Adv Pharm Bull. 2016;6(1):111-118.
doi: 10.15171/apb.2016.017
PMID: 27123426
PMCID: PMC4845543
Scopus id: 84962343644
  Abstract View: 552
  PDF Download: 335

Original Research

The Effects of Cetirizine on P-glycoprotein Expression and Function In vitro and In situ

Mehran Mesgari Abbasi 1,2, Hadi Valizadeh 1, Hamed Hamishekar 1, Leila Mohammadnejad 3, Parvin Zakeri-Milani 4 *

1 Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
2 Students Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
3 Immunology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
4 Liver and Gastrointestinal Diseases Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.


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.
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