Lindén C, Alm A
Department of Ophthalmology, Umeå University, Sweden.
Drugs Aging. 1999 May;14(5):387-98. doi: 10.2165/00002512-199914050-00006.
Prostaglandin (PG) analogues are a new class of ocular hypotensive drugs that have been developed for the treatment of open angle glaucoma. Two of these drugs, latanoprost and unoprostone, are presently commercially available. Latanoprost was introduced in 1996 in the US and Europe. Presently it enjoys the most widespread use and is the most well documented drug of this group. It reduces the intraocular pressure (IOP) by a mechanism of action different from other drugs; namely by increasing the uveoscleral outflow. The aqueous inflow is not affected. The optimal dose regimen is one drop of 50 microg/ml once daily, which reduces the IOP by approximately 30% in patients with glaucoma. A more pronounced ocular hypotensive effect is demonstrated when latanoprost is combined with other glaucoma therapies, including beta-blockers, adrenergic and cholinergic agonists or carbonic anhydrase inhibitors. Latanoprost is well tolerated. The drug reaches a plasma concentration below that needed for stimulation of the FP-receptor, which may explain its favourable systemic tolerability profile. The major ocular adverse effect is increased iris pigmentation, which is due to increased synthesis of melanin in the melanocytes of the iris stroma. It is most frequently seen in green-brown eyes and it is probably permanent. A low frequency of cystoid macular oedema has also been reported, predominantly in predisposed eyes. Unoprostone was launched in Japan in 1994, but there is little experience with this drug outside the Japanese market and the documentation is more limited. Its main mechanism of action is on outflow, but this is not yet fully elucidated. The recommended dosage regimen is 1 drop of 1.2 mg/ml twice daily. No comparative studies in humans between the 2 drugs have yet been published.
前列腺素(PG)类似物是一类新型的降眼压药物,已被开发用于治疗开角型青光眼。其中两种药物,拉坦前列素和乌诺前列酮,目前已在市场上销售。拉坦前列素于1996年在美国和欧洲推出。目前它的使用最为广泛,是该类药物中记录最完善的药物。它通过与其他药物不同的作用机制降低眼压;即通过增加葡萄膜巩膜外流。房水流入不受影响。最佳剂量方案是每天一次滴入一滴50微克/毫升的溶液,这可使青光眼患者的眼压降低约30%。当拉坦前列素与其他青光眼治疗药物联合使用时,包括β受体阻滞剂、肾上腺素能和胆碱能激动剂或碳酸酐酶抑制剂,可表现出更显著的降眼压效果。拉坦前列素耐受性良好。该药物达到的血浆浓度低于刺激FP受体所需的浓度,这可能解释了其良好的全身耐受性。主要的眼部不良反应是虹膜色素沉着增加,这是由于虹膜基质黑素细胞中黑色素合成增加所致。最常见于绿褐色眼睛,可能是永久性的。也有报道称囊样黄斑水肿的发生率较低,主要发生在易感眼中。乌诺前列酮于1994年在日本上市,但在日本市场以外对该药物的经验很少,相关文献也较为有限。其主要作用机制是影响房水外流,但尚未完全阐明。推荐的剂量方案是每天两次滴入一滴1.2毫克/毫升的溶液。目前尚未发表这两种药物在人体中的比较研究。