COMPOSITION:
Each tablet contains
Tranexamic acid 500mg
DESCRIPTION:
Tranexamic acid belongs to the
antifibrinolytics class of drugs.
Chemical structure:
4-(Aminomethyl cyclohexanecarboxylic acid)
PHARMACODYNAMIC:
Tranexamic acid inhibits the
activation of plasminogen to plasmin. At high concentrations, it is also a weak
inhibitor of plasmin. Plasmin is responsible for the lyses of fibrin in formed
clots and hence increases the tendency towards bleeding. Tranexamic acid, by
preventing formation of plasmin, reduces the process of fibrinolysis. This
helps in stabilizing the formed clot.
Tranexamic acid is 7-10 times
more potent than E-aminocaproic acid (EACA).
PHARAMCOKINETICS:
Absorption
Oral
absorption 50%
The absorption
of tranexamic acid following oral administration at a dose of 10mg/kg body
weight produces serum levels of 2 to 3 mg/l.
Food has no
influence on absorption.
Presystemic
metabolism nil
Plasma protein
binding negligible
Distribution
Plasma half life
1.4h
Tranexamic acid
is able to cross the blood-aqueous barrier in the eyes. It can also cross the
blood-brain as shown in patients with ruptured intracranial aneurysm.
Tranexamic acid rapidly diffuses into the joint fluid and the synovial
membrane.
Metabolism
Tranexamic acid
under goes negligible metabolism in the body.
Excretion mainly eliminated unchanged in the urine.
Excretion occurs by glomerular filter via kidney.
INDICATION:
1)
primary
menorrhagia
2)
IUD
induced menorrhagia
3)
Dysfunctional
uterine bleeding
4)
Cervical
conization
5)
Treatment
of gastric and intestinal haemorrhage: e.g. upper GI haemorrhage associated
with peptic ulcers, mucosal erosions; or lower GI haemorrhage leading malena.
6)
Treatment
of recurrent epitaxis
7)
Prevention
of spontaneous or post operative corneal oedema.
8)
Surgical
hyphema
9)
Following
tooth extraction
10) Prevention of bleeding after surgery or
trauma
a)
Tonsillectomy
b)
Adenoidectomy
c)
Prostatic
surgery
11) Treatment of hereditary and
non-hereditary angioneurotic oedema
12) Other uses
a)
Prevention
of bleeding in acute promyelocytic leukaemia
b)
Prevention
of bleeding after Cardiopulmonary bypass
c)
Prevention
of bleeding in total knee replacement
13) Treatment of streptokinase-induced
fibrinolysis.
DOSAGE & ADMINISTRATION
The dose of
tranexamic acid ranges from 0.5 to 0.6 gm per day in divided doses. The oral
dose of tranexamic acid is 1 to 1.5 gm orally three or four times in a day.
CONTRAINDICATIONS:
1.
Severe
renal insufficiency.
2.
massive
upper urinary tract infection
3.
impaired
liver function
4.
Subarachnoid
bleeding.
5.
Thrombophlebitis
ADVERSE EFFECTS:
Adverse effects
of tranexamic acid are rare and mainly limited to nausea or diarrhea, and
occasionally an orthostatic reaction.
There is a
theoretical risk of an increased thrombotic tendancy, like deep vein
thrombosis, during prolonged treatment with fibrinolysis inhibitors.
