diacetyl nadolol

Diacetyl nadolol is a lipophilic prodrug of the non-selective beta-adrenergic antagonist nadolol, specifically designed for topical ophthalmic use. Nadolol itself possesses poor corneal permeability due to its hydrophilic nature; the addition of acetyl groups increases the molecule's lipophilicity, thereby enhancing its penetration into the eye. Once absorbed, diacetyl nadolol is enzymatically hydrolyzed to its active form, nadolol, which reduces intraocular pressure (IOP) by decreasing the production of aqueous humor. Developed primarily for the treatment of glaucoma and ocular hypertension, clinical investigations in the early 1980s showed it was effective in lowering IOP, though it was associated with a significant incidence of local allergic reactions, such as periorbital dermatitis, which limited its clinical adoption.

Other names

diacetylnadolol