The Effects of Cetirizine on P-glycoprotein Expression and Function In vitro and In situ
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…
Read the paper
Related studies
- Artificial Intelligence in Medicine: Cross-Sectional Study Among Medical Students on Application, Education, and Ethical Aspects
- Information quality of videos related to esophageal cancer on tiktok, kwai, and bilibili: a cross-sectional study
- The quality and reliability of short videos about hypertension on TikTok: a cross-sectional study
- Quality and reliability evaluation of pancreatic cancer-related video content on social short video platforms: a cross-sectional study
- Quality and reliability of pediatric pneumonia related short videos on mainstream platforms: cross-sectional study
- Association between metabolic score for insulin resistance (METS-IR) and hypertension: a cross-sectional study based on NHANES 2007–2018
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.