Thread: Potentiating gabapentin using grapefruit juice

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    Potentiating gabapentin using grapefruit juice 
    Is gabapentin metabolized by any of the same enzymes that grapefruit juice affects? Would drinking grapefruit juice before taking gabapentin potentiate it any?
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    Bluelighter laCster's Avatar
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    Nov 2010
    gabapentin isn't metabolized through 2D6 or 3A4 so GFJ wouldn't potentiate shit
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    If you're curious about the mechanism of action, I found a few quotes that may help:

    Like gabapentin, pregabalin binds to the α2δ (alpha2delta) subunit of the voltage-dependent calcium channel in the central nervous system. Pregabalin decreases the release of neurotransmitters such as glutamate, noradrenaline, and substance P (Australian Medicines Handbook). Pregabalin increases neuronal GABA levels by producing a dose-dependent increase in glutamic acid decarboxylase activity.[1] Glutamic acid decarboxylase (GAD) is the enzyme that converts the excitatory neurotransmitter glutamate into the inhibitory GABA in a single step. For this reason, pregabalin greatly potentiates benzodiazepines, barbiturates & other depressants.

    Found here:

    And this:

    Actually pregabalin "doesn't" raise levels of dopamine. It is inactive at serotonin and dopamine receptors and does not inhibit dopamine, serotonin, or noradrenaline reuptake. Pregabalin does not bind directly to GABAA, GABAB, or benzodiazepine receptors, does not block sodium channels, is not active at opiate receptors, and does not alter cyclooxygenase enzyme activity. Pregabalin is a structural analogue of gamma-aminobutyric acid (GABA) Pregabalin does not show direct GABA-mimetic effects, but increases neuronal GABA levels. Pregabalin reduces neuronal calcium currents by binding to the alpha-2-delta subunit of calcium channels, and this particular mechanism may be responsible for effects in neuropathic pain, anxiety, and other pain syndromes.

    Found here:

    As far as I can tell, the mechanism of action is the same for pregabalin and gabapentin. Correct me if I'm wrong.
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