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. 1995 May;4(7):S31–S38. doi: 10.1155/S0962935195000822

Treatment of allergic rhinoconjunctivitis: a review of the role of topical levocabastine

R Gerth van Wijk 1
PMCID: PMC2365679  PMID: 18475688

Abstract

Lcocabastine is an extremely potent and highly selective H1-receptor antagonist which has been specifically developed as eye drops and nasal spray for the treatment of allergic rhinoconjunctivitis. Clinical experience to date suggests that this topical antihistamine is at least as effective as other current first-line therapeutic approaches for the treatment of this condition, including oral H1-receptor antagonists and sodium cromoglycate. Onset of action is rapid, with clinical effects apparent within minutes of instillation. Moreover, duration of action is sufficiently long to permit a convenient twice-daily dosing regimen. Topical levocabastine is well tolerated with an adverse-effect profile comparable with that of placebo and sodium cromoglycate. As might be expected from the route of drug administration, application site reactions are the most frequent adverse effect associated with levocabastine eye drops and nasal spray with an incidence comparable with that seen in placebotreated controls. The availability of effective and well-tolerated topical antihistamines, such as levocabastine, is an important advance which broadens the range of therapeutic approaches available for the clinical management of allergic rhinoconjunctivitis. Levocabastine appears to be an attractive alternative to oral antihistamines as a first-line therapeutic option for the treatment of this atopic condition.

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Selected References

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  1. Abelson M. B., Smith L. M. Levocabastine. Evaluation in the histamine and compound 48/80 models of ocular allergy in humans. Ophthalmology. 1988 Nov;95(11):1494–1497. [PubMed] [Google Scholar]
  2. Aberg N. Asthma and allergic rhinitis in Swedish conscripts. Clin Exp Allergy. 1989 Jan;19(1):59–63. doi: 10.1111/j.1365-2222.1989.tb02345.x. [DOI] [PubMed] [Google Scholar]
  3. Awouters F., Niemegeers C. J., Jansen T., Megens A. A., Janssen P. A. Levocabastine: pharmacological profile of a highly effective inhibitor of allergic reactions. Agents Actions. 1992 Jan;35(1-2):12–18. doi: 10.1007/BF01990945. [DOI] [PubMed] [Google Scholar]
  4. Azevedo M., Castel-Branco M. G., Oliveira J. F., Ramos E., Delgado L., Almeida J. Double-blind comparison of levocabastine eye drops with sodium cromoglycate and placebo in the treatment of seasonal allergic conjunctivitis. Clin Exp Allergy. 1991 Nov;21(6):689–694. doi: 10.1111/j.1365-2222.1991.tb03197.x. [DOI] [PubMed] [Google Scholar]
  5. Badhwar A. K., Druce H. M. Allergic rhinitis. Med Clin North Am. 1992 Jul;76(4):789–803. doi: 10.1016/s0025-7125(16)30326-1. [DOI] [PubMed] [Google Scholar]
  6. Bahmer F. A., Ruprecht K. W. Safety and efficacy of topical levocabastine compared with oral terfenadine. Ann Allergy. 1994 May;72(5):429–434. [PubMed] [Google Scholar]
  7. Bahmer F. A. Topical levocabastine--an effective alternative to oral antihistamines in seasonal allergic rhinoconjunctivitis. Clin Exp Allergy. 1995 Mar;25(3):220–227. doi: 10.1111/j.1365-2222.1995.tb01032.x. [DOI] [PubMed] [Google Scholar]
  8. Bende M., Pipkorn U. Topical levocabastine, a selective H1 antagonist, in seasonal allergic rhinoconjunctivitis. Allergy. 1987 Oct;42(7):512–515. doi: 10.1111/j.1398-9995.1987.tb00374.x. [DOI] [PubMed] [Google Scholar]
  9. Connell J. T. Quantitative intranasal pollen challenges. 3. The priming effect in allergic rhinitis. J Allergy. 1969 Jan;43(1):33–44. doi: 10.1016/0021-8707(69)90018-5. [DOI] [PubMed] [Google Scholar]
  10. Davies B. H., Mullins J. Topical levocabastine is more effective than sodium cromoglycate for the prophylaxis and treatment of seasonal allergic conjunctivitis. Allergy. 1993 Oct;48(7):519–524. doi: 10.1111/j.1398-9995.1993.tb01108.x. [DOI] [PubMed] [Google Scholar]
  11. Dechant K. L., Goa K. L. Levocabastine. A review of its pharmacological properties and therapeutic potential as a topical antihistamine in allergic rhinitis and conjunctivitis. Drugs. 1991 Feb;41(2):202–224. doi: 10.2165/00003495-199141020-00006. [DOI] [PubMed] [Google Scholar]
  12. Friedlaender M. H. Current concepts in ocular allergy. Ann Allergy. 1991 Jul;67(1):5-10, 13. [PubMed] [Google Scholar]
  13. Frostad A. B., Olsen A. K. A comparison of topical levocabastine and sodium cromoglycate in the treatment of pollen-provoked allergic conjunctivitis. Clin Exp Allergy. 1993 May;23(5):406–409. doi: 10.1111/j.1365-2222.1993.tb00346.x. [DOI] [PubMed] [Google Scholar]
  14. Ishizaki T., Koizumi K., Ikemori R., Ishiyama Y., Kushibiki E. Studies of prevalence of Japanese cedar pollinosis among the residents in a densely cultivated area. Ann Allergy. 1987 Apr;58(4):265–270. [PubMed] [Google Scholar]
  15. Juniper E. F., Guyatt G. H. Development and testing of a new measure of health status for clinical trials in rhinoconjunctivitis. Clin Exp Allergy. 1991 Jan;21(1):77–83. doi: 10.1111/j.1365-2222.1991.tb00807.x. [DOI] [PubMed] [Google Scholar]
  16. Leino M., Ennevaara K., Latvala A. L., Nordgren P., Posti A. M., Suves R., Takalo E. Double-blind group comparative study of 2% nedocromil sodium eye drops with 2% sodium cromoglycate and placebo eye drops in the treatment of seasonal allergic conjunctivitis. Clin Exp Allergy. 1992 Oct;22(10):929–932. doi: 10.1111/j.1365-2222.1992.tb02066.x. [DOI] [PubMed] [Google Scholar]
  17. Merkus F. W., Schüsler-van Hees M. T. Influence of levocabastine suspension on ciliary beat frequency and mucociliary clearance. Allergy. 1992 Jun;47(3):230–233. doi: 10.1111/j.1398-9995.1992.tb00655.x. [DOI] [PubMed] [Google Scholar]
  18. Palma-Carlos A. G., Chieira C., Conde T. A., Cordeiro J. A. Double-blind comparison of levocabastine nasal spray with sodium cromoglycate nasal spray in the treatment of seasonal allergic rhinitis. Ann Allergy. 1991 Oct;67(4):394–398. [PubMed] [Google Scholar]
  19. Palma-Carlos A. G., Palma-Carlos M. L., Rombaut N. The effect of levocabastine nasal spray in nasal provocation tests. Int J Clin Pharmacol Res. 1988;8(1):25–30. [PubMed] [Google Scholar]
  20. Rajakulasingam K., Polosa R., Lau L. C., Church M. K., Holgate S. T., Howarth P. H. Comparative nasal effects of bradykinin and histamine: influence on nasal airways resistance and plasma protein exudation. Thorax. 1993 Apr;48(4):324–329. doi: 10.1136/thx.48.4.324. [DOI] [PMC free article] [PubMed] [Google Scholar]
  21. Rimås M., Kjellman N. I., Blychert L. O., Björkstén B. Topical levocabastine protects better than sodium cromoglycate and placebo in conjunctival provocation tests. Allergy. 1990 Jan;45(1):18–21. doi: 10.1111/j.1398-9995.1990.tb01079.x. [DOI] [PubMed] [Google Scholar]
  22. Simons F. E. H1-receptor antagonists. Comparative tolerability and safety. Drug Saf. 1994 May;10(5):350–380. doi: 10.2165/00002018-199410050-00002. [DOI] [PubMed] [Google Scholar]
  23. Stafford C. T. Allergic rhinitis. A useful guide to diagnosis and treatment. Postgrad Med. 1987 Jan;81(1):147-51, 154, 157. doi: 10.1080/00325481.1987.11699668. [DOI] [PubMed] [Google Scholar]
  24. Stokes T. C., Feinberg G. Rapid onset of action of levocabastine eye-drops in histamine-induced conjunctivitis. Clin Exp Allergy. 1993 Sep;23(9):791–794. doi: 10.1111/j.1365-2222.1993.tb00368.x. [DOI] [PubMed] [Google Scholar]
  25. Topical levocabastine compared with oral loratadine for the treatment of seasonal allergic rhinoconjunctivitis. Swedish GP Allergy Team. Allergy. 1994 Sep;49(8):611–615. doi: 10.1111/j.1398-9995.1994.tb00127.x. [DOI] [PubMed] [Google Scholar]
  26. Vermeulen J., Mercer M. Comparison of the efficacy and tolerability of topical levocabastine and sodium cromoglycate in the treatment of seasonal allergic rhinoconjunctivitis in children. Pediatr Allergy Immunol. 1994 Nov;5(4):209–213. doi: 10.1111/j.1399-3038.1994.tb00241.x. [DOI] [PubMed] [Google Scholar]
  27. Weeke E. R. Epidemiology of hay fever and perennial allergic rhinitis. Monogr Allergy. 1987;21:1–20. [PubMed] [Google Scholar]
  28. van de Heyning P. H., van Haesendonck J., Creten W., Rombaut N. Effect of topical levocabastine on allergic and non-allergic perennial rhinitis. A double-blind study, levocabastine vs. placebo, followed by an open, prospective, single-blind study on beclomethasone. Allergy. 1988 Jul;43(5):386–391. doi: 10.1111/j.1398-9995.1988.tb00433.x. [DOI] [PubMed] [Google Scholar]
  29. von Mutius E., Martinez F. D., Fritzsch C., Nicolai T., Roell G., Thiemann H. H. Prevalence of asthma and atopy in two areas of West and East Germany. Am J Respir Crit Care Med. 1994 Feb;149(2 Pt 1):358–364. doi: 10.1164/ajrccm.149.2.8306030. [DOI] [PubMed] [Google Scholar]

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