The Resource P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of HIV-protease inhibitor, ritonavir, and its interaction with pure herbal constituents, by Jignesh Patel, (electronic resource)

P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of HIV-protease inhibitor, ritonavir, and its interaction with pure herbal constituents, by Jignesh Patel, (electronic resource)

Label
P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of HIV-protease inhibitor, ritonavir, and its interaction with pure herbal constituents
Title
P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of HIV-protease inhibitor, ritonavir, and its interaction with pure herbal constituents
Statement of responsibility
by Jignesh Patel
Creator
Contributor
Thesis advisor
Subject
Genre
Language
eng
Summary
Part-I. Simultaneous efflux, mediated by P-gp and metabolism mediated by CYP3A4 constitute a highly efficient barrier to oral anti-HIV therapy. Furthermore, P-gp mediated efflux from HIV sanctuary sites, like lungs, necessities the development of mechanistic insights that allows us to predict the drug-drug interactions, extent of first pass clearance, and bioavailability of orally administered anti-HIV drugs. Hence, a novel, absorption-metabolism classification system (AMCS) has been proposed to classify all currently marketed anti-HIV drugs based on their specificities towards P-gp and CYP3A4. A theoretical model, explaining interactions of P-gp-mediated efflux and CYP3A4-mediated metabolism within or amongst various AMCS classes of anti-HIV agents, has been thus developed and validated using HIV-protease inhibitor{u2014}ritonavir as a model drug. Various interactions involving anti-retroviral agents from different classes of AMCS were determined using 1Ü, 25-dihydroxy vitamin D3 treated Caco-2 and Calu-3 cells, expressing enhanced levels of P-gp, representing intestinal and alveolar barriers respectively. Part-II. The purpose of this study is to determine various efflux and metabolism interactions of HIV-protease inhibitors with purified herbal constituents and thereby to delineate the factors responsible for altered oral bioavailability of HIV-protease inhibitors taken along with complimentary and alternative medicine (CAM). A major population of the United States, detected with HIV, uses CAM to overcome their mental and physiological instability. HIV-protease inhibitors and herbal agents are reported to interact with P-gp as well as CYP3A4. Various harmful as well as beneficial interactions have been reported between herbal agents and anti-HIV drugs. In order to avoid the discrepancies reported in clinical and in vivo studies, an in vitro pharmacokinetic and metabolic characterization of pure constituents of herbal products [St John's Wort (hypericin, hyperforin, and quercetin), ginseng (kaempferol), milk-thistle (silibinin) and garlic (allicin)] was performed with ritonavir as a model drug. Induction profile on the expression of P-gp and CYP3A4 on prolonged exposure of these pure herbal constituents to Caco-2 cells was also established using appropriate molecular biology techniques
Additional physical form
Online version of the print edition.
Cataloging source
UMK
http://library.link/vocab/creatorDate
1973-
http://library.link/vocab/creatorName
Patel, Jignesh
Degree
Ph. D.
Dissertation year
2004.
Granting institution
School of Pharmacy and Dept. of Chemistry. University of Missouri--Kansas City
Index
no index present
Literary form
non fiction
Nature of contents
  • dictionaries
  • bibliography
  • theses
http://library.link/vocab/relatedWorkOrContributorDate
1954-
http://library.link/vocab/relatedWorkOrContributorName
Mitra, Ashim K.
http://library.link/vocab/subjectName
  • Cytochrome P-450
  • P-glycoprotein
  • Protease inhibitors
  • Herbs
  • Drug interactions
  • Drugs
  • Pharmacokinetics
  • HIV (Viruses)
Label
P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of HIV-protease inhibitor, ritonavir, and its interaction with pure herbal constituents, by Jignesh Patel, (electronic resource)
Instantiates
Publication
Note
  • "A dissertation in pharmaceutical science and chemistry."
  • Advisor: Ashim K. Mitra
  • Typescript
  • Vita
  • Title from "catalog record" of the print edition
  • Description based on contents viewed Feb. 27, 2006
Bibliography note
Includes bibliographical references (leaves 175-199)
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier.
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent.
Contents
Literature review -- Coordinated functions of P-gp and CYP3A4 in simultaneous efflux and metabolism of HIV-protease inhibitor, ritonavir, across cultured epithelial cells -- Efflux of HIV-protease inhibitors across P-glycoprotein induced 1[alpha], 25 di-hydroxy vitamin D3 treated calu-3 cell monolayers -- Mathematical model to explain the co-ordinated functions of efflux and metabolism limiting the transport of anti-HIV agents across intestinal epithelium -- Correlation of in vitro ritonavir efflux and metabolism with bioavailability in male Sprague-Dawley rats -- An integrated in vitro technology for the simultaneous assessment of absorption and metabolism of drugs -- Interactions of pure herbal constituents with P-gp and CYP3A4 -- In vitro interaction of HIV-protease inhibitor, ritonavir, with herbal constituents: changes in P-gp and CYP3A4 activity -- Summary and recommendations
Control code
69649017
Dimensions
28 cm.
Extent
xviii, 199 leaves
Form of item
electronic
Media category
computer
Media MARC source
rdamedia.
Media type code
  • c
Other physical details
illustrations
Reproduction note
Electronic reproduction.
Specific material designation
remote
Label
P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of HIV-protease inhibitor, ritonavir, and its interaction with pure herbal constituents, by Jignesh Patel, (electronic resource)
Publication
Note
  • "A dissertation in pharmaceutical science and chemistry."
  • Advisor: Ashim K. Mitra
  • Typescript
  • Vita
  • Title from "catalog record" of the print edition
  • Description based on contents viewed Feb. 27, 2006
Bibliography note
Includes bibliographical references (leaves 175-199)
Carrier category
online resource
Carrier category code
  • cr
Carrier MARC source
rdacarrier.
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent.
Contents
Literature review -- Coordinated functions of P-gp and CYP3A4 in simultaneous efflux and metabolism of HIV-protease inhibitor, ritonavir, across cultured epithelial cells -- Efflux of HIV-protease inhibitors across P-glycoprotein induced 1[alpha], 25 di-hydroxy vitamin D3 treated calu-3 cell monolayers -- Mathematical model to explain the co-ordinated functions of efflux and metabolism limiting the transport of anti-HIV agents across intestinal epithelium -- Correlation of in vitro ritonavir efflux and metabolism with bioavailability in male Sprague-Dawley rats -- An integrated in vitro technology for the simultaneous assessment of absorption and metabolism of drugs -- Interactions of pure herbal constituents with P-gp and CYP3A4 -- In vitro interaction of HIV-protease inhibitor, ritonavir, with herbal constituents: changes in P-gp and CYP3A4 activity -- Summary and recommendations
Control code
69649017
Dimensions
28 cm.
Extent
xviii, 199 leaves
Form of item
electronic
Media category
computer
Media MARC source
rdamedia.
Media type code
  • c
Other physical details
illustrations
Reproduction note
Electronic reproduction.
Specific material designation
remote

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