Ethylmethylhydroxypyridine succinate (Tablets, Solution) Instructions for Use
ATC Code
N07XX (Other drugs for the treatment of nervous system diseases)
Active Substance
Ethylmethylhydroxypyridine succinate
Clinical-Pharmacological Group
Antioxidant drug
Pharmacotherapeutic Group
Other agents for the treatment of nervous system diseases
Pharmacological Action
An inhibitor of free radical processes – a membrane protector, also possessing antihypoxic, stress-protective, nootropic, antiepileptic, and anxiolytic effects. Belongs to the class of 3-oxypyridines.
The mechanism of action is due to its antioxidant and membrane-protective properties. It suppresses lipid peroxidation, increases the activity of superoxide dismutase, improves the lipid-protein ratio, and enhances the structure and function of cell membranes. It modulates the activity of membrane-bound enzymes (Ca2+-independent PDE, adenylate cyclase, acetylcholinesterase) and receptor complexes (benzodiazepine, GABA, acetylcholine), which promotes their binding to ligands, preserves the structural and functional organization of biomembranes, neurotransmitter transport, and improves 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 disorders, ethanol intoxication, and intoxication with antipsychotic drugs).
It improves 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 preserve the structural and functional organization of cardiomyocyte membranes, stimulating the activity of membrane enzymes – PDE, adenylate cyclase, acetylcholinesterase. It maintains the activation of aerobic glycolysis developing during acute ischemia and promotes the restoration of mitochondrial redox processes under hypoxic conditions, increasing 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 incidence 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, increases coronary blood flow in the ischemic 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 after oral administration (half-absorption period – 0.08-1 h). Tmax after IM administration – 0.3-0.58 h, after oral administration – 0.46-0.5 h. Cmax after IM administration at a dose of 400-500 mg – 2.5-4 mcg/ml, after oral administration – 50-100 ng/ml.
Rapidly distributed in organs and tissues. The mean residence time of the drug in the body after IM administration is 0.7-1.3 h, after oral administration – 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 glucuronide conjugates.
T1/2 after oral administration – 4.7-5 h. Rapidly excreted in the urine mainly as metabolites (50% within 12 h) and in small amounts unchanged (0.3% within 12 h). Excretion is most intensive during the first 4 hours after drug administration. The excretion parameters of the unchanged drug and metabolites 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 autonomic-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
| ICD-10 code | Indication |
| F07 | Personality and behavioral disorders due to disease, damage or dysfunction of the brain |
| F10.3 | Withdrawal state |
| F45.3 | Somatoform dysfunction of the autonomic nervous system |
| F48.0 | Neurasthenia |
| F48.9 | Unspecified neurotic disorder |
| G93.4 | Unspecified encephalopathy |
| I20 | Angina pectoris |
| I21 | Acute myocardial infarction |
| I61 | Intracerebral hemorrhage (cerebrovascular accident of hemorrhagic type) |
| I63 | Cerebral infarction |
| I67.2 | Cerebral atherosclerosis |
| K65.0 | Acute peritonitis (including abscess) |
| K85 | Acute pancreatitis |
| T43 | Poisoning by psychotropic drugs, not elsewhere classified |
| ICD-11 code | Indication |
| 6A8Z | Affective disorders, unspecified |
| 6B6Z | Dissociative disorders, unspecified |
| 6C20.Z | Bodily distress disorder, unspecified |
| 6C40.4Z | Alcohol withdrawal syndrome, unspecified |
| 6E68 | Secondary emotionally labile personality disorder |
| 6E6Z | Unspecified secondary mental or behavioral syndromes |
| 8B00.Z | Intracerebral hemorrhage of unspecified site, unspecified |
| 8B11 | Cerebral ischemic stroke |
| 8E47 | Encephalopathy, not elsewhere classified |
| 8E4A.0 | Paraneoplastic or autoimmune disorders of the central nervous system, including brain and spinal cord |
| 8E63 | Post-cardiopulmonary bypass encephalopathy |
| BA40.Z | Angina pectoris, unspecified |
| BA41.Z | Acute myocardial infarction, unspecified |
| BD55 | Asymptomatic stenosis of intracranial or extracranial artery |
| DC31.Z | Acute pancreatitis, unspecified |
| DC50.0 | Primary peritonitis |
| DC50.2 | Peritoneal abscess |
| DC50.Z | Peritonitis, unspecified |
| NE60 | Poisoning by drugs, medicaments or biological substances, not elsewhere classified |
Dosage Regimen
| The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen. |
Determine the dose, frequency, and duration of therapy individually based on the specific indication and clinical presentation.
For oral administration using tablets, administer a total daily dose of 250 mg to 500 mg.
Divide the total daily dose into two or three separate administrations.
Do not exceed the maximum daily oral dose of 600 mg to 800 mg.
For parenteral administration using the solution, administer via intramuscular (IM) or intravenous (IV) routes.
The single parenteral dose ranges from 50 mg to 400 mg.
The maximum daily parenteral dose is 1200 mg.
For intravenous bolus injection, administer the dose slowly to avoid adverse effects like a metallic taste or sensation of warmth.
For intravenous drip infusion, dilute the required dose in an appropriate volume of infusion solution.
In cases of acute myocardial infarction, initiate parenteral therapy from the first days of the event.
For anxiety disorders and withdrawal syndrome, titrate the dose based on the severity of neurosis-like and autonomic symptoms.
For cerebrovascular accidents and cognitive disorders, use as part of a comprehensive combination therapy regimen.
Adjust the treatment course duration according to the disease severity and therapeutic response; typical courses last several weeks.
Monitor patients for tolerance and potential adverse reactions, especially during prolonged therapy or with high-dose regimens.
Adverse Reactions
When taken orally nausea, dry mouth, diarrhea, drowsiness, 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 shortness of breath (generally 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
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 the treatment period, 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.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Solution for intravenous and intramuscular administration 50 mg/1 ml: amp. 2 ml, 5 ml, or 10 ml 5 or 10 pcs.
Marketing Authorization Holder
Binnopharm JSC (Russia)
Dosage Form
 |
Ethylmethylhydroxypyridine succinate | Solution for intravenous and intramuscular administration 50 mg/1 ml: amp. 2 ml, 5 ml, or 10 ml 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
Solution for IV and IM administration colorless or slightly colored, transparent.
| 1 ml | |
| Ethylmethylhydroxypyridine succinate | 50 mg |
Excipients : water for injections.
2 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
2 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.
10 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
10 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.
Film-coated tablets, 125 mg
Film-coated tablets 250 mg
Marketing Authorization Holder
Obnovlenie Pfc, JSC (Russia)
Dosage Forms
|
Ethylmethylhydroxypyridine succinate | Film-coated tablets, 125 mg |
| Film-coated tablets 250 mg |
Dosage Form, Packaging, and Composition
Film-coated tablets
| 1 tab. | |
| Ethylmethylhydroxypyridine succinate | 125 mg |
10 pcs. – contour cell packaging (2 pcs.) – cardboard packs (20 pcs.) – By prescription
10 pcs. – contour cell packaging (3 pcs.) – cardboard packs (30 pcs.) – By prescription
10 pcs. – contour cell packaging (6 pcs.) – cardboard packs (60 pcs.) – By prescription
10 pcs. – contour cell packaging (9 pcs.) – cardboard packs (90 pcs.) – By prescription
14 pcs. – contour cell packaging – cardboard packs (14 pcs.) – By prescription
14 pcs. – contour cell packaging (2 pcs.) – cardboard packs (28 pcs.) – By prescription
14 pcs. – contour cell packaging (4 pcs.) – cardboard packs (56 pcs.) – By prescription
15 pcs. – contour cell packaging (2 pcs.) – cardboard packs (30 pcs.) – By prescription
15 pcs. – contour cell packaging (4 pcs.) – cardboard packs (60 pcs.) – By prescription
15 pcs. – contour cell packaging (6 pcs.) – cardboard packs (90 pcs.) – By prescription
Film-coated tablets
| 1 tab. | |
| Ethylmethylhydroxypyridine succinate | 250 mg |
10 pcs. – contour cell packaging (2 pcs.) – cardboard packs (20 pcs.) – By prescription
10 pcs. – contour cell packaging (3 pcs.) – cardboard packs (30 pcs.) – By prescription
10 pcs. – contour cell packaging (6 pcs.) – cardboard packs (60 pcs.) – By prescription
10 pcs. – contour cell packaging (9 pcs.) – cardboard packs (90 pcs.) – By prescription
14 pcs. – contour cell packaging – cardboard packs (14 pcs.) – By prescription
14 pcs. – contour cell packaging (2 pcs.) – cardboard packs (28 pcs.) – By prescription
14 pcs. – contour cell packaging (4 pcs.) – cardboard packs (56 pcs.) – By prescription
15 pcs. – contour cell packaging (2 pcs.) – cardboard packs (30 pcs.) – By prescription
15 pcs. – contour cell packaging (4 pcs.) – cardboard packs (60 pcs.) – By prescription
15 pcs. – contour cell packaging (6 pcs.) – cardboard packs (90 pcs.) – By prescription
Solution for intravenous and intramuscular administration 50 mg/1 ml: amp. 2 ml 10 pcs. or 5 ml 5 pcs.
Marketing Authorization Holder
Pharmamed, LLC (Russia)
Manufactured By
Ozon, LLC (Russia)
Dosage Form
|
Ethylmethylhydroxypyridine succinate | Solution for intravenous and intramuscular administration 50 mg/1 ml: amp. 2 ml 10 pcs. or 5 ml 5 pcs. |
Dosage Form, Packaging, and Composition
Solution for IV and IM administration transparent, colorless or with a yellowish or brownish tint.
| 1 ml | |
| Ethylmethylhydroxypyridine succinate | 50 mg |
Excipients : water for injections – up to 1 ml.
2 ml – glass ampoules (5) – contour cell packaging (2) – cardboard packs.
5 ml – glass ampoules (5) – contour cell packaging (1) – cardboard packs.
Solution for intravenous and intramuscular injection 50 mg/ml
Marketing Authorization Holder
PFKO-1, LLC (Russia)
Manufactured By
Obnovlenie Pfc, JSC (Russia)
Dosage Form
|
Ethylmethylhydroxypyridine succinate Renewal | Solution for intravenous and intramuscular injection 50 mg/ml |
Dosage Form, Packaging, and Composition
Solution for intravenous and intramuscular injection
| 1 ml | |
| Ethylmethylhydroxypyridine succinate | 50 mg |
2 ml – ampoules (10 pcs.) – cardboard packs – By prescription
2 ml – ampoules (100 pcs.) – cardboard boxes – for hospitals
2 ml – ampoules (20 pcs.) – cardboard boxes – for hospitals
2 ml – ampoules (20 pcs.) – cardboard packs – By prescription
2 ml – ampoules (5 pcs.) – cardboard packs – By prescription
2 ml – ampoules (50 pcs.) – cardboard boxes – for hospitals
5 ml – ampoules (10 pcs.) – cardboard packs – By prescription
5 ml – ampoules (100 pcs.) – cardboard boxes – for hospitals
5 ml – ampoules (15 pcs.) – cardboard packs – By prescription
5 ml – ampoules (20 pcs.) – cardboard boxes – for hospitals
5 ml – ampoules (5 pcs.) – cardboard packs – By prescription
5 ml – ampoules (50 pcs.) – cardboard boxes – for hospitals
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