Dipivefrin (hydrochloride)

Dipivefrin is a prodrug of epinephrine that is hydrolyzed by cholinesterase and other esterases in the cornea to epinephrine. It reduces the density of cultured bovine primary trabecular meshwork cells (IC50 = 115 µM). Additionally, it induces an elongated, fibroblast-like morphology and disrupts the actin cytoskeleton in bovine primary trabecular meshwork cells when used at a concentration of 103 µM. In cultured bovine corneal endothelial cells, dipivefrin (28 µM) enhances calcium signaling and induces cytotoxicity. Dipivefrin also suppresses primary human corneal keratinocyte proliferation when used at a concentration of 280 µM. Formulations containing dipivefrin have been used alone and in combination with β-adrenergic receptor antagonists for the treatment of glaucoma.