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:

Nexus Pharmaceuticals Inc

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 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 a colorless to slightly yellow solution. NDC 14789-500-10 10 × 10 mL Single Dose Vials   STORAGE Store at 25°C (77°F); excursions permitted to 15°–30°C (59°–86°F) [see USP Controlled Room Temperature].   Rx only Manufactured in the USA for Nexus Pharmaceuticals Inc., Vernon Hills, IL 60061.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TRANEXAMIC ACID- TRANEXAMIC ACID INJECTION, SOLUTION
NEXUS PHARMACEUTICALS INC
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TRANEXAMIC ACID INJECTION
Antifibrinolytic agent
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 up to 10 mg per
mL blood has no influence on the platelet count, the coagulation time
or various coagulation factors in
whole blood or citrated blood from normal subjects. On the other hand,
tranexamic acid in
concentrations of 10 mg and 1 mg per mL blood prolongs the thrombin
time. 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
the unchanged dru