Edaravone
Edaravone Uses, Dosage, Side Effects, Food Interaction and all others data.
Edaravone is a free radical scavenger approved in May, 2017 for the treatment of amyotrophic lateral scleorosis (ALS). Clinical studies showed that the treatment attenuated deterioration of the disease when compared to placebo. It has been previously investigated for the treatment of ischemic stroke, reperfusion Injury, and myocardial Infarction as it possesses antioxidant and anti-apoptotic properties. Being a low molecular weight molecule with good water and lipid-soluble properies, it is therapeutically advantageous in crossing the blood-brain barrier to mediate nootropic and neuroprotective effects. Oral formulation of edaravone is currently under development.
Edaravone scavenges free hydroxyl radicals and peroxynitrite radicals which are highly associated with neuronal damage/death from many cerebral vascular disorders such as ischemic strokes and degenerative neurological disorders such as ALS. It exerts a neuroprotective and antioxidant effect and delays disease progression by limiting the extent of lipid peroxidation via free radical generation and cell membrane damage from oxidative stress. It reversed the reduction in regional blood flow and cerebral edema in a case of ischemic stroke.
| Trade Name | Edaravone |
| Availability | Prescription only |
| Generic | Edaravone |
| Edaravone Other Names | Edaravone, Methylphenylpyrazolone, Norphenazone, Phenyl methyl pyrazolone, Phenylmethylpyrazolone |
| Related Drugs | riluzole, Radicava, Radicava ORS, Rilutek, Exservan, Tiglutik |
| Weight | 30mg/100ml, |
| Type | Intravenous Solution, Intravenous |
| Formula | C10H10N2O |
| Weight | Average: 174.203 Monoisotopic: 174.07931295 |
| Protein binding | The in vitro binding rates of edaravone to human serum protein and albumin are 92% and 89-91%, respectively, with no concentration-dependence. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Edaravone is a free radical scavenger used to delay the progression of ALS.
Indicated for improving neurological symptoms and damage from acute ischemic stroke and delaying disease progression of ALS.
Edaravone is also used to associated treatment for these conditions: Amyotrophic Lateral Sclerosis (ALS)
How Edaravone works
Nootropic and neuroprotective effects are mediated through inhibiting lipid peroxidation and scavenging free radicals. Edaravone acts to increase prostacyclin production, decrease lipoxygenase metabolism of arachidonic acid by trapping hydroxyl radicals, and inhibit alloxan-induced lipid peroxidation and quench active oxygen species. It targets various kinds of cells, including neurons, endothelial cells and myocardial cells . There is also evidence of reduction of neuronal nitric oxide synthase (nNOS) levels and potentiation of SOD1 levels after transient ischemia in rabbits thus preventing spinal cord injury.
Toxicity
No reported evidence of carcinogenic, mutagenic or teratogenic potential. Oral LD50 value is 1,915 mg/kg (Rat). Adverse effects include rashes, hypertension, altered hepatic function, and acute renal impairment. Hematological abnormalities, lung injury and rhabomyolysis may occur with no known incidences.
Food Interaction
No interactions found.Volume of Distribution
The mean Vd value following an intravenous infusion of a single 30mg dose is 18.5L/kg .
Elimination Route
The peak plasma concentration of the parent drug is reached at the end of infusion, without accumulation of the drug with multiple dosing regimen. The mean Cmax value in healthy male adults is 888ng/mL for intravenous infusion. The values of AUC and Cmax are increased in a dose-proportional relationship. The oral bioavailability in mouse studies is 38% of the I.V. delivery .
Half Life
The mean terminal elimination half-life of edaravone is 4.5 to 6 hours and the half-lives of its metabolites are 2 to 2.8 hours.
Clearance
The mean total plasma drug clearance following an intravenous infusion of a single 30mg dose is 0.1L/min .
Elimination Route
About 0.7-0.9% of the dose is excreted as unchanged drug and 71.0-79.9% of the dose is excreted as metabolites (mostly as glucuronide conjugates) through mainly renal elimination.
Innovators Monograph
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