A comparison of ebastine 10 mg fast-dissolving tablet with oral desloratadine and placebo in inhibiting the cutaneous reaction to histamine in healthy adults.
OBJECTIVE
Ebastine is a long-acting, second-generation selective histamine H(1) receptor antagonist. The pharmacodynamics of a new 10mg fast-dissolving tablet (FDT) oral lyophilisate tablet formulation of ebastine were compared with those of desloratadine and placebo following histamine skin intradermal test challenge. The acceptability of the FDT was also assessed.


METHODS
This was a double-blind, double-dummy, placebo-controlled, randomised, crossover, three-period study in 36 healthy adults. The histamine skin intradermal test (0.05 mL of 100 microg/mL solution) was administered into volunteers' forearms, and wheal area was measured 15 minutes later. Ebastine 10 mg FDT, desloratadine 5mg capsule or placebo were given on days 1-5. On day 1, a skin intradermal test was performed at baseline, then every 20 minutes for 2 hours after administration and at 24 hours. The final skin intradermal test was on day 6, 24 hours after the last drug dose. Subjective symptoms (itching, heat and pain) were assessed on day 1 for 2 hours following the first drug dose. There was a washout period of 7-10 days between treatments. At study end, the acceptability of the new ebastine formulation was evaluated using a questionnaire.


RESULTS
Ebastine 10mg inhibited the wheal response to histamine significantly more than desloratadine 5 mg or placebo 24 hours after 5 days' treatment (mean difference between treatments in wheal area reduction from baseline: 26.7%, p < 0.0001; 46.9%, p < 0.0001, respectively), and after 24 hours on day 1 (mean difference: 16.2%, p = 0.0082; 34.2%, p < 0.0001, respectively). The results with desloratadine were also significantly different from placebo on day 1 and after 5 days, but less than with ebastine after 5 days (difference, desloratadine vs placebo: 20.2%, p = 0.0001). No differences in itching, heat and pain were observed between the treatments. Most participants (70%) preferred the FDT, and all reported that it made adherence easier.


CONCLUSIONS
Ebastine 10 mg FDT demonstrated significantly superior antihistamine activity compared with desloratadine and placebo.
Antonijoan
Rosa M
RM
Department of Clinical Pharmacology, Hospital de la Santa Creu i Sant Pau, Barcelona, Spain.
García-Gea
Consuelo
C
Puntes
Montserrat
M
Valle
Marta
M
Esbri
Ramon
R
Fortea
Josep
J
Barbanoj
Manuel J
MJ
D000328:Adult; D002090:Butyrophenones / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D002626:Chemistry, Pharmaceutical; D003877:Dermatitis, Contact / Q000473:pathology / Q000517:prevention & control*; D004311:Double-Blind Method; D005260:Female; D006632:Histamine; D006634:Histamine H1 Antagonists / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D017336:Loratadine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000627:therapeutic use; D008297:Male; D010147:Pain Measurement; D010342:Patient Acceptance of Health Care; D010880:Piperidines / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D012867:Skin / Q000473:pathology; D013607:Tablets; D016896:Treatment Outcome
D002090:Butyrophenones; D006634:Histamine H1 Antagonists; D010880:Piperidines; D013607:Tablets; D017336:Loratadine; D006632:Histamine; C121345:desloratadine; C058249:ebastine