Suppression of the skin reaction to histamine by ebastine.
BACKGROUND
Ebastine is a nonsedating histamine H-1 antagonist undergoing evaluation for treatment of allergic rhinitis and urticaria.


OBJECTIVE
To compare the suppression of prick and intradermal skin reactions to histamine over a period of 24 hours produced by a single dose of ebastine. Also to record side effects and assess changes in the electrocardiogram, particularly the QTc interval.


METHODS
Single doses of 1, 3, 10, and 30 mg of ebastine or placebo were administered double-blind at approximately 8 AM after baseline measurement of the reaction to intradermal testing with 5 micrograms histamine base and prick skin testing with three concentrations of histamine. Intradermal testing with histamine was repeated hourly for four hours, every two hours for eight hours, and after 24 hours. Titrated prick skin testing with histamine was performed at 6, 12, and 24 hours. Potential side effects were recorded each time skin testing was performed. Electrocardiograms were repeated at 4 and 24 hours.


RESULTS
Intradermal skin test reactions were suppressed between 4 and 24 hours and prick skin tests to 10 mg/mL histamine base were suppressed between 6 and 24 hours with all doses of ebastine. Prick skin test reactions were significantly smaller at 12 and 24 hours in the group receiving the 30 mg dose of ebastine than in all other groups.


CONCLUSIONS
Ebastine is a potent antihistamine that suppresses skin reactions to histamine for 24 hours following single doses in the doses tested (1 to 30 mg). No differences from placebo were noted in either the incidence of side effects or in the QTc intervals of serial electrocardiograms.
Nelson
H S
HS
Division of Allergy and Immunology, National Jewish Center for Immunology and Respiratory Medicine, Denver, Colorado, USA.
Bucher
B
B
Buchmeier
A
A
Oppenheimer
J
J
Garcia
J
J
D000328:Adult; D000707:Anaphylaxis / Q000139:chemically induced / Q000517:prevention & control; D002090:Butyrophenones / Q000009:adverse effects / Q000627:therapeutic use*; D017449:Dermatitis, Allergic Contact / Q000276:immunology / Q000517:prevention & control*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005260:Female; D006634:Histamine H1 Antagonists / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D008875:Middle Aged; D010880:Piperidines / Q000009:adverse effects / Q000627:therapeutic use*; D012867:Skin / Q000276:immunology; D012882:Skin Tests
D002090:Butyrophenones; D006634:Histamine H1 Antagonists; D010880:Piperidines; C058249:ebastine