TRANEXAMIC ACID injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

TRANEXAMIC ACID (UNII: 6T84R30KC1) (TRANEXAMIC ACID - UNII:6T84R30KC1)

Available from:

Acella Pharmaceuticals

INN (International Name):

TRANEXAMIC ACID

Composition:

TRANEXAMIC ACID 100 mg in 1 mL

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Tranexamic Acid Injection is indicated in patients with hemophilia for short-term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction. Tranexamic Acid Injection is contraindicated: - In patients with acquired defective color vision, since this prohibits measuring one endpoint that should be followed as a measure of toxicity (see WARNINGS). - In patients with subarachnoid hemorrhage. Anecdotal experience indicates that cerebral edema and cerebral infarction may be caused by Tranexamic Acid Injection  in such patients. - In patients with active intravascular clotting. - In patients with hypersensitivity to tranexamic acid or any of the ingredients

Product summary:

Tranexamic Acid Injection 100 mg/mL is supplied as a sterile, clear, colorless, preservative-free aqueous solution in single use 10 mL vials, boxes of 10. (NDC 42192-605-10, 10 vials of 10 mL).

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TRANEXAMIC ACID- TRANEXAMIC ACID INJECTION, SOLUTION
ACELLA PHARMACEUTICALS
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TRANEXAMIC ACID INJECTION
DESCRIPTION
Each mL of the sterile solution for intravenous injection contains 100
mg tranexamic acid and Water for
Injection to 1 mL.
FORMULATION
Chemical Name: trans-4-(aminomethyl) cyclohexanecarboxylic acid.
Structural Formula:
Tranexamic acid is a white crystalline powder. The aqueous solution
for injection has a pH of 6.5 to
8.0.
CLINICAL PHARMACOLOGY
Tranexamic acid is a competitive inhibitor of plasminogen activation,
and at much higher concentrations,
a noncompetitive inhibitor of plasmin, i.e., actions similar to
aminocaproic acid. Tranexamic acid is
about 10 times more potent in vitro than aminocaproic acid.
Tranexamic acid binds more strongly than aminocaproic acid to both the
strong and weak receptor sites
of the plasminogen molecule in a ratio corresponding to the difference
in potency between the
compounds. Tranexamic acid in a concentration of 1 mg per mL does not
aggregate platelets in vitro.
Tranexamic acid in concentrations as low as 1 mg per mL, can prolong
the thrombin time. However,
tranexamic acid in concentrations up to 10 mg per mL in blood showed
no influence on the platelet
count, the coagulation time or coagulation factors in whole blood or
citrated blood from normal
subjects.
The plasma protein binding of tranexamic acid is about 3% at
therapeutic plasma levels and seems to be
fully accounted for by its binding to plasminogen. Tranexamic acid
does not bind to serum albumin.
After an intravenous dose of 1 g, the plasma concentration time curve
shows a triexponential decay with
a half-life of about 2 hours for the terminal elimination phase. The
initial volume of distribution is about
9 to 12 liters. Urinary excretion is the main route of elimination via
glomerular filtration. Overall renal
clearance is equal to overall plasma clearance (110 to 116 mL/min) and
more than 95% of the dose is
excreted in the urine as unchanged drug. Excretion of tranexamic acid
is about 90% at 24