excipients: sodium metabisulfite (E 223), sodium chloride, sodium hydroxide, phosphoric acid, water for injections.
Dosage form. Injection.
Main physicochemical properties: clear colorless or slightly yellowish liquid.
Pharmacotherapeutic group. Other drugs for the treatment of diseases of the central nervous system. ATX N07 XX.
Pharmacological properties.
Pharmacodynamics.
Among the major factors in cerebrovascular disease associated with ischemia are free radicals such as hydroxyl radicals (OH); with ischemia or bleeding during recovery of accuracy due to an abnormal increase in arachidonic acid production, the amount of free radicals produced increases. These free radicals lead to peroxidation of unsaturated fatty acids that make up the lipids of cell membranes and damage them, leading to brain dysfunction.
In the acute phase of cerebral ischemic infarction, the drug has a protective effect that suppresses the onset and development of ischemic cerebrovascular diseases such as brain tumors, neurological symptoms and slow neuronal death.
The etiology of the onset and development of amyotrophic lateral sclerosis (ALS) has not yet been fully elucidated. However, it has been suggested that oxidative stress caused by free radicals may be an etiological factor of this pathology. Edaravone inhibits the development of the disease by reducing oxidative damage to brain cells (vascular endothelial cells / nerve cells) due to its inhibitory effect on lipid peroxidation by binding free radicals.
Pharmacokinetics.
Pharmacokinetics of the drug in 5 healthy male volunteers and five healthy male volunteers in the elderly
the dose of the drug (0,5 mg / kg) was studied twice a day for 2 days, 30 minutes after repeated administration. In both groups, the unchanged drug concentration in the blood plasma decreased equally without traces of accumulation.
Pharmacokinetic parameters
Healthy volunteers (n = 5)
Summer volunteer health (n = 5)
Maximum (ng / ml)
888 171 ±
1041 106 ±
ta (d)
0,27 0,11 ±
0,17 0,03 ±
t ½ b (d)
2.27 0.80 ±
1,84 0,17 ±
The binding rate of edaravon to serum proteins and serum albumins is 92% and 89-91%, respectively (in vitro).
Sulfate conjugates in blood plasma are the major metabolites of edaravone; glucuronic acid conjugates were also found. Most of the urine was found to contain glucuronides and to a lesser extent sulfates.
12 hours after administration, 0,7-0,9% of the drug is excreted unchanged in the urine and 71,0-79,9% is excreted as metabolites.
Instructions for use.
Relief of neurological symptoms, manifestations of impaired activity in daily life, and functional disorders associated with acute ischemic stroke.
Slowing down the development of functional disorders in patients with amyotrophic lateral sclerosis.
Contraindications.
Severe renal failure.
Hypersensitivity to the components of the drug.
Interactions with other drugs and other types of interactions.
Concomitant use of antibiotics with renal type (cefazolin sodium, cefotiam hydrochloride, sodium pyperatsillin, etc.) may increase the risk of renal dysfunction, if used in combination, you should regularly analyze and monitor its performance. kidneys.
Before use, Havron should be dissolved in 100 ml of physiological sodium chloride solution. Mixing the drug with intravenous solutions containing various sugars may lead to a decrease in the concentration of edaravon.
The drug should not be mixed with solutions for parenteral nutrition and / or solutions containing amino acids, as well as administered through the same infusion systems.
Do not mix the drug with anticonvulsants, including diazepam, sodium phenytoin, etc., due to the possibility of turbidity. Also, do not mix with potassium carrenoate.
Method of administration and dosage.
Neurological symptoms associated with acute ischemic stroke, manifestations of daily dysfunction, elimination of various types of dysfunction: 30 mg edaravon (1 ampoule) twice a day, morning and evening, intravenous administration for 30 minutes. Before use, the contents of the ampoule should be dissolved in 100 ml of 0,9% sodium chloride. Therapy should be started within 24 hours after the onset of symptoms, the duration of treatment is at least 14 days.
Inhibitory effect on the development of amyotrophic lateral sclerosis (ALS) dysfunction: 60 mg edaravon (2 ampoules) by intravenous administration for 60 minutes, 1 time per day. Before use, the contents of the ampoule should be dissolved in an amount of 0,9% sodium chloride. As a rule, the duration of medication and the rest period is a total of 28 days and is considered 1 course, such courses are repeated. The first course consists of 14 days of drug administration, followed by a 14-day break and rest, the second course and subsequent courses consist of 10 days of 14-day medication, followed by a 14-day break. starts.
In patients with acute ischemic stroke, the duration of therapy may be shortened depending on the clinical condition of the patient.
Elderly patients.
Because physiological functions are usually reduced in elderly patients, the drug should be discontinued and appropriate precautions taken when adverse effects occur. There are many published examples showing that elderly patients often lead to death, so monitoring should be especially careful.
Children. The safety of the drug in children has not been established.
Experience with acute ischemic stroke in children is insufficient; There is no clinical experience with children in ALS.
Adverse reactions.
From the urinary system: acute renal failure, nephrotic syndrome.
On the skin: rash, redness, swelling, itching, erythema.
From the hepatobiliary system: impaired liver function, liver failure, fulminant hepatitis, jaundice.
From the nervous system: insomnia, headache.
By the cardiovascular system: an increase in blood pressure. From the gastrointestinal tract: nausea, vomiting. From the musculoskeletal system: rhabdomyolysis. From the immune system: shock, anaphylactic shock (urticaria, hypotension, shortness of breath, etc.).
