Parys W, Blockhuys S, Janssens M
Janssen Research Foundation, Beerse, Belgium.
Doc Ophthalmol. 1992;82(4):353-60. doi: 10.1007/BF00161023.
Histamine is the key mediator producing itching, redness and chemosis in allergic conjunctivitis. Histamine levels in tears are increased ten-fold in patients with this allergic condition. Levocabastine is a newly synthesized histamine H1 antagonist which has been formulated as both eye drops and nasal spray. In well established assays of antihistamine activity, levocabastine was found to be the most potent antihistamine compound available, being 15,000 times more potent than chlorpheniramine. Ocular provocation studies in man have shown that levocabastine protects against the symptoms of allergen-induced conjunctivitis. Ophthalmological examinations, including slit lamp and ophthalmoscopy showed no adverse effects. Data from therapeutic studies are available for more than 1700 patients with allergic conjunctivitis treated for 2-16 weeks. One drop of levocabastine (0.5 mg/ml) per eye given two to four times daily provided significantly better symptom control than placebo, with good to excellent results in 71% of patients on levocabastine compared to 55% on placebo (p < 0.001). Levocabastine has a fast onset of action. In one study 94% of patients experienced symptom relief within 15 minutes after the first instillation. The effects observed with levocabastine were at least as good as those with ocular cromoglycate or oral terfenadine. The incidence of adverse experiences was not different from placebo. Levocabastine promises to be a valuable treatment for patients with allergic conjunctivitis.
组胺是过敏性结膜炎中产生瘙痒、发红和结膜水肿的关键介质。患有这种过敏病症的患者眼泪中的组胺水平会增加10倍。左卡巴斯汀是一种新合成的组胺H1拮抗剂,已制成滴眼液和鼻喷雾剂两种剂型。在成熟的抗组胺活性测定中,发现左卡巴斯汀是现有最有效的抗组胺化合物,其效力比氯苯那敏强15000倍。人体眼部激发试验表明,左卡巴斯汀可预防变应原诱导的结膜炎症状。包括裂隙灯检查和检眼镜检查在内的眼科检查均未显示出不良反应。有超过1700例过敏性结膜炎患者接受了2至16周治疗的治疗研究数据。每天每眼滴入一滴左卡巴斯汀(0.5mg/ml),给药2至4次,其症状控制明显优于安慰剂,使用左卡巴斯汀的患者中有71%取得了良好至极佳的效果,而使用安慰剂的患者这一比例为55%(p<0.001)。左卡巴斯汀起效迅速。在一项研究中,94%的患者在首次滴入后15分钟内症状得到缓解。观察到的左卡巴斯汀的效果至少与眼用色甘酸钠或口服特非那定的效果一样好。不良事件的发生率与安慰剂无异。左卡巴斯汀有望成为治疗过敏性结膜炎患者的一种有价值的药物。