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

Description

EUFILLIN COMPOSITION
active substance: theophylline

1 ml of theophylline monohydrate in terms of theophylline 20 mg

excipients: sodium acetate trihydrate, water for injection.

EUFILLIN DOSAGE FORM
Injection.

EUFILLIN MAIN PHYSICAL AND CHEMICAL PROPERTIES:
transparent colorless or slightly yellowish solution.

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

PHARMACOLOGICAL PROPERTIES.
Pharmacological.

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. It also relaxes the smooth muscles of the gastrointestinal tract, biliary tract, uterus.

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 F 2alpha), 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 (CNS) 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 perifocal and general cerebral edema, reduces cerebrospinal fluid and, consequently, intracranial pressure. Reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation. Increases renal blood flow, has a moderate diuretic effect.

Therapeutic effects develop 5-15 minutes after injection.

Pharmacokinetics.

Bioavailability is 80-100%. The connection with plasma proteins is about 60%.

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

CONTRAINDICATIONS
Hypersensitivity to the components of the drug, other xanthine derivatives (caffeine, pentoxifylline, theobromine) acute heart failure, angina pectoris, acute myocardial infarction, paroxysmal tachycardia, extrasystole, severe arterial hyper- and hypotension, widespread atherosclerosis of blood vessels, pulmonary edema, hemorrhagic retina, history of bleeding, gastric ulcer and duodenal ulcer in the acute stage, gastroesophageal reflux, epilepsy, glaucoma, increased convulsive readiness, uncontrolled hypothyroidism, hyperthyroidism, thyrotoxicosis, severe hepatic insufficiency, and / or porphyria concurrently with ephedrine.