RADICAVA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RADICAVA (RADICAVA).
Radicava (edaravone) is a free radical scavenger that protects neuronal cells from oxidative stress by scavenging oxygen-derived free radicals and inhibiting lipid peroxidation in the central nervous system.
| Metabolism | Edaravone is metabolized primarily via glucuronidation by UGT1A9, UGT1A6, and UGT2B7, and also undergoes sulfation by SULT1A1 and SULT1A3. It is a substrate for organic anion transporter OAT3. |
| Excretion | Primarily renal excretion of unchanged drug (~88% of dose), with approximately 6% recovered in feces. Biliary excretion is negligible. |
| Half-life | Terminal elimination half-life is approximately 4.5 hours. This short half-life supports twice-daily dosing; no accumulation occurs upon repeated administration. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily human serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 1.04 L/kg, indicating extensive distribution into tissues, including the central nervous system. |
| Bioavailability | Oral bioavailability is approximately 97% (high), allowing for direct switching between intravenous and oral formulations without dose adjustment. |
| Onset of Action | Intravenous infusion: clinical effects observed within weeks (typically 2-4 weeks) based on ALSFRS-R slope changes in clinical trials; oral administration: similar onset due to rapid absorption. |
| Duration of Action | Duration of therapeutic effect is approximately 12 hours, correlating with the dosing interval (every 12 hours). Continuous therapy is required to maintain suppression of oxidative stress. |
60 mg administered intravenously over 60 minutes once daily for 14 days, followed by a 14-day drug-free period; subsequent cycles repeat this 28-day cycle indefinitely.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (eGFR 30-89 mL/min/1.73 m²). Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m²) or end-stage renal disease. |
| Liver impairment | No dose adjustment required for mild hepatic impairment (Child-Pugh class A). Not studied in moderate to severe hepatic impairment (Child-Pugh class B or C). |
| Pediatric use | Safety and efficacy not established in pediatric patients below 18 years of age; no recommended dosing. |
| Geriatric use | No specific dose adjustment recommended; clinical studies included patients aged up to 75 years with no observed differences in safety or efficacy. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RADICAVA (RADICAVA).
| Breastfeeding | It is unknown whether edaravone is excreted in human breast milk. No studies on milk production or excretion have been conducted. The M/P ratio has not been determined. Due to potential serious adverse reactions in nursing infants, breastfeeding should be discontinued during treatment with RADICAVA. |
| Teratogenic Risk | In animal studies, edaravone (RADICAVA) has not shown teratogenicity at clinically relevant doses. There are no adequate and well-controlled studies in pregnant women. The drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Risk cannot be ruled out for all trimesters. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to edaravone or any ingredient in the formulation"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis and angioedema","Sulfite allergy (contains sodium bisulfite)","Renal impairment (no dose adjustment recommended, but monitor renal function)"] |
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| Fetal Monitoring | Monitor for hypersensitivity reactions (e.g., urticaria, dyspnea) and laboratory abnormalities, including hepatic function tests (e.g., ALT, AST) and renal function. No specific fetal monitoring is recommended, but routine prenatal care should be maintained. |
| Fertility Effects | Animal studies have shown no impairment of fertility in male and female rats at doses up to 2 times the human clinical dose based on body surface area. Human data on fertility effects are not available. |