title: An ophthalmic beta antagonist with rapid systemic deactivation.
abstract: The intraocular pressure response to ACC-9447, a topical beta adrenergic antagonist, in six drug concentrations from 0.2% to 4.0%, was evaluated in 17 normal human subjects. ACC-9447 employs a new strategy for reducing systemic effects of ocular drugs by exploiting physiologic blood esterases to deactivate the drug rapidly after systemic absorbtion. Each patient received the test drug in one eye and placebo in the fellow eye. Intraocular pressure was measured nine times over the subsequent 24-hour period. The tests were repeated for six increasing concentrations over six weekend days. Although the eyes receiving ACC-9447 exhibited a significant 24-hour reduction in pressure from baseline, the effect was not different in placebo-treated eyes. Further studies are planned in ocular hypertensive patients using matched patient rather than fellow eye controls.
authors.forename: E M
authors.initials: EM
authors.lastname: Van Buskirk
authors.forename: J R
authors.initials: JR
authors.lastname: Samples
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000378:metabolism / Q000494:pharmacology*; D000328:Adult; D004950:Esterases / Q000378:metabolism; D006801:Humans; D008658:Inactivation, Metabolic; D007429:Intraocular Pressure / Q000187:drug effects*; D009930:Organic Chemicals
chemical_list: D000319:Adrenergic beta-Antagonists; D009930:Organic Chemicals; C046421:ACC 9447; D004950:Esterases