Tranexamic acid-injection

Cyklokapron

Contraindications

Hypersensitivity

Acquired defective color vision

Subarachnoid hemorrhage

Active intravascular clotting

Cautions

Use caution in renal impairment, subarachnoid hemorrhage, vascular disease

DIC

Visual defects (color vision change or visual loss) reported

Thrombembolic history

Ureteral obstruction resulting from clot formation reported; use caution in patients with upper urinary tract bleeding

Thromboembolism or venous and arterial thrombosis reported

Ligneous conjunctivitis has been reported

Concurrent use with anti-inhibitor coagulant complex/factor IX complex concentrates

Concurrent use with tretinoin may exacerbate procoagulant effects

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Shortness of breath.
• Coughing up blood.
• Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight.
• Very bad headache.
• Any unexplained bruising or bleeding.
• Change in eyesight, eye pain, or very bad eye irritation.
• Swelling, warmth, numbness, change of color, or pain in a leg or arm.
• Chest pain or pressure.
• Feeling very tired or weak.
• Seizures.
• Very bad dizziness or passing out.

• If you need to store tranexamic acid injection at home, talk with your doctor, nurse, or pharmacist about how to store it.

Each mL of the sterile solution for intravenous injection contains 100 mg tranexamic acid USP 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.

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 other 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 hours after intravenous administration of 10 mg per kg body weight.

An antifibrinolytic concentration of tranexamic acid remains in different tissues for about 17 hours, and in the serum, up to seven or eight hours.

Tranexamic acid passes through the placenta. The concentration in cord blood after an intravenous injection of 10 mg per kg to pregnant women is about 30 mg per liter, as high as in the maternal blood. Tranexamic acid diffuses rapidly into joint fluid and the synovial membrane. In the joint fluid, the same concentration is obtained as in the serum. The biological half-life of tranexamic acid in the joint fluid is about three hours.

The concentration of tranexamic acid in a number of other tissues is lower than in blood. In breast milk, the concentration is about one hundredth of the serum peak concentration. Tranexamic acid concentration in cerebrospinal fluid is about one tenth of that of the plasma. The drug passes into the aqueous humor, the concentration being about one tenth of the plasma concentration.

Tranexamic acid has been detected in semen where it inhibits fibrinolytic activity but does not influence sperm migration.

Tranexamic Acid Injection is contraindicated:

1. In patients with acquired defective color vision, since this prohibits measuring one endpoint that should be followed as a measure of toxicity (see WARNINGS).
2. In patients with subarachnoid hemorrhage. Anecdotal experience indicates that cerebral edema and cerebral infarction may be caused by Tranexamic Acid Injection in such patients.
3. In patients with active intravascular clotting.
4. In patients with hypersensitivity to tranexamic acid or any of the ingredients.

Cases of overdosage of Tranexamic Acid Injection have been reported. Based on these reports, symptoms of overdosage may be gastrointestinal, e.g., nausea, vomiting, diarrhea; hypotensive, e.g., orthostatic symptoms; thromboembolic, e.g., arterial, venous, embolic; neurologic, e.g., visual impairment, convulsions, headache, mental status changes; myoclonus; and rash.

NDC 42571-189-56
Tranexamic Acid
Injection
1000 mg/10 mL
(100 mg/mL)
Solution for
Intravenous Injection
Rx Only
10 mL Ampule
Single-Dose ONLY.
Discard any remaining
portion after single use.
MICRO LABS

NDC 42571-189-56         Rx Only
Tranexamic Acid Injection
1000 mg/10 mL (100 mg/mL)
Solution for Intravenous Injection
Single-Dose ONLY.
Discard any remaining portion after single use.
Contains 1 Ampule 10 mL
MICRO LABS