Abstract
ABSTRACT
The ocular β-adrenoceptor antagonist activity of dihydrolevobunolol (DHLB), the major ocular and systemic metabolite of levobunolol was investigated by determining its ability to block isoproterenol-induced ocular hypotension in normotensive rabbits. Topically-applied 0.001% and 0.01% DHLB virutally abolished the response to isoproterenol, indicating a β-blocking potency similar to that of timolol. Thus, the ocular metabolism of levobunolol leads to the formation of a highly potent β-adrenoceptor antagonist that may contribute to its clinical efficacy.
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