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 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, 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 to 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 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. T^1/2 in children older than 6 months. - 3.7 hours; in adults, 8.7 hours; in "smokers" (20-40 cigarettes a day) - 4-5 hours (after quitting the normalization pharmacokinetics 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 (emphysema, chronic obstructive bronchitis), pulmonary hypertension, pulmonary heart, nocturnal apnea.

Contraindications:

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

Carefully:

Heavy coronary insufficiency (acute phase of myocardial infarction, angina), common atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent extras asystole, increased convulsive readiness, liver and / or renal failure, gastric ulcer and duodenum 12 (history), gastrointestinal tract bleeding a recent history of uncontrolled hypothyroidism (possibility of cumulation) or hyperthyroidism, prolonged pyrexia, gastro-oesophageal reflux, prostate adenoma, pregnancy, etc. IRS lactation, elderly, children's age (older than 3 years).

Pregnancy and lactation:

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

Dosing and Administration:

Inside, 150 mg per reception 1-3 times a day after meals. Children should be appointed at the 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: palpitations, tachycardia (including the fetus in pregnant while taking III trimester), arrhythmias, cardialgia, reduced blood pressure, increased frequency of angina attacks.

From the digestive system: gastralgia, nausea, vomiting, gastro-oesophageal reflux, heartburn, aggravation of peptic ulcer disease, diarrhea, Propafenone - decreased appetite.

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

Overdose:

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

Treatment: withdrawal of the drug, gastric lavage, the appointment of activated carbon, laxative drugs, washing the intestine with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasmasorption, hemodialysis (efficacy is not high, peritoneal dialysis is not effective), symptomatic therapy. 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 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, 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 glomerular filtration), reduces the effectiveness of drugs Li⁺ and beta-blockers. FROM use caution at the same time as anticoagulants. Compatible with antispasmodics, do not use together with other xanthine derivatives.

Special instructions:

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

Form release / dosage:

Tablets 150 mg.

Packaging:

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

For 3, 5 contour squares with instructions for use are placed in a pack of cardboard. For 20 contour packagings with an equal number of instructions for use are placed in a pack of cardboard. The unit cell packs with an equal number of instructions for use are placed in a group package.

Storage conditions:

In a dry, 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:LSR-002209/07

Date of registration:15.08.2007

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Information update date: & nbsp21.04.2011

Illustrated instructions

Instructions

Eufillin (Euphyllini)