Eufillin - instructions for use, dose, side effects, contraindications

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. Aminophylline lowers vascular resistance,reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys), dilates the coronary vessels, lowers the pressure in the pulmonary artery system, improves the contraction of the diaphragm, increases mucociliary clearance, inhibits the release of mediators (histamine and leukotrienes) from mast cells, stimulates the respiratory center, increases the adrenaline release of the adrenal glands, inhibits platelet aggregation (suppresses the platelet and prostaglandin E2 alpha activation factor), increases the resistance of erythrocytes to deformation (improves re logical properties of blood), reduces thrombogenesis and normalize microcirculation.

Pharmacokinetics:

The bioavailability of the preparation is 90-100%, the time required to reach the maximum concentration for intravenous administration of 0.3 g is 15 minutes, the maximum concentration is 7 μg / ml. The volume of distribution is in the range 0.3-0.7 l / kg (30-70% of the "ideal" body weight), averaging 0.45 l / kg. 60% of aminophylline in healthy adults and 36% in newborns binds to plasma proteins and is distributed in the blood, extracellular fluid and muscle tissue. Aminophylline penetrates the placental and blood-brain barrier, does not accumulate in adipose tissue. 90% of the drug is metabolized in the liver, Metabolites are secreted by the kidneys, 7-13% of the drug is excreted 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, alcohol significantly affect the metabolism and excretion of the drug, in particular among smokers this period is significantly reduced and ranges from 4 to 5 hours. Elimination of the drug is prolonged in patients with respiratory failure, with renal and heart failure, with viral infections and hyperthermia.

Indications:

Bronchoobstructive syndrome with bronchial asthma, bronchitis, emphysema; hypertension in a small circle of blood circulation.

Violation of cerebral circulation by ischemic type (as part of combination therapy to reduce intracranial pressure). Left ventricular failure with bronchospasm and respiratory depression by the type of Cheyne-Stokes, edematous syndrome of renal genesis (as part of complex therapy).

Contraindications:

Hypersensitivity to the drug, as well as to other xanthine derivatives: caffeine, pentoxifylline, theobromine.

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 anamnesis.

Carefully:age over 55 years and uncontrolled hypothyroidism (the possibility of cumulation), widespread atherosclerosis of vessels, sepsis, prolonged hyperthermia, gastroesophageal reflux, peptic ulcer and a duodenal ulcer (in the anamnesis), prostatic hyperplasia, children under 14 years of age (due to possible side effects phenomena).

Pregnancy and lactation:

If it is necessary to prescribe the drug during pregnancy, one should compare the expected benefit to the mother and the potential risk to the fetus.If you need to use the drug during breastfeeding, breast-feeding should be discontinued.

Dosing and Administration:

Method of administration: intravenously. Adults inject slowly (for 4-6 minutes) to 5-10 ml of a 24 mg / ml solution (0.12-0.24 g), which is previously diluted in 10-20 ml of isotonic sodium chloride solution. With the appearance of palpitations, dizziness, nausea, the rate of administration slows down or changes to drop introduction, for which 10-20 ml of a 24 mg / ml solution (0.24-0.48 g) is diluted in 100-150 ml of isotonic sodium chloride solution; injected at a rate of 30-50 drops per minute. The drug is administered up to 3 times a day, no more than 14 days.

Higher doses of euphyllin for adults with intravenous administration: single - 0.25 g, daily - 0.5 g.

If necessary, children are injected with intravenous drip at the rate of 2-3 mg / kg.

Higher doses for children with intravenous administration: single dose - 3 mg / kg, daily - at the age of up to 3 months - 0,03-0,06 g, from 4 to 12 months - 0,06-0,09 g, from 2 to 3 years 0.09-0.12 g, from 4 to 7 lys - 0.12-0.24 g, from 8 to 18 years - 0.25-0.5 g.

Side effects:

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

From the side of the central nervous system: headache, anxiety, anxiety, irritability, dizziness, insomnia, tremors, convulsions.

From the cardiovascular system: palpitation, tachycardia, cardialgia, heart rhythm disturbance, increased frequency of angina attacks, lowering blood pressure right up to collapse - with rapid intravenous injection.

Allergic reactions: skin rash, skin itching, exfoliative dermatitis, febrile reaction.

Local reactions: reactions at the injection site - hyperemia, tenderness, denseness. Other: chest pain, tachypnea, albuminuria, hematuria, hypoglycemia, increased sweating, a sensation of "hot flashes" to the face, increased diuresis.

Overdose:

Symptoms: skin hyperemia, insomnia, motor excitement, anxiety, photophobia, anorexia, diarrhea, nausea, vomiting (including with blood), epigastric pain, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized convulsions, hyperventilation, a sharp drop in blood pressure. In severe poisoning, epileptic seizures may develop (especially in children withoutoccurrence of any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria.

Treatment: withdrawal of the drug, stimulation of excretion of the drug from the body (forced diuresis, hemosorption, plasmasorption, hemodialysis (efficacy is low), peritoneal dialysis is ineffective), symptomatic therapy (incl. metoclopramide). If seizures occur, maintain airway patency and conduct oxygen therapy. For cramping seizures - intravenously diazepam 0,1 -0,3 mg / kg (but not more than 10 mg). Do not use barbiturates.

Interaction:

Ephedrine, beta-adrenostimulators, caffeine and furosemide increase the effect of the drug. Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), funds for general anesthesia (the risk of ventricular arrhythmias increases). In combination with phenobarbital, phenytoin, rifampicin, isoniazid, carbamazepine or sulphinpyrazone, a decrease in the effectiveness of euphyllin is observed, which may require an increase in the doses used. Aminoglutethimide, moracizin, being inducers of microsomal oxidation, increase the clearance of euphyllin, which may require an increase in its dose.

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 change the metabolism of euphyllin). If used in combination with enoxacin and other fluoroquinolones, small doses of ethanol, disulfiram, recombinant interferon alpha, methotrexate, propafenone, thiabendazole, ticlopidine, verapamil, and when vaccinated against influenza, the intensity of the action of euphyllin may increase, which may require a reduction in its dose. 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 euphyllin with agents that excite the central nervous system (increases neurotoxicity). The drug can not be used with solutions of dextrose, is incompatible with solutions of fructose and levulose. The pH of the mixed solutions should be taken into account: pharmaceutically incompatible with acid solutions.

Special instructions:

Elderly patients are advised to reduce the dose of the drug due to delayed excretion of it from the body. Smoking patients are advised to increase the dose due to accelerated removal of the drug from the body.

Care must be taken when consuming large quantities of caffeine-containing foods or beverages during the treatment period.

Before use, the drug solution must be heated to body temperature.

Effect on the ability to drive transp. cf. and fur:

During treatment, it is not recommended to drive vehicles, as well as engage in activities that require speed of psychomotor reactions and precise movements.

Form release / dosage:

Solution for intravenous administration is 24 mg / ml.

Packaging:

5 ml or 10 ml into neutral glass ampoules.

For 10 ampoules, together with the instructions for use and a knife for opening ampoules or a scarifier ampoule are placed in a cardboard box.

When using ampoules with incisions, break points or rings, the ampoule opener or the ampoule scarifier may not be inserted.

Storage conditions:

In the dark place at a temperature of 2 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001731

Date of registration:18.11.2011

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp18.01.2012

Illustrated instructions

Instructions

Eufillin (Euphyllini)