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Radicava

Last reviewed on RxList: 3/29/2021
Radicava Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

What Is Radicava?

Radicava (edaravone injection) is an intravenous medication indicated for the treatment of amyotrophic lateral sclerosis (ALS).

What Are Side Effects of Radicava?

Common side effects of Radicava include:

Patients whoto are sensitive to sulfites may have an allergic reaction, including anaphylaxis, to Radicava, which contains sodium bisulfite.

Dosage for Radicava

The recommended dosage of Radicava is 60 mg administered as an intravenous infusion over 60 minutes as follows: Initial treatment cycle: daily dosing for 14 days followed by a 14-day drug-free period. Subsequent treatment cycles: daily dosing for 10 days out of 14-day periods, followed by 14-day drug-free periods.

What Drugs, Substances, or Supplements Interact with Radicava?

Radicava may interact with other drugs.

Tell your doctor all medications and supplements you use.

Radicava During Pregnancy and Breastfeeding

Tell your doctor if you are pregnant or plan to become pregnant before using Radicava; it may harm a fetus. It is unknown if Radicava passes into breast milk. Consult your doctor before breastfeeding.

Additional Information

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Our Radicava (edaravone injection) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

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Radicava Consumer Information

Edaravone can cause serious allergic reactions. The symptoms may not appear until after your IV infusion is finished.

Get emergency medical help if you have signs of an allergic reaction: hives, itching; wheezing, difficult breathing; feeling light-headed; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • bronchospasm (wheezing, chest tightness, trouble breathing); or
  • a light-headed feeling, like you might pass out.

Common side effects may include:

  • bruising;
  • headache; or
  • trouble walking.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Radicava (Edaravone Injection)

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The abbreviated term ADHD denotes the condition commonly known as: See Answer
Radicava Professional Information

CLINICAL PHARMACOLOGY

Mechanism Of Action

The mechanism by which RADICAVA exerts its therapeutic effect in patients with ALS is unknown.

Pharmacokinetics

RADICAVA is administered by IV infusion. The maximum plasma concentration (Cmax) 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 Cmax of edaravone. With multiple-dose administration, edaravone does not accumulate in plasma.

Distribution

Edaravone is bound to human serum proteins (92%), mainly to albumin, with no concentration dependence in the range of 0.1 to 50 micromol/L.

Elimination

The mean terminal elimination half-life of edaravone is 4.5 to 6 hours. The half-lives of its metabolites are 2 to 2.8 hours.

Metabolism

Edaravone is metabolized to a sulfate conjugate and a glucuronide conjugate, which are not pharmacologically active. The glucuronide conjugation of edaravone involves multiple uridine diphosphate glucuronosyltransferase (UGT) isoforms (UGT1A6, UGT1A9, UGT2B7, and UGT2B17) in the liver and kidney. In human plasma, edaravone is mainly detected as the sulfate conjugate, which is presumed to be formed by sulfotransferases.

Excretion

In Japanese and Caucasian healthy volunteer studies, edaravone was excreted mainly in the urine as its glucuronide conjugate form (70-90% of the dose). Approximately 5-10% of the dose was recovered in the urine as sulfate conjugate, and only 1% of the dose or less was recovered in the urine as unchanged form. In vitro studies suggest that sulfate conjugate of edaravone is hydrolyzed back to edaravone, which is then converted to the glucuronide conjugate in the human kidney before excretion into the urine.

Specific Populations

Geriatric Patients

No age effect on edaravone pharmacokinetics has been found [see Use In Specific Populations].

Patients With Renal And Hepatic Impairment

No pharmacokinetic data are available in patients with renal impairment or hepatic impairment [see Use In Specific Populations].

Male And Female Patients

No gender effect on edaravone pharmacokinetics has been found.

Racial Or Ethnic Groups

There were no significant racial differences in Cmax and AUC of edaravone between Japanese and Caucasian subjects.

Drug Interaction Studies

The pharmacokinetics of edaravone is not expected to be significantly affected by inhibitors of CYP enzymes, UGTs, or major transporters.

In vitro studies demonstrated that, at clinical dose, edaravone and its metabolites are not expected to significantly inhibit cytochrome P450 enzymes (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP3A4), UGT1A1, UGT2B7, or transporters (P-gp, BCRP, OATP1B1, OATP1B3, OAT1, OAT3, and OCT2) in humans. Edaravone and its metabolites are not expected to induce CYP1A2, CYP2B6, or CYP3A4 at the clinical dose level of RADICAVA.

Clinical Studies

The efficacy of RADICAVA for the treatment of ALS was established in a 6-month, randomized, placebo-controlled, double-blind study conducted in Japanese patients with ALS who were living independently and met the following criteria at screening:

  1. Functionality retained most activities of daily living (defined as scores of 2 points or better on each individual item of the ALS Functional Rating Scale – Revised [ALSFRS-R; described below])
  2. Normal respiratory function (defined as percent-predicted forced vital capacity values of [%FVC] ≥ 80%)
  3. Definite or Probable ALS based on El Escorial revised criteria
  4. Disease duration of 2 years or less

The study enrolled 69 patients in the RADICAVA arm and 68 in the placebo arm. Baseline characteristics were similar between these groups, with over 90% of patients in each group being treated with riluzole.

RADICAVA was administered as an intravenous infusion of 60 mg given over a 60 minute period according to the following schedule:

  • An initial treatment cycle with daily dosing for 14 days, followed by a 14-day drug-free period (Cycle 1)
  • Subsequent treatment cycles with daily dosing for 10 days out of 14-day periods, followed by 14-day drug-free periods (Cycles 2-6).

The primary efficacy endpoint was a comparison of the change between treatment arms in the ALSFRS-R total scores from baseline to Week 24. The ALSFRS-R scale consists of 12 questions that evaluate the fine motor, gross motor, bulbar, and respiratory function of patients with ALS (speech, salivation, swallowing, handwriting, cutting food, dressing/hygiene, turning in bed, walking, climbing stairs, dyspnea, orthopnea, and respiratory insufficiency). Each item is scored from 0-4, with higher scores representing greater functional ability. The decline in ALSFRS-R scores from baseline was significantly less in the RADICAVA-treated patients as compared to placebo (see Table 2). The distribution of change in ALSFRS-R scores from baseline to Week 24 by percent of patients is shown in Figure 1.

Table 2: Analysis of Change from Baseline to Week 24 in ALSFRS-R Scores

Treatment Change from Baseline LS Mean ± SE (95% CI) Treatment Difference (RADICAVA - placebo [95% CI]) P- value
RADICAVA 60mg -5.01 ± 0.64 2.49 (0.99, 3.98) 0.0013
Placebo -7.50 ± 0.66

Figure 1: Distribution of Change from Baseline to Week 24 in ALSFRS-R Scores

Distribution of
Change from Baseline to Week 24 in ALSFRS-R Scores - Illustration

Read the entire FDA prescribing information for Radicava (Edaravone Injection)

Related Resources for Radicava

© Radicava Patient Information is supplied by Cerner Multum, Inc. and Radicava Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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