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

Bronchodilator, methylxanthine derivative; inhibits phosphodiesterase, increases accumulation in tissues of cyclic 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, stimulates the respiratory center and improves the alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of episodes of apnea.

Has a stimulating effect on the activity of the heart, increases the strength and heart rate, 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 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 and prostaglandin activation factor 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 of 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 the maximum concentration (TCmAh) in the blood - 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. Communication with plasma proteins in adults - 60%, in newborns - 36%, in patients with cirrhosis of the liver - 36%. Penetrates into breast milk (10% of the dose taken), through 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, with the exception of premature newborns and children under 6 months of age, who, due to the extremely long half-life (T1 / 2) of caffeine, cause significant accumulation in the body (up to 30% of that for aminophylline).

In children older than 3 years and in adults, the phenomenon of caffeine cumulation is absent.

The half-life period (T1 / 2) in newborns and children up to 6 months is more than 24 hours; 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 the normalization pharmacokinetics 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. Neonates theophylline about 50% excreted in the urine in an unmodified form against 10% in adults, due to insufficient activity of the liver enzymes.

Indications:

Bronchoobstructive syndrome of any origin: bronchial asthma, chronic obstructive pulmonary disease, hypertension in the "small" circle of the circulation, "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, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, children under 12 years.

Carefully:

Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis of vessels, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive readiness, hepatic and / or renal insufficiency, 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, hyperplastic Ia prostate, old age.

Pregnancy and lactation:

If you need to prescribe the drug during pregnancy and lactation, you should compare the expected benefit to the mother and the potential risk to the fetus or the baby.

Dosing and Administration:

Inside after eating, with lots of fluids.

Adults and adolescents over 16 years of age - 150 mg (1 tablet) 1-3 times a day. Adolescents from 12 to 16 years (with a body weight of more than 40 kg) - 150 mg (1 tablet) 3 times a day with an interval of 6 hours.

The duration of the course of treatment is from several days to several months.

Maximum doses for adults: single dose 500 mg, daily 1500 mg.

The maximum dose for adolescents from 12 years and older is a single 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 fetal III trimester), arrhythmias, lowering blood pressure, cardialgia, an increase in 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, itchy skin, fever.

Other: chest pain, tachypnea, a 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.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including with blood), gastrointestinal bleeding, tachypnea, facial skin hyperemia, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions. In severe poisoning, epileptic seizures, hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, lowering of arterial pressure, skeletal muscle necrosis, confusion, renal insufficiency with myoglobinuria may develop.

Treatment: cancellation of the drug, gastric lavage, intake of activated carbon, laxative drugs, forced diuresis, hemosorption, plasmasorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting). If seizures occur, maintain airway patency and conductoxygen 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 (MCS) (hypernatremia), funds for general anesthesia (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system (increases neurotoxicity).

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.

With the simultaneous use with antibiotics of a group of macrolides, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, small doses ethanol, disulfiram, fluoroquinolones, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil, and with influenza vaccination, the intensity of 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 drugs of lithium ions and beta-adrenoblockers.

Compatible with antispasmodics, do not use together with other xanthine derivatives.

With caution appoint simultaneously with anticoagulants.

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, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Form release / dosage:

Tablets of 150 mg.

Packaging:

10 tablets per contour cell packaging made of polyvinylchloride film and foil of aluminum printed lacquered or paper packaging with polymer coating.

By 10,20, 25,30,40, 50, 60 tablets in cans of polymeric.

Each jar or 1, 2, 3, 4, 5 cell packs along with the instructions for use are placed in a cardboard pack.

Storage conditions:

In dry, 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:P N001998 / 01

Date of registration:17.11.2008

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp09.01.2013

Illustrated instructions

Instructions

Euphyllin-UBF (Euphyllini-UBF)