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

Bronchodilator, Purine Derivative. Inhibits phosphodiesterase, increases accumulation in the tissues of cyclic adenosine monophosphate, blocks adenosine receptors, reduces the intake of Ca²+ 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. Strengthens lung ventilation in hypokalemia.

Has a stimulating effect on the activity of the heart, strengthens the strength and heart rate. Increases coronary blood flow and myocardial oxygen demand. Reduces the tone of the blood 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 the aggregation of platelets, increases the resistance of erythrocytes to deformation, reduces thrombus formation and normalizes microcirculation.

Has tocolytic effect, increases the acidity of gastric juice.

Pharmacokinetics:

After oral administration, it is quickly and completely absorbed. Bioavailability is 90-100%. The maximum concentration in the blood plasma is achieved after 1-2 hours. The volume of distribution is in the range 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), through the placental barrier. Bronchodilating properties of the drug manifests in concentrations of 10-20 μg / ml. Concentration above 20 mg / ml is toxic. The excitatory effect on the respiratory center is realized with a lower content in the blood - 5-10 μg / ml. Metabolized at physiological pH values with the release of free theophylline, which is further exposed metabolism 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. The half-life in adults is 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 (COPD), pulmonary heart disease and pulmonary heart disease - more than 24 hours. It is excreted by the kidneys.10% of theophylline is excreted unchanged in urine.

Indications:

Bronchoobstructive syndrome of any genesis: bronchial asthma (a drug of choice in patients with asthma of physical stress and as an adjunct in other forms), COPD (emphysema of the lung, chronic obstructive bronchitis), hypertension in the "small" circulation, "pulmonary" heart, nocturnal apnea .

Contraindications:

Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine), epilepsy, peptic ulcer and 12 duodenal ulcer (in acute stage - for oral forms, especially non-prolonged tablets), gastritis with high acidity, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage eyes, children's age to 18 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 failure,stomach ulcer and duodenal ulcer (in the anamnesis), bleeding from the gastrointestinal tract in a recent history, uncontrolled hypothyroidism (the possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, pregnancy, lactation period, elderly age.

Dosing and Administration:Inside adults, 1-2 tablets 2-3 times a day after meals. The highest single dose for adults with oral administration is 0.45 g, the highest daily intake for adults with oral administration is 1.5 g.

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 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, exacerbation of peptic ulcer, diarrhea, with prolonged admission - a decrease in 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, 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: 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, plasmosorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (incl. metoclopramide and ondansetron - when vomiting). If seizures occur, maintain airway patency and oxygen toxicity. 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:

Pharmaceutically incompatible with acid solutions.

Increases the likelihood of side effects of glucocorticosteroids (GCS), mineralocorticosteroids (MKS) (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 of 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-adrenostimulators and diuretics (including by increasing glomerular filtration), reduces the effectiveness of drugs Li⁺ and beta-blockers. 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.

Form release / dosage:

Tablets 150 mg.

Packaging:

For 10 tablets in a contour mesh package, 30 tablets per can of glass OC-1.

3 contour mesh packages or a jar along with the instructions for use are placed in a pack of cardboard.

Storage conditions:

List B. In dry, the dark place.

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-004120/09

Date of registration:26.05.2009

The owner of the registration certificate:IRBITSK HFZ, OJSC IRBITSK HFZ, OJSC Russia

Manufacturer: & nbsp

IRBITSK HFZ, OJSC Russia

Information update date: & nbsp26.05.2009

Illustrated instructions

Instructions

Eufillin (Euphyllini)