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

The drug 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 muscles of the bronchi, stops bronchospasm, increases mucociliary clearance, stimulates the 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 reduces the severity and frequency of episodes of apnea.Normalizing respiratory function, promotes saturation of blood with oxygen and decrease in the concentration of carbon dioxide. Strengthens lung ventilation in conditions hypokalemia. Has a stimulating effect on the activity of the heart, increases the strength and heart rate, increases coronary blood flow and the need for myocardium in oxygen. Reduces the tone of blood vessels (mainly vessels of the brain, skin and kidneys). Has peripheral venodilating effect, reduces pulmonary vascular resistance, lowers pressure in the "small" circle of blood circulation.

Increases renal blood flow, has a moderate diuretic effect.

Expands extrahepatic biliary tract. It inhibits platelet aggregation (suppresses the platelet and prostaglandin E2 alpha activation factor), increases the resistance of erythrocytes to deformation (improves rheological properties of blood), reduces thrombus formation and normalizes microcirculation. Has tocolytic effect, increases the acidity of gastric juice. When used in large doses has an epileptogenic effect.

Pharmacokinetics:

Bioavailability for liquid dosage forms is 90-100%.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. Penetrates into breast milk (10% of the dose), through the placental barrier (concentration in the fetal serum is slightly higher than in the mother's serum). 90% of the drug is metabolized in the liver. Metabolites are excreted 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 and alcohol significantly affect the metabolism and release of the drug, particularly among smokers, this period is significantly reduced and ranges from 4 to 5 hours. Removal of the drug 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 the "small circle" of the circulation.

Violation of cerebral circulation by ischemic type (as part of combination therapy to reduce intracranial pressure).

Left ventricular heart failure with bronchospasm and respiratory depression according to the Chain-Stokes type (as part of complex therapy).

Contraindications:

Hypersensitivity to the drug (including other xanthine derivatives: caffeine, pentoxifylline, theobromine). Severe arterial hypotension or hypertension, paroxysmal tachycardia, extrasystole, myocardial infarction with cardiac rhythm disturbances, epilepsy, increased convulsive alertness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and / or renal insufficiency, hemorrhagic stroke, retinal hemorrhage , bleeding in a recent anamnesis, lactation period.

Carefully:

pregnancy, newborn, age over 55 years, and uncontrolled hypothyroidism (possibility of cumulation), widespread atherosclerosis, sepsis, prolonged pyrexia, gastroesophageal reflux disease, peptic ulcer and duodenal ulcer (in history), prostate adenoma.

The drug is not recommended for intravenous administration to children under 14 years of age (due to possible side effects).

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.

Dosing and Administration:

Adults inject slowly (within 4-6 minutes) with 5-10 ml of a solution of 24 mg / ml (0.12-0.24 g), which is previously diluted in 10-20 ml of 0.9% sodium chloride solution. At occurrence of palpitation, a giddiness, a nausea speed of introduction slow down or pass to dropwise introduction for what 10-20 ml of a solution of 24 mg / ml (0,24-0,48) are dissolved in 100-150 ml of 0,9% of a solution of sodium of chloride ; injected at a rate of 30-50 drops per minute. Parenterally enter euphyllin up to 3 times a day, no more than 14 days. If necessary, children are administered intravenous eufillin at a dose of 2-3 mg / kg, preferably drip.

Higher doses of euphyllin for adults intravenously: single - 0.25 g, daily - 0.5 g. Higher doses for children intravenously: single dose - 3 mg / kg, daily - at the age of 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 years - 0,12-0,24 g, from 8 to 18 years - 0,25-0,5 g.

Side effects:

From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor, rarely - convulsions, nausea, vomiting.

On the part of the cardiovascular system: heartbeat, tachycardia (including fetus when taking a pregnant woman in the third trimester), arrhythmias, cardialgia, an increase in the frequency of angina attacks, lowering blood pressure right up to collapse - with a rapid IV injection

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

Allergic reactions: skin rash, skin itching, fever.

Other: chest pain, tachypnea, sensation of hot flashes to the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

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

Overdose:

Symptoms: anorexia, gastralgia, diarrhea, nausea, vomiting, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized convulsions, hyperventilation. In severe poisoning, epileptic seizures may develop (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, lowering blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria.

Treatment: drug withdrawal, forced diuresis, hemosorption, plasmasorption, hemodialysis (peritoneal dialysis is ineffective), the appointment of symptomatic drugs. 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:

Pharmaceutically incompatible with acid solutions. Increases the likelihood of side effects of glucocorticosteroids, mineral corticosteroids (hypernatremia), funds for general anesthesia (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system (increases neurotoxicity).

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracisin, as inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.

With the simultaneous use with antibiotics of a group of macrolides, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses ethanol, disulfiram, fluoroquinolones, recombinant alpha interferon, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and vaccination against influenza, the intensity of action of aminophylline may increase, which may require a reduction in its dose. Strengthens the action of beta-adrenostimulators and diuretics (including by increasing the glomerular filtration), reduces the effectiveness of lithium and beta-blockers.

Compatible with antispasmodics, do not use together with other derivatives of xanthine.

With caution appoint simultaneously with anticoagulants.

Special instructions:

A drug appoint with caution to patients with severe impairment of liver and kidney function, peptic ulcer of the stomach and duodenum.

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.

Be careful when consuming large quantities of caffeine-containing foods or drinks during the treatment period.

Before parenteral administration, the solution must be heated to body temperature.

Form release / dosage:

Solution for intravenous administration of 24 mg / ml in ampoules of 5 ml or 10 ml.

Packaging:

For 10 ampoules with instructions for use, with an ampoule or ampoule ampoule knife in a pack or box of cardboard.

When packaging ampoules that have a break ring or an opening point, the ampoule knife or the ampoule scapegrator is not put in.

5 ampoules in a cassette outline package. 2 cassette contour packs with instructions for use in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of 5 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-002028

Date of registration:14.10.2011

The owner of the registration certificate:MICROGEN FGUP Scientific and Production Association MICROGEN FGUP Scientific and Production Association Russia

Manufacturer: & nbsp

NGO MICROGEN, FSUE Russia

Information update date: & nbsp30.05.2013

Illustrated instructions

Instructions

Eufillin (Euphyllini)