Eufillin, 24 mg/ml 10 ml 10 pcs

Euphylline is a bronchodilator and an FDE inhibitor. It is ethylenediamine salt of theophylline (which facilitates solubility and increases absorption). It has a bronchodilator effect, apparently due to a direct relaxing effect on the smooth muscles of the airways and blood vessels of the lungs.

It is believed that this effect is caused by selective inhibition of the activity of specific FDEs, which leads to an increase in the intracellular concentration of cAMP. The results of experimental studies in vitro show that the main role seems to be played by isoenzymes III and IV types. Suppression of the activity of these isoenzymes may also cause some side effects of aminophylline (theophylline), including vomiting, arterial hypotension and tachycardia. It blocks adenosine (purine) receptors, which may be a factor of action on the bronchi.

It reduces airway hyperresponsiveness associated with the late phase of the response caused by inhaling allergens through an unknown mechanism that is not related to FDE inhibition or adenosine blockade. There are reports that aminophylline increases the number and activity of T suppressors in peripheral blood.
Increases mucociliary clearance, stimulates diaphragm contraction, improves respiratory and intercostal muscle function, stimulates the respiratory center, increases its carbon dioxide sensitivity and improves alveolar ventilation, which ultimately leads to a reduction in the severity and frequency of apnea episodes. By normalizing respiratory function, it promotes blood oxygenation and decreases carbon dioxide concentration. It enhances lung ventilation in conditions of hypokalemia.

It has a stimulating effect on heart activity, increases strength and heart rate, increases coronary blood flow and increases myocardial oxygen demand. Reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys). It has a peripheral venodilator effect, reduces pulmonary vascular resistance, lowers the pressure in the small circle of circulation. Increases renal blood flow, has a moderate diuretic effect. Dilates extrahepatic biliary tracts. Stabilizes membranes of mast cells, inhibits release of mediators of allergic reactions. Inhibits platelet aggregation (inhibits platelet activation factor and PgE2α), increases resistance of red blood cells to deformation (improves rheological properties of blood), reduces thrombosis and normalizes microcirculation. It has a tocolytic effect and increases the acidity of gastric juice. In high doses it has epileptogenic effect.

Pharmacokinetics

In the body aminophylline is metabolized at physiological pH values with release of free theophylline. Bronchodilator properties are evident at plasma theophylline concentrations of 10-20 µg/ml. Concentrations above 20 mg/ml are toxic. The excitatory effect on the respiratory center is realized at lower concentrations of 5-10 µg/ml.
Theophylline’s binding to plasma proteins is approximately 40%; in newborns as well as in adults with disease, the binding decreases. Binding to plasma proteins is approximately 60% in adults, 36% in newborns, and 36% in cirrhotic patients. It penetrates the placental barrier (the concentration in the fetal serum is slightly higher than in the mother’s serum). It is excreted with the breast milk.

Theophylline is metabolized in the liver with the participation of several cytochrome P450 isoenzymes, the most important of which is CYP1A2. During metabolism 1,3-dimethylureic acid, 1-methylureic acid and 3-methylxanthine are formed. These metabolites are excreted in the urine. In adults, 10% is excreted unchanged. In infants a significant portion is excreted as caffeine (due to immaturity of pathways of its further metabolism), unchanged – 50%.
Significant individual differences of hepatic metabolism rate of theophylline cause marked variability of clearance values, plasma concentrations and elimination half-life. Such factors as age, tobacco smoking habits, diet, diseases, and concomitant drug therapy affect hepatic metabolism.

Theophylline’s T1/2 in non-smoking patients with bronchial asthma with practically no pathological changes from other organs and systems is 6-12 hours, in smokers – 4-5 hours, in children – 1-5 hours, in newborns and premature infants – 10-45 hours.

Theophylline T1/2 is increased in the elderly and in patients with heart failure or liver disease.
Clearance is decreased in heart failure, liver function disorders, chronic alcoholism, pulmonary edema, chronic obstructive pulmonary disease.

Ethylenediamine does not affect the pharmacokinetics of theophylline.

Indications

Active ingredient

Composition

Active ingredient:

Aminophylline – 24 mg

Additional ingredients: water d/i – up to 1 ml.

How to take, the dosage

Intravenous administration of the drug should be carried out cautiously and slowly, for at least 5 minutes.

The dose of the drug is adjusted individually, taking into account the possibility of different excretion rates in different patients.

Interaction

Pharmacokinetic interaction Cimetidine, erythromycin, influenza vaccine and oral contraceptives increase the effect of Eufillin, increasing its concentration in plasma of the patient.

In concomitant administration with carbamazepine, phenytoin, rifampicin the level of Eufillin concentration in plasma decreases.

Nicotine activates metabolism and excretion of Eufillin. With concomitant use Eufillin increases excretion of lithium. Pharmacodynamic interaction Concomitant use with Eufillin increases the bronchodilator effect of terbutaline and salbutamol. Concomitant administration of Eufillin with beta-blockers may cause bronchospasm.

Special Instructions

The drug is administered with caution in patients with fever of unclear genesis, the elderly.

Euphylline may increase uric acid levels in urine.

Caution should be exercised when drinking large amounts of caffeinated products or beverages during treatment.

The solution must be warmed to body temperature before parenteral administration.

Contraindications

Side effects

Overdose

In overdose facial hyperemia, insomnia, motor agitation, anxiety, photophobia, anorexia, diarrhea, nausea, vomiting, epigastric pain, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized convulsions, hyperventilation are observed, Severe poisoning may lead to epileptoid seizures (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, skeletal muscle necrosis, confusion, renal failure with myoglobinuria.

The treatment of overdose depends on the clinical picture and includes discontinuation of the drug, stimulation of its elimination from the body (forced diuresis, hemosorption, plasma sorption, hemodialysis, peritoneal dialysis) and administration of symptomatic measures.

Diazepam (in injections) is used to relieve seizures. Barbiturates should not be used. Hemodialysis is recommended in severe intoxication (eufillin content more than 50 g / l).