Eufillin-N (theophylline) 200 ampoules 2% 5 ml. №10

$8.00

Manufacturer: Ukraine

Bronchoobstructive syndrome in bronchial asthma, bronchitis, emphysema of the lungs, violations of the respiratory center (night paroxysmal apnea) “”pulmonary heart”.

Category:

Description

EUFILIN-N COMPOSITION
active substance: theophylline

1 ml of anhydrous theophylline in terms of 100% substance 20 mg

excipients: sodium acetate trihydrate, sodium hydroxide, water for injection.

EUFILIN-N DOSAGE FORM
Injection.

Basic physical and chemical properties: transparent, colorless or slightly yellowish liquid.

EUFILIN-N PHARMACOLOGICAL GROUP
Means for systemic use in obstructive respiratory diseases. Theophylline. ATX code R03D A04.

PHARMACOLOGICAL PROPERTIES
Pharmacological.

Euphyllin is a bronchodilator, antispasmodic agent of the methylxanthine group (purine derivative).

Shows an expressive bronchodilator effect due to direct relaxation of the smooth muscles of the bronchi. The expressiveness of the bronchospasmolytic effect depends on the concentration of theophylline in the blood serum.

It normalizes the respiratory function, contributes to the saturation of blood with oxygen and a decrease in the concentration of carbon dioxide, stimulates the center of respiration. Strengthens ventilation of the lungs in conditions of hypokalemia.

It inhibits platelet aggregation (inhibits the factor of activation of platelets and prostaglandin E 2), increases the resistance of erythrocytes to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation.

Shows a stimulating effect on the central nervous system and heart activity, increases the strength and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly the vessels of the brain, skin and kidneys). Reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation. Increases renal blood flow, has a moderate diuretic effect. Expands the extrahepatic biliary tract.

Therapeutic effects develop 5-15 minutes after injection.

Pharmacokinetics.

Bioavailability is 80-100%. The connection with blood plasma proteins is 40-60% in newborns, as well as in adults with liver diseases, the connection with proteins is reduced.

Penetrates through the blood-brain and placental barriers, into the CSF, saliva, sputum and other body secrets, into breast milk. It is metabolized in the liver (90%) with the participation of several isoenzymes of cytochrome P450 (the most important is CYP1A2). The main metabolites are 1,3-dimethyl uric acid (has a pharmacological activity that is 2-5 times inferior to theophylline) and 3-methylxanthine. Caffeine is an active metabolite and is formed in small quantities, with the exception of premature infants and children under 6 months of age, in which there is a significant accumulation in the body (after a long half-life). At the age of 6 years and older, the phenomenon of caffeine accumulation is absent.

It is excreted by the kidneys in the form of metabolites and unchanged (in adults – 7-13% of the administered dose, in children – 50%).

Due to significant individual differences in the rate of hepatic metabolism of theophylline, its clearance, plasma concentration and half-life are characterized by an expressive variability of values. The metabolic rate of theophylline in the liver depends on age, passion for smoking tobacco, diet, concomitant diseases, drug therapy, is simultaneously carried out.

The optimal therapeutic concentrations of theophylline in blood plasma are: to achieve a bronchodilator effect – 10-20 μg / ml, for an exciting effect on the respiratory center – 5-10 μg / ml. At lower concentrations, the therapeutic effect is weak, at high concentrations, there is no significant increase in the therapeutic effect, while the risk of side effects is significantly increased.

CONTRAINDICATIONS
Hypersensitivity to the components of the drug, including other xanthine derivatives (caffeine, pentoxifylline, theobromine), pulmonary edema, severe arterial hyper- and hypotension, widespread vascular atherosclerosis, acute heart failure, acute myocardial infarction, decompensated chronic heart failure, angina pectoris, paroxysmal tachycardia, extrasystole, epilepsy, increased convulsive readiness, glaucoma, gastroesophageal reflux, gastric ulcer and duodenal ulcer in the acute stage, Severe hepatic and / or renal failure, uncontrolled hypothyroidism, hyperthyroidism stroke, retinal hemorrhage, use in children simultaneously with ephedrine.