Woodward D F, Novack G D, Williams L S, Nieves A L, Potter D E
Eye and Skin Care Group, Allergan Pharmaceuticals, Irvine, California.
J Ocul Pharmacol. 1987 Spring;3(1):11-5. doi: 10.1089/jop.1987.3.11.
The ocular beta-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 virtually abolished the response to isoproterenol, indicating a beta-blocking potency similar to that of timolol. Thus, the ocular metabolism of levobunolol leads to the formation of a highly potent beta-adrenoceptor antagonist that may contribute to its clinical efficacy.
左布诺洛尔的主要眼内和全身代谢产物二氢左布诺洛尔（DHLB）的眼内β-肾上腺素能受体拮抗活性，通过测定其阻断正常血压家兔异丙肾上腺素诱导的眼内低血压的能力进行了研究。局部应用0.001%和0.01%的DHLB几乎完全消除了对异丙肾上腺素的反应，表明其β阻断效力与噻吗洛尔相似。因此，左布诺洛尔的眼内代谢导致形成一种高效的β-肾上腺素能受体拮抗剂，这可能有助于其临床疗效。
