Tranexamic acid is a synthetic derivative of the amino acid lysine that exe
rts its antifibrinolytic effect through the reversible blockade of lysine b
inding 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 t
o 54% in postoperative blood losses in patients undergoing cardiac surgery
with cardiopulmonary bypass (CPB), with statistically significant reduction
s in transfusion requirements in some studies, Tranexamic acid had similar
efficacy to aprotinin 2 x 10(6) kallikrein inhibitory units (KIU) and was s
uperior to dipyridamole in the reduction of postoperative blood losses. Tra
nsfusion requirements were reduced significantly by 43% with tranexamic aci
d and by 60% with aprotinin in 1 study. Meta-analysis of 60 trials showed t
ranexamic acid and aprotinin, unlike E-aminocaproic acid (EACA) and desmopr
essin, 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 morta
lity of 5 to 54% in patients with upper,gastrointestinal bleeding, Meta-ana
lysis 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; th
e drug has also been used to good effect in placental bleeding, postpartum
haemorrhage and conisation of the cervix, Tranexamic acid significantly red
uced mean blood losses after oral surgery in patients with haemophilia and
was effective as a mouthwash in dental patients receiving oral anticoagulan
ts.
Reductions in blood loss were also obtained with the use of the drug in pat
ients undergoing orthotopic liver transplantation or transurethral prostati
c surgery, and rates of rebleeding were reduced in patients with traumatic
hyphaema, Clinical benefit has also been reported with tranexamic acid in p
atients 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 de
monstrated in clinical trials.
Conclusions: Tranexamic acid is useful in a wide range of haemorrhagic cond
itions. The drug reduces postoperative blood losses and transfusion require
ments in a number of types of surgery, with potential cost and tolerability
advantages over aprotinin, and appears to reduce rates of mortality and ur
gent surgery in patients with upper gastrointestinal haemorrhage. Tranexami
c acid reduces menstrual blood loss and is a possible alternative to surger
y in menorrhagia, and has been used successfully to control bleeding in pre
gnancy.