Dinar

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT Dinar (Dinar)

Composition:

Active substance: ethylmethylhydroxypyridine succinate;

1 ml of solution contains ethylmethylhydroxypyridine succinate (calculated as 100% dry substance) – 50 mg;

Excipients: sodium metabisulfite, water for injections.

Pharmaceutical form. Injection solution.

Main physico-chemical properties: clear, colorless or slightly yellowish liquid.

Pharmacotherapeutic group.

Other agents affecting the nervous system. ATC code N07XX.

Pharmacological Properties.

Pharmacodynamics.

Dinar is an inhibitor of free radical processes and a membrane protector, exerting anti-hypoxic, stress-protective, nootropic, anticonvulsant, and anxiolytic effects. The drug increases the organism's resistance to various damaging factors, including oxygen-dependent pathological conditions (shock, hypoxia and ischemia, cerebral circulation disorders, alcohol intoxication, and intoxication with antipsychotic agents (neuroleptics)).

The drug improves cerebral metabolism and cerebral blood supply, enhances microcirculation and rheological properties of blood, and reduces platelet aggregation. It stabilizes blood cell membrane structures (erythrocytes and platelets) during hemolysis. Dinar exerts a hypolipidemic effect, reducing total cholesterol and low-density lipoprotein (LDL) levels. It reduces enzymatic toxemia and endogenous intoxication in acute pancreatitis.

The mechanism of action is due to its antioxidant and membrane-protective properties. It inhibits lipid peroxidation, increases superoxide dismutase activity, improves the lipid-protein ratio, and reduces membrane viscosity. Dinar modulates the activity of membrane-bound enzymes (calcium-independent phosphodiesterase, adenylate cyclase, acetylcholinesterase) and receptor complexes (benzodiazepine, gamma-aminobutyric acid (GABA), acetylcholine), thereby enhancing their ability to bind ligands, promoting the preservation of the structural-functional organization of biomembranes, neurotransmitter transport, and improved synaptic transmission. Dinar increases dopamine levels in the brain. It enhances compensatory activation of aerobic glycolysis and reduces the degree of inhibition of oxidative processes in the Krebs cycle under hypoxic conditions, increasing adenosine triphosphate (ATP) and creatine phosphate levels, activating mitochondrial energy-synthesizing functions, and stabilizing cellular membranes.

Dinar normalizes metabolic processes in ischemic myocardium, reduces the necrotic area, restores and improves myocardial electrical activity and contractility, increases coronary blood flow in the ischemic area, reduces the consequences of reperfusion syndrome in acute coronary insufficiency, and enhances the antianginal activity of nitro compounds. Dinar promotes the preservation of retinal ganglion cells and optic nerve fibers in progressive neuropathy caused by chronic ischemia and hypoxia. It improves retinal and optic nerve functional activity, increasing visual acuity.

Pharmacokinetics.

After intramuscular administration, the drug is detectable in plasma for up to 4 hours after injection. The time to reach maximum concentration is 0.45–0.5 hours. Maximum concentrations at doses of 400–500 mg are 3.5–4.0 µg/mL. Dinar is rapidly absorbed from the bloodstream into organs and tissues and is rapidly eliminated from the body. The drug is excreted in urine, primarily in glucuronide-conjugated form, and in insignificant amounts unchanged.

Clinical characteristics.

Indications.

• Acute cerebrovascular disorders;
• Traumatic brain injury, consequences of traumatic brain injuries;
• Dyscirculatory encephalopathy;
• Vegetative dystonia syndrome;
• Mild cognitive disorders of atherosclerotic origin;
• Anxiety disorders in neurotic and neurosis-like conditions;
• Acute myocardial infarction (from the first day) as part of complex therapy;
• Primary open-angle glaucoma at different stages, as part of complex therapy;
• Management of alcohol withdrawal syndrome with predominant neurosis-like and vegetative-vascular disorders;
• Acute intoxication with antipsychotic agents;
• Acute purulent-inflammatory processes in the abdominal cavity (acute necrotic pancreatitis, peritonitis) as part of complex therapy.

Contraindications.

Acute hepatic or renal failure, increased individual sensitivity to the drug. Pregnancy or breastfeeding period. Pediatric age.

Interaction with other medicinal products and other forms of interactions.

The medicinal product Dinar enhances the effect of benzodiazepine anxiolytics, anticonvulsants (carbamazepine), antiparkinsonian agents (levodopa). Potentiates the effect of nitro-containing drugs and antihypertensive agents. Reduces the toxic effect of ethanol.

Special precautions for use.

In individual cases, especially in predisposed patients, in patients with bronchial asthma, and in those with increased sensitivity to sulfites, severe hypersensitivity reactions may occur. Use with caution in patients with diabetic retinopathy (treatment course not more than 7–10 days) due to the potential to promote proliferative processes.

After completion of parenteral administration, to maintain the therapeutic effect achieved, continuation of the drug orally in tablet form is recommended.

Use during pregnancy or breastfeeding.

The medicinal product Dinаr is contraindicated during pregnancy or breastfeeding.

Ability to affect reaction rate while driving or operating machinery.

During treatment, caution is required when driving or operating machinery, due to the possibility of adverse effects that may influence reaction speed and attention concentration.

Method of Administration and Dosage.

Intramuscularly (i/m) or intravenously (i/v) (bolus or infusion). When administered by infusion, the medicinal product Dinár should be diluted in 0.9% sodium chloride solution.

The medicinal product Dinár should be administered slowly by bolus injection over 5–7 minutes; by infusion, at a rate of 40–60 drops per minute. The maximum daily dose must not exceed 1200 mg.

In acute cerebrovascular disorders: the medicinal product Dinár should be administered i/v by infusion during the first 10–14 days at 200–500 mg 2–4 times daily, followed by i/m administration of 200–250 mg 2–3 times daily for the next 2 weeks.

In traumatic brain injury and its consequences: the medicinal product Dinár should be used for 10–15 days by i/v infusion at 200–500 mg 2–4 times daily.

In decompensated phase of dyscirculatory encephalopathy: the medicinal product Dinár should be administered i/v either by bolus or infusion at a dose of 200–500 mg 1–2 times daily for 14 days. Then i/m at 100–250 mg daily for the following 2 weeks.

For course prophylaxis of dyscirculatory encephalopathy: the product should be administered i/m at a dose of 200–250 mg twice daily for 10–14 days.

In mild cognitive impairment in elderly patients and anxiety disorders: the medicinal product should be administered i/m at a daily dose of 100–300 mg daily for 14–30 days.

In acute myocardial infarction as part of complex therapy: the medicinal product Dinár should be administered i/v or i/m for 14 days alongside conventional therapy for myocardial infarction, including nitrates, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors, thrombolytics, anticoagulant and antiplatelet agents, as well as symptomatic treatments as indicated. For the first 5 days, to achieve maximum effect, i/v administration of Dinár is recommended; for the following 9 days, i/m administration is possible. Intravenous administration should be performed by drip infusion slowly (to avoid adverse effects) in 0.9% sodium chloride solution or 5% dextrose (glucose) solution in a volume of 100–150 ml over 30–90 minutes. If necessary, slow bolus injection of Dinár may be performed over no less than 5 minutes.

Administration of the medicinal product Dinár (i/v or i/m) should be performed 3 times daily every 8 hours. The daily therapeutic dose is 6–9 mg/kg body weight; the single dose is 2–3 mg/kg body weight. The maximum daily dose must not exceed 800 mg; the maximum single dose must not exceed 250 mg.

In open-angle glaucoma of various stages as part of complex therapy: the medicinal product Dinár should be administered i/m at 100–300 mg 1–3 times daily for 14 days.

In alcohol withdrawal syndrome: the medicinal product Dinár should be administered at a dose of 200–500 mg i/v by infusion or i/m 2–3 times daily for 5–7 days.

In acute intoxication with antipsychotic agents: the medicinal product should be administered i/v at a dose of 200–500 mg daily for 7–14 days.

In acute purulent-inflammatory processes of the abdominal cavity (acute necrotic pancreatitis, peritonitis): the medicinal product should be prescribed on the first day both in the preoperative and postoperative periods. Doses depend on the form and severity of the disease, extent of the process, and clinical course variants. Discontinuation of the product should be gradual, only after a sustained positive clinical and laboratory effect.

In acute edematous (interstitial) pancreatitis: the medicinal product Dinár should be administered at 200–500 mg 3 times daily by i/v infusion (in 0.9% sodium chloride solution) and i/m.

Mild degree of necrotizing pancreatitis: 100–200 mg 3 times daily by i/v infusion (in 0.9% sodium chloride solution) and i/m.

Moderate degree: 200 mg 3 times daily by i/v infusion (in 0.9% sodium chloride solution).

Severe course: pulse-dose regimen of 800 mg on the first day administered twice, followed by 200–500 mg twice daily with gradual reduction of the daily dose.

Very severe course: initial dose of 800 mg daily until sustained control of pancreatogenic shock symptoms; after stabilization of the patient's condition, 300–400 mg twice daily by i/v infusion (in 0.9% sodium chloride solution), with gradual reduction of the daily dose.

Children.

No controlled clinical studies on the safety of Dinár in children have been conducted; therefore, the medicinal product Dinár is contraindicated in this patient group.

Overdose.

Symptoms: drowsiness, insomnia.

Treatment: due to low toxicity, overdose is unlikely. Treatment is usually not required; symptoms resolve spontaneously within 24 hours. In cases of pronounced symptoms, supportive and symptomatic treatment should be administered.

Side effects.

To avoid the occurrence of adverse effects, it is recommended to follow the recommended dosing regimen and rate of administration.

The frequency of adverse effects was determined according to the classification of the World Health Organization (WHO): very common (≥ 10%), common (≥ 1%, but < 10%), uncommon (≥ 0.1%, but < 1%), rare (≥ 0.01%, but < 0.1%), very rare (< 0.01%), frequency not known (cannot be determined from available data).

Immune system disorders: very rare – anaphylactic shock, angioneurotic edema, urticaria.

Psychiatric disorders: very rare – drowsiness.

Nervous system disorders: very rare – headache, dizziness (may be related to excessively high rate of administration and is transient in nature).

Vascular disorders: very rare – increased blood pressure, decreased blood pressure (may be related to excessively high rate of administration and is transient in nature).

Respiratory, thoracic and mediastinal disorders: very rare – dry cough, throat irritation, chest discomfort, dyspnea (may be related to excessively high rate of administration and is transient in nature).

Gastrointestinal disorders: very rare – dry mouth, nausea, unpleasant taste sensation, metallic taste in mouth.

Skin and subcutaneous tissue disorders: very rare – itching, rash, hyperemia.

General disorders and administration site conditions: very rare – sensation of warmth.

Shelf life.

2 years.

Do not use after the expiry date stated on the packaging.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Incompatibilities.

The medicinal product must not be mixed with other medicinal products.

Only use solvents specified in the instructions.

Packaging.

2 ml or 5 ml in an ampoule. 10 ampoules per pack. 5 ampoules per blister.

2 blisters per pack.

Prescription category.

Prescription only.

Manufacturers.

1. JSC "FARMAC" (responsible for manufacturing and batch control/testing, excluding batch release).
2. LLC NVP "MIKROKHIM" (responsible for batch release, excluding batch control/testing).

Manufacturers' addresses and locations of their operations.

1. Ukraine, 04080, Kyiv, Kyrylivska Street, 74.
2. Ukraine, 01013, Kyiv, Budynstroi, 5.

Marketing Authorization Holder.

LLC NVP "MIKROKHIM".

Address of the Marketing Authorization Holder.

Ukraine, 01013, Kyiv, Budynstroi, 5.