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Dear all,
I plan to develop a theoretical PK model for compounds showing
nonlinear bioavailability due to saturation of the first pass effect.
The main characteristic of these compounds would be increased
bioavailability with increasing oral dose. Do you know of any
compounds that have this property? Feel free to write to me directly.
Thanks!
Toufigh Gordi
[Salicylamide - http://www.boomer.org/c/p4/c03/c0325.html - db]
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The following message was posted to: PharmPK
Toufigh,
> The main characteristic of these compounds would be increased
> bioavailability with increasing oral dose. Do you know of any
> compounds that have this property?
Perhaps the most widely consumed drug in the world -- ethanol :-)
See
http://www.health.auckland.ac.nz/pharmacology/staff/nholford/
Ethanol_PKPD
for some literature references and a free Excel spreadsheet that
models this kind of process.
Nick
--
Nick Holford, Dept Pharmacology & Clinical Pharmacology
University of Auckland, 85 Park Rd, Private Bag 92019, Auckland, New
Zealand
n.holford.-at-.auckland.ac.nz tel:+64(9)373-7599x86730 fax:+64(9)373-7090
www.health.auckland.ac.nz/pharmacology/staff/nholford
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Hi Toufigh:
You may wish to consider nicardipine, which was described by Wagner
et al. in: Biopharm Drug Dispos. 1987 Mar-Apr;8(2):133-48. Single
intravenous dose and steady-state oral dose pharmacokinetics of
nicardipine in healthy subjects.
Joe
**************************************************
Joseph P. Balthasar, Ph.D.
Associate Professor & Director of Graduate Studies
457B Cooke Hall
Department of Pharmaceutical Sciences
School of Pharmacy and Pharmaceutical Sciences
University at Buffalo
The State University of New York
Buffalo, New York 14260
website: http://www.acsu.buffalo.edu/~jb/
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Propranolol is also a useful clinical example with decreasing
first pass with increasing oral doses.........Dan Sitar
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Hi Toufigh:
Phenytoin is a classic example for this kind of pharmacokinetics.
Madhu
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