European Journal of Clinical Pharmacology

, Volume 35, Issue 3, pp 255–259 | Cite as

Comparison of the central and peripheral effects of cetirizine and terfenadine

  • J. C. Pechadre
  • D. Vernay
  • J. F. Trolese
  • M. Bloom
  • P. Dupont
  • J. P. Rihoux
Originals

Summary

The peripheral and central effects of 10 mg cetirizine 2 HCl and 60 mg terfenadine have been compared with placebo in 9 healthy male volunteers.

The peripheral effect, in terms of cutaneous reactivity to 1 µg histamine i.d., was measured by planimetry of the wheal and erythemas. Central effects were assessed with a self-evaluation visual scale and from the results of electroencephalographic spectrum analysis. Peripheral inhibition of histamine reactivity was more intense and quicker for cetirizine than for terfenadine. On the self-evaluation scale, no significant difference between terfenadine, cetirizine and placebo was noted. The quantified EEG did not show any variation in spectral parameters at any time after cetirizine. By contrast, at 6 h terfenadine had increased slow waves and had inhibited the alpha band. Thus, 10 mg cetirizine 2 HCl had less effect on the central nervous system than terfenadine 60 mg, whilst its peripheral action appeared more quickly and was more intense.

Key words

cetirizine terfenadine CNS-/peripheral effects allergic disorder H1 antagonist 

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. 1.
    De Vos C, Maleux MR, Baltes E, Gobert J (1987) Inhibition of Histamine and allergen skin wheal by Cetirizine in four animal species. Ann Allergy 59: 278–282Google Scholar
  2. 2.
    Fadel R, Herpin-Richard N, Rihoux JP, Henocq E (1987) Inhibitory effect of Cetirizine on eosinophil migration in vivo. Clin Allergy 17: 373Google Scholar
  3. 3.
    Rihoux JP, Dupont P (1987) Comparative study of the peripheral and central effects of Terfenadine and Cetirizine 2 HCl. Ann Allergy 59: 235–238Google Scholar
  4. 4.
    Levander S, Hagermark O, Stahle M (1985) Peripheral antihistamine and central sedative effects of three H1-receptor antagonists. Eur J Clin Pharmacol 28: 523–529Google Scholar
  5. 5.
    Moser L, Hüther KJ, Koch-Weser J, Lundt PV (1978) Effects of Terfenadine and Diphenhydramine alone or in combination with Diazepam or alcohol on psychomotor performance and subjective feelings. Eur J Clin Pharmacol 14: 417–423Google Scholar
  6. 6.
    Kulsrestha VK, Gupta PP, Turner P, Wadsworth J (1978) Some clinical pharmacological studies with Terfenadine, a new antihistamine drug. Br J Clin Pharmacol 6: 25–29Google Scholar
  7. 7.
    Pishkin V, Sengel RA, Lovallo WR, Shurley JT (1983) Cognitive and psychomotor evaluation of clemastine-fumarate, diphenhydramine HCl and hydroxyzine HCl: double blind study. Curr Ther Res 33: 230–237Google Scholar
  8. 8.
    Etevenon P (1977) Etude méthodologique de l'électroencéphalographie quantitative. Application à quelques exemples. Thèse de Doctorat d'Etat ès Sciences Naturelles. Université Pierre et Marie Curie, Paris VI, p 302Google Scholar
  9. 9.
    Rosadini G, Ferillo F, Sannita WG (1984) Physiological and pathological changes in consciousness studied in man by quantitative E.E.G. methods. Congrès International “Traitement du signal en électrophysiologie expérimentale et clinique du système nerveux central”. Paris, Court, Trocherie, Doucet, Ed.Google Scholar
  10. 10.
    Hüther KJ, Renftle G, Barraud N, Burke JT, Koch-Weser J (1977) Inhibitory activity of terfenadine on histamine-induced skin wheals in man. Eur J Clin Pharmacol 12: 195–199Google Scholar
  11. 11.
    Harvey RP, Schocket AL (1980) The effect of H1- et H2-blockade on cutaneous histamine response in man. J Allergy Clin Immunol 65: 1356Google Scholar
  12. 12.
    Milan L, Brandon FACA, Weiner M (1980) Clinical investigation of Terfenadine, a non-sedating antihistamine. Ann Allergy, 44: 71–75Google Scholar
  13. 13.
    Waucquier A, van den Broeck WAE, Awouters F, Janssens PAJ (1981) A comparison between Astemizole and other antihistamines on sleep-wakefulness cycles in dogs. Neuropharmacology 20: 853–859Google Scholar
  14. 14.
    Seppala T, Savolainen K (1982) Effect of Astemizole on human psychomotor performance. Curr Ther Res 31: 538–544Google Scholar
  15. 15.
    Nicholson SN (1983) Antihistamines and sedation. Lancet 2: 211–212Google Scholar
  16. 16.
    Betts T, Markman D, Debenham S, Mortiboy D, McKevitt T (1984) Effects of two antihistamine drugs on actual driving performance. Br Med J 288: 281–282Google Scholar
  17. 17.
    Roehrs TA, Tietz EI, Zorick FJ, Roth T (1984) Daytime sleepiness and antihistamines. Sleep 7: 137–141Google Scholar
  18. 18.
    Kubicki S, Herrmann WM, Oot H, Holler L (1982) On the evaluation of hypnotic drug with E.E.G. and psychological testing. In: Herrmann WM (ed) E.E.G. in drug research. G. Fisher, Stuttgart, pp 1–16Google Scholar
  19. 19.
    Koella WP (1982) Modern neurobiological concept of vigilance. Experienta 38: 1426–1437Google Scholar
  20. 20.
    Matejcek M (1982) Vigilance and the E.E.G.: Psychological, physiological and pharmacological aspects. In: Herrmann WM (ed) E.E.G. in drug research. G. Fisher, Stuttgart, pp 405–508Google Scholar
  21. 21.
    Goldenberg F (1986) Mise au point d'un indice E.E.G. de vigilance diurne. Applications aux essais pharmacologiques. Rev Electroencephalogr Neurophysiol Clin: 16–49Google Scholar
  22. 22.
    Goldstein L, Murphry HB, Pfeiffer CC (1968) Comparative study of E.E.G. effects of antihistamine in normal volunteers. J Clin Pharmacol 8: 42–53Google Scholar
  23. 23.
    Rose C, Quach TT, Llorenc C, Schartz JC (1982) Relationship between occupation of cerebral H1-receptors and sedative properties of antihistamines. Arzneimittelforsch/Drug Res 32: 1171–1173Google Scholar
  24. 24.
    Snyder J, Snowman A (1987) Pharmacological selectivity of Cetirizine. Ann Allergy 59: 4–8Google Scholar
  25. 25.
    Garteiz DA, Hook RH, Walker BJ, Okerholm RA (1982) Pharmacokinetics and biotransformation studies of terfenadine in man. Arzneimittelforsch/Drug Res 32: 1185–1190Google Scholar
  26. 26.
    Wood SG, John BA, Chasseaud LF, Yeh J, Chung M (1987) The metabolism and pharmacokinetics of14C-cetirizine in humans. Ann Allergy 59: 31–34Google Scholar
  27. 27.
    Simons FE, Simons KJ, Chung M, Yeh J (1987) The comparative pharmacokinetics of H1-receptor antagonists. Ann Allergy 59: 20–24Google Scholar
  28. 28.
    Pechadre JC (1987) Hydroxyzine versus diazepam: Quantified EEG results. Gaz MédGoogle Scholar
  29. 29.
    Michel L, de Vos C, Rihoux JP, Burtin C, Beveniste J, Dubertret L (1988) Inhibitoring effect of oral Cetirizine on in vivo antigen induced histamine and PAF Acether release and eosinophil recruitement in human skin. J Allergy Clin Immunol (in press)Google Scholar

Copyright information

© Springer-Verlag 1988

Authors and Affiliations

  • J. C. Pechadre
    • 1
  • D. Vernay
    • 1
  • J. F. Trolese
    • 2
  • M. Bloom
    • 3
  • P. Dupont
    • 3
  • J. P. Rihoux
    • 3
  1. 1.E.E.G. and Functional Exploration of the Nervous System LaboratoryFrance
  2. 2.Laboratory of Medical Pharmacology, I.N.S.E.R.M. U 195, Clermont FerrandFrance
  3. 3.UCB S.A.Belgium

Personalised recommendations