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At least 127 records · Page 7Linked to original sources
PubMed1997

Modification of short peptides using epsilon-aminocaproic acid for improved coating efficiency in indirect enzyme-linked immunosorbent assays (ELISA).

The hydrophobicity of short synthetic peptides of 5-10 residues was enhanced for high coating efficiency as antigens in indirect ELISA. To obtain enhanced hydrophobicity, coupling of epsilon-aminocaproic acids to the synthetic peptides was carried out during solid phase peptide synthesis. As a short peptide model, three analogues of a streptavidin binding peptide consisting of 5 amino acid residues were prepared with four epsilon-aminocaproic acid residues. HPLC analysis showed a dramatic increase in hydrophobicity after modification and the modified peptides showed a better adsorption ability than the unmodified peptides in indirect ELISA. The whole process from antigen coating to color development was carried out within 2.5 to 3 h by dissolving the peptide in methyl alcohol and evaporating the solvent in each well of the microplate. As an application of this method, a peptide assumed to function as one of the epitopes of the human 60 kDa Ro/SSA antigen was selected from hydrophilicity, acrophilicity and hydropathy plots. The peptide was synthesized having an epsilon-aminocaproic acid modification at both N and C terminal ends and was tested with 30 sera from patients with systemic lupus erythematosus (SLE), 20 normal sera and a standard anti-Ro/SSA serum. The ELISA results revealed that the method gave a high signal-to-background ratio without altering the specificity of the assay. Moreover, our process was far simpler and more rapid than conventional methods used in indirect ELISA. Thus this method could be useful in the development of techniques for the diagnosis of SLE.

Aminocaproic Acid↗
PubMed2004

The effect of some epsilon-aminocaproic acid derivatives on platelet responses.

epsilon-Aminocaproic acid (EACA) is a synthetic low molecular drug with antifibrinolytic activity. However, treatment with this drug can be incidentally associated with an increased thrombotic tendency. The aim of the present work was to test synthetic EACA derivatives for their antiplatelet activities. We investigated the effect of three EACA derivatives with antifibrinolytic activity: I. epsilon-aminocaproyl-L-leucine hydrochloride (HCl*H-EACA-L-Leu-OH), II. epsilon-aminocaproyl-L-(S-benzyl)-cysteine hydrochloride (HCl*H-EACA-L-Cys(S-Bzl)-OH) and III. epsilon-aminocaproyl-L-norleucine (H-EACA-L-Nle-OH) on platelet responses (aggregation and adhesion) and on their integrity. It was found that: 1. as judged by LDH release test, none of the tested compounds, up to 20 mM, was toxic to platelets, 2. in comparison with EACA, all the synthetic derivatives inhibited much stronger the ADP- and collagen-induced aggregation of platelets suspended in plasma (platelet rich plasma) and aggregation of these cells in whole blood, 3. EACA and its derivatives exerted a similar inhibitory effect on the thrombin-induced adhesion of platelets to fibrinogen-coated surfaces. Since platelet activation and blood coagulation are tightly associated processes, the antiplatelet properties of EACA derivatives are expected to indicate reduced thrombotic properties of these derivatives compared to EACA.

Adenosine Diphosphate↗
PubMed1976

Gas-chromatographic determination of an antifibrinolytic drug, epsilon-aminocaproic acid.

We describe a modified method for assay of epsilon-aminocaproic acid. Serum or cerebrospinal fluid is deproteinized, followed by cation-exchange column-chromatography, and N-trifluoroacetyl-n-butyl derivatives of amino acids are formed and separated by gas chromatography. Tranexamic acid, a nonprotein amino acid, was used as an internal standard. The assay is sensitive and precise, and results correlate adequately with those obtained with an automated amino acid analyzer (ion-exchange chromatography).

Amino Acids↗
PubMed2002

The pharmacokinetics of epsilon-aminocaproic acid in children undergoing surgical repair of congenital heart defects.

UNLABELLED: epsilon-Aminocaproic acid (epsilonACA) is often administered to children undergoing cardiac surgery by using empiric dosing techniques. We hypothesized that children would have different pharmacokinetic variables and require a dosing scheme different from adults to maintain stable and effective serum epsilonACA concentrations. Eight patients were enrolled in our study. epsilonACA 50 mg/kg was administered three times IV: before, during, and after cardiopulmonary bypass (CPB). Nine serum samples were obtained. epsilonACA plasma concentrations were measured by using high-performance liquid chromatography, and pharmacokinetic modeling was done by using NONMEM. The best fit was seen with a two-compartment model with volume of distribution (V(1)) adjusted for weight and CPB. Compared with published results in adults, modeling suggests that weight-adjusted V(1) is larger in children than in adults before, during, and after CPB. Clearance from the central compartment (k(10)) was also greater in children than adults, and declined during CPB. Redistribution rates from the central compartment, k(12) and k(21), were greater in children and not affected by CPB. We modeled several different dosing regimens for epsilonACA based on the larger V(1), and higher redistribution and clearance variables. We conclude that, because of the developmental differences in pharmacokinetic variables of epsilonACA, when compared with adult patients, a larger initial dose and faster infusion rate as well as an addi-tional dose on CPB are needed to maintain similar concentrations. IMPLICATIONS: Pharmacokinetic modeling of epsilon-aminocaproic acid in children undergoing cardiac surgery suggests that there are developmental differences in pharmacokinetic variables. Based on these data, a dosing modification in children is suggested which may better maintain serum concentrations in children when compared with adults.

Aminocaproic Acid↗
PubMed1984

Aminocaproic acid treatment of recurrent postoperative hyphemas.

Three patients were treated with aminocaproic acid for medically uncontrolled hyphemas that developed after cataract extractions. In all three patients the bleeding stopped after a course of aminocaproic acid was begun. This happened despite a very short course of therapy in two patients. All three patients had to have treatment discontinued because of side effects, in part contributed to by preexisting medical problems, appeared.

Aged↗
PubMed1989

Pepsin fibrinolysis of artificial clots made from fibrinogen concentrate and bovine thrombin: the effect of pH and epsilon aminocaproic acid.

Artificial clots made from fibrin glue with and without an inhibitor of fibrinolysis can be used to treat gastrointestinal bleeding. We have been unable to find descriptions of the effects of acid and pepsin upon such artificial clots. Therefore, 10(-2) mol/l epsilon aminocaproic acid was added to fibrin glue in vitro at acid concentrations of pH 1.0 and pH 5.5. Pepsin was added at 9000 U/50 ml, the expected value for fasting human subjects. There was a highly significant reduction in clot survival at pH 1.0. At pH 5.5, clot weight was also significantly decreased with pepsin, compared to control. Thus pepsin and acidity greatly affect survival of artificial clots, but the addition of epsilon aminocaproic acid did not affect clot survival.

Aminocaproates↗
PubMed1982

Successful treatment of skeletal hemangioma and Kasabach-Merritt syndrome with aminocaproic acid. Is fibrinolysis "defensive"?

A young man presented with a disabling skeletal hemangioma. Fibrinolysis seemed to be a major component of coagulopathy and persisted after steroid therapy and irradiation of the lesions. Three weeks after therapy with epsilon-aminocaproic acid, there was dramatic alleviation of pain and eventual disappearance of laboratory evidence of fibrinolysis. Epsilon-aminocaproic acid therapy was discontinued. The patient remained free from symptoms and coagulopathy. There was evidence of new bone formation nine months later. Fibrinolysis may be a primary or sustaining feature of hemangioma. Epsilon-aminocaproic acid may be beneficial in the treatment of selected patients with these lesions.

Adult↗
PubMed1984

Epsilon aminocaproic acid and the control of post-prostatectomy bleeding: a prospective double-blind study.

We randomized 61 patients undergoing transurethral resection of the prostate in a double-blind parallel fashion to receive epsilon aminocaproic acid or an equivalent volume of placebo solution immediately after the operation. All blood loss during the first 72 hours postoperatively was monitored. Four patients were nonevaluable . The use of epsilon aminocaproic acid caused no significant complication or side effect. There was no significant difference in regard to blood loss, hospital stay or days on catheter drainage between the 2 groups. We conclude that the routine use of epsilon aminocaproic acid after transurethral resection of the prostate is not warranted.

Aminocaproates↗
PubMed1986

Acute renal failure due to high-grade obstruction following therapy with epsilon-aminocaproic acid.

An 18-year-old man with mild factor VIII deficiency developed hematuria and, subsequently, acute renal failure due to high-grade urinary obstruction by clots during therapy with cryoprecipitate, epsilon-aminocaproic acid, and acetazolamide administered for ocular trauma. Discontinuation of therapy with the latter two agents and induction of a brisk diuresis with intravenous (IV) fluid therapy resulted in return of renal function concomitant with spontaneous clot passage. A review of previous literature suggests that hemophiliacs may be more susceptible than nonhemophiliacs to high-grade urinary obstruction due to clot formation when epsilon-aminocaproic acid is administered during episodes of hematuria. Acute flank pain, fever, and delayed dense nephrograms on IV pyelogram are characteristic of the syndrome and distinguish it from other forms of acute renal failure associated with epsilon-aminocaproic acid.

Acute Kidney Injury↗
PubMed1986

[Use of epsilon-aminocaproic acid for treating granulating burn wounds].

Results of the application of synthetic inhibitor of proteolytic enzymes epsilon-aminocaproic acid in the treatment of granulating burn wounds are described. High effectiveness of the aminocaproic acid in healing of granulating wounds after burns is shown as well as in preparing great granulating burn wounds for autodermoplasty and the take of transplanted autodermic flaps.

Adolescent↗
PubMedDate not supplied

Survival of transfused factor VIII in hemophilic patients treated with epsilon aminocaproic acid.

The effect of EACA (epsilon aminocaproic acid) on the survival of factor VIII (F. VIII, antihemophilic factor, AHF) concentrates after infusion in hemophilic subjects was studied using two F. VIII preparations: an intermediate purity "cryoglobulin" and a high purity glycine-precipitated concentrate. In vivo recoveries of F. VIII with both concentrates were found to be close to the values predicted on the basis of concentrate potencies assayed prior to infusion, but not if the labeled potency was used in the calculation. Control studies showed similar first and second phase half-life times and half-disappearance times when the two F. VIII preparations were infused, and both preparations were found to follow a biphasic disappearance curve. The biological half-life (second phase rate of disappearance) was 12 to 13 hours. The administration of EACA in conjunction with the F. VIII concentrates did not prolong the half-life times (first or second phase) or the half-disappearance times.

Adult↗
PubMed1983

Aminocaproic acid decreases secondary hemorrhage after traumatic hyphema.

Forty-eight patients (49 eyes) had nonperforating traumatic hyphema. Twenty-eight patients (28 eyes with hyphema) received oral aminocaproic acid, an antifibrinolytic agent, in a dosage of 100 mg/kg every four hours for five days, up to a maximum daily dose of 30 g. Twenty patients (21 eyes with hyphema) received placebo in an identical regimen. One eye treated with aminocaproic acid rebled; seven eyes receiving the placebo rebled. The results of this study show a statistically significant reduction in the incidence of secondary hemorrhage in the patients receiving aminocaproic acid.

Adolescent↗
PubMed1979

Prevention of early recurrence of spontaneous subarachnoid haemorrhage by epsilon-aminocaproic acid.

A controlled clinical trial of epsilon-aminocaproic acid (E.A.C.A.), 36 g/day, was undertaken to assess its effectiveness in reducing immediate recurrence in patients with spontaneous subarachnoid haemorrhage (S.A.H.) proved by lumbar puncture. Of 83 patients treated with E.A.C.A., 3 (4%) had recurrent haemorrhage, and 1 (33%) of these died. Of 82 control patients who were not given any antifibrinolytic drug, 22 (26%) had recurrent haemorrhage, and 10 (45%) of these patients died. E.A.C.A. produced a striking reduction in the early recurrence of S.A.H. No serious side-effect resulted.

Adolescent↗
PubMedDate not supplied

Topical aminocaproic acid to prevent rebleeding in cases of traumatic hyphema.

PURPOSE: To determine the effect of topical aminocaproic acid on the incidence of rebleeding after traumatic hyphema. PATIENTS AND METHODS: This randomized double blind clinical trial investigated 132 consecutive cases of traumatic hyphema referred to the emergency room of Farabi Eye Hospital in 1998-1999. The patients were randomly divided into three groups: Group 1 received cycloplegic drops only. Group 2 received cycloplegic drops and 2% carboxy polymethylene (CPM) gel as placebo. Group 3 was treated with cycloplegic drops and 25% aminocaproic acid (ACA) in CPM gel (supplied by Messrs. Sina Darou). All patients were treated for five days on an outpatient basis, with a two-week follow-up. The incidence of rebleeding, time needed for clot absorption, and complications of hyphema were recorded and analyzed using the chi-square and Student's t-tests and logistic regression modeling. RESULTS: Rebleeding occurred in 8 eyes of 52 patients in group 1 (15.4%), 7 eyes of the 39 patients in group 2 (17.9%) and 5 eyes of the 41 patients in group 3 (12.2%). This difference was not significant. The time needed for clot absorption in groups 1, 2 and 3 was respectively 9.5 +/- 3.9, 9.3 +/- 4.2 and 11.15 +/- 4.7 days, the difference between group 3 and the other two groups being statistically significant (p<0.04). CONCLUSIONS: Topical 25% ACA is not effective in reducing the incidence of rebleeding and lengthens the time needed for clot absorption.

Administration, Topical↗
PubMed1982

The effects of epsilon aminocaproic acid on contractile properties and catecholamine content of rat carotid arteries.

The prevalent use of epsilon aminocaproic acid (EACA) to prevent rebleeding in the preoperative management of ruptured intracranial aneurysms raises the question of a relationship between this drug and cerebral vasospasm. The effects of EACA on the contractile properties of the rat common carotid artery were measured in vitro, and the effects of EACA on the catecholamine content of these arteries were determined qualitatively. When carotid artery segments from rats that had been infused with lactated Ringer's solution alone were incubated in the presence of 1 mM EACA, they exhibited a decrease in contractile activity brought about by the presence of either serotonin or norepinephrine, and an increase in contractile activity when potassium chloride was used. These changes were not witnessed if the arterial segments came from rats that had been infused with lactated Ringer's solution containing EACA. No effect of epsilon aminocaproic acid was found on the median effective dose values for each vasoconstrictor used. Fluorescence histochemistry showed no qualitative changes in the catecholamine content of carotid arteries following EACA treatment.

Aminocaproates↗
PubMed1986

Epsilon-aminocaproic acid in the treatment of patients with acute promyelocytic leukemia and acquired alpha-2-plasmin inhibitor deficiency.

Patients with acute promyelocytic leukemia often develop bleeding diatheses during treatment. In seven patients who had this disease, the plasma level of alpha-2-plasmin inhibitor was the best predictor of severity of coagulopathy and bleeding. Clinical bleeding occurred when alpha-2-plasmin inhibitor levels measured less than 30% of normal levels. Patients with acute promyelocytic leukemia who had acquired deficiencies of alpha-2-plasmin inhibitor were considered to have deficits similar to those in persons congenitally deficient in alpha-2-plasmin inhibitor, and were assumed to be at increased risk for bleeding. Treatment with the fibrinolytic inhibitor, epsilon-aminocaproic acid, along with heparin resulted in prompt cessation of bleeding, reversal of laboratory evidence of fibrinolysis, and a decreased need for blood product support. The only thrombotic complication--thrombosis around a central venous catheter--resolved when treatment with epsilon-aminocaproic acid was discontinued. Epsilon-aminocaproic acid is a safe and effective therapy for those patients with acute promyelocytic leukemia who develop coagulopathy associated with low levels of alpha-2-plasmin inhibitor.

Aminocaproates↗