Citoflavin 100 tablets

In adults as part of combination therapy:

• consequences of brain infarction;

• other cerebrovascular diseases (cerebral atherosclerosis, hypertensive encephalopathy);

• neurasthenia (increased irritability, fatigue, loss of ability for prolonged mental and physical exertion);

• for the prevention of cognitive disorders after extensive surgical interventions in elderly patients.

Method of application and doses

The tablets should be taken at least 30 minutes before meals, without chewing, and with water (100 ml). It is recommended to take the medication in the morning and daytime (no later than 6 PM). In the complex therapy of the consequences of brain infarction, other cerebrovascular diseases, and neurasthenia, the medication is taken at 2 tablets 2 times a day with an interval of 8-10 hours. The duration of the treatment course is 25 days. Repeating the course is possible with an interval of at least 1 month.

For the prevention of cognitive disorders after extensive surgical interventions in elderly patients, the medication is taken at 2 tablets 2 times a day with an interval of 8-10 hours for 25 days. The start of using the medication "CITOFAVIN® tablets, coated with an enteric-soluble shell" is recommended 144 (± 4) hours after the start of the operation, that is, the next day after completing the treatment course with the medication "CITOFAVIN® solution for intravenous administration".

Composition per tablet:
Active ingredients:
Succinic acid 0.300 g
Inosine 0.050 g
Nicotinamide 0.025 g
Riboflavin (sodium riboflavin phosphate) 0.005 g
Excipients: povidone K 30 - 0.00810 g, calcium stearate - 0.00390 g, hypromellose - 0.00360 g, polysorbate 80 - 0.00040 g.
Enteric coating: methacrylic acid and ethyl acrylate copolymer [1:1] - 0.02902 g, propylene glycol - 0.00291 g,
dye azorubine (carminic acid) (E 122) - 0.00007 g.

Description of the dosage form

Round biconvex tablets coated with a red color. Two layers are visible in a cross-section. The core of the tablets is yellow to yellow-orange in color.

Contraindications

Individual intolerance to the components of the drug. Not recommended for use in children under 18 years of age due to lack of data on efficacy and safety.
With caution

Diseases of the digestive organs (erosions, ulcers of the stomach and/or duodenum, gastritis and duodenitis (during exacerbation)), arterial hypotension, nephrolithiasis, concomitant gout, hyperuricemia. The drug CITOFLOVIN® should be used with caution in patients who have undergone cardiac surgery using a heart-lung machine, due to the lack of clinical studies in this patient group. If you have any of the listed diseases, be sure to consult a doctor before taking the drug.
Use during pregnancy and breastfeeding

It is not recommended to take during pregnancy and breastfeeding due to the lack of clinical data on the efficacy and safety of the drug during these periods.

Special instructions

In cases of hypertension, dose adjustments of antihypertensive medications may be required. In patients with diabetes mellitus, treatment should be conducted under the control of blood glucose levels. Intense yellow coloring of urine may occur.
Effect on the ability to drive vehicles and operate machinery
CITOFLAVIN® does not affect the ability to drive vehicles or operate machinery.

According to the World Health Organization, adverse reactions are classified according to their frequency of occurrence as follows:

• very common (? 1/10);

• common (? 1/100 - < 1/10);• uncommon (? 1/1000 - < 1/100);• rare (? 1/10000 - < 1/1000);• very rare (< 1/10000);• frequency unknown (cannot be determined based on available data). Skin and subcutaneous tissue disorders: very rare - itching, urticaria, rash. Vascular disorders: very rare - hyperemia. Nervous system disorders: very rare - headache. Gastrointestinal disorders: very rare - epigastric pain, discomfort in the epigastric area, nausea. Metabolism and nutrition disorders: very rare - transient hypoglycemia, hyperuricemia, exacerbation of concomitant gout. If any of the adverse reactions listed in the instructions worsen or you notice any other adverse reactions not listed in the instructions, inform your doctor.OverdoseTo date, there have been no reported cases of overdose with the drug CITOFLOVINE®.InteractionSuccinate, inosine, and nicotinamide are compatible with other medications. Riboflavin reduces the activity of certain antibiotics (tetracyclines, erythromycin, lincomycin) and is incompatible with streptomycin. Ethanol, tricyclic antidepressants, and tubular secretion blockers decrease the absorption of riboflavin, while thyroid hormones accelerate its metabolism.

Pharmacodynamics

The pharmacological effects are due to the complex action of the components included in the preparation CITOFAVIN®. Succinic acid is an endogenous intracellular metabolite of the Krebs cycle, performing a universal energy-synthesizing function in the cells of the body. With the participation of the coenzyme flavin adenine dinucleotide (FAD), succinic acid is rapidly transformed by the mitochondrial enzyme succinate dehydrogenase into fumaric acid and further into other metabolites of the tricarboxylic acid cycle. It stimulates aerobic glycolysis and ATP synthesis in cells. The end products of succinic acid metabolism in the Krebs cycle are carbon dioxide and water. Succinic acid improves tissue respiration by activating electron transport in the mitochondria. Riboflavin (vitamin B2) is a flavin coenzyme that activates succinate dehydrogenase and the redox reactions of the Krebs cycle. Nicotinamide (vitamin PP) is an amide of nicotinic acid. Nicotinamide is transformed in cells through a cascade of biochemical reactions into the form of nicotinamide adenine dinucleotide (NAD) and its phosphate (NADP), activating nicotinamide-dependent enzymes of the Krebs cycle, which are necessary for Inosine is a purine derivative, a precursor of ATP. It has the ability to activate a number of enzymes of the Krebs cycle, stimulating the synthesis of key nucleotide enzymes: flavin adenine dinucleotide (FAD) and nicotinamide adenine dinucleotide (NAD). Thus, all components of the preparation CITOFAVIN® are natural metabolites of the body and stimulate tissue respiration. The metabolic energy correction, anti-hypoxic and antioxidant activity of the preparation, which determine the pharmacological properties and therapeutic efficacy of the components, are due to the complementary action of succinic acid, inosine, nicotinamide, and riboflavin.

Pharmacokinetics

CYTOFLAVIN® has high bioavailability. Succinic acid, when taken orally, penetrates from the gastrointestinal tract into the blood and tissues, participating in energy metabolism reactions, and is completely broken down to end products of metabolism (carbon dioxide and water) within 30 minutes. Inosine is well absorbed from the gastrointestinal tract. The time to reach maximum concentration in the blood is 5 hours, the average retention time in the blood is 5.5 hours, and the equilibrium volume of distribution is about 20 liters. Inosine is metabolized in the liver to inosine monophosphate, which is subsequently oxidized to uric acid. A small amount is excreted by the kidneys.

Nicotinamide is rapidly distributed in all tissues (equilibrium volume of distribution is about 500 liters). The time to reach maximum concentration in the blood is 2 hours, and the average retention time in the blood is 4.5 hours. Nicotinamide crosses the placenta and enters breast milk, is metabolized in the liver to N-methyl nicotinamide, and is excreted by the kidneys.

Riboflavin is rapidly absorbed from the gastrointestinal tract, distributed unevenly (with the highest amounts in the myocardium, liver, and kidneys), and is transformed into flavin adenine mononucleotide (FMN) and flavin adenine dinucleotide (FAD) in the mitochondria. It crosses the placenta and enters breast milk; it is excreted by the kidneys, primarily as metabolites.