Drug intelligence / Profile preview

dipivefrin

Development stage
Discontinued
Lead developer
Allergan
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Ophthalmic
01

Overview

Dipivefrin is a sympathomimetic prodrug used in ophthalmic solutions to reduce intraocular pressure in chronic open-angle glaucoma. It is the diester of epinephrine and pivalic acid, which increases its lipophilicity and allows for better corneal penetration compared to epinephrine. Once administered as eye drops, dipivefrin is hydrolyzed by ocular enzymes into active epinephrine within the eye. The released epinephrine acts as an adrenergic agonist at both alpha- and beta-adrenergic receptors in the eye, leading to decreased aqueous humor production and increased outflow facility through the trabecular meshwork. This dual action results in reduced intraocular pressure with fewer side effects than direct topical administration of epinephrine[1][2][4][5][6]. Developers: Allergan Manufacturers: Allergan

Brand names
Propine
Other names
dipivefrin hydrochlorideepinephrine pivalate
02

Targets

ADRB2 (β2)ADRA2A (α2A)ADRA1A (α1A)

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