Himber J, Sallee V L, Andermann G, Bouzoubaa M, Leclerc G, De Santis L
Alcon Research and Development France, Kayserberg.
J Ocul Pharmacol. 1987 Summer;3(2):111-20. doi: 10.1089/jop.1987.3.111.
Changes in intraocular pressure (IOP) following topical administration of falintolol (0.5%-0.25%), a new beta-blocking agent, were studied in conscious albino rabbits with alpha-chymotrypsin-induced ocular hypertension. The drug produced a reduction in IOP equal to that of timolol. A longer duration of activity was noted with falintolol. The rate of transport of topically applied falintolol through the isolated bovine cornea under conditions simulating normal physiology was linear up to three hours and twice as fast as timolol from 3 to 6 hours. Since topical ocular application of beta-adrenergic antagonists useful in glaucoma therapy can also cause a number of troublesome systemic side effects, several conclusive preclinical investigations were carried out with falintolol. Of major concern was the effect falintolol might have on the pupil, cornea, and heart rate when administered topically. The results show that falintolol does not produce any noteworthy side effects and is capable of being an effective beta-blocking agent in open-angle glaucoma therapy.
在由α-糜蛋白酶诱导的高眼压的清醒白化兔中，研究了新型β受体阻滞剂法林洛尔（0.5%-0.25%）局部给药后的眼压（IOP）变化。该药物降低眼压的效果与噻吗洛尔相当。法林洛尔的作用持续时间更长。在模拟正常生理条件下，局部应用的法林洛尔透过离体牛角膜的转运速率在3小时内呈线性，在3至6小时内比噻吗洛尔快两倍。由于用于青光眼治疗的局部眼部应用β肾上腺素能拮抗剂也可能引起一些麻烦的全身副作用，因此对法林洛尔进行了多项结论性的临床前研究。主要关注的是局部给药时法林洛尔可能对瞳孔、角膜和心率产生的影响。结果表明，法林洛尔不会产生任何值得注意的副作用，并且能够成为开角型青光眼治疗中的一种有效β受体阻滞剂。
