Tranexa

Each capsule also contains sodium bisulfite, sodium lauryl sulfate and Yellow No.5 (Sunset Yellow FCF) as inactive ingredients. Each 5% w/v ampoule contains Tranexamic Acid 250 mg/5 mL, has a pH of 7-8 and an osmotic pressure ratio (with respect to physiological saline) of about 1.

Each 10% w/v ampoule contains Tranexamic Acid 250 mg/2.5 mL, has a pH of 7-8 and an osmotic pressure ratio (with respect to physiological saline) of about 2.

Tranexa is trans-4-aminomethylcyclohexanecarboxylic acid. It has a molecular formula of C₈H₁₅NO₂, molecular weight of 157.21 and melting point of 386-390°C (decomposition). It occurs as white crystals or powder, odorless and has bitter taste. It is freely soluble in water or glacial acetic acid; very slightly soluble in ethanol; practically insoluble in ether; soluble in sodium hydroxide TS.

Capsule Size: No.2, total length of 17.6 mm and weight of about 350 mg.

Tranexa™ (Tranexa) Tablets is indicated for the treatment of cyclic heavy menstrual bleeding.

Prior to prescribing Tranexa, exclude endometrial pathology that can be associated with heavy menstrual bleeding.

Tranexa injection is used to control or prevent excessive or heavy bleeding during dental procedures in patients with hemophilia. Tranexa is for short-term use only, usually 2 to 8 days.

Tranexa injection is an antifibrinolytic agent. It works by blocking the breakdown of blood clots. It may also be used for other conditions as determined by your doctor.

Tranexa is available only with your doctor's prescription.

Recommended Dosage

The recommended dose of Tranexa for women with normal renal function is two 650 mg tablets taken three times daily (3900 mg/day) for a maximum of 5 days during monthly menstruation. Tranexa may be administered without regard to meals. Tablets should be swallowed whole and not chewed or broken apart.

Renal Impairment

In patients with renal impairment, the plasma concentration of Tranexa increased as serum creatinine concentration increased. Dosage adjustment is needed in patients with serum creatinine concentration higher than 1.4 mg/dL (Table 1).

Table 1: Dosage of Tranexa in Patients with Renal Impairment

How supplied

Dosage Forms And Strengths

650 mg tablets

Storage And Handling

Tranexa (Tranexa) tablets are provided as white oval-shaped tablets. Each tablet is debossed with the marking “FP650” and are supplied as:

Storage

Store at room temperature 25° C (77° F); excursions permitted to 15-30° C (59-86° F)..

Manufactured for: Ferring Pharmaceuticals Inc. Parsippany, NJ 07054. By: Mikart, Inc. Atlanta, GA 30318. Rev. 10/2013

See also:
What is the most important information I should know about Tranexa?

Thromboembolic Risk

​Do not prescribe Tranexa Tablets to women who are

• ​using combination hormonal contraception
• ​known to have any of the following conditions:
  • Active thromboembolic disease (e.g., deep vein thrombosis, pulmonary embolism, or cerebral thrombosis)
  • A history of thrombosis or thromboembolism, including retinal vein or artery occlusion
  • An intrinsic risk of thrombosis or thromboembolism (e.g., thrombogenic valvular disease, thrombogenic cardiac rhythm disease, or hypercoagulopathy)

Venous and arterial thrombosis or thromboembolism, as well as cases of retinal artery and retinal vein occlusions, have been reported with Tranexa.

Hypersensitivity to Tranexa

Do not prescribe Tranexa Tablets to women with known hypersensitivity to Tranexa.

Use Tranexa as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Tranexa is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Tranexa at home, a health care provider will teach you how to use it. Be sure you understand how to use Tranexa. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.
• Do not use Tranexa if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.
• Keep this product, as well as syringes and needles, out of the reach of children and away from pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Follow all local rules for disposal.
• Continue to use Tranexa for the full course of treatment even if you feel well. Do not miss any doses.
• If you miss a dose of Tranexa, contact your doctor immediately.

Ask your health care provider any questions you may have about how to use Tranexa.

Use: Labeled Indications

Menstrual bleeding, heavy (oral): Treatment of cyclic heavy menstrual bleeding.

Tooth extraction in patients with hemostatic defects (injection, oral [Tranexa; Canadian product]): Short-term use in hemophilia patients to reduce or prevent hemorrhage and reduce need for replacement therapy during and following tooth extraction.

Off Label Uses

Dental procedures in patients on oral anticoagulant therapy

Based on the American College of Chest Physicians guidelines for perioperative management of antithrombotic therapy, Tranexa is recommended to use, when needed, in combination with the continuation of oral anticoagulant therapy for the perioperative management of patients who require minor procedures.

Hemoptysis (nonmassive), treatment

Data from a small, single-center, prospective, randomized, double-blind, placebo-controlled trial suggest that nebulized Tranexa may be beneficial for the control of nonmassive hemoptysis by reducing the duration and volume of bleeding, with a low risk for side effects.

See also:
What other drugs will affect Tranexa?

No drug-drug interaction studies were conducted with Tranexa.

Hormonal Contraceptives

Because Tranexa is antifibrinolytic, concomitant use of hormonal contraception and Tranexa may further exacerbate the increased thrombotic risk associated with combination hormonal contraceptives. For this reason, concomitant use of Tranexa with combination hormonal contraceptives is contraindicated.

Tissue Plasminogen Activators

Concomitant therapy with tissue plasminogen activators may decrease the efficacy of both Tranexa and tissue plasminogen activators. Therefore, exercise caution if a woman taking Tranexa therapy requires tissue plasminogen activators.

Factor IX Complex Concentrates or Anti-Inhibitor Coagulant Concentrates

Tranexa is not recommended for women taking either Factor IX complex concentrates or anti-inhibitor coagulant concentrates because the risk of thrombosis may be increased.

All-Trans Retinoic Acid (Oral Tretinoin)

Exercise caution when prescribing Tranexa to women with acute promyelocytic leukemia taking all-trans retinoic acid for remission induction because of possible exacerbation of the procoagulant effect of all-trans retinoic acid.

See also:
What are the possible side effects of Tranexa?

Clinical Trial Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to the rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Short-term Studies

The safety of Tranexa in the treatment of heavy menstrual bleeding (HMB) was studied in two randomized, double-blind, placebo-controlled studies. One study compared the effects of two doses of Tranexa (1950 mg and 3900 mg given daily for up to 5 days during each menstrual period) versus placebo over a 3-cycle treatment duration. A total of 304 women were randomized to this study, with 115 receiving at least one dose of 3900 mg/day of Tranexa. A second study compared the effects of Tranexa (3900 mg/day) versus placebo over a 6-cycle treatment duration. A total of 196 women were randomized to this study, with 117 receiving at least one dose of Tranexa. In both studies, subjects were generally healthy women who had menstrual blood loss of ≥ 80 mL.

In these studies, subjects were 18 to 49 years of age with a mean age of approximately 40 years, had cyclic menses every 21-35 days, and a BMI of approximately 32 kg/m². On average, subjects had a history of HMB for approximately 10 years and 40% had fibroids as determined by transvaginal ultrasound. Approximately 70% were Caucasian, 25% were Black, and 5% were Asian, Native American, Pacific Islander, or Other. Seven percent (7%) of all subjects were of Hispanic origin. Women using hormonal contraception were excluded from the trials.

The rates of discontinuation due to adverse events during the two clinical trials were comparable between Tranexa and placebo. In the 3-cycle study, the rate in the 3900 mg Tranexa dose group was 0.8% as compared to 1.4% in the placebo group. In the 6-cycle study, the rate in the Tranexa group was 2.4% as compared to 4.1% in the placebo group. Across the studies, the combined exposure to 3900 mg/day Tranexa was 947 cycles and the average duration of use was 3.4 days per cycle.

A list of adverse events occurring in ≥ 5% of subjects and more frequently in Tranexa treated subjects receiving 3900 mg/day compared to placebo is provided in Table 2.

Table 2: Adverse Events Reported by ≥ 5% of Subjects Treated with Tranexa and More Frequently in Tranexa-treated Subjects

Long-term Studies

Long-term safety of Tranexa was studied in two open-label studies. In one study, subjects with physician-diagnosed heavy menstrual bleeding (not using the alkaline hematin methodology) were treated with 3900 mg/day for up to 5 days during each menstrual period for up to 27 menstrual cycles. A total of 781 subjects were enrolled and 239 completed the study through 27 menstrual cycles. A total of 12.4% of the subjects withdrew due to adverse events. Women using hormonal contraception were excluded from the study. The total exposure in this study to 3900 mg/day Tranexa was 10,213 cycles. The average duration of Tranexa use was 2.9 days per cycle.

A long-term open-label extension study of subjects from the two short-term efficacy studies was also conducted in which subjects were treated with 3900 mg/day for up to 5 days during each menstrual period for up to 9 menstrual cycles. A total of 288 subjects were enrolled and 196 subjects completed the study through 9 menstrual cycles. A total of 2.1% of the subjects withdrew due to adverse events. The total exposure to 3900 mg/day Tranexa in this study was 1,956 cycles. The average duration of Tranexa use was 3.5 days per cycle.

The types and severity of adverse events in these two long-term open-label trials were similar to those observed in the double-blind, placebo-controlled studies although the percentage of subjects reporting them was greater in the 27-month study, most likely because of the longer study duration.

A case of severe allergic reaction to Tranexa was reported in the extension trial, involving a subject on her fourth cycle of treatment, who experienced dyspnea, tightening of her throat, and facial flushing that required emergency medical treatment.

Postmarketing Experience

The following adverse reactions have been identified from postmarketing experience with Tranexa. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Based on US and worldwide postmarketing reports, the following have been reported in patients receiving Tranexa for various

Indications:

• Nausea, vomiting, and diarrhea
• Allergic skin reactions
• Anaphylactic shock and anaphylactoid reactions
• Thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism, cerebral thrombosis, acute renal cortical necrosis, and central retinal artery and vein obstruction); cases have been associated with concomitant use of combination hormonal contraceptives
• Impaired color vision and other visual disturbances
• Dizziness