LYSTEDA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LYSTEDA (LYSTEDA).
Competitive inhibition of plasminogen activation, reducing fibrinolysis.
| Metabolism | Primarily excreted unchanged in urine; minimal hepatic metabolism via glucuronidation. |
| Excretion | Primarily renal excretion (>95% unchanged drug via glomerular filtration). Less than 5% is metabolized (mainly acylated derivative). |
| Half-life | Terminal elimination half-life is approximately 2 hours (range 1.5–2.5 hours). In patients with renal impairment, half-life is significantly prolonged (up to 20 hours in severe renal impairment). |
| Protein binding | Approximately 3% bound to plasma proteins (primarily albumin). No significant protein binding displacement interactions. |
| Volume of Distribution | Volume of distribution is approximately 1.2 L/kg (range 1.0–1.5 L/kg), indicating extensive distribution into total body water and tissues. |
| Bioavailability | Oral bioavailability is approximately 34% (range 30–40%) due to incomplete absorption and first-pass metabolism. Intravenous administration yields 100% bioavailability. |
| Onset of Action | Oral: Onset of clinical effect occurs within 2–3 hours after a single 1.3 g dose (three 650 mg tablets). Maximum antifibrinolytic effect is seen at typical therapeutic concentrations. |
| Duration of Action | Duration of action is approximately 6–8 hours following oral administration, corresponding to maintenance of therapeutic plasma concentrations above 10 mcg/mL. Dosing every 6–8 hours is recommended for sustained effect. |
650 mg orally three times daily (total 3.9 g/day) for up to 5 days during menses.
| Dosage form | TABLET |
| Renal impairment | If GFR 30-50 mL/min: 650 mg orally twice daily for up to 5 days. If GFR 10-29 mL/min: 650 mg orally once daily for up to 5 days. If GFR <10 mL/min or dialysis: contraindicated. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe impairment (Child-Pugh C); use caution. |
| Pediatric use | Not indicated for pediatric patients below 18 years of age. |
| Geriatric use | No specific dose adjustment, but consider age-related renal impairment and adjust dose based on GFR per renal adjustment guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LYSTEDA (LYSTEDA).
| Breastfeeding | Excreted in human breast milk; M/P ratio unknown. Caution advised. Consider benefit of breastfeeding vs potential infant exposure. |
| Teratogenic Risk | FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but no adequate human studies in pregnant women. Use only if clearly needed. First trimester: no evidence of teratogenicity. Second and third trimesters: no known fetal harm, but lacks robust human data. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Active thromboembolic disease","History of thrombosis or thromboembolism","Intracranial hemorrhage","Hypersensitivity to tranexamic acid"]
| Precautions | ["Increased risk of thromboembolic events","Concomitant use with hormonal contraceptives increases thrombotic risk","Ocular effects (e.g., visual disturbances)","Seizures","Renal impairment dose adjustment"] |
Loading safety data…
| Monitor for thromboembolic events, visual disturbances, and allergic reactions. No specific fetal monitoring required, but standard prenatal care should continue. |
| Fertility Effects | No known adverse effects on fertility in animal studies. Human data lacking. |