Mechanisms of lower maintenance dose of tacrolimus in obese patients

Drug Metabolism and Pharmacokinetics

Volumn 29, Issue 4, 2014, Pages 341-347

  Sawamoto, Kazuki ^a   Huong, Tran T ^a   Sugimoto, Natsumi ^a   Mizutani, Yuka ^a   Sai, Yoshimichi ^a   Miyamoto, Ken Ichi ^a  

^a KANAZAWA UNIVERSITY   (Japan)

Author keywords

Cyp3a2; Obesity; P gp; Pharmacokinetics; Tacrolimus

Indexed keywords

ALANINE AMINOTRANSFERASE; ASPARTATE AMINOTRANSFERASE; CHOLESTEROL; CYTOCHROME P450 3A2; MULTIDRUG RESISTANCE PROTEIN; TACROLIMUS; TRIACYLGLYCEROL; CYP3A2 PROTEIN, RAT; CYTOCHROME P450 3A;

ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; BODY MASS; BODY WEIGHT; CHOLESTEROL BLOOD LEVEL; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG HALF LIFE; EPIDIDYMAL FAT WEIGHT; FEMALE; HUMAN; LIVER; LIVER WEIGHT; MAINTENANCE DRUG DOSE; MALE; NONHUMAN; OBESITY; OUTPATIENT; PROTEIN EXPRESSION; RAT; RETROSPECTIVE STUDY; SMALL INTESTINE; STEADY STATE; TRIACYLGLYCEROL BLOOD LEVEL; WEIGHT; ZUCKER RAT; ANIMAL; BIOAVAILABILITY; BIOSYNTHESIS; BLOOD; INTESTINE MUCOSA; INTRAVENOUS DRUG ADMINISTRATION; LIVER MICROSOME; METABOLISM; MIDDLE AGED; ORAL DRUG ADMINISTRATION;

ADMINISTRATION, INTRAVENOUS; ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BODY MASS INDEX; CYTOCHROME P-450 CYP3A; FEMALE; HUMANS; INTESTINAL MUCOSA; MALE; MICROSOMES, LIVER; MIDDLE AGED; OBESITY; P-GLYCOPROTEIN; RATS; RATS, ZUCKER; RETROSPECTIVE STUDIES; TACROLIMUS;

EID: 84906965824     PISSN: 13474367     EISSN: 18800920     Source Type: Journal    
DOI: 10.2133/dmpk.DMPK-13-RG-110     Document Type: Article

References (47)

1. World Health Organization: Obesity and Overweight. Available from URL: http://www.who.int/mediacentre/factsheets/fs311/en/ Accessed September 4, 2013.
2. Kotlyar, M. and Carson, S. W.: Effects of obesity on the cytochrome P450 enzyme system. Int. J. Clin. Pharmacol. Ther., 37: 8-19 (1999).
3. Jain, R., and Chung., S. M., Jain, L., Khurana, M., Lau, S. W., and Lee., J. E., Vaidyanathan, J., Zadezensky, I., Choe, S., et al.: Implications of obesity for drug therapy: limitations and challenges. Clin. Pharmacol. Ther., 90: 77-89 (2011).
4. Venkataramanan, R., Jain, A., Cadoff, E., Warty, V., Iwasaki, K., Nagase, K., Krajack, A., Imventarza, O., Todo, S., et al.: Pharmacokinetics of FK 506: preclinical and clinical studies. Transplant. Proc., 22: 52-56 (1990).
5. Japanese FK 506 Study Group: Japanese study of FK 506 on kidney transplantationu: the benefit of monitoring the whole blood FK 506 concentration. Transplant. Proc., 23: 3085-3088 (1991).
6. Saeki, T., Ueda, K., Tanigawara, Y., Hori, R. and Komano, T.: Human P-glycoprotein transports cyclosporin A and FK506. J. Biol. Chem., 268: 6077-6080 (1993).
7. Shiraga, T., Matsuda, H., Nagase, K., Iwasaki, K., Noda, K., Yamazaki, H., Shimada, T. and Funae, Y.: Metabolism of FK506, a potent immunosuppressive agent, by cytochrome P450 3A enzymes in rat, dog and human liver microsomes. Biochem. Pharmacol., 47: 727-735 (1994).
8. Hebert, M. F.: Contributions of hepatic and intestinal metabolism and P-glycoprotein to cyclosporine and tacrolimus oral drug delivery. Adv. Drug Deliv. Rev., 27: 201-214 (1997).
9. Shimada, T., Terada, A., Yokogawa, K., Kaneko, H., Nomura, M., Kaji, K., Kaneko, S., Kobayashi, K. and Miyamoto, K.: Lowered blood concentration of tacrolimus and its recovery with changes in expression of CYP3A and P-glycoprotein after high-dose steroid therapy. Transplantation, 74: 1419-1424 (2002).
10. Masuda, S., Uemoto, S., Hashida, T., Inomata, Y., Tanaka, K. and Inui, K.: Effect of intestinal P-glycoprotein on daily Tacrolimus trough level in a living donor small bowel recipient. Clin. Pharmacol. Ther., 68: 98-103 (2000).
11. Hashida, T., Masuda, S., Uemoto, S., Saito, H., Tanaka, K. and Inui, K.: Pharmacokinetic and prognostic significance of intestinal MDR1 expression in recipients of living-donor liver transplantation. Clin. Pharmacol. Ther., 69: 308-316 (2001).
12. Cheng, P. Y. and Morgan, E. T.: Hepatic cytochrome P450 regulation in disease states. Curr. Drug Metab., 2: 165-183 (2001).
13. Yoshinari, K., Takagi, S., Yoshimasa, T., Sugatani, J. and Miwa, M.: Hepatic CYP3A expression is attenuated in obese mice fed a high-fat diet. Pharm. Res., 23: 1188-1200 (2006).
14. Lam, J. L., Jiang, Y., Zhang, T., Zhang, E. Y. and Smith, B. J.: Expression and functional analysis of hepatic cytochromes P450, nuclear receptors, and membrane transporters in 10- and 25-week-old db/db mice. Drug Metab. Dispos., 38: 2252-2258 (2010).
15. More, V. R. and Slitt, A. L.: Alteration of hepatic but not renal transporter expression in diet-induced obese mice. Drug Metab. Dispos., 39: 992-999 (2011).
16. Ulvestad, M., and Skottheim., I. B., Jakobsen, G. S., Bremer, S., Molden, E., Asberg, A., Hjelmesæth, J., Andersson, T. B., Sandbu, R., et al.: Impact of OATP1B1, MDR1, and CYP3A4 expression in liver and intestine on interpatient pharmacokinetic variability of Atorvastatin in obese subjects. Clin. Pharmacol. Ther., 93: 275-282 (2013).
17. Chua, S. C., Jr., White, D. W., Wu-Peng, X. S., Liu, S. M., Okada, N., Kershaw, E. E., Chung, W. K., Power-Kehoe, L., Chua, M., et al.: Phenotype of fatty due to Gln269Pro mutation in the leptin receptor (Lepr). Diabetes, 45: 1141-1143 (1996).
18. Phillips, M. S., Liu, Q., Hammond, H. A., Dugan, V., and Hey., P. J., Caskey, C. J. and Hess, J. F.: Leptin receptor missense mutation in the fatty Zucker rat. Nat. Genet., 13: 18-19 (1996).
19. Hisaka, A. and Sugiyama, Y.: Analysis of nonlinear and nonsteady state hepatic extraction with the dispersion model using the finite difference method. J. Pharmacokinet. Biopharm., 26: 495-519 (1998).
20. Higashi, K., Tanaka, C., Imanishi, K., Sawamoto, K., Horikawa, T., Ohkawa, H., Matsushita, R., Sai, Y. and Miyamoto, K.: Influence of longterm enteral nutrition on pharmacokinetics of digoxin in rats. Drug Metab. Pharmacokinet., 28: 44-52 (2013).
21. McCullagh, K. J., and Poole., R. C., Halestrap, A. P., O'Brien, M. and Bonen, A.: Role of the lactate transporter (MCT1) in skeletal muscles. Am. J. Physiol., 271(1 Pt 1): E143-E150 (1996).
22. Flechner, S. M., and Kolbeinsson., M. E., Tam, J. and Lum, B.: The impact of body weight on cyclosporine pharmacokinetics in renal transplant recipients. Transplantation, 47: 806-810 (1989).
23. Fukushima, K., Yoshida, K., Ito, Y., Takada, K. and Sugioka, N.: Effects of obesity induced by high-fat diet on the pharmacokinetics of cyclosporine A in rats. Biomed. Prev. Nutr., 1: 195-201 (2011).
24. Rodrigo, E., de Cos, M. A., Sánchez, B., Ruiz, J. C., Piñera, C., Fernández-Fresnedo, G., Palomar, R., Pérez-Ceballos, M. A., Cotorruelo, J. G., et al.: High initial blood levels of tacrolimus in overweight renal transplant recipients. Transplant. Proc., 37: 1453-1454 (2005).
25. Nagase, K., Iwasaki, K., Nozaki, K. and Noda, K.: Distribution and protein binding of FK506, a potent immunosuppressive macrolide lactone, in human blood and its uptake by erythrocytes. J. Pharm. Pharmacol., 46: 113-117 (1994).
26. Zahir, H., and Nand., R. A., Brown, K. F., Tattam, B. N. and McLachlan, A. J.: Validation of methods to study the distribution and protein binding of tacrolimus in human blood. J. Pharmacol. Toxicol. Methods, 46: 27-35 (2001).
27. Barretti, D. L., Magalhães, F. C., Fernandes, T., do Carmo, E. C., Rosa, K. T., Irigoyen, M. C., Negrão, C. E. and Oliveira, E. M.: Effects of aerobic exercise training on cardiac renin-angiotensin system in an obese Zucker rat strain. PLoS ONE, 7: e46114 (2012).
28. Zahir, H., McCaughan, G., Gleeson, M., Nand, R. A. and McLachlan, A. J.: Factors affecting variability in distribution of tacrolimus in liver transplant recipients. Br. J. Clin. Pharmacol., 57: 298-309 (2003).
29. Rao, G. M. and Morghom, L. O.: Erythrocyte count and hemoglobin levels in diabetic women. Eur. J. Appl. Physiol. Occup. Physiol., 52: 272-275 (1984).
30. Rao, G. M. and Morghom, L. O.: Effect of obesity on erythrocyte count and hemoglobin levels in Libyan diabetic patients. Clin. Physiol. Biochem., 4: 277-280 (1986).
31. Simmons, D.: Increased red cell count in diabetes and pre-diabetes. Diabetes Res. Clin. Pract., 90: e50-e53 (2010).
32. Zaluzny, L., Farrell, G. C. and Murray, M.: Effect of genetic obesity and experimental diabetes on hepatic microsomal mixed function oxidase activities. J. Gastroenterol. Hepatol., 5: 256-263 (1990).
33. Kagayama, A., Tanimoto, S., Fujisaki, J., Kaibara, A., Ohara, K., Iwasaki, K., Hirano, Y. and Hata, T.: Oral absorption of FK506 in rats. Pharm. Res., 10: 1446-1450 (1993).
34. Tamura, S., Ohike, A., Ibuki, R., Amidon, G. L. and Yamashita, S.: Tacrolimus is a class II low-solubility high-permeability drug: the effect of P-glycoprotein efflux on regional permeability of tacrolimus in rats. J. Pharm. Sci., 91: 719-729 (2002).
35. Sugioka, N., Haraya, K., Fukushima, K., Ito, Y. and Takada, K.: Effects of obesity induced by high-fat diet on the pharmacokinetics of nelfinavir, a HIV protease inhibitor, in laboratory rats. Biopharm. Drug Dispos., 30: 532-541 (2009).
36. Yokogawa, K., Takahashi, M., Tamai, I., Konishi, H., Nomura, M., Moritani, S., Miyamoto, K. and Tsuji, A.: P-glycoprotein-dependent disposition kinetics of tacrolimus: studies in mdr1a knockout mice. Pharm. Res., 16: 1213-1218 (1999).
37. Hotamisligil, G. S., Arner, P., Caro, J. F., Atkinson, R. L. and Spiegelman, B. M.: Increased adipose tissue expression of tumor necrosis factor-alpha in human obesity and insulin resistance. J. Clin. Invest., 95: 409-415 (1995).
38. Kern, P. A., Saghizadeh, M., Ong, J. M., and Bosch., R. J., Deem, R. and Simsolo, R. B.: The expression of tumor necrosis factor in human adipose tissue. Regulation by obesity, weight loss, and relationship to lipoprotein lipase. J. Clin. Invest., 95: 2111-2119 (1995).
39. Fried, S. K., Bunkin, D. A. and Greenberg, A. S.: Omental and subcutaneous adipose tissues of obese subjects release interleukin-6: depot difference and regulation by glucocorticoid. J. Clin. Endocrinol. Metab., 83: 847-850 (1998).
40. Engeli, S., Janke, J., Gorzelniak, K., Böhnke, J., Ghose, N., Lindschau, C., Luft, F. C. and Sharma, A. M.: Regulation of the nitric oxide system in human adipose tissue. J. Lipid Res., 45: 1640-1648 (2004).
41. Ding, S., and Chi., M. M., Scull, B. P., Rigby, R., Schwerbrock, N. M., Magness, S., Jobin, C. and Lund, P. K.: High-fat diet: bacteria interactions promote intestinal inflammation which precedes and correlates with obesity and insulin resistance in mouse. PLoS ONE, 5: e12191 (2010).
42. de La Serre, C. B., Ellis, C. L., Lee, J., Hartman, A. L., Rutledge, J. C. and Raybould, H. E.: Propensity to high-fat diet-induced obesity in rats is associated with changes in the gut microbiota and gut inflammation. Am. J. Physiol. Gastrointest. Liver Physiol., 299: G440-G448 (2010).
43. Pendyala, S., and Neff., L. M., Suarez-Farinas, M. and Holt, P. R.: Diet-induced weight loss reduces colorectal inflammation: implications for colorectal carcinogenesis. Am. J. Clin. Nutr., 93: 234-242 (2011).
44. de Wit, N. J., Bosch-Vermeulen, H., de Groot, P. J., Hooiveld, G. J., Bromhaar, M. M., Jansen, J., Müller, M. and van der Meer, R.: The role of the small intestine in the development of dietary fat-induced obesity and insulin resistance in C57BL/6J mice. BMC Med. Genomics, 1: 14 (2008).
45. Blokzijl, H., Vander Borght, S., Bok, L. I., Libbrecht, L., Geuken, M., van den Heuvel, F. A., Dijkstra, G., Roskams, T. A., Moshage, H., et al.: Decreased P-glycoprotein (P-gp/MDR1) expression in inflamed human intestinal epithelium is independent of PXR protein levels. Inflamm. Bowel Dis., 13: 710-720 (2007).
46. Nawa, A., Fujita Hamabe, W. and Tokuyama, S.: Inducible nitric oxide synthase-mediated decrease of intestinal P-glycoprotein expression under streptozotocin-induced diabetic conditions. Life Sci., 86: 402-409 (2010).
47. Belliard, A. M., Lacour, B., Farinotti, R. and Leroy, C.: Effect of tumor necrosis factor-alpha and interferon-gamma on intestinal P-glycoprotein expression, activity, and localization in Caco-2 cells. J. Pharm. Sci., 93: 1524-1536 (2004).