MEXellara^® (Solution) Instructions for Use

Marketing Authorization Holder

Ellara, LLC (Russia)

ATC Code

N07XX (Other drugs for the treatment of nervous system diseases)

Active Substance

Ethylmethylhydroxypyridine succinate (Grouping name)

Dosage Form

MEXellara®

Solution for intravenous and intramuscular administration 50 mg/1 ml: 2 ml or 5 ml ampoules, 5, 10, 20, or 25 pcs.

Dosage Form, Packaging, and Composition

Solution for intravenous and intramuscular administration transparent, colorless or slightly yellowish.

Excipients: potassium metabisulfite (potassium disulfite) – 1 mg, water for injection – up to 1 ml.

2 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packaging (4) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packaging (5) – cardboard packs.
2 ml – glass ampoules (5) – cardboard packs.
2 ml – glass ampoules (10) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (4) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (5) – cardboard packs.
5 ml – glass ampoules (5) – cardboard packs.
5 ml – glass ampoules (10) – cardboard packs.

Clinical-Pharmacological Group

Antioxidant drug

Pharmacotherapeutic Group

Other agents for the treatment of nervous system diseases

Pharmacological Action

Free radical process inhibitor – a membrane protector that also has antihypoxic, stress-protective, nootropic, antiepileptic, and anxiolytic effects. Belongs to the class of 3-oxypyridines.

The mechanism of action is due to antioxidant and membrane-protective properties. It suppresses lipid peroxidation, increases superoxide dismutase activity, improves the lipid-protein ratio, and improves the structure and function of cell membranes.

It modulates the activity of membrane-bound enzymes (Ca²⁺-independent PDE, adenylate cyclase, acetylcholinesterase), receptor complexes (benzodiazepine, GABA, acetylcholine), which promotes their binding to ligands, preservation of the structural and functional organization of biomembranes, neurotransmitter transport, and improvement of synaptic transmission. It increases the concentration of dopamine in the brain.

It enhances the compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions with an increase in ATP and creatine phosphate, activating the energy-synthesizing function of mitochondria.

It increases the body’s resistance to the effects of various damaging factors in pathological conditions (shock, hypoxia and ischemia, cerebrovascular accidents, ethanol intoxication, and antipsychotic drugs).

It improves the metabolism and blood supply to the brain, microcirculation and rheological properties of blood, and reduces platelet aggregation. It stabilizes the membranes of blood cells (erythrocytes and platelets), reducing the likelihood of hemolysis.

It has a hypolipidemic effect, reducing the content of total cholesterol and LDL.

It improves the functional state of the ischemic myocardium in myocardial infarction, the contractile function of the heart, and also reduces the manifestations of systolic and diastolic dysfunction of the left ventricle.

Under conditions of a critical decrease in coronary blood flow, it helps to preserve the structural and functional organization of cardiomyocyte membranes, stimulates the activity of membrane enzymes – PDE, adenylate cyclase, acetylcholinesterase.

It maintains the developing activation of aerobic glycolysis during acute ischemia and promotes the restoration of mitochondrial redox processes under hypoxic conditions, increases the synthesis of ATP and creatine phosphate. It ensures the integrity of the morphological structures and physiological functions of the ischemic myocardium.

It improves the clinical course of myocardial infarction, increases the effectiveness of the therapy, accelerates the recovery of the functional activity of the left ventricular myocardium, and reduces the frequency of arrhythmias and intracardiac conduction disturbances.

It normalizes metabolic processes in the ischemic myocardium, reduces the necrosis zone, restores and/or improves the electrical activity and contractility of the myocardium, and also increases coronary blood flow in the ischemia zone, enhances the antianginal activity of nitro drugs, improves the rheological properties of blood, and reduces the consequences of reperfusion syndrome in acute coronary insufficiency.

It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

Pharmacokinetics

Rapidly absorbed when taken orally (half-absorption period – 0.08-1 h). T_max with intramuscular administration – 0.3-0.58 h, when taken orally – 0.46-0.5 h. C_max with intramuscular administration at a dose of 400-500 mg – 2.5-4 µg/ml, when taken orally – 50-100 ng/ml.

Rapidly distributed in organs and tissues. The mean residence time of the drug in the body with intramuscular administration is 0.7-1.3 h, when taken orally – 4.9-5.2 h.

Metabolized in the liver by glucuronidation. Five metabolites have been identified: 3-oxypyridine phosphate – formed in the liver and, with the participation of alkaline phosphatase, breaks down into phosphoric acid and 3-oxypyridine; the 2nd metabolite is pharmacologically active, formed in large quantities and detected in urine 1-2 days after administration; the 3rd is excreted in large quantities in the urine; the 4th and 5th are glucuronoconjugates.

T_1/2 when taken orally – 4.7-5 h. Rapidly excreted in the urine mainly in the form of metabolites (50% within 12 h) and in small amounts – unchanged (0.3% within 12 h). It is most intensively excreted during the first 4 hours after taking the drug. The indicators of excretion of the unchanged drug and metabolites in the urine have significant individual variability.

Indications

Anxiety disorders in neurotic and neurosis-like conditions; vegetative-vascular dystonia; dyscirculatory encephalopathy; mild cognitive disorders of atherosclerotic origin.

Acute cerebrovascular accidents (as part of combination therapy).

Withdrawal syndrome in alcoholism with a predominance of neurosis-like and vegetative-vascular disorders; acute intoxication with antipsychotic drugs.

Acute purulent-inflammatory processes in the abdominal cavity (including acute necrotizing pancreatitis, peritonitis (as part of complex therapy));

Acute myocardial infarction from the first days (parenterally); Coronary artery disease; complex therapy of ischemic stroke (orally) – as part of complex therapy.

ICD codes

Dosage Regimen

Determine the dose, route of administration, and treatment duration individually based on the specific indication and clinical presentation.

For intravenous administration, inject the solution as a slow stream or infusion. Dilute the required dose in 0.9% sodium chloride solution or 5% dextrose solution to a volume of 100-150 ml. Administer the infusion at a rate of 40-60 drops per minute.

For intramuscular administration, inject the solution deeply. The typical single dose ranges from 50 mg to 400 mg.

Administer the drug two to three times daily. Do not exceed the maximum daily dose of 1200 mg.

For acute cerebrovascular accidents, use a dose of 200-500 mg intravenously drip for the first 10-14 days, then switch to intramuscular administration.

For anxiety disorders and withdrawal syndrome, use a dose of 100-300 mg per day via intramuscular or intravenous routes for a treatment course of 2-4 weeks.

For acute myocardial infarction, administer 200-300 mg daily via intramuscular injection as part of complex therapy.

For oral administration, use a daily dose of 0.25-0.5 grams divided into 2-3 doses. The maximum oral daily dose is 0.6-0.8 grams.

The standard duration of parenteral therapy is typically 10-14 days, followed by a transition to oral administration if continued treatment is required.

Adverse Reactions

When taken orally nausea, dry mouth, diarrhea, drowsiness, allergic reactions.

With parenteral administration (especially intravenous bolus) dryness, “metallic” taste in the mouth, sensations of “spreading warmth” throughout the body, unpleasant odor, sore throat and discomfort in the chest, feeling of lack of air (usually associated with an excessively high rate of administration and are short-term); with prolonged use – nausea, flatulence; sleep disorders (drowsiness or difficulty falling asleep).

Contraindications

Hypersensitivity; acute hepatic and/or renal failure; pregnancy; lactation period; childhood.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Contraindication: acute hepatic failure.

Use in Renal Impairment

Contraindication: acute renal failure.

Pediatric Use

The drug is contraindicated for use in children and adolescents under 18 years of age.

Special Precautions

Use with caution in patients with a history of allergic diseases.

During treatment, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Enhances the effect of benzodiazepine anxiolytics, antiepileptic (carbamazepine), antiparkinsonian (levodopa) drugs, nitrates.

Reduces the toxic effects of ethanol.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.