Eufillin - 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 (inhibits the activation factor of platelets and prostaglandins E2 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:

Bioavailability and kinetics of absorption depend on the dosage form of the drug. Bioavailability for liquid dosage forms is 90-100%. Time about reaching the maximum concentration of the drug in the plasma with intravenous administration of 0.3 g - 15 min, the maximum concentration of the drug in the blood - 7 μg / 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 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 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.which, due to the extremely long half-life of caffeine, generates 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.

Half-life in newborns and children up to 6 months. - more than 24 hours; in children older than 6 months. - 3.7 hours; in adults, 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, "pulmonary" heart and lung and heart failure -. more than 24 hours excreted by the kidneys. In neonates, about 50% of theophylline is excreted unchanged in urine against 10% in adults, which is due to inadequate activity of liver enzymes.

Indications:

Bronchoobstructive syndrome with bronchial asthma, bronchitis, emphysema; hypertension in a small circle of blood circulation.

Violation of cerebral circulation by ischemic type (as part of combination therapy to reduce intracranial pressure).

Left ventricular failure with bronchospasm and respiratory failure by the type of Cheyne-Stokes (as part of complex therapy).

Contraindications:

Hypersensitivity to the drug (including other derivatives of xanthine: caffeine, pentoxifylline, theobromine), severe arterial hypotension or hypertension, paroxysmal tachycardia, extrasystole, myocardial infarction with cardiac rhythm disturbances, epilepsy, increased convulsive alertness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and / or renal insufficiency, hemorrhagic stroke , bleeding in the retina of the eye, bleeding in a recent anamnesis.

Carefully:

Heavy coronary insufficiency (acute phase of myocardial infarction, angina), common atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystole, increased convulsive readiness, hepatic and / or renal failure, gastric ulcer and 12 duodenal ulcer (in history), bleeding from the gastrointestinal tract in the recent history of uncontrolled hypothyroidism (possibility of cumulation) or hyperthyroidism, prolonged pyrexia, gastroesophageal reflux disease, prostatic hypertrophy, children's age up to 14 years, old age (over 55 years).

With caution appoint simultaneously with anticoagulants, with other derivatives of theophylline or purine.

Pregnancy and lactation:

If it is necessary to prescribe the drug during pregnancy, one should compare the expected benefit to the mother and the potential risk to the fetus.

If you need to use the drug during lactation, breastfeeding should be discontinued.

Newborns, whose mothers during pregnancy (especially the third trimester) received aminophylline, need medical supervision to control the possible symptoms of methylxanthine intoxication.

Dosing and Administration:

In the vein, adults are slowly injected (for 4-6 minutes) with 5-10 ml of a solution at a concentration of 24 mg / ml (0.12-0.24 g), which is previously diluted in 10-20 ml of isotonic sodium chloride solution. With the appearance of palpitations, dizziness, nausea, the rate of administration slows down or goes to a drop introduction, for which 10-20 ml of a solution with a concentration of 24 mg / ml (0.24-0.48 g) is diluted in 100-150 ml of isotonic sodium chloride solution; injected at a rate of 30-50 drops per minute. Parenterally enter euphyllin up to 3 times a day, no more than 14 days.

Higher doses of euphyllin for adults in the vein: single-dose 0.25 g, daily - 0.5 g.

For children up to 14 years of age, the drug should be used with caution because of possible side effects.

However, if necessary, children are administered intravenous eufillin at a dose of 2-3 mg / kg, preferably drip.

Higher doses for children intravenously: single dose - 3 mg / kg, daily - at the age of up to 3 months. 0.03-0.06 g, from 4 to 12 months. - 0,06-0,09 g, from 2 to 3 years - 0,09-0,12 g, from 4 to 7 years - 0,12-0,24 g, from 8 to 18 years - 0,25- 0.5 g.

Side effects:

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

From the side of 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, peptic ulcer, diarrhea, with prolonged admission - a decrease in appetite.

Allergic reactions: skin rash, skin itching, fever, exfoliative dermatitis. 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.

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: drug cancellation, forced diuresis, hemosorption, plasmosorption, hemodialysis, symptomatic therapy. If seizures occur, maintain airway patency and conduct oxygen therapy. For cramping seizures - intravenously diazepam, 0.1-0.3 mg / kg (but not more than 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (intravenously).

Interaction:

Ephedrine and caffeine increase the effect of the drug.

Pharmaceutically incompatible with acid solutions.

Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (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.

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 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, with other derivatives of theophylline or purine.

Special instructions:

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

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.

Before use, the drug solution must be heated to body temperature.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous administration.

Packaging:

5 or 10 ml in a neutral glass ampoule.

5 ampoules of 5 ml or 10 ml are placed in a contour mesh package made of a polyvinyl chloride film.

2 contour mesh packages are placed in packs of cardboard.

10 ampoules of 10 ml are placed in boxes of cardboard with corrugated paper partitions.

In each pack, a box of cardboard insert instructions for use, a scarifier or knife ampoule. At packing of ampoules with a ring of a break, a point and an intersection the knife ampullum or skarifikator do not put.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003895/07

Date of registration:19.11.2007

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp06.06.2014

Illustrated instructions

Instructions

Eufillin (Euphyllini)