In the body ketamine undergoes extensive metabolism. It is biotransformed by CYP3A4 and CYP2B6 isoenzymes into norketamine, which, in turn, is converted by CYP2A6 and CYP2B6 into hydroxynorketamine and dehydronorketamine. Low oral bioavailability of ketamine is due to the first-pass effect and, possibly, ketamine intestinal metabolism by CYP3A4. As a result, norketamine plasma levels are several-fold higher than ketamine following oral administration, and norketamine may play a role in anesthetic and analgesic action of oral ketamine. This also explains why oral ketamine levels are independent of CYP2B6 activity, unlike subcutaneous ketamine levels.

In 1998, various researchers showed that grapefruit juice, and grapefruit in general, is a potent inhibitor of CYP3A4, which can affect the metabolism of a variety of drugs, increasing their bioavailability.
(...)
Strong inhibitors
(...)
nefazodone (antidepressant)
(...)
green tea extract,
grape seed extract,
dillapiole (compound present in dill plants),
apigenin (compound present in plants such as celery, parsley, and chamomile)
Artemisia annua

Strong:
orphenadrine (anticholinergic)
Artemisia annua

26 lipca 2024london5 pisze:

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