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

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.

Normalizing the respiratory function, contributes to the saturation of blood oxygen and reduce the concentration of carbon dioxide. Strengthens lung ventilation in hypokalemia.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 vessels of the brain, skin and kidneys). Has peripheral vasodilating 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.

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

It inhibits platelet aggregation (inhibits the activation factor of platelets and prostaglandins (PgE2alpha), 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). Bronchodilating 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 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. The half-life period is 3.7 hours in children older than 6 months; in adults, 8.7 hours; (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 - more than 24 hours It is excreted by the kidneys.

Indications:

Bronchoobstructive syndrome of any origin: bronchial asthma, chronic obstructive pulmonary disease (COPD), pulmonary emphysema, chronic obstructive bronchitis, hypertension in the "small" circulation, "pulmonary" heart, nocturnal apnea.

Contraindications:

Hypersensitivity (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- or hypotension, severe tachyarrhythmia, hemorrhagic stroke, retinal hemorrhage, children's age (up to 3 years).

Carefully:

Heavy coronary insufficiency (acute phase of myocardial infarction, angina), common atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive readiness, liver and / or kidney failure, bleeding from the gastrointestinal tract in the recent history of uncontrolled hypothyroidism (possibility cumulation ) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, advanced age, childrens rast (older than 3 years).

Pregnancy and lactation:

During pregnancy and lactation, the appointment is only possible if the benefit to the mother exceeds the potential risk to the fetus and the baby.

Dosing and Administration:

Inside appoint adults to 150 mg per reception 3-4 times a day after meals, if necessary, increase the dose with an interval of 3 days.

Children 3-10 years and / or body weight 20-40 kg - 1 tablet every 12 hours,

Children older than 10 years and / or body weight of more than 40 kg - 1 tablet 3-4 times a day.

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

Side effects:

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

From the cardiovascular system: palpitations, tachycardia (including the fetus when taking a pregnant woman in the third trimester), arrhythmias, lowering blood pressure, cardialgia, an increase in 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: chest pain, tachypnea, feeling the tides to 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 may develop epileptic seizures (especially in children without incurring any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia,reduction in blood pressure, necrosis of skeletal muscles, confusion, renal failure with myoglobinuria.

Treatment: cancellation of the drug, gastric lavage, the appointment of activated charcoal, laxative drugs, washing the intestine with a combination of macrogol and electrolytes (intestinal lavage), forced diuresis, hemosorption, plasmasorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (incl. metoclopramide and ondansetron - when vomiting). With convulsions, maintain airway patency and conduct oxygen therapy. To relieve the epileptic seizure - intravenously diazepam, 0.1-0.3 mg / kg (but not more than 10 mg).

Interaction:

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

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-adrenomimetics 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 because of the risk of developing bleeding.

Special instructions:

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

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

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

Form release / dosage:

Tablets of 150 mg.

Packaging:10 pieces per cell contour package, 3 cell contour packs along with instructions for use in a pack of cardboard box.

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use the product after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000120

Date of registration:04.03.2010

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp17.06.2014

Illustrated instructions

Instructions

Eufillin (Euphyllini)