Effect of P-glycoprotein inhibition on methadone analgesia and brain distribution in the rat

Journal of Pharmacy and Pharmacology

Volumn 56, Issue 3, 2004, Pages 367-374

  Rodriguez, Monica ^a   Ortega, Ignacio ^a   Soengas, Itziar ^a   Suarez, Elena ^a   Lukas, John C ^a,b   Calvo, Rosario ^a  

^a UNIVERSITY OF THE BASQUE COUNTRY UPV EHU   (Spain)

^b UNIVERSITY OF ATHENS   (Greece)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOPROTEIN P; GLYCOPROTEIN P INHIBITOR; METHADONE; VALSPODAR;

ANALGESIC ACTIVITY; ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTINOCICEPTION; AREA UNDER THE CURVE; ARTICLE; BLOOD BRAIN BARRIER; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ANTAGONISM; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG PROTEIN BINDING; DRUG UPTAKE; IN VIVO STUDY; MALE; NEUROMODULATION; NONHUMAN; PLASMA PROTEIN BINDING; RAT; TAIL FLICK TEST;

ADMINISTRATION, ORAL; ANALGESIA; ANIMALS; AREA UNDER CURVE; BLOOD-BRAIN BARRIER; BRAIN; CARBON RADIOISOTOPES; CYCLOSPORINS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG SYNERGISM; HEAT; INFUSIONS, INTRAVENOUS; INJECTIONS, INTRAVENOUS; MALE; METHADONE; P-GLYCOPROTEIN; PAIN MEASUREMENT; RATS; RATS, SPRAGUE-DAWLEY; REACTION TIME;

EID: 1642363368     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/0022357022782     Document Type: Article

References (32)

1. Atadja, P., Watanabe, T., Xu, H., Cohen, D. (1998) PSC-833, a frontier in modulation of P-glycoprotein mediated multidrug resistance. Cancer. Metastasis. Rev. 17: 163-168
2. Augustijns, P. F., Bradshaw, T. P., Gan, L. S., Hendren, R. W., Thakker, D. R. (1993) Evidence for a polarized efflux system in Caco 2 cells capable of modulating cyclosporin A transport. Biochem. Biophys. Res. Commun. 197: 360-365
3. Bouër, R., Barthe, L., Philibert, C., Tournaire, C., Woodley, J., Houin, G. (1999) The roles of P-glycoprotein and intracellular metabolism in the intestinal absorption of methadone: In vitro studies using the rat everted intestinal sac. Fundam. Clin. Pharmacol. 13: 494-500
4. Bourasset, F., Cisternino, S., Temsamani, J., Schermann, J. M. (2003) Evidence for an active transport of morphine-6-beta-D-glucuronide but not P-glycoprotein-mediated at the blood-brain barrier. J. Neurochem. 86: 1564-1567
5. Burton, P. S., Conradi, R. A., Hilgers, A. R., Ho, N. F. (1993) Evidence for a polarized efflux system for peptides in the apical membrane of Caco 2 cells. Biochem. Biophys. Res. Commun. 190: 760-766
6. Callaghan, R., Riordan, J. R. (1993) Synthetic and natural opiates interact with P-glycoprotein in multidrug resistant cells. J. Biol. Chem. 268: 16059-16064
7. Carlos, M., Du Souich, P., Lukas, J. C., Carlos, R., Suarez, E., Calvo, R. (2002) Effect of omeprazole on oral and i.v. RS-methadone: Pharmacokinetics and pharmacodynamics in the rat. J. Pharm. Sci. 91: 1627-1638
8. Cox, D. S., Scott, K. R., Gao, H., Eddington, N. D. (2002) Effect of P-glycoprotein on the pharmacokinetics and tissue distribution of enaminone anticonvulsants: Analysis by population and physiological approaches. J. Pharmacol. Exp. Ther. 302: 1096-1104
9. Eap, C. B., Buclin, T., Baumann, P. (2002) Interindividual variability of the clinical pharmacokinetics of methadone: Implications for the treatment of opioid dependence. Clin. Pharmacokinet. 41: 1153-1193
10. Garrido, M. J., Valle, M., Calvo, R., Trocóniz, I. F. (1999) Altered plasma and brain disposition and pharmacodynamics of methadone in abstinent rats. J. Pharmacol. Exp. Ther. 288: 179-187
11. Gómez, E., Martínez-Jordá, R., Suárez, E., Garrido, M. J., Calvo, R. (1995) Altered methadone analgesia due to changes in protein binding: Role of the route of administration. Gen. Pharmacol. 26: 1273-1276
12. Gourlay, G. K., Cherry, D. A., Cousins, M. J. (1986) A comparative study of the efficacy and pharmacokinetics of oral methadone and morphine in the treatment of severe pain in patients with cancer. Pain. 25: 297-312
13. Huisman, M. T., Smit, J. W., Wiltshire, H. R., Hoetelmans, R. M., Beijnen, J. H., Schinkel, A. H. (2001) P-glycoprotein limits oral availability, brain and fetal penetration of saquinavir even with high doses of ritonavir. Mol. Pharmacol. 59: 806-813
14. Hunter, J., Hirst, B. H., Simmons, N. L. (1993) Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers. Pharm. Res. 10: 743-749
15. Kawahara, I., Kato, Y., Suzuki, H., Achira, M., Ito, K., Crespi, C. L., Sugiyama, Y. (2000) Selective inhibition of human cytochrome P450 3A4 N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1,1-dimethylethylaminocarbonyl) -4-[(furo[2,3-b]pyridin-5-yl) methyl]piperazin-1-yl]-4(S)-hydroxy-2(R) -phenylmethylpentanamide and P-glycoprotein by valspodar in gene transfectant systems. Drug. Metab. Dispos. 28: 1238-1243
16. Le Bars, D., Gozariu, M., Cadden, S. W. (2001) Animal model of nociception. Pharmacol. Rev. 53: 597-652
17. Letrent, S. P., Pollack, G. M., Brouwer, K. R., Brouwer, K. L. (1999) Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphine in the rat. Drug. Metab. Dispos. 27: 827-834
18. Lin, J. H., Yamazaki, M. (2003) Role of P-glycoprotein in pharmacokinetics. Clin. Pharmacokinet. 42(1): 59-98
19. Liu, S. J., Roering, D. L., Wang, R. I. H. (1983) Brain and plasma levels of methadone and their relationship to analgesic activity of methadone in rats. Drug. Metab. Dispos. 11: 335-338
20. MacPhee, I. A., Fredericks, S., Tai, T., Syrris, P., Carter, N. D., Johnston, A., Goldberg, L., Holt, D. W. (2002) Tacrolimus pharmacogenetics: Polymorphisms associated with expression of cytochrome P4503A5 and P-glycoprotein correlate with dose requirement. Transplantation 74: 1486-1489
21. Malingre, M. M., Richel, D. J., Beijnen, J. H., Rosing, H., Koopman, F. J., ten Bokkel Huinink, W. W., Schot, M. E., Schellens, J. H. (2001) Coadministration of cyclosporine strongly enhances the oral bioavailability of docetaxel. J. Clin. Oncol. 19: 1160-1166
22. Martinez, M. N., Amidon, G. L. (2002) A mechanistic approach to understanding the factors affecting drug absorption: A review of fundamentals. J. Clin. Pharmacol. 42: 620-643
23. Meerum Terwgot, J. M., Malingre, M. M., Beijnen, J. H., ten Bokkel Huinink, W. W., Rosing, H., Koopman, F. J., van Tellingen, O., Swart, M., Schellens, J. H. (1999) Co-administration of oral cyclosporin enables oral therapy with paclitaxel. Clin. Cancer. Res. 5: 3379-3384
24. Nilsson, M. I., Anggard, E., Holmstrand, J., Gunne, L. M. (1982) Pharmacokinetics of methadone during maintenance treatment: adaptive changes during the induction phase. Eur. J. Clin. Pharmacol. 22: 343-349
25. Rodriguez, M., Carlos, M. A., Ortega, I., Suarez, E., Calvo, R., Lukas, J. C. (2002) Sex specificity in methadone analgesia in the rat: A population pharmacokinetic and pharmacodynamic approach. Pharm. Res. 19: 858-867
26. Sadeque, A. J., Wandel, C., He, H., Shah, S., Wood, A. J. (2000) Increased drug delivery to the brain by P-glycoprotein inhibition. Clin. Pharmacol. Ther. 68: 231-237
27. Schinkel, A. H., Wagenaar, E., Mol, C. A., van Deemter, L. (1996) P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs. J. Clin. Invest. 97: 2517-2524
28. Sparreboom, A., van Asperen, J., Mayer, U., Schinkel, A. H., Smit, J. W., Meijer, D. K., Borst, P., Nooijen, W. J., Beijnen, J. H., van Tellingen, O. (1997) Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc. Natl Acad. Sci. USA 94: 2031-2035
29. Tanigawara, Y. (2000) Role of P-glycoprotein in drug disposition. Ther. Drug. Monit. 22: 137-140
30. Taylor, E. M. (2002) The impact of efflux transporters in the brain on the development of drugs for CNS disorders. Clin. Pharmacokinet. 41(2): 81-92
31. Thompson, S. J., Koszdin, K., Bernards, C. M. (2000) Opiate-induced analgesia is increased and prolonged in mice lacking P-glycoprotein. Anesthesiology 92: 1392-1399
32. Verschraagen, M., Koks, C. H., Schellens, J. H., Beijnen, J. H. (1999) P-glycoportein system as a determinant of drug interactions: the case of digoxin-verapamil. Pharmacol. Res. 40: 301-306