Cytoflavin, 50 pcs.

Pharmacodynamics

Pharmacological effects are due to the complex action of the ingredients of the drug CITOFLAVIN®.

CITOFLAVIN® promotes activation of aerobic cell metabolism which results in increase of glucose utilization, promotes increased level of beta-oxidation of fatty acids and resynthesis of γ-aminobutyric acid in neurons.

CITOFLAVIN® increases resistance of nerve and glial cell membranes to ischemia, which is manifested by a decrease in the concentration of neuro-specific proteins characterizing the level of destruction of the main structural components of nervous tissue.

CITOFLAVIN® improves coronary and cerebral blood flow, activates metabolic processes in the central nervous system, restores disturbed consciousness, facilitates regress of neurological symptoms and improves cognitive functions of the brain. It has a fast awakening effect in post-arrest depression of consciousness.

When administering CITOFLAVIN® during the first 12 hours from the beginning of stroke a favorable course of ischemic and necrotic processes in the affected area (decrease of the focus), recovery of neurological status and decrease of disability level in a long-term period are observed.

Pharmacokinetics

In intravenous infusion at the rate of about 2 ml/min (in terms of undiluted CITOFLAVIN®) succinic acid and inosine are utilized almost immediately and are not determined in blood plasma.

Amber acid – peak concentration is determined during the first minute after administration, with its further rapid decrease without cumulation and return to the background level due to metabolism to water and carbon dioxide.
Inosine is metabolized in the liver to form inosine monophosphate with its subsequent oxidation to uric acid. A small amount is excreted by the kidneys.

Nicotinamide is rapidly distributed in all tissues, passes through the placenta and into the breast milk, is metabolized in the liver to form N-methylnicotinamide, and is excreted by the kidneys. Period of half-life from plasma is about 1.3 hours, equilibrium volume of distribution – about 60 liters, total clearance – about 0.6 l/min.

Riboflavin is unevenly distributed: most of it in myocardium, liver and kidneys. Half-life from plasma is about 2 hours, the equilibrium volume of distribution is about 40 liters, total clearance is about 0.3 l/min. It penetrates through the placenta and into the breast milk. Binding with plasma proteins is 60%. It is excreted by the kidneys, partially as a metabolite; in high doses it is mainly unchanged.

Indications

Headache, Atherosclerosis, Consequences of stroke, Impaired cerebral circulation

In adults in the complex therapy:

1. acute impairment of cerebral circulation.
2. consequences of cerebrovascular diseases (consequences of cerebral infarction, cerebral atherosclerosis).
3. toxic and hypoxic encephalopathy in acute and chronic poisonings, endotoxemia, post-arrest depression of consciousness, as well as for prevention and treatment of hypoxic encephalopathy during cardiac surgery with artificial circulation.

In children (including prematurely born with gestation period of 28-36 weeks) during the period of newborn infancy:

1. In cerebral ischemia.

Active ingredient

Inosine, Nicotinamide, Riboflavin, Amber acid

Composition

• Amber acid – 0.3 g.
• Riboxin (inosine) – 0.05 g.
• Nicotinamide – 0.025 g.
• Riboflavin mononucleotide (riboflavin) – 0.005 g.

Excipients:

• polyvinylpyrrolidone medium molecular weight (povidone).
• calcium stearate.
• methacrylic acid and ethyl acrylate copolymer.
• 1,2-propylene glycol.
• acid red 2C.

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How to take, the dosage

In adults:
CYTOFLAVIN® is administered only by intravenous drip in the dilution of 100-200 ml of 5-10 % dextrose solution or 0.9 % sodium chloride solution.

1. In acute impairment of cerebral circulation the drug is administered as soon as possible after the disease onset in the volume of 10 ml per injection with 8-12 hour intervals for 10 days. In severe form of the disease the single dose is increased to 20 ml.

2. In case of consequences of cerebrovascular diseases (consequences of cerebral infarction, cerebral atherosclerosis) the drug is administered in the volume of 10 ml once a day during 10 days.

In toxic and hypoxic encephalopathy the drug is administered in the volume of 10 ml by injection twice a day in 8-12 hours during 5 days. In comatose state in the volume of 20 ml per injection diluted in 200 ml of dextrose solution.

In postnarcotic depression, once in the same doses. In therapy of hypoxic encephalopathy during cardiac surgery with application of artificial circulation 20 ml of the preparation are administered in dilution of 200 ml of 5% dextrose solution 3 days before surgery, on the day of surgery, 3 days after surgery.

In children (including prematurely born) in neonatal period with cerebral ischemia daily dose of the preparation CITOFLAVINE® is 2 ml/kg/day. The calculated daily dose of the drug is administered intravenously by drop-flow (slowly) after dilution in 5% or 10% dextrose solution (ratio of not less than 1:5). The time of first administration is the first 12 hours after birth; the optimal time to start therapy is the first 2 hours of life.

It is recommended to administer the prepared solution by infusion pump at a rate of 1 to 4 ml/h, providing equal inflow of the drug into the bloodstream during the day, depending on the estimated daily volume of solutions for basic therapy, hemodynamic state of the patient and acid-base status indicators. The average course of treatment is 5 days.

Interaction

Amber acid, inosine, nicotinamide, compatible with other drugs.

Riboflavin: Reduces the activity of doxycycline, tetracycline, oxytetracycline, erythromycin and lincomycin.

It is not compatible with streptomycin.

Chlorpromazine, imipramine, amitriptyline due to blockade of flavinokinase, disrupts riboflavin incorporation into flavinadeninmononucleotide and flavinadenindinucleotide and increases its excretion with urine.

The thyroid hormones accelerate the metabolism of riboflavin.

Mitigates and prevents the side effects of chloramphenicol (hematopoiesis disorders, optic neuritis).

Compatible with drugs that stimulate hematopoiesis, antihypoxant drugs, anabolic steroids.

Special Instructions

Injection of the drug in newborns (premature infants) should be carried out under control of capillary blood acid-base status indicators at least twice a day (both before and during therapy). If possible, serum lactate and glucose values should be monitored.

The rate of infusion of the solution containing CITOFLAVIN® should be reduced or the infusion should be temporarily stopped in newborn (prematurely born) children:

– being on artificial ventilation, with signs of mixed (respiratory and metabolic) alkalosis, threatened by the development of cerebral circulatory disorders;
– in patients with preserved spontaneous breathing and respiratory support by CPAP method or in those receiving air-oxygen mixture through a mask, with the appearance of laboratory signs of metabolic alkalosis, threatened by the appearance or increase in the frequency of apnea attacks.

In diabetic patients the treatment should be performed under control of blood glucose index.
Intensive yellow staining of urine is possible.
CITOFLAVIN® has no effect on the ability to drive vehicles.

Contraindications

Hypersensitivity, patients undergoing ventilatory ventilation, when the partial pressure of oxygen in the arterial blood is less than 60 mm Hg, the period of breast-feeding.

With caution – nephrolithiasis, gout, hyperuricemia.

Side effects

When rapidly administered by drip, there may be adverse reactions not requiring withdrawal of the drug: skin hyperemia of varying degrees of severity, fever, bitterness and dryness in the mouth, and sore throat.

The rare undesired reactions include: transient pain and discomfort in the epigastric region and chest area, difficulty in breathing, nausea, headache, dizziness, “tingling” in the nose, dysosmia, pale skin of varying severity.

Also allergic reactions in the form of skin itching, transient hypoglycemia, hyperuricemia, gout exacerbation are possible.

In children (including prematurely born) during the period of newbornness, acid-base balance disorders (alkalosis) may develop.

Overdose

To date, no cases of overdose with CITOFLAVIN have been established.

Pregnancy use

It is not recommended during pregnancy and lactation due to the lack of clinical data on the efficacy and safety of the drug during this period.