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Clinical efficacy and pharmacokinetic profiles of intranasal and oral cetirizine in a repeated allergen challenge model of allergic rhinitis.

Korsgren, Magnus LU ; Andersson, Morgan LU ; Borga, Olof; Larsson, Lars; Aldén-Raboisson, Marie; Malmqvist, Ulf LU and Greiff, Lennart LU (2007) In Annals of Allergy, Asthma & Immunology 98(4). p.316-321
Abstract
Background: Intranasal and oral antihistamines are effective in treating allergic rhinitis. Studies comparing these routes of administration of an antihistamine regarding efficacy and pharmacokinetic profile are lacking. Objective: To compare topical and oral routes of administration of cetirizine regarding efficacy, plasma exudation, and systemic drug levels in a repeated allergen challenge model of allergic rhinitis. Methods: Oral cetirizine dihydrochloride, 10 mg once daily, and topical cetirizine dinitrate in a dose corresponding to 4.4 mg of the dihydrochloride salt twice daily were given to grass pollen-sensitive individuals for 12 days in a double-blind, placebo-controlled, crossover design. Timothy grass pollen allergen challenges... (More)
Background: Intranasal and oral antihistamines are effective in treating allergic rhinitis. Studies comparing these routes of administration of an antihistamine regarding efficacy and pharmacokinetic profile are lacking. Objective: To compare topical and oral routes of administration of cetirizine regarding efficacy, plasma exudation, and systemic drug levels in a repeated allergen challenge model of allergic rhinitis. Methods: Oral cetirizine dihydrochloride, 10 mg once daily, and topical cetirizine dinitrate in a dose corresponding to 4.4 mg of the dihydrochloride salt twice daily were given to grass pollen-sensitive individuals for 12 days in a double-blind, placebo-controlled, crossover design. Timothy grass pollen allergen challenges were given once daily for 7 days using a nasal spray device. Nasal symptoms and peak inspiratory flow were recorded in the morning, 10 minutes after allergen challenge, and in the evening. The pharmacokinetics of the treatments was monitored in 8 patients. The remaining 28 patients were challenged topically with histamine 12 and 24 hours after the final topical and oral cetirizine doses, respectively. Nasal lavage levels of alpha(2)-macroglobulin were determined to evaluate histamine-induced mucosal plasma exudation. Results: During the last 3 days of the repeated allergen challenge model, chronic symptoms were established. Both treatments reduced symptoms 10 minutes after allergen challenge (P < .001 vs placebo). Neither treatment reduced morning and evening symptoms or nasal peak inspiratory flow. Topical, but not oral, cetirizine reduced histamine-induced plasma exudation (P < .01 vs placebo) when systemic drug levels were similar in the 2 treatment regimens. Conclusions: Topical and oral cetirizine reduced acute nasal symptoms produced by allergen challenges in patients with established chronic symptoms. There were also antihistaminic effects of topical cetirizine not related to systemic drug levels. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
in
Annals of Allergy, Asthma & Immunology
volume
98
issue
4
pages
316 - 321
publisher
American College of Allergy, Asthma & Immunology
external identifiers
  • wos:000245687000003
  • scopus:34147216577
ISSN
1081-1206
language
English
LU publication?
yes
id
342f5781-1b3d-48b9-8e33-4b540c1a8bc5 (old id 167369)
alternative location
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=17458426&dopt=Abstract
http://caliban.annallergy.org/vl=2754470/cl=47/nw=1/rpsv/cw/acaai/10811206/v98n4/s3/p316
date added to LUP
2007-07-05 12:14:56
date last changed
2017-01-01 04:49:45
@article{342f5781-1b3d-48b9-8e33-4b540c1a8bc5,
  abstract     = {Background: Intranasal and oral antihistamines are effective in treating allergic rhinitis. Studies comparing these routes of administration of an antihistamine regarding efficacy and pharmacokinetic profile are lacking. Objective: To compare topical and oral routes of administration of cetirizine regarding efficacy, plasma exudation, and systemic drug levels in a repeated allergen challenge model of allergic rhinitis. Methods: Oral cetirizine dihydrochloride, 10 mg once daily, and topical cetirizine dinitrate in a dose corresponding to 4.4 mg of the dihydrochloride salt twice daily were given to grass pollen-sensitive individuals for 12 days in a double-blind, placebo-controlled, crossover design. Timothy grass pollen allergen challenges were given once daily for 7 days using a nasal spray device. Nasal symptoms and peak inspiratory flow were recorded in the morning, 10 minutes after allergen challenge, and in the evening. The pharmacokinetics of the treatments was monitored in 8 patients. The remaining 28 patients were challenged topically with histamine 12 and 24 hours after the final topical and oral cetirizine doses, respectively. Nasal lavage levels of alpha(2)-macroglobulin were determined to evaluate histamine-induced mucosal plasma exudation. Results: During the last 3 days of the repeated allergen challenge model, chronic symptoms were established. Both treatments reduced symptoms 10 minutes after allergen challenge (P &lt; .001 vs placebo). Neither treatment reduced morning and evening symptoms or nasal peak inspiratory flow. Topical, but not oral, cetirizine reduced histamine-induced plasma exudation (P &lt; .01 vs placebo) when systemic drug levels were similar in the 2 treatment regimens. Conclusions: Topical and oral cetirizine reduced acute nasal symptoms produced by allergen challenges in patients with established chronic symptoms. There were also antihistaminic effects of topical cetirizine not related to systemic drug levels.},
  author       = {Korsgren, Magnus and Andersson, Morgan and Borga, Olof and Larsson, Lars and Aldén-Raboisson, Marie and Malmqvist, Ulf and Greiff, Lennart},
  issn         = {1081-1206},
  language     = {eng},
  number       = {4},
  pages        = {316--321},
  publisher    = {American College of Allergy, Asthma & Immunology},
  series       = {Annals of Allergy, Asthma & Immunology},
  title        = {Clinical efficacy and pharmacokinetic profiles of intranasal and oral cetirizine in a repeated allergen challenge model of allergic rhinitis.},
  volume       = {98},
  year         = {2007},
}