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J Ocul Pharmacol Ther ; 35(1): 66-75, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-30376399

RESUMEN

PURPOSE: Desmoteplase (DSPA) was evaluated and compared with tissue plasminogen activator (t-PA) for its intraocular fibrinolytic effect and short-term toxicity in an in vivo study using rabbit eyes. METHODS: Fibrin clots were induced in the anterior chamber of 44 rabbit eyes, and drug efficacy was measured by clot size reduction over 24 h. Topical DSPA eye drops (1.4 and 2 mg/mL) were compared with vehicle solution in a multiple-drop regimen in 8 animals per group. Intracameral injections of 0.6 µg DSPA (n = 14) and 25 µg t-PA (n = 14) were evaluated for their fibrinolytic efficacy. Animals were euthanized 24 h after drug application. RESULTS: No significant differences were seen between topically treated DSPA and vehicle-treated animals. Intracameral t-PA had a higher fibrinolytic efficacy than DSPA at early time points, but no significant difference was seen between both groups at 24-h postapplication. Animals with t-PA treatment demonstrated significantly more side effects compared with DSPA-treated animals. DSPA showed no-to-mild side effects after topical and intracameral treatment. Histologically, no toxic effects were observed in any globe. CONCLUSIONS: DSPA is a promising drug with fewer side effects and similar fibrinolytic efficacy compared with t-PA 24 h after intracameral application in rabbit eyes at the tested concentration. Drug efficacy might be improved by increasing intracameral DSPA doses.


Asunto(s)
Ojo/efectos de los fármacos , Fibrinolíticos/farmacocinética , Soluciones Oftálmicas/farmacocinética , Activadores Plasminogénicos/metabolismo , Activador de Tejido Plasminógeno/metabolismo , Administración Tópica , Animales , Relación Dosis-Respuesta a Droga , Ojo/metabolismo , Ojo/patología , Femenino , Fibrinolíticos/administración & dosificación , Inyecciones Intraoculares , Soluciones Oftálmicas/administración & dosificación , Activadores Plasminogénicos/administración & dosificación , Conejos , Activador de Tejido Plasminógeno/administración & dosificación
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