Journal
FUNDAMENTAL & CLINICAL PHARMACOLOGY
Volume 23, Issue 5, Pages 543-548Publisher
WILEY
DOI: 10.1111/j.1472-8206.2009.00724.x
Keywords
absorption; Caco-2 cells; naloxone; naltrexone; oral bioavailability; P-glycoprotein
Categories
Funding
- Department of Anesthesiology, Pharmacology and Intensive care, Geneva University Hospitals [CH-1211 Geneva 14]
Ask authors/readers for more resources
The poor oral bioavailability of the opioid receptor antagonist naloxone (NA) when compared with naltrexone (NX) may be related to a greater interaction of naloxone with the efflux drug transporter P-glycoprotein (P-gp). We studied the involvement of P-gp in the transepithelial transport of the two opioid receptor antagonists, using a validated human in vitro Caco-2 cell monolayer model. The bidirectional transport of NA and NX (1, 50 and 100 mu m) across the monolayers was investigated in the presence and absence of the specific P-gp inhibitor GF120918 (4 mu m). NA and NX showed equal transport rates between the apical-to-basolateral (A-B) and the basolateral-to-apical (B-A) directions and neither the influx nor the efflux transport was affected by the P-gp inhibitor (P > 0.05). In conclusion, NA and NX are not P-gp substrates. The differential oral bioavailability of the two opioid antagonists is P-gp independent.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available