$\require{mediawiki-texvc}$
  • 검색어에 아래의 연산자를 사용하시면 더 정확한 검색결과를 얻을 수 있습니다.
  • 검색연산자
검색연산자 기능 검색시 예
() 우선순위가 가장 높은 연산자 예1) (나노 (기계 | machine))
공백 두 개의 검색어(식)을 모두 포함하고 있는 문서 검색 예1) (나노 기계)
예2) 나노 장영실
| 두 개의 검색어(식) 중 하나 이상 포함하고 있는 문서 검색 예1) (줄기세포 | 면역)
예2) 줄기세포 | 장영실
! NOT 이후에 있는 검색어가 포함된 문서는 제외 예1) (황금 !백금)
예2) !image
* 검색어의 *란에 0개 이상의 임의의 문자가 포함된 문서 검색 예) semi*
"" 따옴표 내의 구문과 완전히 일치하는 문서만 검색 예) "Transform and Quantization"
쳇봇 이모티콘
안녕하세요!
ScienceON 챗봇입니다.
궁금한 것은 저에게 물어봐주세요.

논문 상세정보

흰쥐에서 플루바스타틴이 딜티아젬 및 그 대사체인 데스아세틸딜티아젬의 약물동태에 미치는 영향

Effect of Fluvastatin on the Pharmacokinetics of Diltiazem and its Metabolite, Desacetyldiltiazem in Rats

약학회지 = Yakhak hoeji v.50 no.2 , 2006년, pp.118 - 123  
Abstract

The aim of this study was to investigate the effect of fluvastatin on the pharmacokinetics of diltiazem and its active metabolite, desacetyldiltiazem, in rats. Pharmacokinetic parameters of diltiazem and desacetyldiltiazem were deter-mined after an oral administration of diltiazem (15 mg/kg) to rats pretreated with fluvastatin (0.5 and 1.5 mg/kg). Compared with the control (given diltiazem alone), the pretreatment of fluvastatin significantly (p<0.05) increased the area under the plasma concentration (AUC), peak plasma concentration $(C_{max})\;and\;K_a$ of diltiazem. Relative bioavailability $(RB\%)$ of diltiazem increased from 1.36- to 1.55-fold. However there were no significant changes in $t_{max},\;K_{el}\;and\;t_{1/2}$ of diltiazem. The pretreatment of fluvastatin also altered the pharmacokintic parameters of desacetyldiltiazem. The pretreatment of fluvastatin (1.5 mg/kg) significantly (p<0.05) increased the AUC of desacetyldiltiazem, whereas the metabolite parent ratio (MR) of desacetyldiatlazem was decreased significantly (p<0.05), suggesting that fluvastatin might inhibit the metabolism of diltiazem. The pretreatment of fluvastatin enhanced the bioavailability of diltiazem in a dose dependent manner at doses ranging from 0.5 to 1.5 mg/kg. further studies for the drug Interaction will be needed in the clinical trials when dilitazem is administrated concomitantly with fluvastatin in humans.

참고문헌 (37)

  1. Epstein, M., Loutzenhister, R. D. : Effects of calcium antagonists on renal hemodynamics. Am. J. Kidney Dis. 16, 10 (1990) 
  2. Bianchetti, G., Regazzi, M., Rondanelli, R., Ascalone, V. and Morselli, P. L. : Bioavailability of diltiazem as a function of the administered dose. Biopharm. Drug Dispos. 12, 391 (1991) 
  3. Homsy, W., Lefebvre, M., Caille, G. and du Souich, P. : Metabolism of diltiazem in hepatic and extrahepatic tissues of rabbits: In vitro studies. Pharm. Res. 12, 609 (1995) 
  4. Cohen, L. H., van Leeuwen, R. E., van Thiel, G. C. van Pelt, J. F. and Yap, S. H. : Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm. Drug. Dispos. 21, 353 (2000) 
  5. Kirchheiner, J., Kudlicz, D., Meisel, C., Bauer, S., Meineke, I., Roots, I. and Brockmöller, J. : Influence of CYP 2C9 polymorphisms on the pharmacokinetics and cholesterollowering activity of (-)-3s,5r-fluvastatin and (+)-3r,5s-fluvastatin in healthy volunteers. Clinical Pharmacology & Therapeutics. 74, 186 (2003) 
  6. Goebel, K. J. and Kolle, E. U. : High performance liquid chromatographic dertermination of diltiazem and four of its metabolites in plasma. J. Chromatogr. 345, 355 (1985) 
  7. Rocci, M. L. and Jusko, W. J. : LAGRAN program for area and moments in pharmacokinetic analysis. Computer Programs in Biomedicine. 16, 203 (1983) 
  8. Yusa, K. and Tsuruo, T. : Reversal mechanism of multidrug resistance by verapamil: Direct binding of verapamil to Pglycoprotein on specific sites and transport of verapamil outward across the plasma membrane of K562/ADM cells. Cancer Res. 49, 5002 (1989) 
  9. Watanabe, H., Kosuge, K., Nishio, S., Yamada, H., Uchida, S., Satoh, H., Hayashi, H., Ishizaki, T. and Ohashi, K. : Pharmacokinetic and pharmacodynamic interactions between simvastatin and diltiazem in patients with hypercholesterolemia and hypertension. Life Sci. 76, 281 (2004) 
  10. Schectman, G. and Hiatt, J. : Dose-response characteristics of cholesterol-lowering drug therapies: implications for treatment. Ann. Intern. Med. 125, 990 (1996) 
  11. Eichelbaum, M. and Echizen, H. : Clinical pharmacology of calcium antagonists: A critical review. J. Cardiovas. Pharmacol. 6, 963 (1984) 
  12. Biedler, J. L. and Riehm, H. : Cellular resistance to actinomycin D in Chinese hamster cells in vitro: cross-resistance, radioautographic, and cytogenetic studies. Cancer Res. 30, 1174 (1970) 
  13. Yeo, K. R. and Yeo, W. W. : Inhibitory effects of verapamil and diltiazem on simvastatin metabolism in human liver microsomes. Br. J. Clin. Pharmacol. 51, 461 (2001) 
  14. Homsy, W., Caille, G. and du Souich, P. : The site of absorption in the small intestine determines diltiazem bioavailability in the rabbit. Pharm. Res. 12, 1722 (1995) 
  15. Ehrhardt, M., Lindenmaier, H., Burhenne, J., Haefeli, W. E. and Weiss, J. : Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. Biochemical Pharmacology 67, 285 (2004) 
  16. Kolars, J. C., Schmiedlin-Ren, P., Dobbins, W. O. 3rd., Schuetz, J., Wrighton, S. A. and Watkins, P. B. : Heterogeneity of cytochrome P450IIIA expression in rat. gut epithelia. Gastroenterology 102, 1186 (1992) 
  17. Watkins, P. B., Wrighton, S. A., Schuetz, E. G., Molowa, D. T. and Guzelian, P. S. : Identification of glucocorticoid-inducible cytochromes P-450 in the intestinal mucosa of rats and man. J. Clin. Invest. 80, 1029 (1987) 
  18. Saeki, T., Ueda, K., Tanigawara, Y., Hori, R. and Komano, T. : P-glycoprotein-mediated transcellular transport of MDRreversing agents. FEBS Lett. 324, 99 (1993) 
  19. Plosker, G. L. and Wagstaff, A. J. : Fluvastatin: a review of its pharmacology and use in the management of hypercholesterolaemia. Drugs. 51, 433 (1996) 
  20. Mc Donnell, C. G., Shorten, G. and Van Pelt, F. N. : Effect of atorvastatin and fluvastatin on the metabolism of midazolam by cytochrome P450 in vitro. Anaesthesia. 60, 747 (2005) 
  21. Ruilope, L. M. and Alcaar, J. M. : Renal effects of calcium entry blockers. Cardiovas. Drugs Ther. 4, 979 (1990) 
  22. Langtry, H. D. and Markham, A. : Fluvastatin: a review of its use in lipid disorders. Drugs. 57, 583 (1999) 
  23. Fische, V., Johanson, L. and Heitzl, F. : The 3-hydroxy-3- methylglutaryl coenzyme A reductase inhibitor fluvastatin: effect on human cytochrome P-450 and implications for metabolic drug interactions. Drug. Metab. Dispos. 27, 410 (1999) 
  24. Kirchheiner, J. and Brockmoller, J. : Clinical consequences of cytochrome P450 2C9 polymorphisms. Clin. Pharmacol. Ther. 77, 1 (2005) 
  25. Lefebvre, M., Homsy, W., Caille, G. and du Souich, P. : Firstpass metabolism of diltiazem in anesthetized rabbits: Role of extrahepatic organs. Pharm. Res. 13, 124 (1996) 
  26. Jean-Paul, D. : Clinical implications of the biopharmaceutical properties of fluvastatin. The American Journal of Cardiology 73, 12 (1994) 
  27. Chaudhary, P. M. and Robinson, I. B. : Expression and activity of P-glycoprotein, a multidrug efflux pump, in human hematopoietic stem cells. Cell. 66, 85 (1991) 
  28. Fruehauf, J. P. and Manetta, A. : Use of extreme drug resistance assay to evaluate mechanisms of resistance in ovarian cancer: Taxol resistance and MDR1 expression. Contrib. Gynecol. Obstet. 19, 39 (1994) 
  29. Van Asperen, J., Van Tellingen, O., Sparreboom, A., Schinkel, A. H., Borst, P., Nooijen, W. J. and Beijnen, J. H. : Enhanced oral bilavailability of diltiazem in mice treated with the pglycoprotein blocker SDZ PSC 833. Br. J. Cancer 76, 1181 (1997) 
  30. Chaffman, M. and Brogden, R. N. : Diltiazem: a review of its pharmacological properties and therapeutic efficacy. Drugs. 29, 387 (1985) 
  31. Weir, M. R. : Diltiazem ten years of clinical experience in the treatment of hypertension. J. Clin. Pharmacol. 35, 220 (1995) 
  32. Scholz, H. : Pharmacological aspects of calcium channel blockers. Cardiovas. Drugs Ther. 10, 869 (1997) 
  33. Sterzel, P. B. : Renal actions of calcium antagonists. J. Cardiovas. Pharmacol. 10, 17 (1987) 
  34. Bogman, K., Peyer, A. K., Torok, M., Kusters, E. and Drewe, J. : HMG-CoA reductase inhibitors and P-glycoprotein modulation. Br. J. Pharmacol. 132, 1183 (2001) 
  35. Yeung, P. K., Prescott, C., Haddad, C., Montague, T. J., McGregor, C., Quilliam, M. A., Xei, M., Li, R., Farmer, P. and Klassen, G. A. : Pharmacokinetics and metabolism of diltiazem in healthy males and females following a single oral dose. Eur. J. Drug. Metab. Pharmacokinet. 18, 199 (1993) 
  36. Ford, J. M. : Modulators of multidrug resistancepreclinical studies. Hematol. Oncol. Clin. N. Am. 9, 337 (1995) 
  37. Klaassen, C. D. : Toxicology. 5th ed. New York: McGraw-Hill. 113 (1999) 

이 논문을 인용한 문헌 (0)

  1. 이 논문을 인용한 문헌 없음

원문보기

원문 PDF 다운로드

  • ScienceON :

원문 URL 링크

원문 PDF 파일 및 링크정보가 존재하지 않을 경우 KISTI DDS 시스템에서 제공하는 원문복사서비스를 사용할 수 있습니다. (원문복사서비스 안내 바로 가기)

상세조회 0건 원문조회 0건

DOI 인용 스타일