Tranexamic

Acid
In
Gynaecology & Obstetrics
Blood The essence of Life

STOP
STOP
BLOOD LOSS
BLOOD LOSS

LIFE GOES ON
 Women are always at Risk of
Losing Blood
FROM MENARCHE TO MENOPAUSE

PPH DUB

IN NORMALCY OR PREGNANCY CX
DUB

DUB
APH
IN HEALTH OR DISEASE

HOW TO STOP IT?

 Events in Hemostasis
1) Vasoconstriction
3) Blood clotting
2) Platelet plug formation

4) Fibrinolysis
 Events in Haemostasis
COAGULATION:
Prothrombin Thrombin

Fibrinogen Fibrin

forms
Clot
 Events in Haemostasis
FIBRINOLYSIS:

Plasminogen Plasmin

dissolves
Clot
Events in Hemostasis

COAGULATION
AND FIBRINOLYSIS
Events in Hemostasis
Presenting Tranexamic Acid

Tranexamic
COAGULATION
TRANEXAMIC
AND FIBRINOLYSIS
ACID
Acid
 Tranexamic Acid

Synthetic amino acid, first introduced in

Sweden in1969.
Chemically it is Tranexamic-stereo isomer of 1,
4, -aminomethylcyclohexane carboxylic acid.
Formula C8H15NO2.
Molecular Wt.-157.
Prevents fibrinolysis and breakdown of clot.
It is a competitive inhibitor of plasminogen
activation.
At very high concentration, it is also a non
competitive inhibitor of Plasmin.
It is also a very weak inhibitor of thrombin.
 Tranexamic Acid
Mechanism of Action
Tranexamic acid inhibits conversion of
plasminogen to plasmin, hence
prevents breakdown of clot.
Increases collagen synthesis which
preserves the fibrin matrix and
increases the tensile strength of the clot
These actions of Tranexamic acid help
in stabilizing the clot
 Tranexamic Acid
Pharmacokinetics
Absorption after oral administration is 30-50%
Food has no influence on absorption
Peak plasma concentration after 3 hours
Presystemic metabolism ~ nil. Bioavailability 30
50%
Plasma half-life ~ 1.4h
Is able to cross the blood-aqueous barrier in the
eyes.
Can also cross the damaged blood-brain barrier
Rapidly diffuses into joint fluid and the synovial
membrane.
Crosses placenta and also into breast milk.
Excretion unchanged 2 hours.
 Tranexamic Acid
Pharmacokinetic
s
Plasma protein binding is negligible
Undergoes negligible metabolism in the
body.
Mainly eliminated unchanged in the urine.
Excretion occurs by glomerular filtration
via the kidneys.
Passes through the placenta and its
concentration in the cord blood may
reach that of maternal blood.
 Tranexamic Acid
Clinical Pharmacology
The antifibrinolytic effect of Tranexamic
acid is related mainly to a reversible
complex formation with plasminogen,
which prevents its activation to plasmin.
Tranexamic acid is 7 to 10 times more
potent than Epsilon-aminocaproic acid
[EACA].
Tranexamic acid produces a considerably
higher and more sustained antifbrinolytic
activity in tissues than does EACA.
 Tranexamic Acid
Clinical Pharmacology
Adverse effects- are rare and mainly
limited to
Nausea, Vomiting & Diarrhea, Allergy and
occasionally an Orthostatic reaction.
There is a theoretical risk of an increased
thrombotic tendency, like deep vein thrombosis,
during prolonged treatment as with any
fibrinolysis inhibitors.
Contraindications: -
Severe renal insufficiency
Active intravascular clotting
Thrombo embolic disease
Colour vison disorders
 Tranexamic Acid
Pregnancy And Lactation
Pregnancy:Tranexamic acid crosses over to the
foetus. It is not known whether a reduction of the
normally high fibrinolytic activity in the foetus and
neonate is harmful.
Lactation:Tranexamic acid is secreted in the mother's
milk. This concentration is only a hundredth of the
corresponding serum levels and the drug may be
given during lactation without risk to the child.
CATEGORY B
Ref: Collin Dollery. Tranexamic Acid. In 'Therapeutic Drugs. 2nd edition.
1999.pgT150-T153
 Tranexamic Acid
Uses in OBGYN
To Prevent / reduce blood loss in: -
Dysfunctional Uterine Bleeding
IUD Menorrhagia.
Conization / Amputation of Cervix.
Post Partum Hemorrhage.
Ante Partum Hemorrhage.
During/After Abdominal/Vaginal Surgery
Available in both Oral and Inj. (IV) forms
TRANEXAMIC ACID OTHER
USES
After surgery of the prostate (prostatectomy)
After bladder surgery
Heavy and prolonged menstrual periods (menorrhagia)
Nose bleeds (epistaxis)
Surgery of the cervix (conisation of the cervix)
Bleeding of the cervix
Bleeding caused by inflammation of the colon and bowel
Bleeding inside the eye (traumatic hyphaema)
Surgery or tooth removal (dental extraction) in patients who bleed more
easily than normal (haemophiliacs)
Angioneurotic oedema (an inherited disease involving swelling of the
skin tissue)
Leukaemia
Liver disease
 E B M Tranexamic Acid
Tranexamic acid is an effective treatment for
reducing heavy menstrual blood loss (A)
[RCOG, 1998].
It reduces menstrual blood loss by 40-50%
[Lethaby et al. 2001b].
Being a plasminogen activator inhibitor, its
use is rational as an increase in the level of
plasminogen activators is found in the
endometrium of women with heavy
menstrual bleeding compared to those with
normal menstrual loss.
 Tranexamic Acid in APH &
PPH
Bleeding from placental sites usually
result from the structural weakness &
defects in the placental blood vessels.
Tranexamic acid in doses of 1G
(IV/Oral) TDS, by promoting stable
coagulation at the site of bleeding, can
be of help in-
Placenta Previa (2nd half of pregnancy).
Abruptio Placentae.
Persistent Post Partum Hemorrhage
 Tranexamic Acid Dosage

1-1.5 gm or 15-25mg /kg 2-4 times

daily

Adjust dose in renal impairment

TRANEXAMIC ACID
WARNINGS
Tranexamic acid should be used with caution in: the elderly, children
aged under 15 years with heavy or prolonged menstrual periods
(menorrhagia), kidney disease, patients with blood in their urine,
history of uncontrollable bleeding, pregnancy and breastfeeding,
patients with the blood clotting disorder disseminated intravascular
coagulation (DIC) which is ongoing, increased fibrinolysis (clot
breakdown) caused by DIC, long term treatment of the hereditary
condition angioneurotic oedema, women with irregular menstrual
periods.
It should not be used in: patients with an allergy to tranexamic acid
or to any other ingredients in the medicine or patients with an
allergy to other anti-fibrinolytics, severe kidney problems (kidney
failure), patients who have or have had a blood clot in their blood
vessels (thrombosis) particularly in the leg or lung, patients in whom
a blood clot has caused a stroke, severe bruising, patients with
TRANEXAMIC ACID INTERACTIO

Fibrinolytics such as streptokinase

Hormone replacement therapy (HRT)

Medicines containing oestrogen (such as the oral

contraceptive pill)

Benzylpenicillin
Any other use????...
Tranexamic Acid was originally used to prevent
excessive bleeding in menstrual bleeding ,
haemophilia and surgery. Later on, by accident the
skin whitening qualities of Tranexamic Acid were
discovered. TA is also very stable to light,
temperature, pH, and oxygen, and no special
protections are needed to keep its whitening effect
unlike many other agents. It is quickly becoming
the skin lightener of choice for men and women
who suffer from hyper pigmentation and skin
Blood The essence of Life

STOP BLOOD LOSS WITH

TRANEXAMIC ACID