Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Intravenous:
Radicava: 30 mg/100 mL (100 mL) [contains sodium bisulfite]
Pharmacology
Mechanism of Action
The mechanism by which edaravone slows the decline of physical function in patients with ALS is unknown. Edaravone is a free radical and peroxynitrite scavenger that prevents oxidative damage to cell membranes and may contribute to inhibiting the progression of ALS (Nagase 2016).
Pharmacokinetics/Pharmacodynamics
Metabolism
Metabolized to inactive sulfate and glucuronide conjugates; sulfate conjugate formed by sulfotransferases. Glucuronide conjugation involves UGT1A6, UGT1A9, UGT2B7, and UGT2B17 in the liver and kidney.
Excretion
Urine (70% to 90% as glucuronide conjugate; 5% to 10% as sulfate conjugate; ≤1% unchanged)
Time to Peak
1 hour
Half-Life Elimination
4.5 to 6 hours
Protein Binding
92% (mainly albumin)
Use: Labeled Indications
Amyotrophic lateral sclerosis: Treatment of amyotrophic lateral sclerosis (ALS)
Contraindications
Hypersensitivity to edaravone or any component of the formulation
Dosage and Administration
Dosing: Adult
Amyotrophic lateral sclerosis (ALS): IV:
Initial cycle: 60 mg once daily for 14 days, followed by a 14-day drug-free period.
Subsequent cycles: 60 mg once daily for 10 days within a 14-day period, followed by a 14-day drug-free period.
Dosing: Geriatric
Refer to adult dosing. Use with caution.
Administration
IV: For IV use only. Administer as two consecutive 30 mg infusion bags (60 mg total) over 60 minutes (infusion rate: ~1 mg/minute [3.33 mL/minute]). Do not mix edaravone with other medications. Do not use if the oxygen indicator has turned blue or purple before opening. Promptly discontinue with any signs or symptoms consistent with a hypersensitivity reaction.
Storage
Store at ≤25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light. Once overwrap package is opened, use within 24 hours.
Drug Interactions
There are no known significant interactions.
Adverse Reactions
>10%:
Central nervous system: Abnormal gait (13%)
Hematologic & oncologic: Bruise (15%)
1% to 10%:
Central nervous system: Headache (10%)
Dermatologic: Dermatitis (8%), eczema (7%), tinea (4%)
Endocrine & metabolic: Glycosuria (4%)
Respiratory: Dyspnea (≤6%), hypoxia (≤6%), respiratory failure (≤6%)
<1%, postmarketing, and/or case reports: Anaphylaxis, hypersensitivity reaction
Warnings/Precautions
Concerns related to adverse effects:
- Hypersensitivity: Hypersensitivity reactions (eg, redness, wheals, erythema multiforme) and anaphylaxis have been reported. If hypersensitivity occurs, discontinue treatment and monitor.
Dosage form specific issues:
- Sodium bisulfite: May contain sodium bisulfite; use caution in patients with asthma or a sulfite allergy.
Monitoring Parameters
Hypersensitivity reactions
Pregnancy
Pregnancy Considerations
Adverse events were observed in some animal reproduction studies.
Patient Education
What is this drug used for?
- It is used to treat amyotrophic lateral sclerosis (ALS).
Frequently reported side effects of this drug
- Headache
- Skin irritation
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Severe dizziness
- Passing out
- Shortness of breath
- Bruising
- Trouble walking
- Change in balance
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
