Mesgari Abbasi, Mehran and Valizadeh, Hadi and Hamishekar, Hamed and Mohammadnejad, Leila and Zakeri-Milani, Parvin (2016) The Effects of Cetirizine on P-glycoprotein Expression and Function In vitro and In situ. Advanced Pharmaceutical Bulletin, 6 (1). pp. 111-118. ISSN 2228-5881
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Abstract
Purpose: P-glycoprotein (P-gp) plays a major role in oral absorption of drugs. Induction or inhibition of P-gp by drugs contributes to variability of its transport activity and often results in clinically relevant drug-drug interactions. The purpose of this study was to investigate the effect of cetirizine, a second generation H1 antihistamine, on P-gp function and expression in vitro and in situ. Methods: The in-vitro rhodamin-123 (Rho123) efflux assay in Caco-2 cells was used to study the effect of cetirizine on P-gp function. Western blot analysis was used for surveying the effect of cetirizine on expression of P-gp in Caco-2 cells. Rat in situ single-pass intestinal permeability technique was used to calculate the intestinal permeability of a known P-gp substrate (digoxin) in the presence of cetirizine. The amounts of digoxin and cetirizine in intestinal perfusion samples were analyzed using a HPLC method. Results: The results showed significant increase in Rho123 uptake (P < 0.05) and also P-gp band intensity decrease in cetirizine-treated cells in vitro. Furthermore the intestinal permeability of digoxin was also increased significantly in the presence of cetirizine (P < 0.01). Conclusion: Therefore it is concluded that cetirizine is a P-gp inhibitor and this should be considered in co administration of cetrizine with other P-gp substrate drugs. Further investigations are required to confirm our results and to determine the mechanism underlying P-gp inhibition by cetirizine.
Item Type: | Article |
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Subjects: | STM Digital > Medical Science |
Depositing User: | Unnamed user with email support@stmdigital.org |
Date Deposited: | 19 Apr 2023 08:57 |
Last Modified: | 06 Jul 2024 08:03 |
URI: | http://research.asianarticleeprint.com/id/eprint/612 |