Tranexamic Acid
FDA Drug Information • Also known as: Cyklokapron, Tranexamic Acid, Tranexamic Acid In Sodium Chloride
- Brand Names
- Cyklokapron, Tranexamic Acid, Tranexamic Acid In Sodium Chloride
- Dosage Form
- POWDER
- Product Type
- BULK INGREDIENT
Description
11 DESCRIPTION Tranexamic acid USP tablets is an antifibrinolytic drug administered orally. The chemical name is trans-4-aminomethyl-cyclohexanecarboxylic acid. The structural formula is: Tranexamic acid is a white crystalline powder. It is freely soluble in water and in glacial acetic acid and is very slightly soluble in ethanol and practically insoluble in ether. The molecular formula is C 8 H 15 N0 2 and the molecular weight is 157.2. Tranexamic acid USP tablets are provided as white oval-shaped tablets and are not scored. Each tablet is debossed with the marking “FP650.” The active ingredient in each tablet is 650 mg tranexamic acid. The inactive ingredients contained in each tablet are: microcrystalline cellulose, colloidal silicon dioxide, pregelatinized corn starch, povidone, hypromellose, stearic acid, and magnesium stearate. Chemical Structure
What Is Tranexamic Acid Used For?
1 INDICATIONS AND USAGE Tranexamic acid USP tablets are indicated for the treatment of cyclic heavy menstrual bleeding in females of reproductive potential [see Clinical Studies (14) ]. Tranexamic acid USP tablets is an antifibrinolytic indicated for the treatment of cyclic heavy menstrual bleeding in females of reproductive potential. ( 1 )
Dosage and Administration
2 DOSAGE AND ADMINISTRATION 1,300 mg three times a day (3,900 mg/day) for a maximum of 5 days during monthly menstruation ( 2.1 ) Renal impairment: Lower dosage is needed (for a maximum of 5 days during menstruation) if serum creatinine concentration (Cr) is higher than 1.4 mg/dL ( 2.2 ) Cr above 1.4 mg/dL and ≤ 2.8 mg/dL: 1,300 mg two times a day (2,600 mg/day) Cr above 2.8 mg/dL and ≤ 5.7 mg/dL: 1,300 mg once a day (1,300 mg/day) Cr above 5.7 mg/dL: 650 mg once a day (650 mg/day) 2.1 Recommended Testing Prior to Tranexamic Acid USP Tablets Administration Prior to prescribing tranexamic acid USP tablets, exclude endometrial pathology that can be associated with heavy menstrual bleeding. 2.2 Recommended Dosage The recommended dosage of tranexamic acid USP tablets for patients with normal renal function is 1300 mg orally three times daily (3900 mg/day) for a maximum of 5 days during monthly menstruation. Tranexamic acid USP tablets may be administered with or without food. Swallow tablets whole; do not chew or break apart. 2.3 Dosage Recommendations in Patients with Renal Impairment The recommended dosage (for a maximum of 5 days during monthly menstruation) in patients with renal impairment with serum creatinine concentration higher than 1.4 mg/dL is described in Table 1. Table 1. Recommended Dosage of Tranexamic Acid USP Tablets in Patients with Renal Impairment Serum Creatinine (mg/dL) Recommended Dosage (maximum of 5 days during menstruation) Total Daily Dose Above 1.4 and ≤ 2.8 1300 mg two times a day 2600 mg Above 2.8 and ≤ 5.7 1300 mg once a day 1300 mg Above 5.7 650 mg once a day 650 mg
Side Effects (Adverse Reactions)
6 ADVERSE REACTIONS Most common adverse reactions in clinical trials (≥ 5%, and more frequent in tranexamic acid USP tablets-treated subjects compared to placebo-treated subjects) are headache, sinus and nasal symptoms, back pain, abdominal pain, musculoskeletal pain, joint pain, muscle cramps, migraine, anemia and fatigue. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Nordic Pharma, Inc. at 1-844-267-4641 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 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. Adverse Reactions in Short-term Studies The safety of tranexamic acid USP tablets in the treatment of heavy menstrual bleeding in females of reproductive potential was studied in two randomized, double-blind, placebo-controlled studies [see Clinical Studies (14) ]. Study 1 compared the effects of two doses of tranexamic acid USP tablets (1950 mg and 3900 mg per day 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 tranexamic acid USP tablets. Study 2 compared the effects of tranexamic acid USP tablets (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 tranexamic acid USP tablets. Across the studies, the combined exposure to 3900 mg/day tranexamic acid USP tablets was 947 cycles and the average duration of use was 3.4 days per cycle. 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 body mass index (BMI) of approximately 32 kg/m 2 . On average, subjects had a history of heavy menstrual bleeding 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. A list of adverse reactions occurring in ≥ 5% of subjects and more frequently in tranexamic acid USP tablets-treated subjects receiving 3900 mg/day compared to placebo-treated subjects is provided in Table 2. Table 2. Adverse Reactions * Reported in Women with Heavy Menstrual Bleeding (Studies 1 and 2) Tranexamic acid USP tablets 3900 mg/day n (%) (N=232) Placebo n (%) (N=139) * Adverse reactions that were reported by ≥ 5% of tranexamic acid USP tablets-treated subjects and more frequently in tranexamic acid USP tablets-treated subjects compared to placebo-treated subjects a Includes headache and tension headache b Nasal and sinus symptoms include nasal, respiratory tract and sinus congestion, sinusitis, acute sinusitis, sinus headache, allergic sinusitis and sinus pain, and multiple allergies and seasonal allergies c Abdominal pain includes abdominal tenderness and discomfort d Musculoskeletal pain includes musculoskeletal discomfort and myalgia e Arthralgia includes joint stiffness and swelling Number of Subjects with at Least One Adverse Reaction 208 (89.7%) 122 (87.8%) Headache a 117 (50.4%) 65 (46.8%) Nasal & sinus symptoms b 59 (25.4%) 24 (17.3%) Back pain 48 (20.7%) 21 (15.1%) Abdominal pain c 46 (19.8%) 25 (18.0%) Musculoskeletal pain d 26 (11.2%) 4 (2.9%) Arthralgia e 16 (6.9%) 7 (5.0%) Muscle cramps & spasms 15 (6.5%) 8 (5.8%) Migraine 14 (6.0%) 8 (5.8%) Anemia 13 (5.6%) 5 (3.6%) Fatigue 12 (5.2%) 6 (4.3%) Adverse Reactions in Long-term Studies Long-term safety of tranexamic acid USP tablets was studied in...
Drug Interactions
7 DRUG INTERACTIONS No drug-drug interaction studies were conducted with tranexamic acid USP tablets. Concomitant therapy with tissue plasminogen activators may decrease the efficacy of both tranexamic acid USP tablets and tissue plasminogen activators. ( 7.2 ) 7.1 Combined Hormonal Contraceptives Because tranexamic acid USP tablets are antifibrinolytic, concomitant use of combined hormonal contraception and tranexamic acid USP tablets may increase the thrombotic risk associated with combined hormonal contraceptives. For this reason, concomitant use of tranexamic acid USP tablets with combined hormonal contraceptives is contraindicated [see Contraindications (4) and Warnings and Precautions (5.1) ] . 7.2 Tissue Plasminogen Activators Concomitant therapy with tissue plasminogen activators may decrease the efficacy of both tranexamic acid USP tablets and tissue plasminogen activators. Discontinue tranexamic acid USP tablets if a patient requires tissue plasminogen activators. 7.3 Factor I X Complex Concentrates or Anti-Inhibitor Coagulant Concentrates Tranexamic acid USP tablets are not recommended in patients taking either Factor I X complex concentrates or anti-inhibitor coagulant concentrates because the risk of thrombosis may be increased [see Warnings and Precautions (5.1) ]. 7.4 All-Trans Retinoic Acid (Oral Tretinoin) Tranexamic acid USP tablets are not recommended in patients 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 Warnings and Precautions (5.1) ].
Contraindications
4 CONTRAINDICATIONS Concomitant use of combined hormonal contraceptives ( 4.1 ) Active thromboembolic disease or a history or intrinsic risk of thrombosis or thromboembolism, including retinal vein or artery occlusion ( 4.1 ) Hypersensitivity to tranexamic acid ( 4.2 ) 4.1 Thromboembolic Risk Tranexamic acid USP tablets are contraindicated in females of reproductive potential who are [see Warnings and Precautions (5.1) ]: Using combined 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) 4.2 Hypersensitivity to Tranexamic Acid Tranexamic acid USP tablets are contraindicated in females with reproductive potential with known hypersensitivity to tranexamic acid [see Warnings and Precautions (5.2) and Adverse Reactions (6.1) ] .
Pregnancy and Breastfeeding
8.1 Pregnancy Risk Summary Tranexamic acid USP tablets are not indicated for use in pregnant women. There is no available data on tranexamic acid USP tablets use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Tranexamic acid crosses the placenta. Animal reproduction studies have not identified adverse developmental outcomes with oral administration of tranexamic acid to pregnant rats at doses up to 4 times the recommended human dose (see Data ). In the US general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In a rat embryo-fetal developmental toxicity study, tranexamic acid had no adverse effects on embryo-fetal development when administered during the period of organogenesis (from gestation days 6 through 17) at twice daily doses of 0, 150, 375, and 750 mg/kg (1, 2 and 4 times the recommended human oral dosage of 3900 mg/day based on body surface area (mg/m 2 )). In a perinatal-postnatal developmental toxicity study in rats administered tranexamic acid from gestation day 6 through postnatal day 20 at twice daily doses of 0, 150, 375, and 750 mg/kg, no significant adverse effects on maternal behavior or body weight were observed, and no significant effects on pup viability, body weight, developmental milestones or adult fertility were observed. It was concluded that the no-observed-effect-level (NOEL) for this study was 1500 mg/kg/day in both F 0 and F 1 generations, which is equivalent to 4 times the recommended human oral dose of 3900 mg/day based on body surface area (mg/m 2 ).
Overdosage
10 OVERDOSAGE There are no known cases of intentional overdose with tranexamic acid USP tablets and no subjects in the clinical program took more than 2 times the prescribed amount of tranexamic acid USP tablets in a 24-hour period (>7800 mg/day). However, cases of overdose of tranexamic acid have been reported. Based on these reports, symptoms of overdose may include gastrointestinal (nausea, vomiting, diarrhea); hypotensive (e.g., orthostatic symptoms); thromboembolic (arterial, venous, embolic); visual impairment; mental status changes; myoclonus; or rash. No specific information is available on the treatment of overdose with tranexamic acid USP tablets. In the event of overdose, employ the usual supportive measures (e.g., clinical monitoring and supportive therapy) as dictated by the patient’s clinical status.
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Tranexamic acid USP tablets are provided as white oval-shaped 650 mg tablets. Each tablet is debossed with the marking “FP650”and are supplied as: Quantity Package Type NDC Number 30 tablets HDPE bottle 69918-301-30 Storage Store at room temperature 25° C (77° F); excursions permitted to 15-30° C (59-86° F). [See USP Controlled Room Temperature].
About This Information
This drug information is sourced from FDA-approved labeling via the openFDA database. It is intended for educational and reference purposes only. This is not medical advice. Always consult your healthcare provider before making decisions about medication. Drug information may be updated by the FDA; check with your pharmacist for the most current information.
What are side effects?
Side effects are unwanted reactions that can occur when taking a medication. They range from mild (headache, nausea) to severe (allergic reactions, organ damage). Not everyone experiences side effects, and severity varies. Report any concerning side effects to your doctor.
What are drug interactions?
Drug interactions occur when a medication is affected by another drug, food, or supplement. Interactions can make medications less effective or cause dangerous side effects. Always tell your doctor about all medications and supplements you take.