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

The drug inhibits phosphodiesterase, increases accumulation in the tissues of cyclic adenosine monophosphate, blocks adenosine (purine) receptors; reduces the flow of Ca2 + through the channels of cell membranes, reduces the contractile activity of smooth muscles. Relaxes the muscles of the bronchi, stops bronchospasm, 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 reduces 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 heart, increases 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 the 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 platelet and prostaglandin E2 activation factor, 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:

Bioavailability for liquid dosage forms is 90-100%. TSma) when i / in the introduction of 0.3 g - 15 min, the value of Cmah - 7 mcg / ml. The volume of distribution is in the range of 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), 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 m kg / 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 inferior to theophylline. Caffeine is an active metabolite and is formed in small amounts, with the exception of premature newborns and children younger than 6 months,in which, due to extremely long T1 / 2 caffeine, there is a 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.

T1 / 2 in newborns and children up to 6 months - 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 COPD, a "pulmonary" heart and pulmonary heart failure - more than 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:

Status asthmaticus (additional therapy), neonatal apnea, cerebral circulation on ischemic type (as part of combination therapy), left ventricular insufficiency with bronchospasm and respiratory failure by Cheyne-Stokes type, edematous syndrome of renal origin (in the complex therapy).

Contraindications:

Hypersensitivity to the drug, but also to other xanthine derivatives:. Caffeine, pentoxifylline, theobromine.Severe hypotension or hypertension, paroxysmal tachycardia, arrythmia, myocardial infarction with cardiac arrhythmia, epilepsy, increased convulsive readiness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, lung edema, severe coronary insufficiency, hepatic or renal failure, hemorrhagic stroke, bleeding in the retina, bleeding in a recent anamnesis, lactation period.

Carefully:

Pregnancy, neonatal period, elderly age (over 55 years), uncontrolled hypothyroidism (possibility of cumulation), widespread atherosclerosis of vessels, sepsis, prolonged hyperthermia, prostatic adenoma. The drug is not recommended for intravenous administration to children under 14 years of age (due to possible side effects).

Dosing and Administration:

At urgent conditions adults are injected slowly (within 4-6 minutes) with 5-10 ml of the drug (0.12-0.24 g), which is first diluted in 10-20 ml of 0.9% sodium chloride solution.

When asthmatic status is shown intravenous drip introduction - 720-750 mg. Higher doses for adults intravenously - single 0.25 g, daily 0.5 g.

Higher doses for children intravenously - single 3 mg / kg, daily - at the age of up to 3 months - 0.03-0.06 g, from 4 to 12 months-0.06-0.9 g, from 2 to 3 years 0.09 -0.12g, from 4 to 7 years-0.12-0.24g, from 8 to 18 years-0.25-0.5g.

Side effects:

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

From the side of 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.

Allergic reactions: skin rash, itchy skin, fever.

Other: pain in the chest, 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.

Local reactions: compaction, hyperemia, tenderness at the site of administration.

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 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: cancellation of the drug, forced diuresis, hemosorption, plasmasorption, hemodialysis (efficacy is low), symptomatic therapy (incl. metoclopramide and ondansetron - when vomiting). If seizures occur, maintain airway patency and conduct oxygen therapy. For seizure seizure - in / in diazepam 0.1-0.3 mg / kg (but not more than 10 mg). Do not use barbiturates. With severe nausea and vomiting - recommended hemodialysis.

Interaction:

Pharmaceutically incompatible with acid solutions. Increases the likelihood of side effects of GCS, ISS (hypernatremia), funds for general anesthesia (increases the risk of ventricular arrhythmias), drugs that excite the central nervous system (increases neurotoxicity). 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, thiabendazole, ticlopidine, verapamil, and when vaccinated against influenza, the aminophylline 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. Before administration, the solution must be heated to the body temperature.Elderly patients are advised to reduce the dose of the drug due to delayed excretion of it from the body. Smoking patients are advised to increase the dose due to accelerated removal of the drug from the body.

Form release / dosage:

Solution for intravenous administration is 24 mg / ml.

Packaging:Ampoules of 5 ml and 10 ml. 10 ampoules per pack of cardboard along with instructions for use. 5 ampoules per contour cell pack. 1 or 2 contour squares in a pack of cardboard together with instructions for use. In each pack insert knife ampoule or scarifier. When packing ampoules with a point or a ring of fracture, the ampoule knife or scarifier is not inserted.

Storage conditions:

In dry, dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:

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

Terms of leave from pharmacies:On prescription

Registration number:LSR-000883/09

Date of registration:09.02.2009

The owner of the registration certificate:Armavir Biofactory, FKPArmavir Biofactory, FKP Russia

Manufacturer: & nbsp

ARMAVIRSK BIOLOGICAL FACTORY, FSUE Russia

Information update date: & nbsp18.09.2014

Illustrated instructions

Instructions

Eufillin (Euphyllini)