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The following message was posted to: PharmPK
Hello
I am trying to identify a relatively specific CYP3A probe with no
sedative activity. I know Benzodiazepines including midazolam are
commonly used at doses 1-5 mg oral or iv for this purpose but given the
possibility of sedation excludes midazolam from being used in an
outpatient setting. My MD collaborators feel that if we administer
midazolam to patients, we must monitor the patients continuously in a
hospital bed for 2 hours after the dose which will make the study very
costly. The questions are:
1. Are there any other none Benzodiazepine specific CYP3A probes that
can be used instead of midazolam?
2. Have you ever used midazolam outside of a clinical research unit or
an inpatient hospital setting?
I would appreciate any information and/or insights.
Regards
Fatemeh Akhlaghi, PharmD, PhD
Assistant Professor
Biomedical and Pharmaceutical Sciences (BPS)
University of Rhode Island
125 Fogarty Hall, 41 Lower College Road
Kingston, RI 02881
USA
Phone: (401) 874 9205
Fax: (401) 874 2181
Email: fatemeh.at.uri.edu
Laboratory Website:
http://www.uri.edu/pharmacy/faculty/aps/akhlaghi/index
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The following message was posted to: PharmPK
The most important putative CYP3A4 probes used are erthyromycin,
cortisol,
dapsone and off course midazolam. It really depends on the nature of
study
to measure the activity of CYP3A4 whether its in intestine, liver or
kidney. The contribution of CYP3A5 in the human kidney tissues also
creates potential problem concerning urine based test of CYP3A4. Any
further comments on known specific substrates for CYP3A4 and CYP3A5
would
be appreciated. The erythromycin breath test (ERMBT) for measuring the
in
vivo CYP3A4 activity can be considered. The more information on this
technique can be obtained by searching Paul B Watkins papers.
Warmest regards,
Raj
Rajinder K Bhardwaj, Ph.D.
Department of Pharmaceutics
Ernest Mario School of Pharmacy
Rutgers, The State University of New Jersey
160 Frelinghuysen Road
Piscataway, NJ 08854
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The following message was posted to: PharmPK
Hello,
I suggest to you to use 6-beta hydroxycortisol/
cortisol ratio as a marker in urine to estimate
activity of 3A4.
Dr Ehab S EL Desoky
Pharmacology Dept
Faculty of Medicine
Assiut University.
Assiut, Egypt
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