Literature
All literature studies reported results recovered using in vitro systems. Mitragynine and its related alkaloids and extracts appear have slight inhibition potential towards CYP2C9, UGT1A1, and UGT2B7, wih stronger inhibition potency towards CYP2D6. Data has suggested no significant inhibition of CYP2C19 with M. speciosa extract. Mitragynine and various extracts and alkaloids of kratom also demonstrate in vitro inhibition of CYP3A4 and P-gp transporters, although contradictory evidence for this product to act as an inducer also exists. In addition, these compounds appear to induce CYP 1A2, although s evidence suggests moderate inhibition of this enzyme may also occur.
In Vitro
- Preliminary screening of kratom extracts and mitragynine as inhibitors of CYP2D6 and hepatic and intestinal CYP3A4 and UGT activity have been completed by the pharmacology core.
- Strong inhibitory potential of representative kratom extracts and mitragynine towards hepatic CYP2D6 and intestinal CYP3A4 warrant further investigation of the drug interaction liability of kratom.
- The apparent strong inhibitory effects of kratom extracts on intestinal UGT activity may represent a major drug interaction target requiring further investigation.
IVIVE
Pending potential evaluation by the Pharmacology Core
Clinical
Pending potential evaluation by the Pharmacology Core
