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噻吗洛尔滴眼液。其药理特性及在青光眼和高眼压症治疗中的应用综述。

Ocular carteolol. A review of its pharmacological properties, and therapeutic use in glaucoma and ocular hypertension.

作者信息

Chrisp P, Sorkin E M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs Aging. 1992 Jan-Feb;2(1):58-77. doi: 10.2165/00002512-199202010-00007.

Abstract

Carteolol is a relatively potent nonselective beta-adrenoceptor antagonist with partial agonist activity. It is used topically to reduce elevated intraocular pressure (IOP) in patients with glaucoma or ocular hypertension. Twice-daily ocular administration of carteolol 1 or 2% lowers IOP by approximately 32% on average in patients with these conditions, an efficacy equivalent to that of timolol 0.25 or 0.5%. Carteolol eyedrops lack local anaesthetic activity, appear to cause less local irritation than timolol, and produce less pronounced decreases in heart rate or dyspnoea, possibly due to partial agonist activity. The latter activity may also improve retinal perfusion. Thus, although additional comparative trials are needed to accurately assess the precise place of carteolol in therapy, this drug offers a useful alternative to timolol in the management of conditions associated with a raised IOP, and may have advantages in older patients with regard to its tolerability profile, although careful monitoring is still wise.

摘要

卡替洛尔是一种相对强效的非选择性β肾上腺素能受体拮抗剂,具有部分激动剂活性。它局部用于降低青光眼或高眼压症患者的眼压升高。对于这些病症的患者,每日两次眼部滴注1%或2%的卡替洛尔平均可使眼压降低约32%,其疗效与0.25%或0.5%的噻吗洛尔相当。卡替洛尔滴眼液缺乏局部麻醉活性,似乎比噻吗洛尔引起的局部刺激更少,并且心率或呼吸困难的降低不太明显,这可能归因于部分激动剂活性。后者的活性也可能改善视网膜灌注。因此,尽管需要额外的对照试验来准确评估卡替洛尔在治疗中的精确地位,但这种药物在治疗与眼压升高相关的病症方面为噻吗洛尔提供了一种有用的替代药物,并且在老年患者中就其耐受性而言可能具有优势,尽管仍需谨慎监测。

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