What enzyme does Grapefruit juice inhibit concerning Amlodipine metabolism?

Answer

CYP3A4

Amlodipine relies on a specific enzyme located in the liver for its metabolic breakdown, known as CYP3A4. Grapefruit juice contains furanocoumarins, which are compounds known to inhibit, or block the activity of, this CYP3A4 enzyme. When this crucial enzyme's function is inhibited, the body is unable to process and eliminate amlodipine at the normal rate. This metabolic hindrance causes a subsequent increase in the concentration of active amlodipine remaining within the bloodstream. While research indicates that a single instance of consumption might not always cause issues in a small study, the established pharmacological principle advises caution because higher-than-intended drug levels can magnify typical side effects like dizziness or low blood pressure. Consequently, many healthcare providers recommend that individuals taking amlodipine avoid consuming large quantities of grapefruit or grapefruit juice to maintain predictable therapeutic levels of the medication.

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