Pharmacokinetics of losartan and its metabolite, EXP3174, after intravenous and oral administration of losartan to rats with streptozotocin- induced diabetes mellitus

Research Communications in Molecular Pathology and Pharmacology

Volumn 101, Issue 2, 1998, Pages 147-158

  Moon, Chang H ^a   Lee, Hee J ^a   Jung, Yi S ^a   Lee, Soo H ^a   Baik, Eun J ^a  

^a Ajou University School of Medicine   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

2 BUTYL 4 CHLORO 1 [[2' (1H TETRAZOL 5 YL) 4 BIPHENYLYL]METHYL] 5 IMIDAZOLECARBOXYLIC ACID; INULIN; LOSARTAN; PLASMA PROTEIN; STREPTOZOCIN;

ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; GASTROINTESTINAL ABSORPTION; GLOMERULUS FILTRATION RATE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; INTRAVENOUS DRUG ADMINISTRATION; KIDNEY CLEARANCE; MEAN RESIDENCE TIME; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT; STREPTOZOCIN DIABETES;

ADMINISTRATION, ORAL; ANIMALS; ANTIHYPERTENSIVE AGENTS; AREA UNDER CURVE; BLOOD GLUCOSE; BLOOD PROTEINS; DIABETES MELLITUS, EXPERIMENTAL; HALF-LIFE; IMIDAZOLES; INJECTIONS, INTRAVENOUS; LOSARTAN; METABOLIC CLEARANCE RATE; RATS; RATS, SPRAGUE-DAWLEY; TETRAZOLES;

EID: 0031723961     PISSN: 10780297     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (34)

1. Chiou, W.L. (1978). Critical evaluation of potential error in pharmacokinetic studies using the linear trapezoidal rule method for the calculation of the area under the plasma level-time curve. J. Pharmacokinet. Biopharm. 6: 539-546.
2. Chiou, W.L. (1979). New calculation method for mean apparent drug volume of distribution and application to rationale dosage regimens. J. Pharm. Sci. 68: 1067-1069.
3. Chiou, W.L. (1980). New calculation method of mean total body clearance of drugs and its application to dosage regimens. J. Pharm. Sci. 69: 90-91.
4. Chiou, W.L., Liu, C.Y. and Lam, G. (1981). Plasma are method in relative bioavailability evaluation of drugs with changing biological half-lives. J. Pharm. Sci. 70: 109-112.
5. Christ, D.D. (1995). Human plasma protein binding of the angiotensin II receptor antagonist losartan potassium (DuP 753/MK 954) and its pharmacologically active metabollite EXP3174. J. Clin. Pharmacol. 35: 515-520.
6. Christ, D.D., Wong, P.C., Wong, Y. N., Hart, S.D., Quon, C.Y. and Lam, G.N. (1994). The pharmacokinetics and pharmacodynamics of the angiotensin II receptor antagonist losartam potassium (DuP 753/MK 954) in the dog. J. Pharmacol. Exp. Ther. 268: 1199-1205.
7. Craven, P.A., Caines, M.A. and DeRubertis, F.R. (1987). Sequential alterations in glomerular prostaglandin and thromboxane synthesis in diabetic rats: relationship to the hyperfiltration of early diabetes. Metabolism 36: 95-103.
8. D'Souza, M.J., Solomon, H.M., Fowler, L.C. and Pollock, S.H. (1988). Pharmacokinetics of cyclosporine in streptozotocin-induced diabetic rats. Drug Metab. Disposit. 16: 778-780.
9. Eatman, F.B., Colburn, W.A., Boxenbaum, H.G., Posmanter, H.N., Weinfeld, R.E., Ronfeld, R., Weissman, L., Moore, J.D., Gibaldi, M. and Kaplan, S.A. (1977). Pharmacokinetics of diazepam following multiple dose oral administration to healthy human subjects. J. Pharmacokinet. Biopharm. 5: 481-494.
10. Fuller, J.H., Elford, J., Goldblatt, P. and Adelstein, A.M. (1983). Diabetes mortality: new light on an underestimated public health problem. Diabetologia 24: 336-341.
11. nd Ed. Marcel-Dekker, New York, NY, USA.
12. Gwilt, P.R., Nahhas, R. R. and Tracewell, W. G. (1991). The effects of diabetes mellitus on pharmacokinetics and pharmacodynamics in humans. Clin. Pharmacokinet. 20: 477-490.
13. Inskeep, P.B., Reed, A.E., Ronfeld, R.A. (1991). Pharmacokinetics of zopolrestat, a carboxylic acid aldose reductase inhibitor, in normal and diabetic rats. Pharm. Res. 8: 1511-1515.
14. Jensen, P.K., Christiansen, J.S., Steven, K. and Parving, H.-H. (1981). Renal function in streptozotocin-diabetic rats. Diabetologia 21: 409-414.
15. Kim, S.H., Choi, Y.M. and Lee, M.G. (1993). Pharmacokinetics and pharmacodynamics of furosemide in protein-calorie malnutrition. J. Pharmacokinet. Biopharm. 21: 1-17.
16. Lo, M.-W., Goldberg, M.R. McCrea, J.B., Lu, H., Furtek, C.I. and Bjornsson, T.D. (1995). Pharmacokinetics of losartan, an angiotensin II receptor antagonist, and its active metabolite EXP3174 in humans. Clin. Pharmacol. Ther. 58: 641-649.
17. Madacsy, L., Bokor, M. and Kozocsa, G. (1976). Carbenicillin half-life in children with early diabetes mellitus. Int. J. Pharmacol. Biopharm. 14: 155-158.
18. Mehvar, R. (1991). Effect of experimental diabetes mellitus on the pharmacokinetics of atenolol enantiomers in rats. J. Pharm. Sci. 80: 207-211.
19. Mulay, S. and Varma, D.R. (1984). Influence of streptozotocin-diabetes on the pharmacokinetics, placental transfer and tissue localization of dexamethasone in rats. Br. J. Pharmacol. 83: 139-144.
20. Nadai, M., Yoshizumi, H., Kuzuya, T., Hasegawa, T., Johno, I. and Kitazawa, S. (1990). Effect of diabetes on disposition and renal handling of cefazolin in rats. Drug Metab. Dispos. 18:565-570.
21. Nakashima, E., Matsushita, R., Takeda, M., Nakanishi, T. and Ichimura, F. (1992). Comparative pharmacokinetics of cefoperazone and cephradine in untreated streptozotocin diabetic rats. Drug Metab. Disposit. 20: 730-735.
22. Nelson, E., Arcuri, K., Ikeda, L., Snavely, D. and Sweet, C. (1992). Efficacy and safety of losartan in patients with essential hypertension (Abstract). Am. J. Hypertens. 5(suppl): 19A-20A.
23. O'Connor, P. and Feely, J. (1978). Clinical pharmacokinetics and endocrine disorders. Therapeutic implications. Clin. Pharmacokinet. 13: 345-364.
24. Ohtawa, M., Takayama, F., Saitoh, K., Yoshinaga, T. and Nakashima, M. (1993). Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans. Br. J. Clin. Pharmacol. 35: 290-297.
25. Osterby, R. and Gundersen, H.J.G. (1975). Glomerular size and structure in diabetes mellitus. I. Early abnormalities. Diabetologia 11: 225-229.
26. Park, J.M., Moon, C.-H. and Lee, M.G. (1996). Pharmacokinetic changes of methotrexate after intravenous administration to streptozotocin-induced diabetes mellitus rats. Res. Commun. Mol. Pathol. Pharmacol. 93: 343-352.
27. Roe, J.H., Epstein, J.H. and Goldstein, N.P. (1949). A Photometric method for the determination of inulin in plasma and urine. J. Biol. Chem. 178: 839-845.
28. Salmela, P.I., Sotaniemi, E.A. and Pelkonen, R.O. (1980). The evaluation of the drug-metabolizing capacity in patients with diabetes-mellitus. Diabetes 29: 788-794.
29. Stearns, R.A., Chakravarty, P.K., Chen, R. and Chiu, S.-H.L. (1995). Biotransformation of losartan to its active carboxylic acid metabolite in human liver microsomes. Drug Metab. Dispos. 23: 207-215.
30. Tanaka, E., Ishikawa, A., Misawa, S. and Kuroiwa, Y. (1988). Sex-related differences in hepatic drug-oxodizing capacity of streptozotocin-induced diabetic rats. J. Pharmacobiodyn. 11: 416-423.
31. Toda, A., Shimeno, H., Nagamatsu, A. and Shigematsu, H. (1987). Effects of experimental diabetes on aminopyrine metabolism in rats. Xenobiotica 17: 1075-1083.
32. Watkins, J.B. III. and Sherman, S.E. (1992). Long-term diabetes alters the hepatobiliary clearance of acetaminophen, bilirubin and digoxin. J. Pharamcol. Exp. Ther. 260: 1337-1343.
33. Wong, P.C., Price, W.A., Chiu, A.T., Duncia, J.V., Carini, D.J., Wexler, R.R., Johnson, A.L. and Timmermans, P.B.M.W.M. (1990). Nonpeptide angiotensin II receptor antagonists. XI. Pharmacology of EXP3174: an active metabolite of DuP 753, an orally active antihypertensive agent. J. Pharmacol. Exp. Ther. 255: 211-217.
34. Wong, P.C., Christ, D.D., Wong, Y.N. and Lam, G.N. (1996). Nonpeptide angiotensin II receptor antagonist: Pharmacokinetics and pharmacodynamics in rats of EXP3174, an active metabolite of losartan. Pharmacology 52: 25-29.