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2000 Fiscal Year Final Research Report Summary

Analysis of factors on variations in serum levels of protease inhibitors

Research Project

Project/Area Number 11672268
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field 応用薬理学・医療系薬学
Research InstitutionMiyazaki Medical College

Principal Investigator

ARIMORI Kazuhiko  Miyazaki Medical College, Pharmacy, Professor, 医学部, 教授 (70253739)

Co-Investigator(Kenkyū-buntansha) NAKANO Masahiro  Kumamoto University Hospital, Pharmacy, Professor, 医学部・附属病院, 教授 (40002125)
Project Period (FY) 1999 – 2000
Keywordsprotease inhibitor / therapeutic drug monitoring / nelfinavir / ritonavir / saquinavir / phenytoin / p-glycoprotein / AIDS
Research Abstract

The aim of the present study was to elucidate the factors on variations in serum levels of protease inhibitors in human immunodeficiency virus (HIV) infected patients. We determined the serum levels of two protease inhibitors, nelfinavir and saquinavir, in HIV infected patients who took many kinds of drugs. There was great individual variation in the serum levels of the protease inhibitors, probably due to the interaction with co-administered drugs or hepatic dysfunction. In a case of a patient taking phenytoin and nelfinavir, the reduced nelfinavir levels in the serum was attributed to the induction of cytochrome P-450- 3A .
The interaction of HIV protease inhibitors and HIV reverse transcriptase inhibitors was investigated in in-vitro study using L-MDR1 and L-mdr1a cell line, P- glycoprotein (P-gp) overexpressing cell. It was confirmed that saquinavir, ritonavir and nelfinavir were all a substrate for P-gp. Nelfinavir and ritonavir also were an inhibitor for P-gp, whereas other protease inhibitors (saquinavir, indinavir and amprenavir) and five nucleoside reverse transcriptase inhibitors (zidovudine, didanosine, zalcitabine, stavudine and lamivudine) were not. Ritonavir and saquinavir slightly inhibited the function of MRP which is an efflux-transporter as well as P-gp. These results provide useful informations for the treatment of HIV infected patients receiving a combination therapy of protease inhibitors.

  • Research Products

    (4 results)

All Other

All Publications (4 results)

  • [Publications] 藤井淳子 他: "抗HIV薬における血中薬物濃度モニタリング(TDM)の試み"九州薬学会会報. 54. 65-68 (2000)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Shiraki N. et al.: "Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins"Biol.Pharm.Bull.. 23. 1528-1531 (2000)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Junko Fujii et al.: "Attempts at therapeutic drug monitoring of anti-HIV drugs."Kyushu-Yakugakkai-Kaiho. 54. 65-68 (2000)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Shiraki N.et al.: "Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins"Biol.Pharm.Bull.. 23. 1528-1531 (2000)

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 2002-03-26  

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