Cat. No. Name Size Price Add Cart
KI0700Loteprednol etabonate10 mg$176
Loteprednol etabonate100 mg$1232

Chemical Characteristic

Product NameLoteprednol etabonate
SynonymsAlrex
CAS No.82034-46-6
Molecular Weight 466.95
FormulaC24H31ClO7
Chemical NameAndrosta-1,4-diene-17-carboxylicacid,17-[(ethoxycarbonyl)oxy]-11-hydroxy-3-oxo-,chloromethylester,
SmilesC1(=O)C=C[C@]2(C(=C1)CC[C@H]1[C@@H]3CC[C@@]([C@@]3(C)CC([C@H]21)O)(C(=O)OCCl)OC(=O)OCC)C
Chemical Structure

Biological activities

Loteprednol etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology. Loteprednol etabonate exhibits a binding affinity to rat lung type II glucocorticoid receptor which is 4.3 times that of dexamethasone.[1] Loteprednol etabonate blocks the release and action of inflammatory mediators. Loteprednol etabonate relieves ocular surface and lacrimal gland inflammation associated with dry eye and is used in combination with ciclosporin A. Loteprednol etabonate is also effective in the treatment of postoperative ocular inflammation.[2] In vitro, a pronounced binding of loteprednol etabonate to plasma protein (> 90%) and a high erythrocyte-buffer partition coefficient of 7.8 are determined. In vivo, intravenous administration of loteprednol etabonate (5 mg/kg) to dogs reveals a terminal half-life of 2.8 hours, a volume of distribution of 3.7 L/kg, and a total body clearance of 0.9 L/h/kg. After oral administration of loteprednol etabonate (5 mg/kg) to dogs, only metabolites, but no intact drug, is found in the plasma. In rats after oral administration of a 14C-labeled loteprednol etabonate suspension (5 mg/kg), levels of intact loteprednol etabonate and metabolites are highest in liver and kidney.[3]

Protocols

In vivo: Loteprednol etabonate (150mg) is dissolved by sonication in a mixture of 3 mL of ethanol and 4 mL of polyethylene glycol (PEG 200).[3]

References

[1] Druzgala P, et al. Soft drugs--10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: loteprednol etabonate. J Steroid Biochem Mol Biol. 1991, 38(2): 149-154.
[2] Pavesio CE, et al. Treatment of ocular inflammatory conditions with loteprednol etabonate. Br J Ophthalmol. 2008, 92(4): 455-459.
[3] Hochhaus G, et al. Pharmacokinetic characterization and tissue distribution of the new glucocorticoid soft drug loteprednol etabonate in rats and dogs. J Pharm Sci. 1992, 81(12): 1210-1215.

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