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PubMed2002

Pulmonary embolism associated with tranexamic acid in severe acquired haemophilia.

Tranexamic acid (an antifibrinolytic agent) is of proven benefit in the treatment of bleeding in patients with congenital and acquired coagulation disorders. We report the case of a patient with an acquired Factor VIII inhibitor, who was on a prophylactic dose of tranexamic acid because of recurrent bleeding episodes and developed a pulmonary embolism. Although studies using tranexamic acid have not shown a definite increased risk for the development of venous thrombosis, this is the likely cause of the pulmonary embolism in this patient.

Adult↗
PubMed2002

Pharmacokinetics of tranexamic acid during cardiopulmonary bypass.

BACKGROUND: Tranexamic acid (TA) reduces blood loss and blood transfusion during heart surgery with cardiopulmonary bypass (CPB). TA dosing has been empiric because only limited pharmacokinetic studies have been reported, and CPB effects have not been characterized. We hypothesized that many of the published TA dosing techniques would prove, with pharmacokinetic modeling and simulation, to yield unstable TA concentrations. METHODS: Thirty adult patients undergoing elective coronary artery bypass grafting, valve surgery, or repair of atrial septal defect received after induction of anesthesia: TA 50 mg/kg (n = 11), TA 100 mg/kg (n = 10), or TA 10 mg/kg (n = 10) over 15 min, with 1 mg x kg(-1) x hr(-1) maintenance infusion for 10 h. TA was measured in plasma using high performance liquid chromatography. Pharmacokinetic modeling was accomplished using a mixed effects technique. Models of increasing complexity were compared using Schwarz-Bayesian Criterion (SBC). RESULTS: Tranexamic acid concentrations rapidly fell in all three groups. Data were well fit to a 2-compartment model, and adjustments for CPB were supported by SBC. Assuming a body weight of 80 kg, our model estimates V1 = 10.3 l before CPB and 11.9 l during and after CPB; V2 = 8.5 l before CPB and 9.8 l during and after CPB; Cl1 = 0.15 l/s before CPB, 0.11 l/s during CPB, and 0.17 l/s after CPB; and Cl2 = 0.18 l/s before CPB and 0.21 l/s during and after CPB. Based on simulation of previous studies of TA efficacy, we estimate that a 30-min loading dose of 12.5 mg/kg with a maintenance infusion of 6.5 mg x kg(-1) x hr(-1) and 1 mg/kg added to the pump prime will maintain TA concentration greater than 334 microm, and a higher dose based on 30 mg/kg loading dose plus 16 mg x kg(-1) x h(-1) continuous infusion and 2 mg/kg added to the pump prime would maintain TA concentrations greater than 800 microm. CONCLUSIONS: Tranexamic acid pharmacokinetics are influenced by CPB. Our TA pharmacokinetic model does not provide support for the wide range of TA dosing techniques that have been reported. Variation in TA efficacy from study to study and confusion about the optimal duration of TA treatment may be the result of dosing techniques that do not maintain stable, therapeutic TA concentrations.

Adult↗
PubMed1999

Tranexamic acid: a review of its use in surgery and other indications.

UNLABELLED: Tranexamic acid is a synthetic derivative of the amino acid lysine that exerts its antifibrinolytic effect through the reversible blockade of lysine binding sites on plasminogen molecules. Intravenously administered tranexamic acid (most commonly 10 mg/kg followed by infusion of 1 mg/kg/hour) caused reductions relative to placebo of 29 to 54% in postoperative blood losses in patients undergoing cardiac surgery with cardiopulmonary bypass (CPB), with statistically significant reductions in transfusion requirements in some studies. Tranexamic acid had similar efficacy to aprotinin 2 x 10(6) kallikrein inhibitory units (KIU) and was superior to dipyridamole in the reduction of postoperative blood losses. Transfusion requirements were reduced significantly by 43% with tranexamic acid and by 60% with aprotinin in 1 study. Meta-analysis of 60 trials showed tranexamic acid and aprotinin, unlike epsilon-aminocaproic acid (EACA) and desmopressin, to reduce significantly the number of patients requiring allogeneic blood transfusions after cardiac surgery with CPB. Tranexamic acid was associated with reductions relative to placebo in mortality of 5 to 54% in patients with upper gastrointestinal bleeding. Meta-analysis indicated a reduction of 40%. Reductions of 34 to 57.9% versus placebo or control in mean menstrual blood loss occurred during tranexamic acid therapy in women with menorrhagia; the drug has also been used to good effect in placental bleeding, postpartum haemorrhage and conisation of the cervix. Tranexamic acid significantly reduced mean blood losses after oral surgery in patients with haemophilia and was effective as a mouthwash in dental patients receiving oral anticoagulants. Reductions in blood loss were also obtained with the use of the drug in patients undergoing orthotopic liver transplantation or transurethral prostatic surgery, and rates of rebleeding were reduced in patients with traumatic hyphaema. Clinical benefit has also been reported with tranexamic acid in patients with hereditary angioneurotic oedema. Tranexamic acid is well tolerated; nausea and diarrhoea are the most common adverse events. Increased risk of thrombosis with the drug has not been demonstrated in clinical trials. CONCLUSIONS: Tranexamic acid is useful in a wide range of haemorrhagic conditions. The drug reduces postoperative blood losses and transfusion requirements in a number of types of surgery, with potential cost and tolerability advantages over aprotinin, and appears to reduce rates of mortality and urgent surgery in patients with upper gastrointestinal haemorrhage. Tranexamic acid reduces menstrual blood loss and is a possible alternative to surgery in menorrhagia, and has been used successfully to control bleeding in pregnancy.

Antifibrinolytic Agents↗
PubMed2003

Tranexamic acid: a review of its use in the management of menorrhagia.

Tranexamic acid (Transamin), Cyklokapron, Exacyl, Cyklo-f) is a synthetic lysine derivative that exerts its antifibrinolytic effect by reversibly blocking lysine binding sites on plasminogen and thus preventing fibrin degradation. In a number of small clinical studies in women with idiopathic menorrhagia, tranexamic acid 2-4.5 g/day for 4-7 days reduced menstrual blood loss by 34-59% over 2-3 cycles, significantly more so than placebo, mefenamic acid, flurbiprofen, etamsylate and oral luteal phase norethisterone at clinically relevant dosages. Intrauterine administration of levonorgestrel 20 microg/day, however, produced the greatest reduction (96% after 12 months) in blood loss; 44% of patients treated with levonorgestrel developed amenorrhoea. Tranexamic acid 1.5 g three times daily for 5 days also significantly reduced menstrual blood loss in women with intrauterine contraceptive device-associated menorrhagia compared with diclofenac sodium (150 mg in three divided doses on day 1 followed by 25 mg three times daily on days 2-5) or placebo. Tranexamic acid, mefenamic acid, etamsylate, flurbiprofen or diclofenac sodium had no effect on the duration of menses in the studies that reported such data. In a large noncomparative, nonblind, quality-of-life study, 81% of women were satisfied with tranexamic acid 3-6 g/day for 3-4 days/cycle for three cycles, and 94% judged their menstrual blood loss to be 'decreased' or 'strongly decreased' compared with untreated menstruations. The most commonly reported drug-related adverse events are gastrointestinal in nature. The total incidence of nausea, vomiting, diarrhoea and dyspepsia in a double-blind study was 12% in patients who received tranexamic acid 1g four times daily for 4 days for two cycles (not significantly different to the incidence in placebo recipients). In conclusion, the oral antifibrinolytic drug tranexamic acid is an effective and well tolerated treatment for idiopathic menorrhagia. In clinical trials, tranexamic acid was more effective at reducing menstrual blood loss than mefenamic acid, flurbiprofen, etamsylate and oral luteal phase norethisterone. Although it was not as effective as intrauterine administration of levonorgestrel, the high incidence of amenorrhoea and adverse events such as intermenstrual bleeding resulting from such treatment may be unacceptable to some patients. Comparative studies of tranexamic acid with epsilon - aminocaproic acid, danazol and combined oral contraceptives, as well as long-term tolerability studies, would help to further define the place of the drug in the treatment of menorrhagia. Nevertheless, tranexamic acid may be considered as a first-line treatment for the initial management of idiopathic menorrhagia, especially for patients in whom hormonal treatment is either not recommended or not wanted.

Antifibrinolytic Agents↗
PubMed2005

Tranexamic acid reduces postoperative blood loss in cementless total hip arthroplasty.

BACKGROUND: Tranexamic acid, an inhibitor of fibrinolysis that blocks the lysine-binding site of plasminogen to fibrin, has been reported to reduce intraoperative and postoperative blood loss in patients undergoing total hip arthroplasty with cement. However, there have been few reports describing the effects of tranexamic acid on blood loss during and following total hip arthroplasty without cement. METHODS: We investigated the effects of tranexamic acid in twenty-one patients who underwent staged bilateral total hip arthroplasty without cement for the treatment of osteoarthritis of the hip. The average interval between the two procedures was 16 +/- 16 months. On one side, 1000 mg of tranexamic acid was administered intravenously five minutes before the skin incision. On the other side, tranexamic acid was not administered. Baseline hemoglobin and hematocrit values were obtained three weeks before each arthroplasty. The volume of postoperative blood loss was recorded at two-hour intervals for the first twelve hours and then again at twenty-four hours, and the values were compared between the two groups. RESULTS: The total intraoperative blood loss in the tranexamic acid group (607 +/- 298 mL) was similar to that in the control group (633 +/- 220 mL). The postoperative blood loss in the tranexamic acid group was significantly lower than that in the control group at all time-points during the first twenty-four hours (p < 0.001 for all comparisons). The greatest reduction in blood loss was observed during the first four hours after surgery in the tranexamic acid group (p < 0.01). CONCLUSIONS: In patients undergoing total hip arthroplasty without cement, preoperative administration of tranexamic acid is associated with decreased postoperative blood loss during the first twenty-four hours, especially during the first four hours after surgery.

Aged↗
PubMed1985

Pharmacokinetics and absolute bioavailability of intramuscular tranexamic acid in man.

The bioavailability of tranexamic acid after the administration of a single intramuscular dose was estimated in three healthy male volunteers. 500 mg tranexamic acid were given intramuscularly and intravenously, as a bolus injection, to each subject on separate occasions. Following intramuscular administration, the peak plasma concentrations were attained after approximately one hour and the apparent elimination half-life was about two hours. The absolute bioavailability was 105.2 +/- 10.7% (mean +/- SD). At the dose given, the bioavailability of tranexamic acid after intramuscular administration is fast and complete.

Adult↗
PubMed1986

Tranexamic acid derivatives with enhanced absorption.

Derivatives of the antifibrinolytic drug tranexamic acid [trans-4-(aminomethyl)cyclohexanecarboxylic acid] containing one or two tranexamic acid moieties were synthesized. Most of the derivatives have good stability in acidic and neutral solutions but are easily hydrolyzed in plasma. By measuring the amount of tranexamic acid excreted in the urine after an oral dose, relative absorptions of a number of derivatives in the rat were estimated. Most of the derivatives showed greater absorption than tranexamic acid itself. 1-[(Ethoxycarbonyl)oxy]ethyl trans-4-(amino-methyl)cyclohexanecarboxylate hydrochloride was chosen for studies in man.

Animals↗
PubMed1986

Effects of tranexamic acid on fibrinolysis, fibrinogenolysis and amidolysis.

When Glu-plasminogen (Glu-plg) was activated by urokinase (UK) in the presence of fibrinogen or fibrinogen plus tranexamic acid (1 mM), or else tranexamic acid (1 mM), the activation as measured by the hydrolysis of S-2251 was enhanced by tranexamic acid or fibrinogen or both. When plasma or clotted plasma was activated by UK in the presence of 1 mM tranexamic acid, fibrinolysis was completely inhibited. When Lys-plg was activated by UK in the presence of tranexamic acid and fibrin or fibrinogen, fibrinolysis was completely inhibited by 1 mM tranexamic acid, but some inhibition of fibrinogenolysis was observed. The release of B beta 15-42 from fibrin in clotted plasma activated by UK was inhibited to some extent by 1 mM tranexamic acid. The release of B beta 15-42 from fibrin after UK-activation of Lys-plg was partly inhibited by tranexamic acid. In conclusion, tranexamic acid in the concentration of 1 mM enhanced amidolysis, but inhibted fibrinolysis measured by the generation of fibrin-degradation products. Fibrinogenolysis and the release of B beta 15-42 from fibrin were partly inhibited.

Blood Coagulation↗
PubMed2003

Single-dose tranexamic acid reduces postoperative bleeding after coronary surgery in patients treated with aspirin until surgery.

UNLABELLED: Tranexamic acid reduces postoperative bleeding after coronary artery bypass grafting. We evaluated the effects of a single dose of tranexamic acid given immediately before cardiopulmonary bypass (CPB) in patients treated with aspirin until the day before surgery. The study was a prospective, randomized, double-blinded, placebo-controlled, parallel-group trial. Eighty patients were included and divided into two groups: one group received tranexamic acid 30 mg/kg, and one group received placebo (0.9% NaCl) as a bolus injection before CPB. Postoperative blood loss was recorded for 16 h. Transfusions of blood products were recorded for the whole hospital stay. Transfusions of packed red cells were given when the hematocrit value was less than 20% during CPB and less than 25% after surgery. The patients in the tranexamic acid group had significantly less postoperative bleeding compared with the patients in the placebo group (mean [SD]) (475 [274] mL versus 713 [243] mL; P < 0.001). An effective inhibition of fibrinolysis was found in patients receiving tranexamic acid. Tranexamic acid reduces postoperative bleeding in coronary artery bypass grafting patients treated with aspirin until the day before surgery. IMPLICATIONS: Continuation of aspirin medication until the day before coronary artery bypass grafting may increase postoperative bleeding. The administration of a single dose of tranexamic acid (30 mg/kg) immediately before cardiopulmonary bypass significantly reduced postoperative bleeding and inhibited fibrinolysis in these patients.

Aged↗
PubMed1980

Interaction of plasmin with tranexamic acid and alpha 2 plasmin inhibitor in the plasma and clot.

Interaction of urokinase (UK) activated plasmin with tranexamic acid and alpha 2 plasmin inhibitor (alpha 2PI) was studied by using a chromogenic substrate (S-2251) and immunoelectrophoresis. Plasma was activated by UK (P + U) in the presence of tranexamic acid (P + U + t) or in the presence of thrombin (P + U + thr) and thrombin plus tranexamic acid (P + U + thr + t). These mixtures were incubated for 10, 20, and 30 min at 37 degrees C, then an aliquot of each mixture was added to S-2251, and incubated for 3 or 10 min at 37 degrees C. Hydrolysis of S-2251 after 3 min incubation was significant in the presence of tranexamic acid or clot formation, thus the presence of tranexamic acid or clot formation enhancing the UK activation of plasminogen in both plasma and clot. Hydrolysis of S-2251 after 10 min incubation was higher in the presence of tranexamic acid than in its absence or clot formation without tranexamic acid. Tranexamic acid seems to be more effective in enhancement of activation of plasminogen by UK than clot formation. Plasmin formed by UK was coexistent with alpha 2PI in the plasma in contrast to a purified system in which alpha 2PI formed a complex with plasmin instantaneously. In an even purified system, clot formation and the presence of tranexamic acid protected plasmin from its inactivation by alpha 2PI to some extent.

Blood Coagulation↗
PubMed1998

Topical versus intravenous administration of tranexamic acid: a comparison of intraocular and serum concentrations in the rabbit.

BACKGROUND: Tranexamic acid has been shown to greatly reduce the incidence of secondary hemorrhage when administered orally or intravenously. Topical administration of the drug should result in much lower serum concentrations, with fewer adverse effects. We performed a study to determine whether topical application of tranexamic acid would yield higher intraocular concentrations and lower serum concentrations of drug than intravenous administration. METHODS: Ten New Zealand white rabbits received 25 mg/kg of tranexamic acid intravenously every 8 hours for 3 days. Another group of 10 rabbits received one drop (0.05 mL) of commercially available tranexamic acid solution (100 mg/mL) every 8 hours for 3 days to one eye. Tranexamic acid levels in the aqueous humour, vitreous humour and serum 1 hour after administration of the last dose of drug were determined. RESULTS: Analysis of variance showed that aqueous concentrations of tranexamic acid were significantly higher with topical delivery than with intravenous administration (15 vs. 9 micrograms/mL)(p < 0.05). Serum concentrations were significantly lower following topical administration (9 vs. 19 micrograms/mL)(p < 0.01). The drug was not detected in the vitreous humour in either group. INTERPRETATION: Topical delivery of tranexamic acid may prove to be valuable in yielding therapeutic intraocular concentrations of drug in patients with hyphema while minimizing systemic toxicity.

Administration, Topical↗
PubMed2001

Effect of tranexamic acid on blood loss reduction after cardiopulmonary bypass.

OBJECTIVE: We evaluated the effect of tranexamic acid on blood loss in patients undergoing elective cardiopulmonary bypass for coronary artery bypass surgery. METHODS: We randomly assigned 7 of 14 patients to a group receiving 50 mg/kg tranexamic acid before skin incision and after the start of cardiopulmonary bypass and the other 7 as controls. RESULTS: Intraoperative and postoperative blood loss was significantly (p = 0.025) reduced in the tranexamic acid group. A similar decrease in platelet count was observed during cardiopulmonary bypass in both groups. Antithrombin III was significantly (p = 0.013) decreased in both groups during cardiopulmonary bypass. Antithrombin III and thrombin-antithrombin III complexes were significantly (p = 0.001) increased after protamine administration. A significant (p = 0.010) decrease in alpha 2-plasmin inhibitor was noted at 5 and 60 minutes after the start of cardiopulmonary bypass in the tranexamic acid group. alpha 2-plasmin inhibitor-plasmin complexes were significantly (p = 0.001) increased after the start of cardiopulmonary bypass in both groups and were significantly (p = 0.012) decreased after protamine administration. alpha 2-plasmin inhibitor-plasmin complexes in the tranexamic acid group were significantly (p = 0.030) lower than in controls 60 minutes after the start of cardiopulmonary bypass, just prior to the end of cardiopulmonary bypass, and after protamine administration. CONCLUSIONS: These findings showed that tranexamic acid administration effectively prevented perioperative blood loss without thromboembolic complications and that tranexamic acid during cardiopulmonary bypass coordinates the anticoagulative effect of heparin and the antifibrinolytic effect of tranexamic acid.

Aged↗
PubMed1992

Vaginal absorption of low-dose tranexamic acid from impregnated tampons.

Tranexamic acid (TA), an antifibrinolytic drug, is usually administered orally to women with menorrhagia. This route of administration is associated with adverse side-effects, therefore tampons impregnated with TA were used to assess the absorption of the drug across the vaginal epithelium. Blood levels of TA in group A (9 patients), who had one tampon inserted, and group B (10 patients), who had a tampon inserted at 2-hourly intervals so that a total of 3 tampons were administered over a 6-hour period, demonstrated absorption of the drug into the blood stream in low concentrations.

Absorption↗
PubMed1978

Special considerations with regard to the dosage of tranexamic acid in patients with chronic renal diseases.

Tranexamic acid is a potent antifibrinolytic drug frequently used in the treatment of haematuria and a number of other haemorrhagic conditions. Since it is eliminated mainly in the urine, the drug accumulates in patients with uraemia. The excretion of tranexamic acid in patients with renal failure has been investigated and dosage recommendations are given for tranexamic acid therapy in cases of renal failure.

Biological Availability↗
PubMed1980

Comparison of tranexamic acid (Transamin) and traditional therapy for sudden deafness.

The effectiveness of tranexamic acid treatment for sudden deafness was studied in detail. The results of treatment with tranexamic acid administration in 19 cases (25 ears) of sudden deafness and two historical control groups using various treatments were compared by the chi square contingency test. The data suggested that tranexamic acid treatment may be superior to traditional treatments especially if treatment is begun early. Among ears treated with tranexamic acid, 11 ears (44%) were healed or recovered remarkably, 8 ears (32%) recovered slightly and 6 ears (24%) were unchanged or worsened. Fibrinolysis in the inner ear may be the pathophysiology of sudden deafness. Treatment with tranexamic acid starting within 4 days after onset of symptoms was most effective in patients whose initial audiogram was flat or concave, initial average hearing loss at 5 frequencies (250 Hz, 500 Hz, 1000 Hz, 2000 Hz and 4000 Hz) was between 23 dB and 76 dB (mean; 45.1 dB) and was not accompanied by dizziness.

Adult↗
PubMed1988

Degradation of Glu- and Lys-plasminogen by elastase in the presence or absence of tranexamic acid.

Glu-plasminogen (Glu-plg) was degraded by elastase in the presence or absence of tranexamic acid. Glu-plg was degraded faster in the presence of tranexamic acid. Increase in the concentration of tranexamic acid resulted in increase in the appearance of degradation products, reaching a plateau level at 1 mM of tranexamic acid. Fifty percent increase in the concentration of one of degradation products was obtained at 0.22 mM of tranexamic acid, which is similar to a dissociation constant (Kd) of low affinity lysine binding sites (LBS) with tranexamic acid. As to the degradation rate of two isozymes of Glu-plg (Glu-plg I and II), Glu-plg II containing one carbohydrate chain was degraded faster than Glu-plg I containing two carbohydrate chains. Comparison of the degradation rates of Glu-plg and Lys-plg indicated that Lys-plg was degraded faster.

Cyclohexanecarboxylic Acids↗
PubMed2001

Tranexamic acid in aortic valve replacement.

OBJECTIVE: To assess the relative efficacy of tranexamic acid compared with a control group to decrease bleeding and transfusion requirements in a uniform population undergoing aortic valve replacement. DESIGN: Prospective, randomized, double-blind study. SETTINGS: University hospital. PARTICIPANTS: Adult cardiac surgery patients (n = 300). INTERVENTIONS: Patients were randomized into 2 groups to receive either a total of 5 g of tranexamic acid or a saline solution. Bleeding in the postoperative period, transfusions of bank blood products, coagulation profile, intensive care unit stay, and hospital length of stay were recorded. MEASUREMENTS AND MAIN RESULTS: Postoperative bleeding in patients treated with tranexamic acid was significantly lower compared with the control group (p < 0.0001). Packed red blood cells and fresh frozen plasma usage were reduced in the tranexamic acid group compared with the control group (p = 0.0095 and p < 0.0001). Only 24.5% of tranexamic acid patients received blood products versus 45% of control patients (p < 0.01). There was no significant difference in hematologic and coagulation profiles after the operation between the groups. CONCLUSIONS: Tranexamic acid reduces postoperative blood loss and transfusion requirements in elective aortic valve replacement.

Aged↗
PubMed1981

Influence of tranexamic acid on tumour vascularization. An experimental microangiographic study.

Administration of tranexamic acid given from tumour transplantation up to sacrifice 5 days later, inhibited the early vascularization of an intramuscularly transplanted rat sarcoma. A marked reduction of angiographically demonstrated vascular connections between tumour and normal muscle was observed. In older, larger tumours an increased frequency of small non-vascularized and probably necrotic tumour areas was suggested after administration of tranexamic acid. An inhibiting effect of tranexamic acid on tumour growth rate has been earlier reported in both experimental and clinical studies. This effect may be explained by an influence of tranexamic acid on tumour vascularization.

Angiography↗