| In Vitro | In vitro activity: Loteprednol possesses a metabolically labile function, the 17beta-ester, that is designed to be rapidly deactivated in the systemic circulation. Loteprednol etabonate exhibits a binding affinity which is 4.3 times that of dexamethasone, both compounds having a Hill factor close to 1 whereas PJ90 and PJ91 does not show any affinity to the receptor.
Kinase Assay:
Cell Assay: |
|---|
| In Vivo | Loteprednol etabonate administrated directly into the joint effectively blocks the inflammatory response. Loteprednol etabonate prevents the adverse inflammatory effects of antigen action in a rabbit acute experimental model for arthritis. Loteprednol etabonate (LE) (oral) reaches the upper GI tract effectively, but not the colon, due to absorption and/or decomposition in rats. Loteprednol etabonate (LE) shows a rapid, dose-dependent elimination with a total blood clearance (CLtotal) of higher than 60 ml/min/kg in rats. Loteprednol etabonate absorbes systemically, after topical administration, can be rapidly transformed to the inactive metabolites, and eliminates from the body mainly through the bile and urine. |
|---|
