Role of P-glycoprotein in tissue uptake of indinavir in rat

Hamidi, Mehrdad

doi:10.1016/j.lfs.2006.05.010

Cited by 26 publications

(22 citation statements)

References 34 publications

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“…This Kim et al, 1998b;Koudriakova et al, 1998;Lee et al, 1998;Hugen et al, 2000;Zhang et al, 2000;Hochman et al, 2001;van der Sandt et al, 2001;Huisman et al, 2002;Campbell et al, 2004;Jorajuria et al, 2004;Hamidi, 2006;Jung et al, 2008;Annaert et al, 2010 …”

Section: Table 2 List Of the Main Drug Metabolism Enzymes (Cyp450 Andunclassified

The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition

et al. 2012

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Section: Table 2 List Of the Main Drug Metabolism Enzymes (Cyp450 Andunclassified

The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition

et al. 2012

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“…Tissue distribution of P-gp has been studied extensively in human and rodents. The P-gp localization in the epithelial cells of GI tract, canalicular cells of the liver, placenta, kidney, and the BBB has been shown, both structurally and functionally, each having significant roles in pharmacokinetic profiles of different drugs (13,14).…”

Section: Introductionmentioning

confidence: 99%

Lack of Evidence for Involvement of P-Glycoprotein in Brain Uptake of the Centrally Acting Analgesic, Tramadol in the Rat

et al. 2012

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-Purpose. Tramadol Hydrochloride is a widely-used centrally acting analgesic drug, which has some features of being a P-gp substrate. The present study evaluates the functional involvement of Pgp in CNS distribution of tramadol. Methods. The possibe involvement of P-glycoprotein in brain distribution of tramadol was evaluated using a pharmacokinetic approach in two groups of Pgp-inhibited and control rats. Six male Sprague-Dawley rats were used in each group to collect plasma and brain at 1, 5, 10, and 30 min following two tramadol doses of 1 and 10 mg/kg. Results. The brain uptake clearances of tramadol in Pgp-inhibited and control rats were 2.47±0.56 and 2.34±0.56 ml min , respectively, for 10 mg/kg dose. The brain-to-plasma concentration ratio (Kp,app) of more than 1 in all the time points following both the high and low dose cases (sometimes more than 3) indicated the brain accumulation of the drug. Linear correlation was found between tramadol dose and both corresponding plasma and brain concentrations, but the presence of a dose-dependency was not confirmed by the data obtained for brain-to-plasma concentration ratio. Conclusion. Considering the results of the previous studies and the present research, it seems that the brain accumulation of tramadol is not affected by P-gp inhibition which implies that there may be some other transport mechanisms involved in BBB transport of tramadol.

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“…Active efflux transport, carrier mediated transport, receptor mediated transport and adsorptive mediated transport that mediate the transport of endogenous substances across the blood brain barrier have been exploited for specific delivery of drugs into brain. Among various strategies, brain levels can be improved by administration of a Pgp inhibitor, Valspodar (PSC833) along with drug [11] and encapsulation of the drug in nanosized colloidal carrier would by pass the Pgp efflux system [12].…”

Section: Introductionmentioning

confidence: 99%

Brain delivery of transferrin coupled indinavir submicron lipid emulsions—Pharmacokinetics and tissue distribution

Kandadi

Afzal

Kumar

et al. 2011

Colloids and Surfaces B: Biointerfaces

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Role of P-glycoprotein in tissue uptake of indinavir in rat

Cited by 26 publications

References 34 publications

The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition

The Dual Role of Pharmacogenetics in HIV Treatment: Mutations and Polymorphisms Regulating Antiretroviral Drug Resistance and Disposition

Lack of Evidence for Involvement of P-Glycoprotein in Brain Uptake of the Centrally Acting Analgesic, Tramadol in the Rat

Brain delivery of transferrin coupled indinavir submicron lipid emulsions—Pharmacokinetics and tissue distribution

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