocoumarins inhibit the CYP3A4 enzyme, including the P450 enzyme family responsible for metabolizing 90% of drugs.
What a bitter little fella.