Gillies W E, Brooks A M
Clinic 3, Royal Victorian Eye and Ear Hospital, East Melbourne, Victoria.
Aust N Z J Ophthalmol. 1996 May;24(2):111-5. doi: 10.1111/j.1442-9071.1996.tb01563.x.
Since the introduction of carbonic anhydrase inhibitors, a topical preparation has been sought to avoid the complications of systemic medication while retaining the effect of lowering intraocular pressure. Recently, a topical carbonic anhydrase inhibitor, MK-507, has been found superior to others and introduced for multicentre clinical trial.
As part of an international multicentre trial, we compared MK-507 with beta blockers for one year in 20 patients with raised intraocular pressure, both as monotherapy and in combination.
Twelve patients with a mean peak pressure of 31.9 +/- 6.8 mmHg (range, 22 to 49 mmHg) off all medication received MK-507. After two weeks, mean peak pressure was 24.7 +/- 6.1 mmHg (range, 14 to 41 mmHg)--a 22.6% fall in pressure. Six of these patients had a mean peak pressure of 27.8 +/- 6.4 mmHg (range, 21 to 41 mmHg), a fall of 19.2% from day one and were given timolol as add-on therapy. This resulted in a fall to 19.1 +/- 2.8 (range, 15 to 24 mmHg) at year one, a fall of 31.3% after add-on. Four patients on timolol and four on betaxolol gave similar falls in pressure with an additional fall when MK-507 was used as add-on therapy.
MK-507 demonstrated its effectiveness as an ocular hypotensive agent in this trial of patients with an unusually high rise in pressure. It showed a hypotensive effect roughly equivalent to beta blockers. It is likely that either a topical carbonic anhydrase inhibitor or a cardioselective beta blocker will be the medication of first choice in newly diagnosed glaucoma.
自碳酸酐酶抑制剂问世以来，人们一直在寻求一种局部用药制剂，以避免全身用药的并发症，同时保持降低眼压的效果。最近，一种局部碳酸酐酶抑制剂MK-507被发现优于其他同类药物，并已进入多中心临床试验阶段。
作为一项国际多中心试验的一部分，我们将20例眼压升高患者的MK-507与β受体阻滞剂进行了为期一年的比较，试验包括单一疗法和联合疗法。
12例平均眼压峰值为31.9±6.8 mmHg（范围为22至49 mmHg）的患者在停用所有药物后接受了MK-507治疗。两周后，平均眼压峰值为24.7±6.1 mmHg（范围为14至41 mmHg），眼压下降了22.6%。其中6例患者平均眼压峰值为27.8±6.4 mmHg（范围为21至41 mmHg），从第一天起眼压下降了19.2%，随后加用噻吗洛尔作为附加治疗。在第一年时眼压降至19.1±2.8（范围为15至24 mmHg），附加治疗后眼压下降了31.3%。4例使用噻吗洛尔的患者和4例使用倍他洛尔的患者在眼压下降方面情况相似，当加用MK-507作为附加治疗时眼压进一步下降。
在这项针对眼压异常大幅升高患者的试验中，MK-507证明了其作为降眼压药物的有效性。其降压效果大致与β受体阻滞剂相当。对于新诊断的青光眼患者，局部碳酸酐酶抑制剂或心脏选择性β受体阻滞剂很可能会成为首选药物。
