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Grapefruit juice and Trazodone/MCPP

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  • Grapefruit juice and Trazodone/MCPP

    Inhibiting Trazodone being converted to MCPP?

    The parent drug trazodone does help some people with anxiety. However it has now been documented that its active metabolite mCPP may actually antagonize trazodone's efficacy as well as produce additional side effects.

    Trazodone and m-CPP are substrates for CYP2D6. But is it true that trazodone is a substrate for CYP3A4, as well to a lesser extent, and that CYP3A4 is a major isoform involved in the production of mCPP from trazodone ?

    Drugs that inhibit CYP3A4 can inhibit trazodone metabolism and decrease m-CPP formation.

    Is grapefruit juice a strong CYP3A4 inhibitor ? Would it inhibit trazodone being converted to MCPP, reducing any adverse effects this metabolite may produce ?

    However if the active drug trazodone is metabolised by CYP3A4 then would the fruit stop the drug being metabolised ? Leaving elevated concentrations in the body, which can cause adverse effects in its self ? However I think trazodone and MCPP are mainly metabolised by CYP2D6!!

    Thanks in advance. I’m just curious of any drug interaction.