Bronchodilator Euphyllinum is a bronchodilator. Euphyllinum works in several ways: it relaxes muscles in your lungs and chest to allow more air in, decreases the sensitivity of your lungs to allergens and other substances that cause inflammation, and increases the contractions of your diaphragm to draw more air into the lungs. What other drugs will affect Euphyllinum? Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them.
aminophylline 24 mg
Excipients: water d/i – up to 1 ml.
Bronchodilator, 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 type III and type IV isoenzymes. Suppression of the activity of these isoenzymes may also cause some side effects of aminophylline (theophylline), including vomiting, arterial hypotension and tachycardia. Blocks adenosine (purine) receptors, which may be a factor in action on the bronchi.
Reduces airway hyperresponsiveness associated with the late phase of the response induced 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.
It increases mucociliary clearance, stimulates diaphragm contraction, improves respiratory and intercostal muscle function, stimulates the respiratory center, increases its sensitivity to carbon dioxide, 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. Enhances lung ventilation in conditions of hypokalemia.
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.
In the body, aminophylline is metabolized at physiological pH values with release of free theophylline. Bronchodilator properties are manifested at plasma concentrations of theophylline of 10-20 µg/ml. Concentrations above 20 mg/ml are toxic. The excitatory effect on the respiratory center is realized at a lower concentration of 5-10 µg/ml.
Theophylline’s binding to plasma proteins is approximately 40%; in neonates as well as in adults with disease, the binding decreases. Binding to plasma proteins in adults is about 60%, in newborns 36%, in patients with cirrhosis 36%. It penetrates the placental barrier (the concentration in the fetal serum is slightly higher than in the mother’s serum). It is excreted with 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 newborns a significant portion is excreted as caffeine (due to the immaturity of its further metabolic pathways), unchanged – 50%.
Significant individual differences of hepatic metabolic 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.
T1/2 of theophylline in non-smoking patients with bronchial asthma practically without pathological changes from other organs and systems is 6-12 h, in smokers – 4-5 h, in children – 1-5 h, in newborns and premature infants – 10-45 h.
T1/2 of theophylline is increased in elderly people and patients with heart failure or liver diseases.
Clearance decreases in heart failure, liver dysfunction, chronic alcoholism, pulmonary edema, COPD.
Ethylenediamine does not affect the pharmacokinetics of theophylline.
For parenteral use: asthmatic status (additional therapy), neonatal apnea, cerebral circulation disorders of ischemic type (in combination therapy), left ventricular failure with bronchospasm and Cheyne-Stokes type breathing disorders, edema syndrome of renal genesis (in combination therapy), acute and chronic heart failure (in combination therapy).
Oral administration: bronchoobstructive syndrome of different genesis (including bronchial asthma, COPD, including pulmonary emphysema, chronic obstructive bronchitis), hypertension in the small circle of the circulation, pulmonary heart, nighttime apnea, acute and chronic heart failure (in combination therapy).
Severe arterial hyper- or hypotension, tachyarrhythmias, gastric and duodenal ulcer in the acute phase, hyperacid gastritis, severe liver and/or renal dysfunction, epilepsy, hemorrhagic stroke, retinal hemorrhage, concomitant use with ephedrine in children, childhood (under 3 years, for prolonged oral forms under 12 years), hypersensitivity to aminophylline and theophylline.
Nervous system disorders: dizziness, sleep disturbances, anxiety, tremors, convulsions.
Cardiovascular system: palpitations, disorders of heart rhythm, with rapid IV administration – the appearance of pain in the heart, BP decrease, tachycardia (including in the fetus when taken in the III trimester of pregnancy), arrhythmias, BP decrease, cardialgia, increased frequency of angina pectoris attacks.
Digestive system: nausea, vomiting, gastroesophageal reflux, heartburn, aggravation of peptic ulcer disease, diarrhea, with prolonged oral administration – anorexia.
Urinary system: albuminuria, hematuria.
Allergic reactions: skin rash, itching, fever.
Metabolism: rarely – hypoglycemia.
Local reactions: thickening, hyperemia, painfulness at the injection site, irritation of rectal mucosa when using rectally, proctitis.
Other: chest pain, tachypnoea, sensation of hot flashes in the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.
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