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A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects.
Ann Allergy Asthma Immunol. 2002 Feb; 88(2):190-7.AA

Abstract

BACKGROUND

Levocetirizine is the active enantiomer of cetirizine, a potent drug with little metabolism widely used for allergic rhinitis and urticaria.

OBJECTIVE

This study compares the potency, consistency, onset, and duration of action of levocetirizine with other popular antihistamines.

METHODS

Levocetirizine 5 mg, ebastine 10 mg, fexofenadine 180 mg, loratadine 10 mg, mizolastine 10 mg, or placebo in single doses were given to 18 healthy male volunteers in a double-blind, crossover, randomized fashion. Wheal-and-flare responses to epicutaneous histamine dihydrochloride (100 mg/mL) challenge were measured at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, and 24 hours after each dose.

RESULTS

The overall effect of each drug was evaluated by the area under the curve (0 to 24 hours). Levocetirizine was the most potent and consistently effective drug for inhibiting the histamine-induced wheal-and-flare surface areas. Ebastine, fexofenadine, and mizolastine ranked next and had almost identical effects for inhibiting the wheal. Loratadine was the least potent drug. Levocetirizine, fexofenadine, and mizolastine inhibited the wheal-and-flare response after 1 hour and reached their peak for inhibition after 4 hours. Ebastine and loratadine could be distinguished from placebo only after 4 hours. After treatment with levocetirizine, all 18 subjects had >95% inhibition of the wheal response at one timepoint. Fexofenadine, mizolastine, and ebastine were inhibitory in declining order. All treatments were considered safe and well tolerated.

CONCLUSIONS

Levocetirizine, the active enantiomer of cetirizine, is more potent and consistent than other popular H1 antihistamines for blocking the cutaneous response to histamine. These findings may predict the efficacy of this drug in treating allergic disorders.

Authors+Show Affiliations

University of Texas Medical Branch, Galveston77555-1083, USA. jagrant@utmb.eduNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

11868924

Citation

Grant, J Andrew, et al. "A Double-blind, Randomized, Single-dose, Crossover Comparison of Levocetirizine With Ebastine, Fexofenadine, Loratadine, Mizolastine, and Placebo: Suppression of Histamine-induced Wheal-and-flare Response During 24 Hours in Healthy Male Subjects." Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology, vol. 88, no. 2, 2002, pp. 190-7.
Grant JA, Riethuisen JM, Moulaert B, et al. A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects. Ann Allergy Asthma Immunol. 2002;88(2):190-7.
Grant, J. A., Riethuisen, J. M., Moulaert, B., & DeVos, C. (2002). A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects. Annals of Allergy, Asthma & Immunology : Official Publication of the American College of Allergy, Asthma, & Immunology, 88(2), 190-7.
Grant JA, et al. A Double-blind, Randomized, Single-dose, Crossover Comparison of Levocetirizine With Ebastine, Fexofenadine, Loratadine, Mizolastine, and Placebo: Suppression of Histamine-induced Wheal-and-flare Response During 24 Hours in Healthy Male Subjects. Ann Allergy Asthma Immunol. 2002;88(2):190-7. PubMed PMID: 11868924.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects. AU - Grant,J Andrew, AU - Riethuisen,Jean-Michel, AU - Moulaert,Béatrice, AU - DeVos,Christine, PY - 2002/3/1/pubmed PY - 2002/3/26/medline PY - 2002/3/1/entrez SP - 190 EP - 7 JF - Annals of allergy, asthma & immunology : official publication of the American College of Allergy, Asthma, & Immunology JO - Ann Allergy Asthma Immunol VL - 88 IS - 2 N2 - BACKGROUND: Levocetirizine is the active enantiomer of cetirizine, a potent drug with little metabolism widely used for allergic rhinitis and urticaria. OBJECTIVE: This study compares the potency, consistency, onset, and duration of action of levocetirizine with other popular antihistamines. METHODS: Levocetirizine 5 mg, ebastine 10 mg, fexofenadine 180 mg, loratadine 10 mg, mizolastine 10 mg, or placebo in single doses were given to 18 healthy male volunteers in a double-blind, crossover, randomized fashion. Wheal-and-flare responses to epicutaneous histamine dihydrochloride (100 mg/mL) challenge were measured at 0, 0.5, 1, 2, 4, 6, 8, 10, 12, and 24 hours after each dose. RESULTS: The overall effect of each drug was evaluated by the area under the curve (0 to 24 hours). Levocetirizine was the most potent and consistently effective drug for inhibiting the histamine-induced wheal-and-flare surface areas. Ebastine, fexofenadine, and mizolastine ranked next and had almost identical effects for inhibiting the wheal. Loratadine was the least potent drug. Levocetirizine, fexofenadine, and mizolastine inhibited the wheal-and-flare response after 1 hour and reached their peak for inhibition after 4 hours. Ebastine and loratadine could be distinguished from placebo only after 4 hours. After treatment with levocetirizine, all 18 subjects had >95% inhibition of the wheal response at one timepoint. Fexofenadine, mizolastine, and ebastine were inhibitory in declining order. All treatments were considered safe and well tolerated. CONCLUSIONS: Levocetirizine, the active enantiomer of cetirizine, is more potent and consistent than other popular H1 antihistamines for blocking the cutaneous response to histamine. These findings may predict the efficacy of this drug in treating allergic disorders. SN - 1081-1206 UR - https://www.unboundmedicine.com/medline/citation/11868924/A_double_blind_randomized_single_dose_crossover_comparison_of_levocetirizine_with_ebastine_fexofenadine_loratadine_mizolastine_and_placebo:_suppression_of_histamine_induced_wheal_and_flare_response_during_24_hours_in_healthy_male_subjects_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1081-1206(10)61995-3 DB - PRIME DP - Unbound Medicine ER -