Table 3B Pharmacokinetics and Pharmacodynamics of H1 Antihistamines for Intranasal/Ophthalmic Use
From: H1 Antihistamines: Current Status and Future Directions
H1 Antihistamine (Metabolite) | Time to Maximum Plasma Concentration (tmax, h) After a Single Dose§ | Terminal Elimination Half-Life (t1/2, h)§ | Clinically Relevant Drug/Drug Interactions§ | Onset/Duration of Action, h|| |
|---|---|---|---|---|
Instranasl/Ophthalmic | Â | Â | Â | Â |
   Azelastine (desmethylazelastine) | 5.3 ± 1.6 (20.5) | 22-27.6 (54 ± 15) | No | 0.5/12 |
   Emedastine | 1.4 ± 0.5 | 7 | No | 0.25/12 |
   Epinastine | 2-3 | 6.5 | No | 0.1/12 |
   Ketotifen | 2-4 | 20-22 | No | 0.25/12 |
   Levocabastine | 1-2 | 35-40 | No | 0.25/12 |
   Olopatadine | 0.5-2 | 7.1-9.4 | No | 0.25/12 |