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Does anyone have any information on how to predict whether or not a drug
is high or low extraction ?
I am trying to determine what the consequences of a decrease in hepatic
perfusion (CHF) will have on a drug that is eliminated almost entirely
via hepatic metabolism.
any help would be appreciated ...
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Christopher Houle wrote:
>
> PharmPK - Discussions about Pharmacokinetics
> Pharmacodynamics and related topics
>
> Does anyone have any information on how to predict whether or not a drug
> is high or low extraction ?
>
> I am trying to determine what the consequences of a decrease in hepatic
> perfusion (CHF) will have on a drug that is eliminated almost entirely
> via hepatic metabolism.
>
> any help would be appreciated ...
>
> Also see: http://www.cpb.uokhsc.edu/pkin/pkin.html
>
hey chris,
Trying to get other people to do your work for you again huh?
Just kidding. I think a high partition coefficient is a hint that a
drug will be a high extraction drug. e.g. Propranolol, lidocaine etc.
Hope you get better answers than this one though. good luck!
Steve
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! PharmPK - Discussions about Pharmacokinetics
! Pharmacodynamics and related topics
!
! Does anyone have any information on how to predict whether or not a drug
! is high or low extraction ?
!
! I am trying to determine what the consequences of a decrease in hepatic
! perfusion (CHF) will have on a drug that is eliminated almost entirely
! via hepatic metabolism.
!
! any help would be appreciated ...
!
! Also see: http://www.cpb.uokhsc.edu/pkin/pkin.html
!
There are 2 papers which might help you. They show the usefulness of
hepatocytes or liver microsomes (rat and human) to classify compounds into
Low/Int/High hepatic extraction ratio, based on their in vitro metabolic
stability :
J. B. Houston, Biochem. Pharmacol. 47, 1469-1479, 1994
Th. Lave et al., Pharm. Res., 14, 152-155, 1997
I hope this info can be helpful
Regards
Thierry Lave
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