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

Eufillin - a bronchodilator, a derivative of xanthine; 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, increases mucociliary clearance, stimulates the contraction of the diaphragm,improves the function of 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 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, reduces pressure in the "small" circle of blood circulation.

Increases renal blood flow, has a moderate diuretic effect.

Expands extrahepatic biliary tract.

TOrthositis 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 enileptogenic 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. Time to reach C_m_Oh - 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 acid (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. Half-life in children older than 6 months - 3.7 h; in adults, 8.7 hours; in "smokers" (20-40 cigarettes a 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 - over 24 hours. It is excreted by the kidneys.

Indications:

Bronchoobstructive syndrome of any origin: bronchial asthma (a drug of choice in patients with asthma of physical stress and as an additional remedy for other forms), chronic obstructive pulmonary disease, pulmonary emphysema, chronic obstructive bronchitis, pulmonary hypertension, pulmonary heart, nocturnal apnea.

Contraindications:

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

Carefully:

Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis of vessels, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive alertness, hepatic and / or renal failure, peptic ulcer and duodenal ulcer (in the anamnesis), bleeding from gastrointestinal tract in a recent history, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, hyperplasia prostate gland, pregnancy, lactation period, elderly age, children's age. Assign simultaneously with anticoagulants.

Pregnancy and lactation:

With care, pregnancy, lactation.

Dosing and Administration:

Inside, adult Euphyllin 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 inside: single - 0.5 g, daily - 1.5 g. Higher doses for children inside: single dose - 7 mg / kg, daily - 15 mg / kg.

Side effects:

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

From the side of the cardiovascular system: palpitations, tachycardia (including the fetus when taking a pregnant woman in the III trimester), arrhythmias, cardialgia, lowering blood pressure, increasing the frequency of angina attacks.

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

Allergic reactions: skin rash, itching, fever.

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

Overdose:

Symptoms: loss of 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 any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, lowering blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria.

Treatment: drug cancellation, gastric lavage, application activated carbon, laxatives, intestinal washing with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasmosorption, hemodialysis (efficacy 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. For seizure seizure - in / in diazepam 0.1-0.3 mg / kg (but not more than 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 liver enzymes, 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, tiabendazole, ticlopidine, verapamil and influenza vaccination, the 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.

Special instructions:

Be careful when consuming large quantities of caffeine-containing foods or beverages.

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

During the treatment period, it is necessary to refrain from driving transport and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, 150 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

10, 20, 30, 40, 50, 60 or 100 tablets are placed in a polymer can with the first opening control and a shock absorber, or a polymer can with the first opening control, or a can of polyethylene terephthalate for drugs with closures.

If necessary Tablet-free space in cans is filled with cotton absorbent medical cotton.

One jar or 1, 2, 3, 4, 5, 6 or 10 contour mesh packages together with the instruction for use are placed in a cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 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:LP-003432

Date of registration:02.02.2016

Expiration Date:02.02.2021

The owner of the registration certificate:UZOLE-SIBERIAN CHEMICAL PLANT, OJSC UZOLE-SIBERIAN CHEMICAL PLANT, OJSC Russia

Manufacturer: & nbsp

UZOLE-SIBERIAN CHEMICAL PLANT, OJSC Russia

Information update date: & nbsp02.08.2016

Illustrated instructions

Instructions

Eufillin (Euphyllini )