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

Bronchodilator, purine derivative; inhibits phosphodiesterase, increases accumulation in tissues of adenosine monophosphate (cAMP), 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 leads to a reduction in 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 increases 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 membranes 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 of 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, caffeine and 1,3-dimethylurea (45-55%), which has pharmacological activity, but 1-5 times less than theophylline. Caffeine is also an active metabolite, but is formed in small amounts. In children over 3 years and in adults (unlike younger children), the phenomenon of caffeine cumulation is absent. Half-life of it in children older than 6 months is 3.7 hours, for adults 8.7 hours, for smokers (20-40 cigarettes per day) -4-5 hours (after quitting smoking, normalization of pharmacokinetics after 3-4 months); in adults with chronic obstructive pulmonary disease, pulmonary heart disease and pulmonary heart disease - more than 24 hours. Metabolites are excreted through the kidneys.

Indications:

Bronchoobstructive syndrome of any origin; bronchial asthma (the drug of choice in patients with asthma of physical stress and as an adjunct in other forms), chronic obstructive pulmonary disease (chronic obstructive bronchitis, emphysema). Pulmonary hypertension, "pulmonary" heart, nocturnal apnea.

Contraindications:

Hypersensitivity to the drug (including other xanthine derivatives: caffeine, pentoxifylline, theobromine), epilepsy, peptic ulcer and duodenal ulcer (at the stage of exacerbation), gastritis with high acidity, severe arterial hyper- and hypotension, tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, children's age (up to 3 years).

Carefully:

Coronary heart disease (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis of the blood vessels, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive alertness, hepatic and / or renal insufficiency, peptic ulcer and duodenal ulcer (in the anamnesis), gastro- intestinal hemorrhage in a recent medical history, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostate adenoma s, pregnancy, lactation, old age, children's age.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the risk to the fetus.

If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

Inside, adults should be prescribed 0.15 g 1-3 times daily 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 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, head rash, insomnia, agitation, anxiety, irritability, tremor.

From the cardiovascular system: palpitation, tachycardia (including the fetus when taking a pregnant woman in the III 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 of the stomach, 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, epileptic seizures may develop (especially in children without precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria. Treatment: drug withdrawal, gastric lavage, the appointment of activated carbon, laxative drugs, washing the intestine with a combination of polyethylene glycol and electrolyte, forced diuresis, hemosorption, plasmosorption, hemodialysis (efficacy is not great, 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 seizures, diazepam intravenously at a dose of 0.1-0.3 mg / kg (not more than 10 mg). With severe nausea and vomiting - metoclopramide and ondansetron (intravenously).

Interaction:

It increases the likelihood of side effects of glucocorticosteroids and mineralokortikosteroidov (hypernatremia), funds for general anesthesia (the risk of ventricular arrhythmias), xanthine and means that excite the central nervous system (increases neurotoxicity), beta-agonists.

Antidiarrhoeal drugs and enterosorbents reduce the absorption of aminophylline.

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, Oral estrogen-containing contraceptives and moratsizin, as inducers of microsomal oxidation increase aminophylline clearance, which may require increasing the dose.

While the use of antibiotic macrolide, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses of ethanol, disulfiram. fluoroquinolones, recombinant interferon-alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine ,, verapamil and influenza vaccination rate of aminophylline action may increase, which may require a reduction of the dose.Increases the effect of beta-adrenostimulators and diuretics (including by increasing 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.

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

During the period of drug treatment, care should be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 150 mg.

Packaging:For 10, 15, 20 tablets in a planar cell package. By 1, 2, 3 or 5 contour squares with instructions in a cardboard box.

Storage conditions:Store at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Shelf life:

5 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-001105

Date of registration:22.12.2009

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp24.12.2014

Illustrated instructions

Instructions

Eufillin (Euphyllini)