COMPARATIVE EVALUATION OF CNS DEPRESSIVE ACTIVITY OF CHLORPHENIRAMINE MALEATE AND EBASTINE IN WISTAR RATS USING ROTARAD AND PHOTOACTOMETER

Authors

  • LENIN R. Department of Pharmacology, Govt Villupuram Medical College, Villupuram, Tamilnadu, India
  • UMAMAHESHWARI C. Department of Pharmacology, Govt Villupuram Medical College, Villupuram, Tamilnadu, India
  • RAJARAM G. Department of Pharmacology, Govt Villupuram Medical College, Villupuram, Tamilnadu, India

DOI:

https://doi.org/10.22159/ijcpr.2026v18i1.8030

Keywords:

Chlorpheniramine maleate, CNS depression, Ebastine, Photoactometer, Rotarod, Wistar rats

Abstract

Objective: Allergic conditions are commonly treated with Antihistamines. Though the first-generation H1 antihistamines like Chlorpheniramine Maleate (CPM) are effective, they can cause sedation because of its blood-brain barrier crossing capacity leading to central nervous system (CNS) depression. But Ebastine, a 2nd-generation H1 antihistamine, is considered to be a non-sedating drug because of its limited CNS penetration. Hence, evaluating the CNS effects of these drugs is crucial for guiding safe and rational clinical practice. Aim of this study was to compare the CNS depressant effects of Chlorpheniramine Maleate and Ebastine in Wistar rats using Rotarod and Photoactometer behavioral models.

Methods: This was a prospective cross-sectional study conducted at Department of Pharmacology, Government Villupuram Medical College and Hospital, Villupuram, Tamilnadu, India between January to June 2025. Eighteen adult Wistar rats were randomly assigned into three groups, with 6 rats in each group viz, Group 1: Control rats receiving Normal saline, Group 2: rats receiving CPM and Group 3: rats receiving Ebastine. CNS activity was assessed 60 min after drug administration. Motor coordination was measured using the Rotarod test and locomotor activity was assessed using a digital photoactometer. Data were analyzed using one-way ANOVA followed by Tukey’s post hoc test.

Results: Chlorpheniramine Maleate significantly reduced the fall-off time on the Rotarod (71.6±7.8 sec) and decreased locomotor activity (124.2±14.8 counts), indicating CNS depression (p<0.01). Ebastine-treated rats showed no significant difference in either parameter compared to the control group (fall-off time: 139.7±12.6 sec; locomotor activity: 284.4±19.2 counts).

Conclusion: Chlorpheniramine Maleate produces significant CNS depressant activity while Ebastine does not impair motor coordination or spontaneous activity in rats. These findings support the evidence that Ebastine as a non-sedating antihistamine and favor its use in clinical practice where sedation is undesirable.

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References

1. Simons FE. Advances in H1-antihistamines. N Engl J Med. 2004;351(21):2203-17. doi: 10.1056/NEJMra033121, PMID 15548781.

2. Church MK, Maurer M, Simons FE, Bindslev Jensen C, Van Cauwenberge P, Bousquet J. Risk of first-generation H(1)-antihistamines: a GA(2)LEN position paper. Allergy. 2010;65(4):459-66. doi: 10.1111/j.1398-9995.2009.02325.x, PMID 20146728.

3. Kawauchi H, Yanai K, Wang DY, Itahashi K, Okubo K. Antihistamines for allergic rhinitis treatment from the viewpoint of nonsedative properties. Int J Mol Sci. 2019 Jan;20(1):213. doi: 10.3390/ijms20010213, PMID 30626077.

4. Noveck RJ, Preston RA, Swan SK. Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment. Clin Pharmacokinet. 2007;46(6):525-34. doi: 10.2165/00003088-200746060-00006, PMID 17518511.

5. Simons FE. Comparative pharmacology of H1 antihistamines: clinical relevance. Am J Med. 2002;113(Suppl 9A):38S-46S. doi: 10.1016/S0002-9343(02)01436-5, PMID 12517581.

6. Festing MF, Altman DG. Guidelines for the design and statistical analysis of experiments using laboratory animals. ILAR J. 2002;43(4):244-58. doi: 10.1093/ilar.43.4.244, PMID 12391400.

7. Vogel HG. Drug discovery and evaluation: pharmacological assays. 3rd ed. Springer; 2008.

8. Sharma HL, Sharma KK. Principles of pharmacology. 2nd ed. Paras Medical Publisher; 2013.

9. Zar JH. Biostatistical Analysis. 5th ed. Upper Saddle River (NJ): Prentice-Hall/Pearson Education; 2010.

10. Kulkarni SK. Handbook of experimental pharmacology. 4th ed. New Delhi: Vallabh Prakashan; 2012.

11. Yanai K, Yoshikawa T, Yanai A, Nakamura T, Iida T, Leurs R. The clinical pharmacology of non-sedating antihistamines. Pharmacol Ther. 2017 Oct;178:148-56. doi: 10.1016/j.pharmthera.2017.04.004, PMID 28457804.

12. Sastre J. Ebastine in the treatment of allergic rhinitis and urticaria: 30 y of clinical studies and real-world experience. J Investig Allergol Clin Immunol. 2020;30(3):156-68. doi: 10.18176/jiaci.0401, PMID 30977465.

13. Tagawa M, Kano M, Okamura N, Higuchi M, Matsuda M, Mizuki Y. Differential cognitive effects of ebastine and (+)-chlorpheniramine in healthy subjects: correlation between cognitive impairment and plasma drug concentration. Br J Clin Pharmacol. 2002;53(3):296-304. doi: 10.1046/j.0306-5251.2001.01183.x, PMID 11874393.

14. Shamil KS, Prakruti PP, Anuradha MG, Bela JS, Chetna KD. Old versus new antihistamines: effects on cognition and psychomotor functions. J Fam Med Prim Care. 2022 Oct;11(10):5909-17. doi: 10.4103/jfmpc.jfmpc_77_22, PMID 36618177.

Published

15-01-2026

How to Cite

R., LENIN, et al. “COMPARATIVE EVALUATION OF CNS DEPRESSIVE ACTIVITY OF CHLORPHENIRAMINE MALEATE AND EBASTINE IN WISTAR RATS USING ROTARAD AND PHOTOACTOMETER”. International Journal of Current Pharmaceutical Research, vol. 18, no. 1, Jan. 2026, pp. 69-71, doi:10.22159/ijcpr.2026v18i1.8030.

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