Kanno M, Araie M, Koibuchi H, Masuda K
Department Opthalmology, University of Tokyo School of Medicine, Japan.
Br J Ophthalmol. 2000 Mar;84(3):293-9. doi: 10.1136/bjo.84.3.293.
To study the effects of topical nipradilol, a non-selective beta blocker with alpha blocking and nitroglycerin-like activities, on intraocular pressure (IOP) and aqueous humour dynamics in normal humans and in patients with ocular hypertension.
Nipradilol (0.06%, 0.125%, 0.25%, 0.5%) was applied to normal volunteers (n = 12) to test for IOP lowering effects. In a second group of normal volunteers (n = 11), nipradilol (0.125% and 0.25%) and timolol (0. 5%) were compared for IOP lowering effects. After a single administration of 0.25% nipradilol, IOP, flare intensity in the anterior chamber, aqueous flow, uveoscleral outflow, tonographic outflow facility, and episcleral venous pressure were either directly measured or mathematically calculated. Topical nipradilol (0.25%) was administered to 24 patients with ocular hypertension twice daily for 8 weeks.
Administration of 0.25% nipradilol decreased IOP with a maximum reduction of 4.2 mm Hg lasting 12 hours. A single instillation of both 0.25% nipradilol and 0.5% timolol reduced the IOP in normotensive human subjects to the same degree. A single instillation of 0.25% nipradilol decreased the aqueous flow rate in the treated eye by 20%. Nipradilol produced no significant effect in tonographic outflow facility or episcleral venous pressure, but uveoscleral outflow was increased. In patients with ocular hypertension, twice daily instillation of 0.25% nipradilol decreased IOP without tachyphylaxis for the 8 week test period.
Topical nipradilol (0.25%) reduced IOP by decreasing the aqueous flow rate and probably also by increasing uveoscleral outflow. Nipradilol should be further investigated as a new antiglaucoma drug.
研究尼普地洛(一种具有α阻断和硝酸甘油样活性的非选择性β受体阻滞剂)对正常人及高眼压症患者眼压(IOP)和房水动力学的影响。
将尼普地洛(0.06%、0.125%、0.25%、0.5%)应用于正常志愿者(n = 12)以测试其降低眼压的效果。在另一组正常志愿者(n = 11)中,比较尼普地洛(0.125%和0.25%)与噻吗洛尔(0.5%)降低眼压的效果。单次给予0.25%尼普地洛后,直接测量或通过数学计算得出眼压、前房闪光强度、房水流量、葡萄膜巩膜流出量、眼压描记流出系数和巩膜静脉压。将0.25%尼普地洛局部应用于24例高眼压症患者,每日两次,持续8周。
给予0.25%尼普地洛可降低眼压,最大降幅为4.2 mmHg,持续12小时。单次滴注0.25%尼普地洛和0.5%噻吗洛尔均可使正常血压受试者的眼压降低至相同程度。单次滴注0.25%尼普地洛可使治疗眼的房水流量降低20%。尼普地洛对眼压描记流出系数或巩膜静脉压无显著影响,但葡萄膜巩膜流出量增加。在高眼压症患者中,每日两次滴注0.25%尼普地洛可降低眼压,在8周的测试期内无快速耐受现象。
局部应用0.25%尼普地洛可通过降低房水流量并可能还通过增加葡萄膜巩膜流出量来降低眼压。尼普地洛作为一种新型抗青光眼药物应进一步研究。