Dipivefrin (hydrochloride)

Dipivefrin is a prodrug of epinephrine that is hydrolyzed by cholinesterase and other esterases in the cornea to epinephrine.¹ It reduces the density of cultured bovine primary trabecular meshwork cells (IC₅₀ = 115 µM).² 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.² In cultured bovine corneal endothelial cells, dipivefrin (28 µM) enhances calcium signaling and induces cytotoxicity.^3,4 Dipivefrin also suppresses primary human corneal keratinocyte proliferation when used at a concentration of 280 µM.⁵ Formulations containing dipivefrin have been used alone and in combination with β-adrenergic receptor antagonists for the treatment of glaucoma.

WARNING This product is not for human or veterinary use.

1. Nakamura, M., Shirasawa, E., and Hikida, M. Characterization of esterases involved in the hydrolysis of dipivefrin hydrochloride. Ophthalmic Res. 25(1), 46-51 (1993).

2. Kawa, J.E., Higginbotham, E.J., Change, I.L., et al. Effects of antiglaucoma medications on bovine trabecular meshwork cells in vitro. Exp. Eye Res. 57(5), 557-565 (1993).

3. Wu, K.Y., Hong, S.J., and Wang, H.Z. Effects of antiglaucoma drugs on calcium mobility in cultured corneal endothelial cells. Kaohsiung J. Med. Sci. 22(2), 60-67 (2006).

4. Wu, K.Y., Wang, H.Z., and Hong, S.J. Cellular cytotoxicity of antiglaucoma drugs in cultured corneal endothelial cells. Kaohsiung J. Med. Sci. 23(3), 105-111 (2007).

5. Wu, K.Y., Wang, H.Z., and Hong, S.J. Effects of antiglaucoma drugs on cellular proliferation in cultured human corneal keratocytes. Kaohsiung J. Med. Sci. 22(3), 120-125 (2006).