Euphyllin injection solution ampoules 2.4% 5ml N10
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Description
Injection solution 2.4% aminophylline in ampoules - a drug with a bronchodilator effect.
Composition
Aminophylline, incl. theophylline, ethylenediamine.
Pharmacological effect
Bronchodilator, PDE inhibitor. It is theophylline ethylene diamine salt (which facilitates solubility and increases absorption). It has a bronchodilator effect, apparently due to a direct relaxing effect on the smooth muscles of the respiratory tract and blood vessels of the lungs. It is believed that this action is caused by the selective inhibition of the activity of specific PDEs, 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 play isoenzymes III and IV types. Suppression of the activity of these isoenzymes may also cause some side effects of aminophylline (theophylline), including vomiting, hypotension and tachycardia. Blocks adenosine (purine) receptors, which may be one of the factors of action on the bronchi. Reduces airway hyperreactivity associated with the late phase of the reaction caused by inhalation of allergens through an unknown mechanism that does not relate to the inhibition of PDE or to the blockade of adenosine action. There are reports that aminophylline increases the number and activity of T-suppressors in peripheral blood. Increases mucociliary clearance, stimulates contraction of the diaphragm, improves the function of the respiratory and intercostal muscles, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of episodes of apnea. Normalizing the respiratory function, helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide. Strengthens ventilation of the lungs in the conditions of a hypokalemia. It has a stimulating effect on the activity of the heart, increases strength and heart rate, increases coronary blood flow and increases the need for oxygen in the myocardium. Reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, lowers pressure in the pulmonary circulation.Increases renal blood flow, has a moderate diuretic effect. Expands extrahepatic biliary tract. Stabilizes the membranes of mast cells, inhibits the release of mediators of allergic reactions. It inhibits platelet aggregation (inhibits platelet activating factor and PgE2α), increases erythrocyte resistance to deformation (improves the rheological properties of blood), reduces thrombosis and normalizes microcirculation. It has a tocolytic effect, increases the acidity of gastric juice. In high doses, it has an epileptogenic effect.
Pharmacokinetics
In the body, aminophylline is metabolized at physiological pH values with the release of free theophylline. Bronchodilating properties appear at plasma concentrations of theophylline 10–20 mcg / ml. Concentration over 20 mg / ml is toxic. The stimulating effect on the respiratory center is realized at a lower concentration - 5-10 μg / ml. Binding of theophylline to plasma proteins is approximately 40%, in newborns, as well as in adults with diseases, the binding decreases. Plasma protein binding is about 60% in adults, 36% in newborns, and 36% in patients with liver cirrhosis. Penetrates through the placental barrier (the concentration in the serum of the fetus is slightly higher than in the mother's serum). It is excreted in breast milk. Theophylline is metabolized in the liver with the participation of several cytochrome P450 isoenzymes, the most important of which is CYP1A2. In the process of metabolism 1,3-dimethyl uric acid, 1-methyl uric acid and 3 methylxanthine are formed. These metabolites are excreted in the urine. Unchanged in adults is 10%. In newborns, a significant part is excreted in the form of caffeine (due to the immaturity of the pathways of its further metabolism), unchanged - 50%. Significant individual differences in the rate of hepatic metabolism of theophylline are the reason for the pronounced variability of clearance values, plasma concentrations, and half-life. The hepatic metabolism is influenced by such factors as age, addiction to tobacco smoking, diet, diseases, simultaneously conducted drug therapy. T1 / 2 of theophylline in non-smoking patients with asthma with virtually 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 babies - 10- 45 hours. T1 / 2 of theophylline is increased in the elderly and in patients with heart failure or liver disease.Clearance decreases with heart failure, abnormal liver function, chronic alcoholism, pulmonary edema, chronic obstructive pulmonary disease. Ethylenediamine does not affect theophylline pharmacokinetics.
Indications
For parenteral use: asthmatic status (adjuvant therapy), neonatal apnea, ischemic type cerebral circulation disorder (as part of combination therapy), left ventricular failure with bronchospasm and Cheyne-Stokes type respiratory disorder, edematous syndrome of renal genesis (as part of complex therapy) , acute and chronic heart failure (as part of combination therapy). For oral administration: broncho-obstructive syndrome of various genesis (including bronchial asthma, COPD, including pulmonary emphysema, chronic obstructive bronchitis), hypertension in the pulmonary circulation, pulmonary heart, sleep apnea, acute and chronic heart failure (as part of a combination therapy ).
Contraindications
Severe arterial hyper- or hypotension, tachyarrhythmias, gastric ulcer and duodenal ulcer in the acute phase, hyperacid gastritis, severe dysfunction of the liver and / or kidneys, epilepsy, hemorrhagic stroke, retinal hemorrhage, concurrent use with ephedrine in children, pediatric and pediatric, pediatric (up to 3 years, for prolonged oral forms - up to 12 years), hypersensitivity to aminophylline and theophylline.
Precautionary measures
Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina), widespread atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive readiness, in case of hepatic and / or renal failure, gastric ulcer, increased convulsive readiness, in case of hepatic and / or renal failure, gastric ulcer and hemorrhage, increased convulsive readiness, in case of hepatic and / or renal failure, gastric ulcer and hemorrhage, increased convulsive readiness, in case of hepatic and / or renal failure, gastric ulcer and hemorrhage, increased convulsive readiness, in case of hepatic and / or renal failure, gastric ulcer and hemorrhagic arrhythmia, increased convulsive readiness with recent bleeding from the gastrointestinal tract, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, with prolonged hyperthermia, gastroesophageal At reflux, hypertrophy of the prostate gland, in patients in the elderly, in children (especially inside). Correction of the dosing regimen of aminophylline may be required for heart failure, abnormal liver function, chronic alcoholism,fever, orz. Elderly patients may require a dose reduction. When replacing the used dosage form of aminophylline to another, clinical observation and control of theophylline concentration in the blood plasma is necessary. Aminophylline is not used simultaneously with other xanthine derivatives. During treatment, you should avoid eating foods containing xanthine derivatives (strong coffee, tea). With caution used simultaneously with anticoagulants, with other derivatives of theophylline or purine. Avoid simultaneous use with beta-blockers. Aminophylline should not be used simultaneously with glucose solution. Do not use rectally in children
Use during pregnancy and lactation
Theophylline penetrates the placental barrier. The use of aminophylline during pregnancy can lead to the creation of potentially dangerous concentrations of theophylline and caffeine in the plasma of the newborn. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) need medical supervision to control the possible symptoms of theophylline intoxication. Theophylline is excreted in breast milk. When aminophylline is used in a lactating mother during lactation, irritability of the baby may occur. Thus, the use of aminophylline during pregnancy and lactation (breastfeeding) is possible in cases where the intended benefit of therapy for the mother outweighs the potential risk to the fetus or child.
Dosage and administration
Individual, depending on the evidence, age, clinical situation, route of administration, nicotine addiction.
Side effects
From the side of the central nervous system: dizziness, sleep disturbance, anxiety, tremor, convulsions. From the side of the cardiovascular system: feeling of heartbeat, heart rhythm disturbances, with fast i / v administration - the appearance of pain in the heart area, decrease in blood pressure, tachycardia (including in the fetus during admission in the third trimester of pregnancy), arrhythmia, decrease HELL, cardialgia, an increase in the frequency of strokes. On the part of the digestive system: nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with prolonged ingestion - anorexia.From the urinary system: albuminuria, hematuria. Allergic reactions: skin rash, itching, fever. Metabolism: rarely - hypoglycemia. Local reactions: induration, hyperemia, soreness at the injection site, rectal irritation of the rectal mucosa, proctitis. Other: pain in the chest, tachypnea, sensation of hot flashes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.
Interaction with other drugs
With simultaneous use with sympathomimetics, mutual enhancement of action occurs, with beta-blockers and lithium preparations - the action mutually decreases. The intensity of the action of aminophylline may decrease (due to an increase in its clearance), while being used with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin, and also in smokers. The intensity of the action of aminophylline may increase (due to a decrease in its clearance) with simultaneous use with macrolide antibiotics, lincomycin, quinolones, allopurinol, beta-adrenergic blockers, cimetidine, disulfiram, fluvoxamine, hormonal contraceptives for ipoprostinamia, ioprenamide, hormonal contraceptives for inhalation, isopropyne, hormone contraceptives for inhalation, ioprenylamino, hormonal contraceptives, cimetidine, disulfiram, fluvoxamine the flu. Xanthine derivatives can potentiate hypokalemia caused by the action of stimulators β2-adrenoreceptors, corticosteroids and diuretics. Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline. Pharmaceutical incompatible with acid solutions.
special instructions
With care: patients of advanced age (reduction of a dose can be required). Contraindicated in severe violations of the liver. Use caution when liver failure. Contraindicated in severe renal impairment. Use caution in renal failure. Contraindications: children (up to 3 years, for prolonged oral forms - up to 12 years). Do not use rectally in children.