Version May 2024
Amyotrophic lateral sclerosis :
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.
Oral:
Initial cycle: 105 mg (5 mL) once daily for 14 days, followed by a 14-day drug-free period.
Subsequent cycles: 105 mg (5 mL) once daily for 10 days within a 14-day period, followed by a 14-day drug-free period.
Switching from IV to oral therapy: Patients treated with 60 mg IV may be switched to 105 mg orally at the same dosing frequency; follow food consumption dosing recommendations.
eGFR ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.
eGFR <30 mL/minute/1.73 m2: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
No dosage adjustment necessary.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for intravenous formulation in adults.
>10%:
Hematologic & oncologic: Bruise (15%)
Nervous system: Abnormal gait (13%)
1% to 10%:
Dermatologic: Dermatitis (8%), eczema (7%), tinea (4%)
Genitourinary: Glycosuria (4%)
Nervous system: Headache (10%)
Respiratory: Dyspnea (≤6%), hypoxia (≤6%), respiratory failure (≤6%)
Postmarketing: Hypersensitivity: Anaphylaxis, hypersensitivity reaction
Hypersensitivity to edaravone or any component of the formulation
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.
• Port infections: Port infections leading to hospitalization may occur, in both early and long-term treatment with edaravone (Witzel 2022).
Dosage form specific issues:
• Sodium bisulfite: May contain sodium bisulfite; use caution in patients with asthma or a sulfite allergy.
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]
Suspension, Oral:
Radicava ORS: 105 mg/5 mL (50 mL) [contains sodium bisulfite]
Radicava ORS Starter Kit: 105 mg/5 mL (35 mL) [contains sodium bisulfite]
No
Solution (Radicava Intravenous)
30 mg/100 mL (per mL): $7.48
Suspension (Radicava ORS Oral)
105 mg/5 mL (per mL): $320.71
Suspension (Radicava ORS Starter Kit Oral)
105 mg/5 mL (per mL): $320.71
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
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]
Suspension, Oral:
Radicava: 105 mg/5 mL (35 mL, 50 mL) [contains sodium bisulfite]
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.
Oral: Administer orally in the morning on an empty stomach after overnight fasting (8 hours for high-fat meal [800 to 1,000 calories; 50% fat]; 4 hours for a low-fat meal [400 to 500 calories, 25% fat], or 2 hours for caloric supplement [250 calories, eg, protein drink]); do not consume food (except water) for 1 hour after administration. Invert bottle upside down and shake vigorously for ≥30 seconds prior to opening. Administer using the provided calibrated measuring device (5 mL oral syringe); do not use a household teaspoon or tablespoon (overdosage may occur).
Gastrostomy/NG tube: Administer enterally via a silicone, PVC, or polyurethane percutaneous endoscopic gastrostomy or NG tube. Flush tube with at least 30 mL of water before and after administration. Administer on an empty stomach after overnight fasting (8 hours for high-fat meal [800 to 1,000 calories; 50% fat]; 4 hours for a low-fat meal [400 to 500 calories, 25% fat], or 2 hours for caloric supplement [250 calories, eg, protein drink]).
Amyotrophic lateral sclerosis: Treatment of amyotrophic lateral sclerosis (ALS)
None known.
There are no known significant interactions.
A high-fat meal decreased Cmax and AUC by 82% and 61%, respectively, compared to the fasted state. Management: Must be taken on an empty stomach following fasting schedule.
Adverse events were observed in some animal reproduction studies.
It is not known if edaravone is present in breast milk. According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
Hypersensitivity reactions
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).
Absorption: Oral: Cmax decreased by 82% and AUC decreased by 61% when administered with a high-fat meal compared to fasted conditions; following administration 4 hours after a high-fat meal, Cmax decreased by 44% and AUC decreased by 24%; following administration 2 hours after a low-fat meal, Cmax decreased by 45% and AUC decreased by 21%.
Protein binding: 92% (mainly albumin).
Distribution: Vd: IV: 63.1 L.
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.
Bioavailability: Oral: 57%.
Half-life elimination: ~4.5 to 9 hours.
Time to peak: IV: 1 hour; Oral: 0.5 hours (range: 0.25 to 0.75 hours).
Excretion: Urine (60% to 80% as glucuronide conjugate; 6% to 8% as sulfate conjugate; ≤1% unchanged).
Altered kidney function: Following a single 30 mg IV infusion, mean Cmax and AUC0-∞ of unchanged edaravone were 1.15- and 1.20-fold greater in subjects with mild impairment (eGFR 60 to 89 mL/minute/1.73 m2), and 1.25- and 1.29-fold greater in subjects with moderate impairment (eGFR 30 to 59 mL/minute/1.73 m2) when compared to subjects with normal renal function, respectively.
Hepatic function impairment: Following a single 30 mg IV infusion, mean Cmax and AUC0-∞ of unchanged edaravone were 1.20- and 1.07-fold greater in the subjects with mild impairment (Child-Pugh score 5 or 6), 1.24- and 1.14-fold greater in subjects with moderate impairment (Child-Pugh score 7 to 9), and 1.20- and 1.19-fold greater in the subjects with severe impairment (Child-Pugh score 10 to 14) when compared to subjects with normal hepatic function, respectively.
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