ERFA-TRANEXAMIC SOLUTION

Country: Canada

Language: English

Source: Health Canada

Active ingredient:

TRANEXAMIC ACID

Available from:

SEARCHLIGHT PHARMA INC

ATC code:

B02AA02

INN (International Name):

TRANEXAMIC ACID

Dosage:

100MG

Pharmaceutical form:

SOLUTION

Composition:

TRANEXAMIC ACID 100MG

Administration route:

INTRAVENOUS

Units in package:

5/10/50ML

Prescription type:

Prescription

Therapeutic area:

HEMOSTATICS

Product summary:

Active ingredient group (AIG) number: 0114760002; AHFS:

Authorization status:

APPROVED

Authorization date:

2016-09-06

Summary of Product characteristics

PRODUCT MONOGRAPH
PR
ERFA-TRANEXAMIC
TRANEXAMIC ACID FOR INJECTION
Solution, 100 mg/mL, Intravenous
Ph. Eur.
Antifibrinolytic Agent
Searchlight Pharma Inc.
1600 Notre-Dame West, suite 312
Montreal, Quebec
H3J 1M1
Date of Preparation:
OCT 18, 2022
Submission Control No.: 267412
_ERFA-TRANEXAMIC, 100 mg/mL _
Page 2 of 16
PRODUCT MONOGRAPH
PR
ERFA-TRANEXAMIC
TRANEXAMIC ACID FOR INJECTION, PH. EUR.
100 mg/mL
THERAPEUTIC CLASSIFICATION
Antifibrinolytic Agent
ACTION
Tranexamic acid produces an antifibrinolytic effect by competitively
inhibiting the activation of
plasminogen to plasmin. It is also a weak non-competitive inhibitor of
plasmin. These properties
make possible its clinical use as an antifibrinolytic in the treatment
of both general and local
fibrinolytic hemorrhages. It has an action mechanism similar to, but
about 10 times more potent
_in vitro_, than that of E amino caproic acid (EACA).
Tranexamic acid binds considerably more strongly than EACA to both the
strong and weak sites
in the plasminogen molecule in a ratio corresponding to the difference
in potency between the
compounds. The pharmacological significance of the binding to these
different sites has not yet
been evaluated.
Tranexamic acid does not bind to serum albumin. The plasma protein
binding seems to be fully
accounted for by its binding to plasminogen and appears to be
negligible at therapeutic plasma
levels of 5-10 mg/L.
Possible routes of biotransformation are acetylation or deamination
followed by oxidation or
reduction. After oral administration approximately 50% of the parent
compound, 2% of the
deaminated dicarboxylic acid, and 0.5% of the acetylated product are
excreted.
Tranexamic acid is eliminated by glomerular filtration, excretion
being about 30% at one hour,
55% at three hours and 90% at 24 hours after intravenous
administration of 10 mg per kg body
weight. After oral administration of 10-15 mg per kg body weight,
excretion was 1% at one hour,
7% at three hours and 39% at 24 hours.
Intravenous administration of 10 mg per kg body w