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The following message was posted to: PharmPK
Dear All,
I am doing a studies on an NCE which we are suspecting to be a P-gp
substrate.Idecided toperform an in vivo study byco-administering a
P-gpinhibitor. I selected verapamil as the inhibitor. I administered
verapamil intravenously to male Wistar rats at 5 mg/Kg and after5 min
I have givenour compound under test through oral route. Finally I
foundstatistically significant difference betweenverapamil pretreated
and verapamil untreated group.
NowIam planning to give the P-gp inhibitor orallyand the compound
under test also through the same route and check the effect of the
inhibitor on the compound's systemic exposure. But I am notable to
know at what dose I should administer verapamil orally to Wistar
rats.If any body is knowing the doseI request you to pass it on to me.
Regards,
Ravi Kanth Bhamidipati
Ravi Kanth Bhamidipati
Senior Pharmacologist
Dept.of Drug Metabolism and Pharmacokinetics
Discovery Research Division
Dr.Reddy's Laboratories Ltd.
Bollaram Road , Miyapur
Hyderabad - 500 050
Andhra Pradesh
India
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The following message was posted to: PharmPK
Dr.Ravikanth,
In P-gp studies in rats , verpamil is admisnistered in
a per body weight basis than absolute micro- or
millimolar concentrations.( approximately 5 mg/kg by
oral gavage preferrably ).
More details can be found in the following reference :
Intestinal secretion is a major route for parent
ivermectin elimination in the rat.
Drug Metab Dispos 2002 Jun;30(6):626-30
Laffont CM, Toutain PL, Alvinerie M, Bousquet-Melou A.
Regards,
Santosh
Doctoral Student
College of Pharmacy
Department of Pharmaceutical Sciences ( Biopharmaceutics)
University of Cincinnati Medical center
3223, Eden Avenue
Cincinnati , OH 45267-004
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The following message was posted to: PharmPK
Dear Santosh,
As I am planning to give verapamil (P-gp inhibitor) orally, can I go
for co-administration or should I administer verapamil few minutes
before the administration of compound under test.
Regards,
Ravi Kanth Bhamidipati
Senior Pharmacologist
Dept.of Drug Metabolism and Pharmacokinetics
Discovery Research Division
Dr.Reddy's Laboratories Ltd.
Bollaram Road , Miyapur
Hyderabad - 500 050
Andhra Pradesh
India
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The following message was posted to: PharmPK
Dr.Ravi,
1) Verapamil can be used at a dose of 20 mg / kg orally in Rats.
2) One can administer it together with the test compound or 15 minutes
prior to test drug.
3) We have made a time response effect in our lab with Verapamil and 15
minutes pretreatment gives us an optimal response.
Yati Chugh Ph.D
Wockhardt Research Centre
Aurangabad.
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