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Percentage of brain H1 receptor occupancy (mean) after oral administration of antihistamines using PET67,69–73
| Dose (mg) | Mean H1 receptor occupancy on PET (%) | |
|---|---|---|
| Bilastine67 | 20 | −3.92 |
| Fexofenadine73 | 120 | −0.1 |
| Ebastine72 | 10 | 9.9–14.4 |
| Terfenadine69,70 | 60 | 12.1–17.2 |
| Azelastine70 | 1 | 20.3 |
| Cetirizine73 | 20 | 26.0 |
| d-Chlorpheniramine71 | 1 | 40.4 |
| Hydroxyzine67 | 25 | 53.95 |
| d-Chlorpheniramine69–71 | 2 | 60.4–76.8 |
| d-Chlorpheniramine71 | 5 | 85.5 |
Abbreviation: PET, positron emission tomography.
