Percentage of recovered radioactivity representing intact brimonidine and metabolites 1 h or 15 days after the final dose administrated to cynomolgus monkeys in the multiple 0.5% dose study
| Tissues/Fluids | Time After | Extraction | Brimonidine | MIIIa | MIV | MV |
|---|---|---|---|---|---|---|
| % | ||||||
| Tear (Schirmer strip) | 1 h | 87.4 ± 2.3 | 89.8 ± 5.4 | 4.4 ± 2.7 | 2.6 ± 2.1 | 3.2 ± 1.3 |
| 15 days | 78.5 ± 6.1 | N.A. | N.A. | N.A. | N.A. | |
| Lower bulbar conjunctiva | 1 h | 64.8 ± 13.0 | 93.8 ± 2.2 | 1.3 ± 0.5 | 1.6 ± 1.3 | 3.4 ± 2.1 |
| 15 days | 40.3 ± 3.3 | 91.1 ± 2.7 | 2.1 ± 1.1 | 2.7 ± 2.2 | 4.1 ± 2.3 | |
| Upper bulbar conjunctiva | 1 h | 82.7 ± 4.2 | 95.1 ± 0.5 | 1.4 ± 0.6 | 1.8 ± 1.1 | 1.7 ± 0.9 |
| 15 days | 50.6 ± 3.3 | 93.9 ± 1.6 | 1.3 ± 0.8 | 1.5 ± 1.0 | 3.5 ± 1.7 | |
| Cornea | 1 h | 82.1 ± 8.7 | 92.1 ± 1.6 | 1.5 ± 0.5 | 2.4 ± 0.7 | 4.1 ± 0.6 |
| 15 days | 53.1 ± 6.4 | 89.8 ± 5.2 | 1.6 ± 1.0 | 3.3 ± 1.8 | 5.4 ± 3.4 | |
| Aqueous humor | 1 h | 100.0 ± 0.0 | 82.7 ± 5.9 | 4.9 ± 3.3 | 7.0 ± 1.4 | 5.4 ± 2.2 |
| 15 days | 100.0 ± 0.0 | N.A. | N.A. | N.A. | N.A. | |
| Iris | 1 h | 92.6 ± 5.6 | 96.8 ± 0.5 | 0.8 ± 0.5 | 0.9 ± 0.4 | 1.5 ± 0.6 |
| 15 days | 97.6 ± 0.5 | 96.2 ± 0.5 | 1.4 ± 0.4 | 0.9 ± 0.3 | 1.6 ± 0.4 | |
| Ciliary body | 1 h | 88.8 ± 3.8 | 95.5 ± 1.0 | 0.5 ± 0.4 | 1.2 ± 0.3 | 2.9 ± 1.1 |
| 15 days | 92.3 ± 2.3 | 97.7 ± 1.7 | 0.3 ± 0.3 | 0.6 ± 0.5 | 1.5 ± 0.9 | |
Results were obtained by HPLC of extracts of ocular tissues and tear samples; data shown are means ± S.D. of values from four eyes (two animals).
N.A., data not available; levels of radioactivity were too low for parent and metabolite profiling.