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

Bronchodilator, purine derivative; inhibits phosphodiesterase, increases accumulation in cAMP tissues, 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, 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 the respiratory function, contributes to the saturation of blood oxygen and reduce the concentration of carbon dioxide.

Has a stimulating effect on the activity of the heart, increases the strength and number of heartbeats, increases coronary blood flow and the need for myocardium in oxygen. Reduces the tone of blood vessels (mainly, the 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.

Stabilizes the membrane of mast cells, inhibits the release of mediators of allergic reactions.

It inhibits platelet aggregation (suppresses the platelet activation factor and PgE2 alpha), increases the resistance of erythrocytes to deformation (improves the rheological properties of the 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:

After oral administration, it is quickly and completely absorbed, bioavailability is 90-100%. Food reduces the rate of absorption, without affecting its magnitude (large volumes of fluid and proteins speed up the process). The higher the dose taken, the lower the absorption rate. The time to reach the maximum concentration is 1-2 hours. The volume of distribution is in the range 0.3-0.7 l / kg (30-70% of the "ideal" body weight), an average of 0.45 l / kg. The connection with plasma proteins in adults is 60%, in patients with cirrhosis of the liver - 36%. 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).

Bronchodilator properties aminophylline shows in concentrations of 10-20 μg / ml. Concentration above 20 mg / ml is toxic. Exciting effect on the respiratory center is realized with a lower content of the drug in the blood - 5-10 μg / ml.

Metabolized at physiological pH values with the release of free theophylline, which is further metabolized in the liver with the participation of several cytochrome P450 isoenzymes. As a result, 1,3-dimethylurea (45- 55%) is formed, which has pharmacological activity, but is 1-5 times inferior to theophylline. Caffeine is an active metabolite and is formed in small amounts.In children over 3 years and in adults (unlike younger children), the phenomenon of caffeine cumulation is absent.

T1 / 2 in children older than 6 months - 3.7 hours; in adults - 8.7 hours; in "smokers" (20-40 cigarettes a day) - 4-5 h (after quitting smoking, normalization of pharmacokinetics through 3-4 months); the

adults with chronic obstructive pulmonary disease, "pulmonary" heart and legochnoserdechnoy failure -. more than 24 hours excreted by the kidneys.

Indications:

Bronchial obstruction of any genesis: bronchial asthma (drug of choice in patients with asthma physical stress and as an adjunct with other forms.), Chronic obstructive pulmonary disease (chronic obstructive bronchitis, emphysema).

Pulmonary hypertension, "pulmonary" heart, sleep apnea.

Contraindications:Increased sensitivity to the drug (incl to other xanthine derivatives.: caffeine, pentoxifyllineTheobromine), epilepsy, peptic ulcer and 12 duodenal ulcer (in the acute stage), gastritis with high acidity, arterial hyper- or hypotension, severe, tachyarrhythmias, hemorrhagic stroke, bleeding in the retina of the eye, children's age (up to 3 years) .

Carefully:

coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis of vessels, hypertrophic obstructive cardiomyopathy, frequent extrasystole, increased convulsive readiness, hepatic and / or renal insufficiency, peptic ulcer and 12 duodenal ulcer (a history), gastrointestinal bleeding in a recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostate adenoma, pregnancy, lactation period old age, children's age (over 3 years old).

Pregnancy and lactation:

Application in pregnancy and lactation is possible only for "vital" indications.

Dosing and Administration:

Inside, adults should be prescribed 150 mg at the reception 1-3 times a day after meals. Children inside should be prescribed at a rate of 7-10 mg / kg per day in 4 divided doses. The duration of the course of treatment is from several days to several months, depending on the course of the disease and the tolerability of the drug.

Higher doses of euphyllin for adults: single-dose 0.5 g, daily - 1.5 g.

Higher doses for children: single dose - 7 mg / kg, daily - 15 mg / kg.

Side effects:

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

From the cardiovascular system: palpitation, tachycardia (including the fetus when taking a pregnant woman in the third trimester), arrhythmias, cardialgia, a decrease in blood pressure, an increase in the frequency of angina attacks.

From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with prolonged admission - a decrease in appetite.

Allergic reactions: skin rash, itching, fever.

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

Side effects decrease with a decrease in the dose of the drug.

Overdose:

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial skin hyperemia, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions .In severe poisoning may develop epileptic seizures (especially in children without incurring any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, necrosis of skeletal muscles, confusion, renal failure with myoglobinuria.

Treatment: removal of the drug, gastric lavage, appointment of activated charcoal, laxative drugs, intestinal lavage combination of polyethyleneglycol and electrolytes, diuresis, hemosorbtion, plasmasorption, hemodialysis (efficiency is not high, peritoneal dialysis is not effective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting). If seizures occur, maintain airway patency and conduct oxygen therapy. To stop the seizure - intravenously diazepam - 0.1-0.3 mg / kg (not to exceed 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (w / w).

Interaction:

Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), funds for general anesthesia (increases the risk of ventricular arrhythmias), xanthines and drugs that excite the central nervous system (increases neurotoxicity), beta-adrenostimulants.

Antidiarrhoeal drugs and enterosorbents reduce the absorption of aminophylline.

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.

When combined with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon-alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil, and with influenza vaccination, the intensity 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 xanthine derivatives. With caution appoint simultaneously with anticoagulants.

Form release / dosage:

Tablets 150 mg.

Packaging:For 30 tablets in banks of type BTS - OS; 10, 20 or 25 tablets per contour cell package. Each bank or 1, 2, 3, 4 or 5 contour cellular packs, together with instructions for use, are placed in a pack of cardboard.

Storage conditions:List B. In dry, protected from light, out of reach of children, at a temperature not exceeding 25 ° C.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015616 / 01

Date of registration:18.05.2009

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp24.03.2011

Illustrated instructions

Instructions

Eufillin (Euphyllini)