L. Andersson, I. Nilsson, J. Niléhn
Apr 24, 2009
Citations
3
Influential Citations
132
Citations
Quality indicators
Journal
Scandinavian journal of haematology
Abstract
1. Amino methyl cyclohexane carboxylic acid is a potent inhibitor of plasminogen activation. A preparation of the active isomer, AMCA, was found to be 6–8 times more potent than e-ACA and to have an inhibitory effect demonstrable in a concentration of 10-4M. AMCA had no antiplasmin effect in concentrations up to 0.15 M. 2. In high concentrations, 1 mg per ml blood, AMCA prolonged the thrombin time, but it had no other effect on the coagulation mechanism. 3. Metabolic studies showed that the half-life of AMCA in serum was short, about 1–2 hours. It was rapidly excreted in unchanged form in the urine and 90 per cent of a single intravenous dose of AMCA was excreted from the urine within 24 hours. 4. AMCA was given to 50 subjects, including 20 with increased fibrinolytic activity and/or bleeding symptoms. It proved an effective antifibrinolytic agent and stopped bleeding caused by general or local fibrinolysis. Judging from in vivo tests the inhibiting effect of AMCA was about 7 times that of e-ACA. – Dizziness occurred in 6 cases, but no other side reactions or toxic effects of the drug were observed. 5. AMCA is recommended as a useful clinical fibrinolytic inhibitor. A dosage of 0.015–0.020 g per kg bodyweight given intravenously every 4–6 hours appears to be adequate. For oral therapy doses of 0.05–0.1 g per kg bodyweight are required every 4–6 hours.