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

Pharmacodynamics: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 muscles of the bronchi, increases mucociliary clearance, stimulates the contraction of the diaphragm, improves the function of the respiratory and intercostal muscles,It stimulates the respiratory center and increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a reduction in the severity and frequency of apnea episodes. 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. 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), averaging 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 P 450 isoenzymes.As a result, 1, 3-dimethylurea acid (45-55%) is formed, which has pharmacological activity, but is 1-5 times less than 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 hours; in adults, 8.7 hours; in "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, a "pulmonary" heart and pulmonary heart failure - over 24 hours. It is excreted by the kidneys.

Indications:

Bronchoobstructive syndrome of any genesis: 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,gastric ulcer and duodenal ulcer (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 anamnesis), bleeding from gastrointestinal tract in a recent history, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, hyperplas asia prostate gland, pregnancy, lactation, elderly age, children's age.

Assign simultaneously with anticoagulants.

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 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 cardiovascular system: palpitation, 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, 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.

Overdose:

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including with blood),gastrointestinal bleeding, tachypnea, facial flushing, tachycardia, ventricular arrhythmia, insomnia, motor agitation, anxiety, photophobia, tremors, convulsions. In severe poisoning may develop epilepgoidnye 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, administration of activated charcoal, laxatives drugs, intestinal lavage combination of polyethylene glycol 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 (but not more than 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (intravenously).

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:

Care should be taken when consuming large quantities of caffeine-containing foods or beverages during the treatment period, it is necessary to refrain from driving vehicles and practicing other potentially dangerous activities that require increased attention and speed of psychomotor reactions.

Effect on the ability to drive transp. cf. and fur:it is necessary to refrain from driving transport and employment by other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets 150 mg.

Packaging:

10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil or paper with polyethylene coating.

30 tablets in a jar of orange glass type BTS.

30 tablets in a can of polymer type BP.

Each bank or 1, 2, 3 contoured cells with instructions for use are placed in a pack of cardboard.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 20 ° 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-001569

Date of registration:18.03.2011

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp18.03.2011

Illustrated instructions

Instructions

Eufillin (Euphyllini)