Neurophazol (Concentrate) Instructions for Use

Marketing Authorization Holder

Lekko, CJS (Russia)

ATC Code

N05BX04 (Fabomotizole)

Active Substance

Fabomotizole (Rec.INN WHO registered)

Dosage Form

Neurophazol

Concentrate for solution for infusion 10 mg/2 ml: vial 10 pcs.

Dosage Form, Packaging, and Composition

2 ml – dark glass vials (1) – plastic contour packs (5) – cardboard packs.

Clinical-Pharmacological Group

Anxiolytic (tranquilizer)

Pharmacotherapeutic Group

Anxiolytic agent (tranquilizer)

Pharmacological Action

Neurophazol has neuroprotective properties.

The mechanism of action of Neurophazol is due to interaction with sigma₁ receptors, through which the restoration of the phospholipid framework of cell surface receptor structures is carried out; normalization of calcium balance; counteraction to glutamate excitotoxicity and increased production of nitric oxide; restoration of the deficiency of nerve growth factors.

Neurophazol increases neuronal survival and reduces the severity of cytotoxic reactions during damaging effects of oxidative stress and glutamate, normalizes the level of caspase-3, one of the main enzymes activated during apoptosis.

The drug has a stimulating effect on the formation of brain neurotrophic factors – NGF (nerve growth factor) and BDNF (brain-derived neurotrophic factor).

The drug has a protective effect on cells of the penumbra zone under conditions of local ischemia, reduces the severity of post-stroke disorders and accelerates the recovery of neurological functions.

In cerebral ischemia, Neurophazol suppresses the NO-synthase pathway of nitric oxide formation in brain neurons and prevents an increase in NO-synthase activity.

It causes improvement in energy metabolism by restoring succinate dehydrogenase activity during cerebral ischemia.

Promotes an increase in cerebral blood flow under ischemic conditions without affecting systemic blood pressure.

The involvement of the GABAergic system in the implementation of the cerebrovascular and neuroprotective action of the drug has been established.

Pharmacokinetics

T_1/2 of Neurophazol is 0.82 hours.

The elimination rate constant from blood plasma is 2.12 h^-1.

The concentration of the drug in blood plasma increases proportionally to the increase in the dose of Neurophazol.

After IV administration, it is rapidly taken up by cells of various organs and tissues.

Penetrates well through the blood-brain barrier.

According to experimental data, it undergoes intensive metabolism in the liver.

It is excreted from the body mainly in the form of metabolites.

24 hours after administration, 0.07% is registered in the urine and 0.05% in the feces in unchanged form from the administered dose.

Indications

• Cerebral infarction (ischemic stroke).

ICD codes

Dosage Regimen

Administer Neurophazol exclusively as an intravenous drip infusion.

Prepare the infusion by diluting the contents of one 10 mg vial in 150-200 ml of a 0.9% sodium chloride solution.

Infuse the prepared solution at a rate of 40-60 drops per minute.

The standard dosage is 10 mg, administered twice daily.

Maintain a minimum interval of 8 hours between consecutive infusions.

Initiate therapy within the first 6 hours from the onset of ischemic stroke symptoms.

Continue treatment for a total duration of 10 days.

Do not administer the drug via bolus intravenous injection.

Inspect the solution visually for particulate matter or discoloration prior to administration; do not use if present.

Use the prepared infusion solution immediately; do not store.

Adverse Reactions

Headache, dizziness, and general weakness may develop, which are short-term in nature and resolve on their own.

Allergic reactions are possible.

According to the results of clinical studies, a single case of paroxysmal atrial fibrillation was recorded (the relationship with taking the drug has not been established).

Contraindications

• Pregnancy;
• Lactation period;
• Age under 18 years;
• Hypersensitivity to the components of the drug,

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Pediatric Use

Contraindicated under the age of 18 years.

Overdose

Exceeding the daily dose may result in the appearance of a sedative effect and increased drowsiness.

Sodium caffeine benzoate (caffeine) 20% solution in 1 ml ampoules 2-3 times/day subcutaneously is used as emergency care.

Drug Interactions

Neurophazol can be used in combination with acetylsalicylic acid, enalapril, indapamide, atenolol, nifedipine, digoxin, rheopolyglucin dextran.

It does not affect the narcotic effect of ethanol or the hypnotic effect of thiopental.

It potentiates the anticonvulsant effect of carbamazepine.

It causes an enhancement of the anxiolytic effect of diazepam.

Storage Conditions

Store in a place protected from light, at a temperature from 0°C (32°F) to 25°C (77°F).

Do not freeze.

Keep out of the reach of children.

Shelf Life

Shelf life – 2 years. Do not use after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.