Active substanceAminophyllineAminophylline
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  • Dosage form: & nbspsolution for intramuscular injection
    Composition:

    Active substance: aminophylline (euphyllin for injection) (in terms of dry matter) 240 mg

    Excipients: water for injection - up to 1ml.

    Description:transparent colorless or light yellow liquid.
    Pharmacotherapeutic group:bronchodilator.
    ATX: & nbsp

    R.03.D.A.05   Aminophylline

    Pharmacodynamics:

    The xanthine derivative inhibits phosphodiesterase, increases accumulation in the tissues of cyclic adenosine monophosphate, blocks adenosine (purine) receptors; reduces the flow of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles.

    Relaxes the musculature of the bronchi, it relieves bronchospasm. Has a moderate inotropic and diuretic effect.

    Reduces vascular resistance,It reduces the tonus of blood vessels (mainly the brain, skin and kidney), dilates coronary vessels, reduces the pressure in the pulmonary artery, improves contraction of the diaphragm, increases mucociliary clearance, stimulating the respiratory center, increases the release of adrenal glands, inhibits platelet aggregation, improves.

    Pharmacokinetics:

    60% of euphillin (in healthy adults) and 36% (in newborns) binds to plasma proteins and is distributed in the blood, extracellular fluid and muscle tissue. Eufillin penetrates through the placental and blood-brain barrier, in adipose tissue does not accumulate. 90% of euphyllin is metabolized in the liver. Metabolites are excreted by the kidneys, 7-13% of euphyllinus is released unchanged. The half-life is for non-smokers from 5 to 10 hours, for children over 10 months from 2.5 to 5 hours. Smoking and alcohol significantly affect the metabolism and release of euphyllin, in particular, this period is significantly reduced for smokers and ranges from 4 to 5 hours. The excretion of euphyllinum is prolonged in patients with respiratory failure, with hepatic and cardiac failure, with viral infections and hyperthermia.

    Indications:

    Bronchoobstructive syndrome in bronchial asthma, bronchitis, pulmonary emphysema, cardiac asthma (mainly for relief of seizures); hypertension in a small circle of blood circulation.

    Relief of cerebral vascular crises of atherosclerotic origin, and as part of combination therapy for ischemic stroke and chronic cerebrovascular insufficiency to reduce intracranial pressure and cerebral edema.

    Contraindications:

    Severe arterial hypotension or hypertension, paroxysmal tachycardia, extrasystole, myocardial infarction with heart rhythm disturbances, epilepsy, increased convulsive alertness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and / or renal insufficiency, hemorrhagic stroke, retinal hemorrhage eyes, bleeding in a recent medical history, hypersensitivity to the drug.

    Carefully:

    Pregnancy, newborn, age over 55 years, and uncontrolled hypothyroidism (possibility of cumulation), sepsis, prolonged pyrexia, gastroesophageal reflux disease, prostate adenoma.

    The drug is administered with caution to patients with severe impairment of liver and kidney function, peptic ulcer of the stomach and duodenum.

    Pregnancy and lactation:

    Use in pregnancy is possible in cases where the intended benefit of therapy for the mother exceeds the potential risk to the fetus. For the duration of treatment, stop breastfeeding.

    Dosing and Administration:

    Euphyllin is prescribed intramuscularly, deep into the upper quadrant of the gluteus muscle, 1 ml (240 mg) of the solution.

    Parenterally enter euphyllin up to 3 times a day, no more than 14 days.

    The concentration of euphyllin in serum should not exceed 20 μg / ml.

    Higher doses of euphyllin for adults intramuscularly: single - 0.5 g, daily - 1.5 g. Higher doses for children intramuscularly: single - 7 mg / kg, daily - 15 mg / kg.

    Correction of the dosing regimen may be required for heart failure, violations of liver function, chronic alcoholism. In elderly patients, a dose reduction may be required (a single dose of 0.3 g). Smoking patients are recommended to increase the dose in connection with the accelerated removal of the drug from the body (a single dose of 0.7 g).

    Side effects:

    From the digestive system: gastroesophageal reflux, gastralgia, nausea, vomiting, heartburn, exacerbation of peptic ulcer.

    From the nervous system: headache, insomnia, agitation, anxiety, anxiety, irritability, dizziness, tremor.

    From the cardiovascular system: palpitations, arrhythmias, tachycardia, cardiac rhythm disturbance, lowering of arterial pressure, cardialgia, an increase in the frequency of angina attacks.

    Allergic reactions: skin rash, skin itching, fever.

    Local reactions: reactions at the injection site - hyperemia, tenderness.

    Other: chest pain, tachypnea, albuminuria, hematuria, hypoglycemia, increased sweating, increased diuresis.

    Overdose:

    When an overdose occurs, anorexia, diarrhea, nausea, vomiting, epigastric pain, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized convulsions, hyperventilation, a sharp drop in blood pressure.

    Treatment of overdose depends on the clinical picture, includes the abolition of the drug, stimulation of its removal from the body (forced diuresis, hemosorption, plasmosorption,hemodialysis, peritoneal dialysis) and the use of symptomatic agents. For cramping seizures applied diazepam (in injections). Do not use barbiturates.

    At the expressed intoxication (the maintenance of an eufillina more than 50 g / l) the hemodialysis is recommended.

    Interaction:

    Ephedrine, beta-adrenostimulators, caffeine and furosemide increase the effect of the drug. In combination with phenobarbital, diphenin, rifampicin, isoniazid, carbamazepine or sulfinpyrazone, a decrease in the efficacy of euphyllin is observed, which may require an increase in the applied doses of the drug.

    The clearance of the drug is reduced when it is administered in combination with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, which may require a dose reduction.

    Oral estrogen-containing contraceptives, antidiarrheal drugs, intestinal sorbents weaken, and H2-histaminoblockers, slow calcium channel blockers, mexiletine intensify the action (bind to the enzymatic system of cytochrome P450 and slow the metabolism of euphyllin).When used in combination with epoxacin and other fluoroquinolines, the dose of euphyllin is reduced. The drug inhibits the therapeutic effects of lithium carbonate and beta-blockers. The administration of beta-blockers inhibits the bronchodilating action of euphyllin and can cause bronchospasm. Eufillin potentiates the action of diuretics by increasing the glomerular filtration and reducing tubular reabsorption. With caution, euphyllin is prescribed concomitantly with anticoagulants, with other theophylline derivatives or purine. It is not recommended to use eufillin with agents that excite the central nervous system (increases neurotoxicity). Eufillin solution for intramuscular injection can not be diluted or mixed with other solutions.

    Special instructions:

    Under the skin, solutions of euphyllin are not administered, since they have a locally irritating effect.

    Effect on the ability to drive transp. cf. and fur:When treating the drug, patients are advised not to perform a work that requires quick reaction and associated risks, for example, to drive vehicles within 24 hours.
    Form release / dosage:

    Solution for intramuscular injection 240 mg / ml.

    Packaging:

    1 ml per ampoule of neutral glass. 10 ampoules together with instructions for use and a knife for opening ampoules or a scarifier ampoule in a box of cardboard. 5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil printed lacquered, or without foil. 2 contoured cell packs together with instructions for use and a knife for opening ampoules or a scarifier ampullum in a pack of cardboard.

    When using ampoules with notches, rings and dots, an ampoule scarifier or a knife for opening ampoules is allowed not to be put.
    Storage conditions:

    At a temperature of 5 to 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years. Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000590
    Date of registration:25.02.2011
    The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.02.2011
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