Abstract
ABSTRACT
Because of the need to develop ocular hypotensive agents with low incidence of side effects, the dextrorotatory enantiomers of adrenergic agents have prompted some attention. In the present study, the relative potency and efficacy of various adrenergic stereoisomers with respect to their ocular hypotensive and mydriatic effects have been determined after topical administration to conscious rabbits. The relative order of potency was found to be, iris: 1-epinephrine >>> d-epinephrine ≃ 1-norepinephrine ≃ dl-alpha-methyl-norepinephrine > dl-alpha-methyl-epinephrine > d-norepinephrine; intraocular pressure (IOP): 1-epinephrine > dl-alpha-methyl-epinephrine > d-epinephrine > dl-alpha-methyl-norepinephrine > d-norepinephrne ≃ 1-norepinephrine. The pupil and the initial ocular hypertensive responses clearly demonstrated the phenomenon of stereoselectivity of adrenergic stimulants, in that the 1-form was relatively more potent than the d-form. However, such order of potency does not seem to hold for IOP. The apparent discrepancy and reversal of order of potency for IOP responses may be related to the hypothesis that the net ocular hypotensive effect of adrenergic agents is the summation of the initial hypertension and the delayed hypotension produced by these agents. It is anticipated that the results of the present study may improve our understanding of ocular pharmacology of adrenergic stereoisomers. The ability to separate the dose-response profiles of pupillary and IOP effects of these agents may have potential therapeutic significance and thus warrants further investigation in other species.
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