Effects of a P-glycoprotein modulator on the pharmacokinetics and distribution of free levobupivacaine and bupivacaine in rats

International Journal of Pharmaceutics

Volumn 396, Issue 1-2, 2010, Pages 127-133

  Wu, Yu Tse ^a   Kao, Yi Lin ^a   Lin, Lie Chwen ^a,b   Tsai, Tung Hu ^a,c,d  

^a NATIONAL YANG MING UNIVERSITY   (Taiwan)

^b Institute of Traditional Medicine   (Taiwan)

^c CHINA MEDICAL UNIVERSITY   (Taiwan)

^d TAIPEI CITY HOSPITAL   (Taiwan)

Author keywords

Bupivacaine; Free form pharmacokinetics; Levobupivacaine; Microdialysis

Indexed keywords

BUPIVACAINE; CYCLOSPORIN; CYCLOSPORIN A; GLYCOPROTEIN P; LEVOBUPIVACAINE; LOCAL ANESTHETIC AGENT; MULTIDRUG RESISTANCE PROTEIN; PROTEIN BINDING;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BRAIN CORTEX; CONTROLLED STUDY; CORPUS STRIATUM; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG DISTRIBUTION; DRUG EXCRETION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIPPOCAMPUS; MALE; MICRODIALYSIS; NONHUMAN; PRIORITY JOURNAL; RAT; ANALOGS AND DERIVATIVES; ANIMAL; BILE; BLOOD; BRAIN; COMPARATIVE STUDY; DRUG EFFECTS; INTRAVENOUS DRUG ADMINISTRATION; METABOLISM; REPRODUCIBILITY; SPRAGUE DAWLEY RAT; TISSUE DISTRIBUTION; TRANSPORT AT THE CELLULAR LEVEL;

ANESTHETICS, LOCAL; ANIMALS; BILE; BIOLOGICAL TRANSPORT; BRAIN; BUPIVACAINE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; CYCLOSPORINE; INJECTIONS, INTRAVENOUS; MALE; MICRODIALYSIS; P-GLYCOPROTEIN; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; REPRODUCIBILITY OF RESULTS; TISSUE DISTRIBUTION;

EID: 77955056083     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2010.06.038     Document Type: Article

References (53)

1. Akhlaghi F., McLachlan A.J., Keogh A.M., Brown K.F. Effect of simvastatin on cyclosporine unbound fraction and apparent blood clearance in heart transplant recipients. Br. J. Clin. Pharmacol. 1997, 44:537-542.
2. Bansal T., Mishra G., Jaggi M., Khar R.K., Talegaonkar S. Effect of P-glycoprotein inhibitor, verapamil, on oral bioavailability and pharmacokinetics of irinotecan in rats. Eur. J. Pharm. Sci. 2009, 36:580-590.
3. Begley D.J. ABC transporters and the blood-brain barrier. Curr. Pharm. Des. 2004, 10:1295-1312.
4. Bertera F.M., Di Verniero C.A., Mayer M.A., Bramuglia G.F., Taira C.A., Höcht C. Is urethane-chloralose anaesthesia appropriate for pharmacokinetic-pharmacodynamic assessment? Studies with carvedilol. J. Pharmacol. Toxicol. Methods 2009, 59:13-20.
5. Bupivacaine. MICROMEDEX 1.0 (Healthcare Series) [accessed on June 1, 2010].
6. Burm A.G., Stienstra R., Brouwer R.P., Emanuelsson B.M., van Kleef J.W. Epidural infusion of ropivacaine for postoperative analgesia after major orthopedic surgery: pharmacokinetic evaluation. Anesthesiology 2000, 93:395-403.
7. Burm A.G., van der Meer A.D., van Kleef J.W., Zeijlmans P.W., Groen K. Pharmacokinetics of the enantiomers of bupivacaine following intravenous administration of the racemate. Br. J. Clin. Pharmacol. 1994, 38:125-129.
8. Casati A., Putzu M. Bupivacaine, levobupivacaine and ropivacaine: are they clinically different?. Best Pract. Res. Clin. Anaesthesiol. 2005, 19:247-268.
9. Castagne V., Bonhomme-Faivre L., Urien S., Ben Reguiga M., Soursac M., Gimenez F., Farinotti R. Effect of recombinant interleukin-2 pretreatment on oral and intravenous digoxin pharmacokinetics and P-glycoprotein activity in mice. Drug Metab. Dispos. 2004, 32:168-171.
10. Center for Drug Evaluation and Research, Center for Biologics Evaluation and Research Estimating the Safe Starting Dose in Clinical Trials for Therapeutics in Adult Healthy Volunteers 2002, U.S. Food and Drug Administration, Rockville, MD, USA.
11. Chien C.F., Wu Y.T., Lee W.C., Lin L.C., Tsai T.H. Herb-drug interaction of Andrographis paniculata extract and andrographolide on the pharmacokinetics of theophylline in rats. Chem. Biol. Interact. 2010, 184:458-465.
12. Clement R., Malinovsky J., Le Corre P., Dollo G., Chevanne F., Le Verge R. Spinal biopharmaceutics of bupivacaine and lidocaine by microdialysis after their simultaneous administration in rabbits. Int. J. Pharm. 2000, 203:227-234.
13. Clement R., Malinovsky J.M., Dollo G., Le Corre P., Chevanne F., Le Verge R. In vitro and in vivo microdialysis calibration using retrodialysis for the study of the cerebrospinal distribution of bupivacaine. J. Pharm. Biomed. Anal. 1998, 17:665-670.
14. Clement R., Malinovsky J.M., Le Corre P., Dollo G., Chevanne F., Le Verge R. Cerebrospinal fluid bioavailability and pharmacokinetics of bupivacaine and lidocaine after intrathecal and epidural administrations in rabbits using microdialysis. J. Pharmacol. Exp. Ther. 1999, 289:1015-1021.
15. de Barros Duarte L., Moises E.C., Carvalho Cavalli R., Lanchote V.L., Duarte G., Pereira da Cunha S. Placental transfer of bupivacaine enantiomers in normal pregnant women receiving epidural anesthesia for cesarean section. Eur. J. Clin. Pharmacol. 2007, 63:523-526.
16. Elmquist W.F., Sawchuk R.J. Application of microdialysis in pharmacokinetic studies. Pharm. Res. 1997, 14:267-288.
17. Funao T., Oda Y., Tanaka K., Asada A. The P-glycoprotein inhibitor quinidine decreases the threshold for bupivacaine-induced, but not lidocaine-induced, convulsions in rats. Can. J. Anaesth. 2003, 50:805-811.
18. Garner C.E., Solon E., Lai C.M., Lin J., Luo G., Jones K., Duan J., Decicco C.P., Maduskuie T., Mercer S.E., Gan L.S., Qian M., Prakash S., Shen H.S., Lee F.W. Role of P-glycoprotein and the intestine in the excretion of DPC 333 [(2R)-2-{(3R)-3-amino-3-[4-(2-methylquinolin-4-ylmethoxy)phenyl]-2-oxopyrr olidin-1-yl}-N-hydroxy-4-methylpentanamide] in rodents. Drug Metab. Dispos. 2008, 36:1102-1110.
19. Garrison K.E., Pasas S.A., Cooper J.D., Davies M.I. A review of membrane sampling from biological tissues with applications in pharmacokinetics, metabolism and pharmacodynamics. Eur. J. Pharm. Sci. 2002, 17:1-12.
20. Groen K., Mantel M., Zeijlmans P.W., Zeppenfeldt B., Olieman W., Stienstra R., van Kleef J.W., Burm A.G. Pharmacokinetics of the enantiomers of bupivacaine and mepivacaine after epidural administration of the racemates. Anesth. Analg. 1998, 86:361-366.
21. Gross A.S., Somogyi A.A. Interaction of the stereoisomers of basic drugs with the uptake of tetraethylammonium by rat renal brush-border membrane vesicles. J. Pharmacol. Exp. Ther. 1994, 268:1073-1080.
22. Guidance for Industry Bioanalytical Method Validation, Center for Drug Evaluation and Research 2001, US Food and Drug Administration, Rockville, MD, (May).
23. Han Y.H., Hato Y., Sugiyama Y. Nonlinear disposition kinetics of a novel antifolate, MX-68, in rats. J. Pharmacol. Exp. Ther. 1999, 291:204-212.
24. Ho R.H., Tirona R.G., Leake B.F., Glaeser H., Lee W., Lemke C.J., Wang Y., Kim R.B. Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology 2006, 130:1793-1806.
25. Hooiveld G.J., van Montfoort J.E., Meijer D.K., Muller M. Function and regulation of ATP-binding cassette transport proteins involved in hepatobiliary transport. Eur. J. Pharm. Sci. 2001, 12:525-543.
26. Javaid J.I., Davis J.M. Cocaine disposition in discrete regions of rat brain. Biopharm. Drug Dispos. 1993, 14:357-364.
27. Kalvass J.C., Olson E.R., Pollack G.M. Pharmacokinetics and pharmacodynamics of alfentanil in P-glycoprotein-competent and P-glycoprotein-deficient mice: P-glycoprotein efflux alters alfentanil brain disposition and antinociception. Drug Metab. Dispos. 2007, 35:455-459.
28. Kamisako T., Leier I., Cui Y., Konig J., Buchholz U., Hummel-Eisenbeiss J., Keppler D. Transport of monoglucuronosyl and bisglucuronosyl bilirubin by recombinant human and rat multidrug resistance protein 2. Hepatology 1999, 30:485-490.
29. Kawano T., Oshita S., Takahashi A., Tsutsumi Y., Tomiyama Y., Kitahata H., Kuroda Y., Nakaya Y. Molecular mechanisms of the inhibitory effects of bupivacaine, levobupivacaine, and ropivacaine on sarcolemmal adenosine triphosphate-sensitive potassium channels in the cardiovascular system. Anesthesiology 2004, 101:390-398.
30. Kopacz D.J., Bernards C.M., Allen H.W., Landau C., Nandy P., Wu D., Lacouture P.G. A model to evaluate the pharmacokinetic and pharmacodynamic variables of extended-release products using in vivo tissue microdialysis in humans: bupivacaine-loaded microcapsules. Anesth. Analg. 2003, 97:124-131. [table of contents].
31. Kusuhara H., Sugiyama Y. Efflux transport systems for drugs at the blood-brain barrier and blood-cerebrospinal fluid barrier (Part 1). Drug Discov. Today 2001, 6:150-156.
32. Lacy C.F., Armstrong L.L., Goldman M.P., Lance L.L. Lexi-Comp's Drug Information Handbook International: With Canadian and International Drug Monographs 2005, Lexi-Comp Inc., Ohio. 13th ed.
33. Lin J.H., Yamazaki M. Role of P-glycoprotein in pharmacokinetics: clinical implications. Clin. Pharmacokinet. 2003, 42:59-98.
34. Mather L.E., Huang Y.F., Veering B., Pryor M.E. Systemic and regional pharmacokinetics of levobupivacaine and bupivacaine enantiomers in sheep. Anesth. Analg. 1998, 86:805-811.
35. McDonald S., Faibushevich A.A., Garnick S., McLaughlin K., Lunte C. Determination of local tissue concentrations of bupivacaine released from biodegradable microspheres and the effect of vasoactive compounds on bupivacaine tissue clearance studied by microdialysis sampling. Pharm. Res. 2002, 19:1745-1752.
36. Perriere N., Yousif S., Cazaubon S., Chaverot N., Bourasset F., Cisternino S., Decleves X., Hori S., Terasaki T., Deli M., Scherrmann J.M., Temsamani J., Roux F., Couraud P.O. A functional in vitro model of rat blood-brain barrier for molecular analysis of efflux transporters. Brain Res. 2007, 1150:1-13.
37. Punke M.A., Friederich P. Lipophilic and stereospecific interactions of amino-amide local anesthetics with human Kv1.1 channels. Anesthesiology 2008, 109:895-904.
38. Schweitzer S.A., Morgan D.J. Plasma bupivacaine concentrations during postoperative continuous epidural analgesia. Anaesth. Intensive Care 1987, 15:425-430.
39. Scott D.A., Emanuelsson B.M., Mooney P.H., Cook R.J., Junestrand C. Pharmacokinetics and efficacy of long-term epidural ropivacaine infusion for postoperative analgesia. Anesth. Analg. 1997, 85:1322-1330.
40. Shen J., Jiao Z., Yu Y.Q., Zhang M., Zhong M.K. Quantification of total and free mycophenolic acid in human plasma by liquid chromatography with fluorescence detection. J. Chromatogr. B: Analyt. Technol. Biomed. Life Sci. 2005, 817:207-213.
41. Tamai I., Safa A.R. Competitive interaction of cyclosporins with the Vinca alkaloid-binding site of P-glycoprotein in multidrug-resistant cells. J. Biol. Chem. 1990, 265:16509-16513.
42. Tian X., Swift B., Zamek-Gliszczynski M.J., Belinsky M.G., Kruh G.D., Brouwer K.L. Impact of basolateral multidrug resistance-associated protein (Mrp) 3 and Mrp4 on the hepatobiliary disposition of fexofenadine in perfused mouse livers. Drug Metab. Dispos. 2008, 36:911-915.
43. Tsai T.H. Pharmacokinetics of pefloxacin and its interaction with cyclosporin A, a P-glycoprotein modulator, in rat blood, brain and bile, using simultaneous microdialysis. Br. J. Pharmacol. 2001, 132:1310-1316.
44. Tsai T.H. Assaying protein unbound drugs using microdialysis techniques. J. Chromatogr. B: Analyt. Technol. Biomed. Life Sci. 2003, 797:161-173.
45. Tsai T.H., Lee C.H., Yeh P.H. Effect of P-glycoprotein modulators on the pharmacokinetics of camptothecin using microdialysis. Br. J. Pharmacol. 2001, 134:1245-1252.
46. Tsai T.H., Shum A.Y., Chen C.F. Enterohepatic circulation of chloramphenicol and its glucuronide in the rat by microdialysis using a hepato-duodenal shunt. Life Sci. 2000, 66:363-370.
47. Tsen L.C., Tarshis J., Denson D.D., Osathanondh R., Datta S., Bader A.M. Measurements of maternal protein binding of bupivacaine throughout pregnancy. Anesth. Analg. 1999, 89:965-968.
48. Varma M.V., Ashokraj Y., Dey C.S., Panchagnula R. P-glycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol. Res. 2003, 48:347-359.
49. Veering B.T., Burm A.G., Feyen H.M., Olieman W.J.H.M.S., Van Kleef J.W. Pharmacokinetics of bupivacaine during postoperative epidural infusion: enantioselectivity and role of protein binding. Anesthesiology 2002, 96:1062-1069.
50. Wright J.D., Boudinot F.D., Ujhelyi M.R. Measurement and analysis of unbound drug concentrations. Clin. Pharmacokinet. 1996, 30:445-462.
51. Wu Y.T., Lin L.C., Tsai T.H. Measurement of free hydroxytyrosol in microdialysates from blood and brain of anesthetized rats by liquid chromatography with fluorescence detection. J. Chromatogr. A 2009, 1216:3501-3507.
52. Yang H., Elmquist W.F. The binding of cyclosporin A to human plasma: an in vitro microdialysis study. Pharm. Res. 1996, 13:622-627.
53. Yamazaki M., Neway W.E., Ohe T., Chen I., Rowe J.F., Hochman J.H., Chiba M., Lin J.H. In vitro substrate identification studies for P-glycoprotein-mediated transport: species difference and predictability of in vivo results. J. Pharmacol. Exp. Ther. 2001, 296:723-735.