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P-glycoprotein is not involved in the differential oral potency of naloxone and naltrexone

Kanaan, Mouna
Published in Fundamental and Clinical Pharmacology. 2009, vol. 23, no. 5, p. 543-8
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 microm) across the monolayers was investigated in the presence and absence of the specific P-gp inhibitor GF120918 (4 microm). 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.
Keywords Acridines/pharmacologyAdministration, OralBiological AvailabilityBiological TransportBlotting, WesternCaco-2 CellsElectric ImpedanceHumansMicroscopy, Electron, TransmissionMolecular StructureNaloxone/administration & dosage/chemistry/pharmacokineticsNaltrexone/administration & dosage/chemistry/pharmacokineticsNarcotic Antagonists/administration & dosage/chemistry/pharmacokineticsP-Glycoprotein/antagonists & inhibitors/metabolism/physiologyTetrahydroisoquinolines/pharmacology
PMID: 19656202
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Research groups Pharmaco-omiques et médecine de précision (1003)
Groupe Desmeules Jules (pharmacologie/toxicologie) (567)
Groupe Pierre Dayer (pharmacologie/toxicologie) (78)
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KANAAN, Mouna et al. P-glycoprotein is not involved in the differential oral potency of naloxone and naltrexone. In: Fundamental and Clinical Pharmacology, 2009, vol. 23, n° 5, p. 543-8. doi: 10.1111/j.1472-8206.2009.00724.x https://archive-ouverte.unige.ch/unige:5492

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Deposited on : 2010-03-19

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