Ehsan Zamani - Department of Pharmacology and Toxicology, School of Pharmacy, Guilan University of Medical Sciences, Rasht, Iran.
Saba Mahboubi - Student Research Committee, School of Pharmacy, Guilan University of Medical Sciences, Rasht, Iran.
Mehdi Evazalipour - Department of Pharmaceutical Biotechnology, School of Pharmacy, Guilan University of Medical Sciences, Rasht, Iran.

Background: Chlorpheniramine is an H۱ receptor inverse agonist, which belongs to the first-generation class. It is generally regarded as a strong antihistamine with a wide variety of indications in allergic and non-allergic diseases. The extensive consumption of chlorpheniramine might culminate in less evident adverse effects, such as genotoxicity. Objectives: In this study, we attempted to assess the possible potential of chlorpheniramine in inducing genotoxicity.  Methods: Human lymphocytes were separated into groups as follows: control group (Phosphate Buffered saline), Chlorpheniramine group (۰.۱, ۰.۵, ۰.۷۵, ۱.۵ mM), and Positive control group (cisplatin ۰.۴ µg/mL). After ۲۴ hours of incubation, we conducted an alkaline comet assay to evaluate the DNA damage. Also, oxidative stress damage was evaluated by the levels of lipid peroxidation and glutathione oxidation. Results: Significant increases were observed in DNA percentage in tail and tail moment at high concentration (۱.۵mM, P<۰.۰۵). Likewise, at the same concentration, the MDA levels increased significantly in addition to the significant depletion in the level of glutathione. Conclusion: High concentration of chlorpheniramine significantly induced genotoxicity in human lymphocytes. In addition, we showed that oxidative stress was one of the mechanisms elaborated in chlorpheniramine genotoxicity at high concentrations.

Chlorpheniramine, Oxidative stress, Genotoxicity, Lymphocytes, Comet assay.