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Twenty-four hours of activity of cetirizine and fexofenadine in the skin.
Ann Allergy Asthma Immunol. 2001 Apr; 86(4):387-92.AA

Abstract

BACKGROUND

Cetirizine and fexofenadine, the active metabolite of terfenadine, are powerful and well-tolerated H1 receptor antagonists effective in the treatment of skin and nose atopic diseases.

OBJECTIVE

We have compared the pharmacodynamic activity of the two antihistamines at therapeutic dosages, cetirizine at 10 mg and fexofenadine at 120 mg and 180 mg, on histamine-induced skin reactivity during a 24-hour period after single intake.

METHODS

Twenty-six healthy volunteers participated in a randomized, double-blind, crossover, placebo-controlled study. The areas of wheal and flare induced by histamine (100 mg/mL) administered by prick test were measured at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, and 24 hours postdose. Statistical analysis of the areas under the time-response curves was performed by a Friedman's ANOVA followed by a Wilcoxon test and Bonferroni's correction.

RESULTS

The three active treatments clearly inhibited the wheal and flare areas throughout the 24-hour period compared with placebo. Maximal inhibition occurred at 4 hours postdose. Between 4 and 24 hours postdose, the time course of inhibition by cetirizine differed significantly (P < 0.001) from that by fexofenadine at either dose, which did not differ from each other. At 24 hours, fexofenadine inhibited <40% of the skin reaction, whereas cetirizine reduced 60% of the wheal. The duration of effect, considered as the time for wheal to be inhibited by at least 70%, also significantly favored cetirizine (19 hours) compared with fexofenadine (9.3 and 8.5 hours for 180 and 120 mg, respectively; P < 0.001). Consistency of activity was evaluated by the frequency of total inhibition of the wheal (> or =95%). Consistency was observed in 26 of 26 participants for cetirizine, 21 of 26 for fexofenadine, 180 mg, and 10 of 26 for fexofenadine, 120 mg (P < 0.001), suggesting better consistency for cetirizine. There was no serious adverse event.

CONCLUSIONS

Our study clearly shows better duration of action and consistency of the antihistaminic activity of cetirizine compared with fexofenadine (120 and 180 mg) in the histamine-induced skin reaction during a 24-hour period.

Authors+Show Affiliations

Purohit A
Institut National de la Santé et de la Recherche Médicale, H pitaux Universitaires, Strasbourg, France.
Duvernelle C
No affiliation info available
Melac M
No affiliation info available
Pauli G
No affiliation info available
Frossard N
No affiliation info available

MeSH

AdolescentAdultAnti-Allergic AgentsCetirizineCross-Over StudiesDermatitis, AtopicDouble-Blind MethodDrug EvaluationFemaleHistamineHistamine H1 AntagonistsHumansMaleMiddle AgedRhinitisSkinSkin TestsTerfenadineTime Factors

Pub Type(s)

Clinical Trial
Comparative Study
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

11345280

Citation

Purohit, A, et al. "Twenty-four Hours of Activity of Cetirizine and Fexofenadine in the Skin." Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology, vol. 86, no. 4, 2001, pp. 387-92.
Purohit A, Duvernelle C, Melac M, et al. Twenty-four hours of activity of cetirizine and fexofenadine in the skin. Ann Allergy Asthma Immunol. 2001;86(4):387-92.
Purohit, A., Duvernelle, C., Melac, M., Pauli, G., & Frossard, N. (2001). Twenty-four hours of activity of cetirizine and fexofenadine in the skin. Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology, 86(4), 387-92.
Purohit A, et al. Twenty-four Hours of Activity of Cetirizine and Fexofenadine in the Skin. Ann Allergy Asthma Immunol. 2001;86(4):387-92. PubMed PMID: 11345280.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Twenty-four hours of activity of cetirizine and fexofenadine in the skin. AU - Purohit,A, AU - Duvernelle,C, AU - Melac,M, AU - Pauli,G, AU - Frossard,N, PY - 2001/5/10/pubmed PY - 2001/5/25/medline PY - 2001/5/10/entrez SP - 387 EP - 92 JF - Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology JO - Ann Allergy Asthma Immunol VL - 86 IS - 4 N2 - BACKGROUND: Cetirizine and fexofenadine, the active metabolite of terfenadine, are powerful and well-tolerated H1 receptor antagonists effective in the treatment of skin and nose atopic diseases. OBJECTIVE: We have compared the pharmacodynamic activity of the two antihistamines at therapeutic dosages, cetirizine at 10 mg and fexofenadine at 120 mg and 180 mg, on histamine-induced skin reactivity during a 24-hour period after single intake. METHODS: Twenty-six healthy volunteers participated in a randomized, double-blind, crossover, placebo-controlled study. The areas of wheal and flare induced by histamine (100 mg/mL) administered by prick test were measured at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, and 24 hours postdose. Statistical analysis of the areas under the time-response curves was performed by a Friedman's ANOVA followed by a Wilcoxon test and Bonferroni's correction. RESULTS: The three active treatments clearly inhibited the wheal and flare areas throughout the 24-hour period compared with placebo. Maximal inhibition occurred at 4 hours postdose. Between 4 and 24 hours postdose, the time course of inhibition by cetirizine differed significantly (P < 0.001) from that by fexofenadine at either dose, which did not differ from each other. At 24 hours, fexofenadine inhibited <40% of the skin reaction, whereas cetirizine reduced 60% of the wheal. The duration of effect, considered as the time for wheal to be inhibited by at least 70%, also significantly favored cetirizine (19 hours) compared with fexofenadine (9.3 and 8.5 hours for 180 and 120 mg, respectively; P < 0.001). Consistency of activity was evaluated by the frequency of total inhibition of the wheal (> or =95%). Consistency was observed in 26 of 26 participants for cetirizine, 21 of 26 for fexofenadine, 180 mg, and 10 of 26 for fexofenadine, 120 mg (P < 0.001), suggesting better consistency for cetirizine. There was no serious adverse event. CONCLUSIONS: Our study clearly shows better duration of action and consistency of the antihistaminic activity of cetirizine compared with fexofenadine (120 and 180 mg) in the histamine-induced skin reaction during a 24-hour period. SN - 1081-1206 UR - https://www.unboundmedicine.com/medline/citation/11345280/Twenty_four_hours_of_activity_of_cetirizine_and_fexofenadine_in_the_skin_ DB - PRIME DP - Unbound Medicine ER -