Tabriz University of Medical Sciences About    Newsletter    Contact Us    Create Account    Log in  
Advanced Pharmaceutical Bulletin
ISSN: 2228-5881      eISSN: 2251-7308  
Services
Export citation
EndNote
Reference Manager
BibTeX
Medlars
Refworks
Mendeley

Cite by
Google Scholar
PMC(0)


Article History
Submitted: 31 Dec 2015
Revised: 03 Feb 2016
Accepted: 09 Mar 2016
First published online: 17 Mar 2016

Article Access Statistics
Abstract Page Views: 371
PDF Downloads: 217
Full Text Views: 0

Adv Pharm Bull. 2016;6(1):111-118 doi: 10.15171/apb.2016.017
PMID:27123426        PMCID:PMC4845543

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

Original Research

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.



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.





Comments
First name  
Last name  
Email address  
Comments  
Security code



This Article
PDF

Google Scholar
Articles by Mesgari Abbasi M
Articles by Valizadeh H
Articles by Hamishekar H
Articles by Mohammadnejad L
Articles by Zakeri-Milani P

PubMed
Articles by Mesgari Abbasi M
Articles by Valizadeh H
Articles by Hamishekar H
Articles by Mohammadnejad L
Articles by Zakeri-Milani P

Similar articles in PubMed

Share this article!

Press Manuscript Online. Powered by MAADRAYAN