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At least 145 records · Page 8Linked to original sources

epsilon-Aminocaproic acid plasma levels during cardiopulmonary bypass.

epsilon-Aminocaproic acid (EACA) concentrations achieved during cardiopulmonary bypass (CPB) have not been previously reported. It is unknown whether plasma concentrations reported to inhibit fibrinolysis in vitro (130 microg/mL) are achieved or whether differences in these levels relate to variability in postoperative bleeding. EACA (total intraoperative dose 270 mg/kg) was administered to 27 patients undergoing cardiac reoperation. The plasma EACA concentration was measured by using high-pressure liquid chromatography: 1) 30 min after initiation of drug administration (baseline); 2) 30 min (CPB + 30) after initiation of CPB; 3) 90 min after initiation of CPB. (CPB + 90); and 4) at cardiopulmonary bypass termination (end CPB). Plasma EACA concentrations (microg/mL, min - max, mean +/- SD) were 276-998, 593 +/- 154 at baseline; 147-527, 302 +/- 95 at CPB + 30; 112-500, 314 +/- 100 at CPB + 90; and 84-537, 317 +/- 100 at end CPB. Twenty-four-hour postoperative thoracic drainage and allogeneic red blood cell transfusions were not associated with plasma levels at any time. Although plasma EACA concentrations greater than 130 microg/mL were consistently achieved, we observed a marked variability (more than sixfold) in plasma concentrations and bleeding outcomes despite the use of a weight-based dosing regimen. This variability in drug levels appears to have little relevance to bleeding outcomes, possibly since mean plasma levels exceeded 130 microg/mL during CPB, and nearly all patients (26 of 27) achieved that target level.

Aged↗

Aminocaproic acid. Use in control of hemorrhage in patients with amegakaryocytic thrombocytopenia.

The bleeding complications of some forms of thrombocytopenia are difficult to control. Many patients become refractory to platelet transfusions even when HLA-matched. We have successfully used aminocaproic acid to control bleeding in 13 patients with amegakaryocytic thrombocytopenia. Four patients receiving long-term therapy with this drug had striking reductions in the number of platelet transfusions required for capillary bleeding. No adverse effects have been noted save for orthostatic hypotension, which is ameliorated by a reduction in dosage. Quantitative platelet function changes have been impossible to demonstrate, but no changes were noted in four patients with normal platelet counts who were receiving high-dose aminocaproic acid for treatment of subarachnoid hemorrhage. Aminocaproic acid has proved to be a valuable agent in the management of patients with amegakaryocytic thrombocytopenia, especially in decreasing the need for platelet transfusions.

Adolescent↗

Noninflammatory bullae associated with epsilon-aminocaproic acid infusion.

Three patients who had cardiac surgery developed a transient, noninflammatory subepidermal bullous eruption on the legs after epsilon-aminocaproic acid infusion. Fibrin thrombi were demonstrated in papillary dermal vessels. The use of epsilon-aminocaproic acid as an antifibrinolytic agent may predispose patients to cutaneous vascular thromboses.

Adult↗

Safety and efficacy of intravesical aminocaproic acid for bleeding after transurethral resection of prostate.

There appears to be no clinically significant difference in blood loss or transfusion requirements after transurethral resection of the prostate (TURP) when intravesical 0.5% aminocaproic acid is compared with 0.9% sodium chloride irrigation in patients during the first three days after surgery. This is probably because early post-TURP bleeding is due to inadequate hemostasis or perforation of the prostatic capsule, and not excessive local or systemic fibrinolysis. However, we suggest that intravesical aminocaproic acid might be a useful alternative to systemic antifibrinolytic therapy in patients with delayed, recurrent, excessive post-prostatectomy bleeding, which is thought to be due to fibrinolysis. Since aminocaproic acid is not systemically absorbed after bladder instillation, intravesical administration causes few side effects and does not necessitate screening patients for disseminated intravascular coagulation prior to treatment.

Aged↗

Effect of epsilon-aminocaproic acid on postvitrectomy hemorrhage.

We performed a prospective study involving 96 patients undergoing vitrectomy for proliferative diabetic retinopathy to determine the effect of epsilon-aminocaproic acid on the occurrence of postoperative intraocular hemorrhage. epsilon-Aminocaproic acid significantly reduced postoperative vitreous hemorrhage during the immediate postoperative period. Follow-up examinations two to six weeks after discharge from the hospital disclosed no statistically significant difference in the severity of vitreous hemorrhage between the treated and untreated groups. The loss of drug effect at this stage was in part due to spontaneous repeated bleeding in the treated group and in part to spontaneous clearing of hemorrhage in the untreated group. There was no statistically significant difference in the rate of repeated bleeding between the two groups or in rate of spontaneous clearing.

Aminocaproates↗

[The inhibiting effect of epsilon-aminocaproic acid on the incidence of induced tumors of the esophagus, nervous system and kidneys].

The anticarcinogenic properties of epsilon-aminocaproic acid were studied in two rat models of carcinogenesis. Esophageal tumors were induced by oral instillations of a total dose of 54 mg/kg body weight N-methyl-N-benzylnitrosamine whereas tumors of the nervous system and kidney-by transplacental injection of 75 mg/kg body weight N-ethyl-N-nitrosourea. epsilon-Aminocaproic acid given at a concentration of 1 milligram drinking water at the post-initiation stage of the carcinogenesis was shown to inhibit the induction of cancer and papilloma of the esophagus, brain glioma, peripheral nerve neurinoma and mesenchymal tumors of the kidney.

Aminocaproic Acid↗

Nitrophenylated derivatives of epsilon-aminocaproic acid: synthesis and physico-chemical characterization.

Methods for the synthesis of the mono-, di- and tri-nitro derivatives of epsilon-aminocaproic acid are presented. Special attention is given to the purification procedure, as we have found that methods recommended in the literature do not produce a single product. Evidence is presented which shows that recrystallizing the haptens from hot ethanol produces a by-product which is the ethyl ester of the haptens. Characterization methods and physical properties of the nitro-phenylated derivates of epsilon-aminocaproic acid are summarized.

Aminocaproates↗

Stabilizing effect of epsilon-aminocaproic acid on allergenic extracts.

The effect of epsilon-aminocaproic acid (EACA) on the degradation of an aqueous Lolium perenne extract was studied by intracutaneous tests and by RAST inhibition. Extracts for skin testing stored at 4 degrees C for 12 months and at 37 degrees C for 6 weeks were significantly protected from degradation by addition of 0.1 mol/L of EACA before storage. Extracts were stored for RAST inhibition at 4 degrees C for 6 months and at 37 degrees C for 7 days. Shelf life was twofold to threefold increased when 0.1 mol/L of EACA was added to the dilution medium. EACA also protected the extracts from the effect of freezing and thawing. Comparison with the effect of human serum albumin indicated a rather short activity of human serum albumin, whereas the effect of EACA lasted longer. It is suggested that EACA can be used to increase the stability of aqueous allergen extracts for skin testing and for hyposensitization therapy.

Allergens↗

Gender does not influence epsilon-aminocaproic acid concentrations in adults undergoing cardiopulmonary bypass.

Epsilon-aminocaproic acid (epsilon-ACA) is administered to cardiac surgery patients to reduce blood transfusions. Highly water-soluble drugs, such as epsilon-ACA, often have larger distribution volumes in males than in females. We hypothesized that epsilon-ACA concentrations using this dosing scheme would differ by gender because of differences in body composition and weight-adjusted volumes of distribution. Ten men and 10 women undergoing elective coronary artery surgery with cardiopulmonary bypass (CPB) received a 50 mg/kg epsilon-ACA initial dose over 20 min and a 25 mg. kg(-1) x h(-1) epsilon-ACA maintenance infusion for 4 h. The area under the epsilon-ACA arterial concentration versus time curves was compared by using analysis of variance. Measured epsilon-ACA concentrations were smaller than predicted by the published model, but the area under the concentration versus time curves was not significantly different between men and women. Combining the present concentration data with that previously published, our updated two-compartment model included the following estimated population pharmacokinetic values: V(1) (11.8 L pre-CPB, 14.9 L during and after CPB), V(2) (12.0 L pre-CPB, 15.0 L during and after CPB), Cl(1) (0.125 L/min pre-CPB, 0.037 L/min during CPB, 0.156 L/min after CPB), Cl(2) (0.155 L/min pre-CPB, 0.013 L/min during CPB, 0.193 L/min after CPB).

Aged↗

Clinical and laboratory investigation of the effects of epsilon-aminocaproic acid on hemostasis.

We previously reported that epsilon-aminocaproic acid (EACA) prolonged the bleeding time in patients with intracranial aneurysms when given in doses of 36 to 48 gm/day. We now show that doses of 24 gm/day also prolong the bleeding time, but only after 72 hours of continuous infusion. The effect on the bleeding time correlates with the duration of EACA therapy but not with the plasma level of the drug. Bleeding times return toward normal within 72 hours of discontinuing EACA infusions. The factors responsible for the bleeding time prolongation were investigated. In vitro, EACA inhibited adenosine diphosphate- and collagen-induced platelet aggregation and the release of platelet adenosine triphosphate and serotonin. It also prevented the adenosine diphosphate-stimulated binding of fibrinogen to intact as well as to chymotrypsin-treated platelets. However, platelets obtained from patients who had received EACA showed little functional impairment. This observation indicates that the focus of EACA activity in vivo is probably not the platelet per se, but the platelet-vessel wall interaction or a vascular component alone. EACA did not enhance prostacyclin production or release from cultured bovine endothelial cells. The fact that the effects of the drug on the bleeding time were related to the duration of EACA therapy suggests that an accumulation of the drug on the vessel wall may be required before alterations in hemostasis are observed. EACA in a daily dose of 24 gm significantly impaired fibrinolysis, but supranormal levels of fibrinolytic activity were observed within 72 hours of stopping the drug.(ABSTRACT TRUNCATED AT 250 WORDS)

Aminocaproates↗