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- Title
P-glycoprotein is not involved in the differential oral potency of naloxone and naltrexone.
- Authors
Kanaan, Mouna; Daali, Youssef; Dayer, Pierre; Desmeules, Jules
- Abstract
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 μm) across the monolayers was investigated in the presence and absence of the specific P-gp inhibitor GF120918 (4 μm). 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.
- Subjects
P-glycoprotein; NALOXONE; NALTREXONE; BIOLOGICAL transport; OPIOID receptors
- Publication
Fundamental & Clinical Pharmacology, 2009, Vol 23, Issue 5, p543
- ISSN
0767-3981
- Publication type
Article
- DOI
10.1111/j.1472-8206.2009.00724.x