Sex-related differences in the gastrointestinal disposition of ivermectin in the rat: P-glycoprotein involvement and itraconazole modulation

Journal of Pharmacy and Pharmacology

Volumn 58, Issue 8, 2006, Pages 1055-1062

  Lifschitz, Adrian ^a,b   Ballent, M ^a,b   Virkel, G ^a,b   Sallovitz, J ^a   Lanusse, C ^a,b  

^a UNIVERSIDAD NACIONAL DEL CENTRO DE LA PROVINCIA DE BUENOS AIRES   (Argentina)

^b Facultad de Ciencias Naturales e Instituto M Lillo   (Argentina)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOPROTEIN P; ITRACONAZOLE; IVERMECTIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; BLOOD SAMPLING; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISPOSITION; DRUG TRANSPORT; FEMALE; GASTROINTESTINAL TRACT; GASTROINTESTINAL TRANSIT; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VIVO STUDY; INTESTINE WALL; MALE; MAXIMUM ALLOWABLE CONCENTRATION; NONHUMAN; RAT; SEX DIFFERENCE;

ANIMALS; ANTIFUNGAL AGENTS; ANTIPROTOZOAL AGENTS; AREA UNDER CURVE; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DRUG INTERACTIONS; FEMALE; INTESTINES; ITRACONAZOLE; IVERMECTIN; MALE; P-GLYCOPROTEIN; RATS; RATS, WISTAR; STOMACH;

EID: 33747076103     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/jpp.58.8.0005     Document Type: Article

References (34)

1. Alvinerie, M., Sutra, J. F., Galtier, P. (1993) Ivermectin in goat milk after subcutaneous injection. Vet. Res. 24: 417-421
2. th International Conference of the World Association for the Advancement of Veterinary Parasitology, Abstract g.7.01. Danish Centre for Experimental Parasitology, Copenhagen
3. American Veterinary Medical Association (2001) Report of the AVMA Panel on Euthanasia. JA VMA 218: 669-696
4. Ayrton, A., Morgan, P. (2001) Role of transport proteins in drug absorption, distribution and excretion. Xenobiotica 31: 469-497
5. Ballent, M., Lifschitz, A., Virkel, G., Sallovitz J., Lanusse, C. (2006) Modulation of the P-glycoprotein-mediated intestinal secretion of ivermectin: in vitro and in vivo assessments. Drug Metab. Dispos. 34: 457-463
6. Canadian Council on Animal Care (1980) Guide to the care and use of experimental animals. Vol. 1. Canadian Council on Animal Care, Ottawa
7. Chiu, S., Green, M., Baylis, F., Eline, D., Rosegay, A., Meriwether, H., Jacob, T. (1990) Absorption, tissue distribution, and excretion of tritium-labelled ivermectin in cattle, sheep, and rat. J. Agric. Food. Chem. 38: 2072-2078
8. Cummins, C. L., Wu, C. Y., Benet, L. Z. (2002) Sex-related differences in the clearance of cytochrome P450 3 A4 substrates may be caused by P-glycoprotein. Clin. Pharmacol. Ther. 72: 474-489
9. Dantzig, A. H., Alwis, D. P., Burgess, M. (2003) Considerations in the design and development of transport inhibitors as adjuncts to drug therapy. Adv. Drug Deliv. Rev. 55: 133-150
10. De Montigny, P., Shim, J., Pivinichny, J. (1990) Liquid Chromatographic determination of ivermectin with trifluoro-acetic anhydride and N-methylimidazole as the derivatization reagent. J. Pharm. Biomed. Anal. 8: 507-511
11. Didier, A., Loor, F. (1996) The abamectin derivative ivermectin is a potent P-glycoprotein inhibitor. Anticancer Drugs 7: 745-751
12. Dupuy, J., Eeckhoutte, C., Sutra, J. F., Mage, C., Alvinerie, M. (1999) Lack of sex-influence on the in vitro metabolism of ivermectin by hepatic microsomal preparations from cattle. Vet. Res. Commun. 23: 223-227
13. Dupuy, J., Derlon, A., Sutra, J. F., Cadiergues, M. C., Franc, M., Alvinerie, A. (2004) Pharmacokinetics of selamectin in dogs after topical application. Vet. Res. 28: 407-413
14. nd edn. Marcel Dekker, Inc., New York
15. Hooper, W. D., Qing, M. S. (1990) The influence of age and sex on the stereoselective metabolism and pharmacokinetics of mephobarbital in humans. Clin. Pharmacol. Ther. 48: 633-640
16. Hulst, L. K., Fleishaker, J. C., Peters, G. R., Harry, J. D., Wright, D. M., Ward, P. (1994) Effect of age and sex on tirilazad pharmacokinetics in humans. Clin. Pharmacol. Ther. 55: 378-384
17. Krecic-Shepard, M., Barnas, C., Slimko, J., Schwartz, J. (2000) Faster clearance of sustained release verapamil in men versus women: continuing observations on sex-specific differences after oral administration of verapamil. Clin. Pharmacol. Ther. 68: 286-292
18. Laffont, C. M., Toutain, P. L., Alvinerie, M., Bousquet-Melou, A. (2002) Intestinal secretion is a major route for parent ivermectin elimination in the rat. Drug Metab. Dispos. 30: 626-630
19. Leveque, D., Jehl, F. (1995) P-glycoprotein and pharmacokinetics. Anticancer Res. 15: 331-336
20. Lifschitz, A., Virkel, G., Sallovitz, J., Sutra, J. F., Galtier, P., Alvinerie, M., Lanusse, C. (2000) Comparative distribution of ivermectin and doramectin to tissues of parasite location in cattle. Vet. Parasitol. 87: 327-338
21. Lifschitz, A., Virkel, G., Sallovitz, J., Imperiale, F., Pis, A., Lanusse C. (2004) Loperamide modifies the tissue disposition kinetics of ivermectin in rats. J. Pharm. Pharmacol. 56: 61-67
22. Meibohm, B., Beierle, I., Derendorf, H. (2002) How important are sex differences in pharmacokinetics? Clin. Pharmacokinet. 41: 329-342
23. Paine, M., Ludington, S., Chen, M., Stewart, P., Huang, S., Watkins, P. (2005) Do men and women differ in proximal small intestinal CYP 3A or P-glycoprotein expression? Drug Metab. Dispos. 33: 426-433
24. Pouliot, J. F., L'Heureux, F., Liu, Z., Prichard, R., Georges, E. (1997) Reversal of P-glycoprotein-associated multidrug resistance by ivermectin. Biochem. Pharmacol. 53: 17-25
25. Salphati, L., Benet, L. (1998) Modulation of P-glycoprotein expression by cytochrome P450 3A inducers in male and female rat livers. Biochem. Pharmacol. 55: 387-395
26. Schinkel, A., Smit, J., van Telligen, O., Beijnen, J., Wagenaar, E., van Deemter, L., Mol, C., van der Valk, M., Rocabus-Maandag, E., Riele, H., Berns, A., Borst, P. (1994) Disruption of the mouse mdrla P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell 77: 491-502
27. Schinkel, A., Wagenaar, E., van Deemter, L., Mol, C., Borst, P. (1995) Absence of the mdr-1aP-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin and cyclosporin A. J. Clin. Invest. 96: 1698-1705
28. Schinkel, A., Wagenaar, E., Mol, C., 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
29. Shin, J., Choi, K., Kim, Y., Lee, M. (2004) Dose-dependent pharmacokinetics of itraconazole after intravenous or oral administration to rats: intestinal first-pass effect. Antimicrob. Agents Chemother. 48: 1756-1762
30. Stephens, R. H., O'Neill, C. A., Warhurst, A., Carlson, G. L., Rowland, M., Warhurst, G. (2001) Kinetic profiling of P-glycoprotein-mediated drug efflux in rat and human intestinal epithelia. J. Pharmacol. Exp. Ther. 296: 584-591
31. Toutain, P. L., Upson, D., Terhune, T., McKenzie, M. (1997) Comparative pharmacokinetics of doramectin and ivermectin in cattle. Vet. Parasitol. 72: 3-8
32. Van Asperen, J., Telligen, O., Beijnen, J. (2000) The role of MDR1 P-glycoprotein in the biliary and intestinal secretion of doxorubicin and vinblastine in mice. Drug Metab. Dispos. 28: 264-267
33. Waxman, D., Ram, P., Pampori, N., Shapiro, B. (1995) Growth hormone regulation of male-specific rat liver P450s 2A2 and 3A2: induction by intermittent growth hormone pulses in male but not female rats rendered growth hormone deficient by neonatal monosodium glutamate. Mol. Pharmacol. 48: 790-797
34. Zeng, Z., Andrew, N. W., Arison, B. H., Luffer-Atlas, D., Wang, R. W. (1998) Identification of cytochrome P4503A4 as the major enzyme responsible for the metabolism of ivermectin by human liver microsomes. Xenobiotica 28: 313-312