PharmPK Discussion - Ki inhibitor constant (part II)

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On 27 Oct 1997 at 10:49:36, "Alex Hemeryck" (Alex.Hemeryck.-at-.rug.ac.be) sent the message


Dear reader,

In reply to the answers I receaved, i would like to ask the following
question:

Fluoxetine and paroxetine are known as potent inhibitors of CYP2D6
substrates. Ki value's in the range of 0.1 - 1 M are found in the
literature for CYP2D6-substrates such as desipramine.  Also in vivo
interactions between these two SSRI's and CYP2D6 substrates have been
described. In fact these interactions could be predicted from the Ki
value of the SSRI, in combination with its plasma levels and
plasma:liver partition coefficient.
Suppose one finds a Ki value of the SSRI's for another substrate
studied, wich is ten times higher than for desipramine (due to the
fact that the substrate studied has a much lower Km than
desipramine), what should be expected  in vivo for this new substrate
?

My best regards,

Alex

**********************************
Alex Hemeryck
Pharmacist
Heymans Institute of Pharmacology
University of Ghent
Medical School
De Pintelaan 185
B-9000 Gent
Tel: +32-9-2403370
Fax: +32-9-2404988
e-mail: Alex.Hemeryck.aaa.rug.ac.be
**********************************

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