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At least 19 recordsLinked to original sources
PubMed1996

A Review of Post--Cardiopulmonary Bypass Bleeding, Aminocaproic Acid, Tranexamic Acid, and Aprotinin.

OBJECTIVE: To review the mechanism and cause of hemostatic defects following cardiopulmonary bypass (CPB) and determine the safety and efficacy of antifibrinolytic agents for use in cardiac surgery and patients likely to benefit. DATA SOURCES: A MEDLINE search (1966 to present) of the English-language literature pertaining to aminocaproic acid (ACA), tranexamic acid (TA), and aprotinin was performed. Additional literature was obtained from reference citations of pertinent articles identified through the search. STUDY SELECTION AND DATA EXTRACTION: While all articles of relevance were considered for inclusion, this review evaluates only clinical trials with emphasis on prospective, randomized, controlled studies. DATA SYNTHESIS: In reported trials, ACA and TA each reduce mediastinal blood losses by about one-third, while transfusion needs remain unchanged. ACA and TA dosing inconsistencies, omission of transfusion criteria, and unidentified surgical risk factors prevent optimal findings. Thromboembolic complications could not be ascribed to either ACA or TA in more than 950 patients studied. Aprotinin decreased mean mediastinal blood losses by 42%, 67% and 48% in primary coronary artery bypass grafting (CABG), reoperative CABG, and in CABG patients receiving aspirin, respectively. Transfusion needs were reduced 42% in primary CABG patients and 55% to 88% in high-risk patients. Patients at high risk of bleeding (i.e., reoperative CABG and patients on aspirin) demonstrated greater transfusion needs and blood loss than primary CABG patients. As blood conservation measures may eliminate the need for transfusions among primary CABG patients, patients at higher risk may benefit most from the addition of antifibrinolytic prophylaxis. CONCLUSION: The efficacy of all antifibrinolytic agents in cardiac surgery has been established, but comparative data is inconclusive to suggest an agent of choice. Thromboembolic complications have been rare and difficult to ascribe to antifibrinolytic agents. Future trials comparing efficacy of agents in high risk patients and rigorously evaluating thromboembolic events will allow unconditional recommendations.

Journal Article↗
PubMed1981

Pharmacokinetics and bioavailability of tranexamic acid.

Tranexamic acid 1 g was given intravenously to three healthy volunteers. Plasma concentrations decayed in three monoexponential phases. Most elimination took place during the first eight hours, giving an apparent elimination half-life of approximately two hours. Plasma clearance ranged between 110-116 ml/min. The urinary recovery of tranexamic acid exceeded 95% of the dose. Ten healthy volunteers were given tranexamic acid 2 g orally on an empty stomach, and together with a meal. Food had no influence on the absorption of tranexamic acid, as judged by comparison of the peak plasma concentration, the time required to reach the peak, the AUC from zero to six hours, and the urinary excretion data. The oral bioavailability of tranexamic acid, calculated from 24 h urinary excretion after oral and intravenous administration, was 34% of the dose.

Administration, Oral↗
PubMed1996

Treatment of menorrhagia during menstruation: randomised controlled trial of ethamsylate, mefenamic acid, and tranexamic acid.

OBJECTIVE: To compare the efficacy and acceptability of ethamsylate, mefenamic acid, and tranexamic acid for treating menorrhagia. DESIGN: Randomised controlled trial. SETTING: A university department of obstetrics and gynaecology. SUBJECTS: 76 women with dysfunctional uterine bleeding. INTERVENTIONS: Treatment for five days from day 1 of menses during three consecutive menstrual periods. 27 patients were randomised to take ethamsylate 500 mg six hourly, 23 patients to take mefenamic acid 500 mg eight hourly, and 26 patients to take tranexamic acid 1 g six hourly. MAIN OUTCOMES MEASURES: Menstrual loss measured by the alkaline haematin method in three control menstrual periods and three menstrual periods during treatment; duration of bleeding; patient's estimation of blood loss; sanitary towel usage; the occurrence of dysmenorrhoea; and unwanted events. RESULTS: Ethamsylate did not reduce mean menstrual blood loss whereas mefenamic acid reduced blood loss by 20% (mean blood loss 186 ml before treatment, 148 ml during treatment) and tranexamic acid reduced blood loss by 54% (mean blood loss 164 ml before treatment, 75 ml during treatment). Sanitary towel usage was significantly reduced in patients treated with mefenamic acid and tranexamic acid. CONCLUSIONS: Tranexamic acid given during menstruation is a safe and highly effective treatment for excessive bleeding. Patients with dysfunctional uterine bleeding should be offered medical treatment with tranexamic acid before a decision is made about surgery.

Adult↗
PubMed1995

Microscopic haematuria as a relative contraindication for tranexamic acid.

Tranexamic acid has been advocated for patients with severe bleeding tendency due to thrombocytopenia not responding to platelet transfusions. Macroscopic haematuria is a well-known contraindication for its use in such patients. We present three clinical cases with microscopic haematuria, in whom tranexamic acid caused problems of clot formation in the urinary tract, indicating that microscopic haematuria should also be considered as a contraindication for tranexamic acid.

Adult↗
PubMed2004

Comparison of epsilon aminocaproic acid and tranexamic acid in pediatric cardiac surgery.

OBJECTIVE: This study compared the efficacy of aminocaproic acid and tranexamic acid in reducing postoperative blood loss, as well as blood and blood product requirements in children with cyanotic congenital heart disease. DESIGN: A prospective randomized study. SETTING: Cardiac center of a tertiary care, referral hospital. PARTICIPANTS: One hundred fifty children in the age group of 2 months to 14.5 years with cyanotic congenital heart disease undergoing corrective surgery on cardiopulmonary bypass (CPB). INTERVENTIONS: Patients were randomized into 3 groups. Group A was given aminocaproic acid in a dose of 100 mg/kg after anesthetic induction, 100 mg/kg on CPB and 100 mg/kg after protamine. Group T was given tranexamic acid, 10 mg/kg, after anesthetic induction, 10 mg/kg on CPB, and 10 mg/kg after protamine. Group C was the control group. MAIN RESULT: Control group had the longest sternal closure time, maximum blood loss at 24 hours, and maximum requirements of blood and blood products. Among the 2 groups given antifibrinolytics, there was no significant difference in postoperative blood loss, blood and product requirement, and reexploration rates. CONCLUSION: Aminocaproic acid and tranexamic acid are equally effective in reducing postoperative blood loss, as well as blood and blood product requirements in children with cyanotic heart disease undergoing corrective surgery as compared with the control group.

Adolescent↗
PubMed1987

Clinical pharmacology of tranexamic acid.

Tranexamic acid (AMCA) is a potent antifibrinolytic drug occurring in two isomeric forms; the antifibrinolytic potency resides in the transisomeric form. The main action of AMCA is blocking of the lysine-binding sites of the plasminogen molecule, which are of importance for the binding to fibrin. This prevents activation of plasminogen by plasminogen activator also absorbed to fibrin. AMCA can be administered perorally or intravenously and is excreted into the urine. It enters tissues and fluids in various concentrations and crosses the placenta. There is no evidence of a thrombogenic effect of AMCA, but in accordance with its action, it prolongs dissolution of fibrin deposits already formed. AMCA is a drug of high clinical value for the treatment of bleedings due to both systemic and local fibrinolysis.

Animals↗
PubMed1997

The use of low-dose aprotinin, epsilon-aminocaproic acid or tranexamic acid for prevention of mediastinal bleeding in patients receiving aspirin before coronary artery bypass operations.

Patients undergoing primary myocardial revascularization were randomized to one of three drug regimens (low-dose aprotinin, epsilon-aminocaproic Acid or tranexamic Acid) to determine which drug regimen would most effectively reduce post-operative bleeding and the need for blood products. All patients had received 325 mg of aspirin within 48 h before operation. All three drug regimens reduced the requirements for blood products and postoperative bleeding after coronary artery bypass operations. There was, however, no significant difference between drug regimens.

Aminocaproic Acid↗
PubMedDate not supplied

The preventative effect of the antifibrinolytic agents, epsilon-aminocaproic acid and tranexamic acid, on stress ulcer formation in rats.

The effect of the antifibrinolytic agents, epsilon-aminocaproic acid (EACA) and tranexamic acid (t-AMCHA), on acute gastric ulcers induced by cold restraint stress in rats was studied. Intravenous administration of 500 mg/Kg of EACA and t-AMCHA before exposure to stress significantly reduced the severity of gastric bleeding and ulcer formation (P less than 0.01). These agents did not affect gastric acid secretion in pylorus-ligated rats. The results indicate that antifibrinolytic agents may be beneficial in the prevention of stress ulcers in man and support the concept that local gastric fibrinolysis may play a role in the pathogenesis of stress ulcers.

Aminocaproates↗
PubMed1998

Aminocaproic acid and tranexamic acid increase the rate of acute corneal reepithelialization in Sprague Dawley rats.

Antifibrinolytic agents, epsilon-aminocaproic acid (EACA) and tranexamic acid (TXA), have been reported to be efficacious in the treatment of chronic persistent epithelial defects. Within the regulatory mechanism of corneal reepithelialization, fibronectin serves as a primary adhesive component in the healing process and anchors regenerating epithelial cells to underlying stroma. EACA and TXA inhibit the activation of plasmin thereby decreasing plasmin-induced catabolism of fibronectin. In this study, acute reepithelialization following treatment with EACA and TXA was evaluated in the cultured rat cornea model. Sprague Dawley rat corneal explants with 3 mm corneal defects, induced with 1 N NaOH, were cultured with either EACA or TXA. After 12 or 24 hr incubation periods, corneal explants were stained with bromodeoxyuridine stain for measuring cellular division and migration or Trypan Blue for measuring the extent of dead cells. Both EACA and TXA increased the rate of reepithelialization in comparison to an untreated control. EACA was up to 35% more efficacious than TXA. Thus, this study demonstrated an acute effect for EACA and TXA versus the previously reported efficacy of chronic therapy required for persistent epithelial defects. Broad applications may prove beneficial in the clinical treatment of corneal abrasions, persistent corneal epithelial defects, or alkali burns.

Aminocaproic Acid↗
PubMed1992

Antifibrinolytic activities of alpha-N-acetyl-L-lysine methyl ester, epsilon-aminocaproic acid, and tranexamic acid. Importance of kringle interactions and active site inhibition.

alpha-N-acetyl-L-lysine methyl ester (NALME) is a lysine analogue that reportedly binds to low-affinity lysine binding sites in plasmin(ogen) and miniplasmin(ogen). In the studies presented here, we show that NALME has antifibrinolytic activity; however, unlike the therapeutic agents epsilon-amino-n-caproic acid (epsilon ACA) and tranexamic acid (TEA), the activity of NALME is based on inhibition of the plasmin active site. NALME (0.1-10 mM) significantly inhibited the amidase activity of plasmin, miniplasmin, and streptokinase-plasmin complex without affecting alpha-thrombin or tissue plasminogen activator. epsilon ACA and TEA (0.1-10 mM) did not affect the amidase activity of plasmin or miniplasmin. A kinetic analysis showed that NALME is a competitive inhibitor of D-Val-L-Lys-p-nitroanilide HCl (S-2251) hydrolysis by plasmin; NALME binding to plasmin completely prevented S-2251 binding. The Kl for the plasmin-NALME interaction was 0.4 mM. epsilon ACA and TEA inhibited fibrin monomer digestion by plasmin and miniplasmin without binding to the active site of either enzyme. This result suggests that epsilon ACA and TEA function as antifibrinolytics by disrupting the noncovalent association of fibrin monomer with a domain common to both plasmin and miniplasmin (probably kringle 5). NALME inhibited fibrin monomer digestion principally by decreasing amidase activity. NALME was the only lysine analogue that prevented fragment X formation; TEA and epsilon ACA primarily inhibited the formation of fragments Y and D. When plasmin was incubated simultaneously with alpha 2-antiplasmin and alpha 2-macroglobulin, epsilon ACA increased the fraction of plasmin reacting with alpha 2-macroglobulin; NALME had no effect on the plasmin distribution.(ABSTRACT TRUNCATED AT 250 WORDS)

Amidohydrolases↗
PubMed1981

Comparative clinical trial of epsilon amino-caproic acid and tranexamic acid in the prevention of early recurrence of subarachnoid haemorrhage.

A comparative controlled clinical trial of epsilon aminocaproic acid (EACA), 36 g/day and tranexamic acid (TEA), 6 g/day, was undertaken to assess their effectiveness in reducing early recurrence of subarachnoid haemorrhage (SAH). Of 90 patients treated with EACA recurrent haemorrhage was seen in 8% of these patients and 7% of the patients developed delayed ischaemic deficit. The total pre-operative mortality in EACA-group was 11%. Of 61 patients treated with TEA, 10% had recurrent haemorrhage and delayed ischaemic deficit occurred in 5% of the patients. The total pre-operative mortality in TEA-group was 11%. No difference was found between the effectiveness and side-effects of these drugs.

Adolescent↗
PubMed1988

Absorption of tranexamic acid as a prodrug in healthy volunteers.

The absorption of trans-4-(aminomethyl)cyclohexanecarboxylic acid (tranexamic acid, Cyklokapron) administered as the prodrug trans-4-(aminomethylcyclohexanecarboxylate hydrochloride (Kabi 2161) was investigated in 3 healthy volunteers. Kabi 2161 was given orally in doses of 1, 2, 3 and 3.5 mmol, respectively, and as a reference a clinical dose of 1.5 g tranexamic acid (9.6 mmol) was administered. At 3 mmol of Kabi 2161 the same maximum plasma concentration of tranexamic acid was obtained as with the reference drug but with Kabi 2161 it appeared earlier. The recovery of tranexamic acid in the urine 0-48 h after administration of Kabi 2161 was 84.7, 82.4, 89.4 and 97.5%, resp., of the increasing doses. For the tranexamic acid 37.0% could be recovered. A similar result was seen in the areas under the plasma concentration-time curves normalized for dose. With Kabi 2161, 13.1, 19.6, 14.4 and 14.3 mg.h/l.mmol were found compared to 8.0 mg.h/l.mmol with tranexamic acid. From these results it was concluded that Kabi 2161 markedly increased the bioavailability of tranexamic acid in man.

Adult↗
PubMed1980

Different assessment of plasmin with different substrates. In vitro alteration of plasmin, influence of epsilon-aminocaproic acid and tranexamic acid upon its activity.

The alteration of human and porcine plasmin and the influence of EACA and AMCHA on their activity were investigated. Solutions of both plasmins undergo storage induced alteration, which is best recorded by Chromozym PL, whereas the other chromogenic substrates, S-2251 and S-2302, and casein are less sensitive, and the fibrin plate inadequate. Plasmin amidolytic and fibrinolytic activity is maximally enhanced at 7.6 x 10(-3) M EACA and 6.4 x 10(-4) M AMCHA, and decay through storage is reversed. The caseinolytic activity seems slightly inhibited at the same EACA and AMCHA concentrations. Our results show: 1. The quotient: plasmin activity towards Chromozym PL/Activity towards S-2251 is a useful indicator of "plasmin quality". The quotient decreases markedly upon storage of plasmin solutions. 2. Plasmin stability is improved in the presence of AMCHA. 3. It is valueless to add EACA or AMCHA to inhibit plasmin in amidolytic assays since the chosen concentration enhances the amidolytic activity of already formed plasmin.

Aminocaproates↗