Mexidant^® (Solution) Instructions for Use

Marketing Authorization Holder

CV FMT Mexidant, LLC (Russia)

Manufactured By

Altair LLC (Russia)

Or

Experimental Production of MBP RK NPC (Russia)

Contact Information

CV FMT MEKSIDANT LLC (Russia)

ATC Code

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

Active Substance

Ethylmethylhydroxypyridine succinate

Dosage Forms

	Mexidant®	Solution for intravenous and intramuscular administration 50 mg/1 ml: amp. 5 or 10 pcs.
		Solution for intravenous and intramuscular administration 100 mg/2 ml: amp. 5 or 10 pcs.
		Solution for intravenous and intramuscular administration 250 mg/5 ml: amp. 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for IV and IM administration transparent, practically colorless or slightly colored.

Excipients: water for injections.

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

Solution for IV and IM administration transparent, practically colorless or slightly colored.

Excipients: water for injections.

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

Solution for IV and IM administration transparent, practically colorless or slightly colored.

Excipients: water for injections.

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

Clinical-Pharmacological Group

Antioxidant drug

Pharmacotherapeutic Group

Antioxidant agent

Pharmacological Action

Mexidant^® is an antioxidant drug. It belongs to the class of 3-oxypyridines. It has antioxidant, antihypoxic, membrane-stabilizing, nootropic, and anxiolytic effects. The drug inhibits lipid peroxidation processes, increases the activity of the antioxidant enzyme system (superoxide dismutase, catalase, peroxidase), restores impaired membrane structure and functions, has a modulating effect on calcium and potassium ion channels, neurotransmitter transport, and improves synaptic transmission.

The drug increases the body’s resistance to the effects of various damaging factors (shock, hypoxia, ischemia, trauma, cerebrovascular accidents) by activating the energy-synthesizing functions of mitochondria and improving energy metabolism in the cell.

The mechanism of action is due to the ability to enhance compensatory activation of aerobic glycolysis, reduce the degree of inhibition of oxidative processes in the Krebs cycle under hypoxia with an increase in ATP and creatine phosphate content and stabilization of cell membranes.

Mexidant^® improves and stabilizes the metabolism and blood supply to the brain, improves the rheological properties of blood, and suppresses platelet aggregation. It has a modulating effect on the atrombogenic properties of the vascular wall endothelium and contributes to the improvement of brain perfusion characteristics.

Against the background of Mexidant^® administration, memory and performance improve. Mexidant^® has an anxiolytic effect, eliminating anxiety, fear, tension, and restlessness. It has a hypolipidemic effect, reducing the level of total cholesterol and LDL.

Pharmacokinetics

With single and course administration of Mexidant^®, C_max in blood plasma is reached after 0.58 hours. When administered at a dose of 400-500 mg, C_max in blood plasma is 3.5-4 µg/ml. It is rapidly distributed in organs and tissues. The mean residence time of the drug is 0.7-1.3 hours. At the same time, it is rapidly eliminated from the blood plasma and after 4 hours is practically undetectable in it.

Pharmacokinetic profiles do not differ significantly with both single and constant administration. It is excreted in the urine, both unchanged and in the form of glucuronoconjugates. Five metabolites have been identified: the 1st metabolite, 3-oxypyridine phosphate, is formed in the liver, which in the blood under the influence of alkaline phosphatase breaks down into phosphoric acid and 3-oxypyridine; the 2nd metabolite is formed in large quantities and is detected in the urine on days 1-2 of drug administration, it is pharmacologically active; the 3rd metabolite is also excreted in large quantities in the urine; the 4th and 5th metabolites are glucuronoconjugates.

Indications

As part of complex therapy for

• Acute cerebrovascular accident;
• Traumatic brain injury;
• Dyscirculatory encephalopathy;
• Vegetative-vascular dystonia;
• Neurotic disorders with anxiety syndrome;
• Intellectual-mnestic disorders of various origins (including memory impairment in the elderly);
• Relief of withdrawal syndrome in alcoholism with the presence of neurotic and vegetative-vascular disorders in the clinical picture.

ICD codes

Dosage Regimen

Mexidant^® is prescribed as part of complex therapy intramuscularly or intravenously (bolus or drip). Doses are selected individually. Treatment begins with the drug at a dose of 50-100 mg 1-3 times/day, gradually increasing the dose until a therapeutic effect is obtained. The duration of treatment and the choice of individual dose depend on the severity of the patient’s condition and the effectiveness of treatment. The maximum daily dose is 800 mg.

Bolus Mexidant^® is administered over 5-7 minutes. For infusion administration, the drug is diluted in 200 ml of physiological 0.9% sodium chloride solution and administered drip-wise at a rate of 60 drops/min.

For the treatment of acute cerebrovascular accident, Mexidant^® is prescribed in the first 7-8 days at a dose of 200-300 mg once/day IV (drip), and then IM – 100 mg 3 times/day.

For traumatic lesions of the CNS, Mexidant^® is administered IV (drip) at a dose of 400-600 mg/day for 7-8 days, followed by IM administration of 300 mg/day for 10-14 days.

For dyscirculatory encephalopathy in the decompensation phase, Mexidant^® is prescribed IV bolus or drip at a dose of 100 mg once/day for 14 days. Then the drug is administered IM at 100 mg 2-3 times/day for the next 14 days.

For the prevention of dyscirculatory encephalopathy, Mexidant^® is administered IM at a dose of 100 mg 2 times/day for 10-14 days.

For intellectual-mnestic and cognitive disorders, the drug is prescribed IM at a dose of 100-300 mg/day for 14 days.

For withdrawal syndrome, Mexidant^® is administered at a dose of 100-200 mg IM 2-3 times or IV (drip) 1-2 times/day.

For neurotic disorders and vegetative-vascular dystonia, the drug is prescribed IM at a dose of 50-400 mg/day for 14 days.

Adverse Reactions

From the digestive system: rarely – nausea, dry mouth, diarrhea.

From the CNS: rarely – drowsiness.

Other: possibly – allergic reactions.

With parenteral administration (especially IV 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 in nature); with prolonged use – nausea, flatulence; sleep disorders (drowsiness or difficulty falling asleep).

Contraindications

• Acute impairment of liver and kidney function;
• Pregnancy;
• Lactation period;
• Childhood;
• Hypersensitivity to the drug or intolerance to the drug.

With caution, the drug should be prescribed for a history of allergic diseases.

Use in Pregnancy and Lactation

The use of the drug is contraindicated during pregnancy and lactation.

Special Precautions

Currently, a number of medicinal products with the same active substance – Ethylmethylhydroxypyridine succinate – are being produced, which should be taken into account when conducting therapy for other diseases in the treatment of which medicinal products with this substance may be used.

Influence on the ability to drive vehicles and mechanisms

At the beginning of treatment with the drug, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: sleep disorders (insomnia, in some cases – drowsiness); with IV administration – a slight and short-term (up to 1.5-2 hours) increase in blood pressure.

Treatment: as a rule, is not required, the symptoms disappear on their own within a day. In severe cases with insomnia, the administration of nitrazepam at a dose of 10 mg, or oxazepam (10 mg) or diazepam (5 mg) is indicated. With an excessive increase in blood pressure – antihypertensive therapy under blood pressure control.

Drug Interactions

With combined use, Mexidant^® enhances the effect of anticonvulsants (carbamazepine), tranquilizers (bromdihydrochlorphenylbenzodiazepine, diazepam), antiparkinsonian drugs (levodopa); reduces the toxic effects of ethyl alcohol.

Storage Conditions

List B. The drug should be stored in a place protected from light, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

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.