Factors affecting therapeutic concentration of topical aminocaproic acid in traumatic hyphema.
Epsilon-aminocaproic acid (EACA) decreases rebleeding in traumatic hyphema through antifibrinolytic activity. Therapeutic levels were achieved in aqueous humor of rabbits after topical application. Aqueous humor EACA levels were significantly higher after pretreatment with 0.5% proparacaine. Use of EACA (60%) in a carboxypolymethylene (CPM) vehicle (0.5%, 1%, 2%, 3%, and 4%) was examined. Aqueous humors levels at 4 hours ranged from 6.18-20.42 micrograms/ml. The 2% and 3% formulas achieved the highest concentrations in aqueous. Use of EACA (15%, 30%, 40%, and 60%) in 4% CPM was also studied. At 2 and 4 hours after treatment, the 30% EACA solution most effectively achieved therapeutic levels. Velcro closure devices were attached to the rabbit's eyelids, and 200 microliters of 30% EACA in 2% CPM was administered. After 3 hours the patched eyes had a mean aqueous EACA level of 60.09 micrograms/ml compared with 8.97 micrograms/ml in unpatched eyes. When dose size was studied in patched eyes, 200-microliters doses achieved aqueous levels of 60.09 micrograms/ml, and 100-microliters doses resulted in levels of 10.40 micrograms/ml. Since epithelial toxicity was observed in eyes that had been patched, the optimum topical regimen appeared to be 200 microliters of 30% EACA in 2% CPM every 6 hours in unpatched eyes.
Ehlers
W H
WH
Department of Ophthalmology, Eastern Virginia Medical School, Norfolk 23502.
Crouch
E R
ER
Williams
P B
PB
Riggs
P K
PK
D000180:Acrylic Resins; D000287:Administration, Topical; D015119:Aminocaproic Acid / Q000008:administration & dosage / Q000378:metabolism / Q000627:therapeutic use* / Q000633:toxicity; D000818:Animals; D001082:Aqueous Humor / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D015807:Eye Injuries, Penetrating / Q000150:complications*; D005135:Eye Protective Devices; D005260:Female; D006988:Hyphema / Q000188:drug therapy* / Q000209:etiology; D014677:Pharmaceutical Vehicles; D011145:Polyvinyls / Q000008:administration & dosage / Q000633:toxicity; D011292:Premedication; D011430:Propoxycaine / Q000627:therapeutic use; D011817:Rabbits
D000180:Acrylic Resins; D014677:Pharmaceutical Vehicles; D011145:Polyvinyls; C006912:carboxypolymethylene; C005717:proxymetacaine; D011430:Propoxycaine; D015119:Aminocaproic Acid