Dosing and uses of Lysteda (tranexamic acid oral)
Adult dosage forms and strengths
tablet
- 650mg
Menorrhagia
Indicated for the treatment of cyclic heavy menstrual bleeding
1300 mg PO TID for up to 5 days during menstruation
Renal impairment
- SCr >1.4 mg/dL and ≤2.8 mg/dL: 1300 mg PO BID
- SCr >2.8 mg/dL and ≤5.7 mg/dL: 1300 mg PO qDay
- SCr >5.7 mg/dL: 650 mg PO qDay
- Each regimen listed above may be administered for up to 5 days during menstruation
Hereditary Angioedema (Off-label)
Long term prophylaxis: 1000-1500 mg PO q8-12hr; reduce dose to 500 mg/dose PO qDay or q12hr when frequency of attacks reduces
Short term prophylaxis: 75 mg/kg/day PO divided q8-12hr for 5 days before and after the event
Treatment of acute HAE attack: 25 mg/kg/dose PO/IV; not to exceed 1000 mg/dose q3-4hr; not to exceed 75 mg/kg/day or 1000 mg PO q6hr for 48 hr
Cone Biopsy (Off-label)
1000-1500 mg q8-12hr x12 days postop
Epistaxis (Off-label)
1000-1500 mg q8-12hr x10 days
Hyphema (Off-label)
1000-1500 mg q8-12hr x7 days
Hereditary Angioedema (Off-label)
1000-1500 mg PO BID/TId
Administration
May take with or without food
Swallow whole, do not chew, break, or crush
Pediatric dosage forms and strengths
Indicated for women of reproductive age and is not intended for use in premenarcheal girls
Based on a pharmacokinetic study in 20 adolescent females, aged 12-16 years, no dose adjustment is needed in the adolescent population
Lysteda (tranexamic acid oral) adverse (side) effects
>10%
Headache (50.4%)
Nasal and sinus symptoms (25.4%)
Back pain (20.7%)
Abdominal pain (19.8%)
Musculoskeletal pain (11.2%)
1-10%
Arthralgia (6.9%)
Muscle cramps and spasms (5.8%)
Migraine (6%)
Anemia (5.6%)
Fatigue (5.2%)
Postmarketing Reports
Nausea, vomiting, and diarrhea
Allergic skin reactions
Anaphylactic shock and anaphylactoid reactions
Thromboembolic events (eg, DVT, 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
Warnings
Contraindications
Hypersensitivity
Women using combination hormonal contraceptives
Active thromboembolic disease (eg, DVT, pulmonary embolism, or cerebral thrombosis)
History of thrombosis or thromboembolism, including retinal vein or artery occlusion
Intrinsic risk of thrombosis or thromboembolism (eg, thrombogenic valvular disease, thrombogenic cardiac rhythm disease, or hypercoagulopathy)
Cautions
Increased risk for thrombosis when coadministered with combination oral contraceptive (see Contraindications), Factor IX complex concentrates, anti-inhibitor coagulant concentrates, or oral tretinoin
Retinal venous and arterial occlusion has been reported
Severe allergic reaction reported; anaphylactic shock reported with IV product
May cause cerebral edema and cerebral infarction in women with subarachnoid hemorrhage
Ligneous conjunctivitis reported
Pregnancy and lactation
Pregnancy category: B; not indicated in pregnant women
Reproduction studies have been performed in mice, rats, and rabbits and have revealed no evidence of impaired fertility or harm to the fetus due to tranexamic acid; however, tranexamic acid is known to cross the placenta and appears in cord blood at concentrations approximately equal to the maternal concentration
Lactation: Distributed in human breast milk at a concentration of about 1/100th of the corresponding serum concentration; should be used during lactation only if clearly needed
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Lysteda (tranexamic acid oral)
Mechanism of action
Antifibrinolytic; synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure
Absorption
Bioavailability: 45%
Peak plasma time: 2.5 hr
Peak plasma concentration: 16.41 mcg/mL (steady-state)
AUC: 80.19 mcg•hr/mL
Distribution
Protein bound: 3%
Vd: 0.18 L/kg (initial); 0.39 L/kg (steady-state)
Metabolism
Small fraction is metabolized
Elimination
Half-life: 11.08 hr
Eliminated by urinary excretion primarily via glomerular filtration
Excretion: 90% urine; >95% of the dose excreted unchanged
