PharmPK Discussion - Interactant drugs for in vivo inhibition of renal organic and cation clearance

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On 27 Nov 2003 at 17:41:07, SBOOM.aaa.PRDBE.jnj.com sent the message


Dear collegues,

I'm setting up a study in humans to investigate interaction for renal
excretion. The drug has affinity for both organic cation and anion
transport, no pgp known. What would be the best and most specific in
vivo interactant drugs for 1. the OAT (organic anion transporter) and
2. OCT (organic cation transporter)?

Best regards, Sandra Boom

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On 29 Nov 2003 at 09:50:24, "sajjad desai" (drsdesai.-a-.rediffmail.com) sent the message


Hello Sandra Boom
Here is the list of in-vivo interactant drugs for OAT and OCT
1)OAT - Acetylesalicylate ,
         Indomethacin,Bumetanide,Furosemide,Methotrexate,Valproate
2)OCT - Amiloride,Atropine,Cimetidine,Morphine,Procaine,Quinine as well
         some cytostatic agents.
Thanks and Regards
Dr.Sajjad A. Desai

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On 29 Nov 2003 at 11:18:52, "Paul Beringer" (beringer.-at-.usc.edu) sent the message


The following message was posted to: PharmPK

Since you are proposing to conduct the study in humans, the safety
profile of the both the inhibitor compound and the drug of interest will
be important. The safety profile of probenecid (inhibitor of OAT) and
cimetidine (inhibitor of OCT) are well known. You mentioned that your
compound is not a P-gp substrate; however, is it a substrate for MRP? A
three-way crossover design would be ideal to separate out the relative
contributions of the transporters to the renal clearance of your
compound.

A detailed summary of renal drug transporters and substrate/inhibitor
compounds has recently been published:

Lee Wooin, Kim R. Transporters and renal drug elimination. Annu Rev
Pharmacol Toxicol. Online publication Aug 2003.

Paul Beringer, Pharm.D.

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