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.