Carmine A A, Brogden R N, Heel R C, Speight T M, Avery G S
Drugs. 1982 May;23(5):329-53. doi: 10.2165/00003495-198223050-00001.
Trifluridine (trifluorothymidine) is an antiviral agent for topical use in the eye, and is structurally related to idoxuridine. In vitro studies have shown that it effectively inhibits the replication of herpes simplex virus type 1, which causes primary keratoconjunctivitis and recurrent epithelial keratitis in man. In masked comparative studies, predominantly in patients with dendritic ulcers, trifluridine 1% solution was effective in over 90% of patients; in such studies it was comparable with vidarabine in treating dendritic ulcers, and was at least as effective as, and in some studies more effective than, idoxuridine. The drug was also effective in treating a small number of patients with geographic ulcers (sometimes associated with the usage of topical corticosteroids), and this could be an important advantage if confirmed in further well-designed studies. However, experience at present is too limited to reliably determine the usual response rate in this difficult therapeutic area. In open studies the drug proved to be particularly useful in treating ulcers previously unresponsive to idoxuridine or vidarabine, and in treating patients intolerant of idoxuridine, with a high success rate and minimal side effects being reported. The role of trifluridine in treating deep stromal disease, uveitis, or adenovirus kerato-conjunctivitis has not been established. The drug is well tolerated and cross-hypersensitivity and cross-toxicity between trifluridine, idoxuridine and vidarabine are rare. Thus, trifluridine is an effective alternative to the drugs available for treating herpetic keratitis, and seems especially useful in 'difficult' cases.
曲氟尿苷（三氟胸腺嘧啶核苷）是一种用于眼部局部治疗的抗病毒药物，其结构与碘苷相关。体外研究表明，它能有效抑制1型单纯疱疹病毒的复制，该病毒可引起人类原发性角膜结膜炎和复发性上皮性角膜炎。在主要针对树枝状溃疡患者的双盲对照研究中，1%曲氟尿苷溶液对超过90%的患者有效；在此类研究中，它在治疗树枝状溃疡方面与阿糖腺苷相当，且在某些研究中至少与碘苷一样有效，甚至比碘苷更有效。该药物在治疗少数地图状溃疡患者（有时与局部使用皮质类固醇有关）时也有效，如果在进一步精心设计的研究中得到证实，这可能是一个重要优势。然而，目前的经验有限，无法可靠地确定在这个困难治疗领域的通常有效率。在开放性研究中，该药物被证明在治疗先前对碘苷或阿糖腺苷无反应的溃疡以及治疗对碘苷不耐受的患者方面特别有用，报告显示成功率高且副作用最小。曲氟尿苷在治疗深层基质疾病、葡萄膜炎或腺病毒角膜结膜炎方面的作用尚未确立。该药物耐受性良好，曲氟尿苷、碘苷和阿糖腺苷之间的交叉过敏和交叉毒性很少见。因此，曲氟尿苷是治疗疱疹性角膜炎现有药物的有效替代品，在“困难”病例中似乎特别有用。
