Edaravone

Brand Names: Radicava Ors

Drug Class: General Prescription

Overview

11 DESCRIPTION The active ingredient in RADICAVA and RADICAVA ORS is edaravone, which is a member of the substituted 2-pyrazolin-5-one class. The chemical name of edaravone is [3-methyl-1-phenyl-2-pyrazolin-5-one]. The molecular formula is C 10 H 10 N 2 O and the molecular weight is 174.20. The chemical structure is: Edaravone is a white crystalline powder with a melting point of 129.7°C.

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism by which RADICAVA and RADICAVA ORS exert their therapeutic effect in patients with ALS is unknown. 12.2 Pharmacodynamics Cardiac Electrophysiology At exposures at least 5 times higher than that of the recommended doses of RADICAVA and RADICAVA ORS, edaravone does not prolong the QT interval to any clinically relevant extent. 12.3 Pharmacokinetics RADICAVA is administered by IV infusion. The maximum plasma concentration (C max ) of edaravone was reached by the end of infusion. There was a trend of more than dose-proportional increase in area under the concentration-time curve (AUC) and C max of edaravone. With multiple-dose administration, edaravone does not accumulate in plasma.

Indications

  • 1 INDICATIONS AND USAGE RADICAVA and RADICAVA ORS are indicated for the treatment of amyotrophic lateral sclerosis (ALS). RADICAVA and RADICAVA ORS are indicated for the treatment of amyotrophic lateral sclerosis (ALS). ( 1 )

Common Doses

  • 60 mg
  • 105 mg
  • 5 mL
  • 30 mg

Dosage

2 DOSAGE AND ADMINISTRATION RADICAVA: The recommended dosage is 60 mg administered as an intravenous infusion over 60 minutes ( 2.1 ) RADICAVA ORS: The recommended dosage is 105 mg (5 mL) taken orally or via feeding tube in the morning after overnight fasting. Food should not be consumed for 1 hour after administration except water ( 2.1 , 2.3 ) For RADICAVA and RADICAVA ORS: Initial treatment cycle: daily dosing for 14 days followed by a 14-day drug-free period ( 2.1 ) Subsequent treatment cycles: daily dosing for 10 days out of 14-day periods, followed by 14-day drug-free periods ( 2.1 ) 2.

Contraindications

  • 4 CONTRAINDICATIONS RADICAVA and RADICAVA ORS are contraindicated in patients with a history of hypersensitivity to edaravone or any of the inactive ingredients in this product. Hypersensitivity reactions and anaphylactic reactions have occurred [see Warnings and Precautions (5.1 , 5.2) ]. Patients with a history of hypersensitivity to edaravone or any of the inactive ingredients in RADICAVA and/or RADICAVA ORS ( 4 )

Side Effects

  • 6 ADVERSE REACTIONS The following serious adverse reactions are described elsewhere in the labeling: Hypersensitivity Reactions [see Warnings and Precautions (5.1) ] Sulfite Allergic Reactions [see Warnings and Precautions (5.2) ] Most common adverse reactions (at least 10% of patients treated with RADICAVA and greater than placebo) are contusion, gait disturbance, and headache ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Shionogi Inc. at 1-888-292-0058 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.

Interactions

  • No major interactions listed on the FDA label. Always consult a healthcare professional.