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

The drug inhibits phosphodiesterase increases the accumulation of cAMP in tissues, inhibit adenosine (purine) receptors, reduces the flow of calcium ions through the cell membrane channels, reduces smooth muscle contractile activity.

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 strength and frequency cardiac contractions, 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, increases the adrenaline release of the adrenal glands. Has a moderate diuretic effect. Expands extrahepatic biliary tract. It inhibits platelet aggregation (suppresses the platelet and prostaglandin E2 alpha activation factor), increases the resistance of erythrocytes to deformation (improves rheological properties of 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 of the drug is 90-100%.

The maximum concentration (7 μg / ml) with intravenous administration of 300 mg is achieved after 15 minutes.

The volume of distribution is in the range of 300-700 ml / kg (30-70% of the "ideal" body weight), an average of 450 ml / kg.

Relationship 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 (the concentration in the fetal serum is slightly higher than in the mother's blood 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 less than theophylline. Caffeine is an active metabolite and is formed in small amounts, with the exception of premature newborns and children younger than 6 months, who, due to the extremely long half-life of caffeine, there is a significant accumulation in the body (up to 30 % from that for aminophylline).

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

Half-life in infants and children up to 6 months - more than 24 hours; in children older than 6 months - 3.7 h; in adults, 8.7 hours; smokers (20-40 cigarettes a day) - 4-5 hours (after quitting smoking, the normalization of pharmacokinetics occurs 3-4 months); in adults with chronic obstructive pulmonary disease (COPD), pulmonary heart disease - more than 24 hours.

It is 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 of any genesis: bronchial asthma (a drug of choice in patients with bronchial asthma of physical stress and as an additional remedy in other forms), chronic obstructive pulmonary disease, emphysema, chronic obstructive bronchitis, hypertension in the "small" circulation, night apnea. Violation of cerebral circulation by ischemic type (as part of combination therapy to reduce intracranial pressure).

Left ventricular heart failure (as part of complex therapy).

Contraindications:

Hypersensitivity to the drug, as well as to xanthine derivatives: caffeine, pentoxifylline, theobromine. Severe arterial hypotension or hypertension, paroxysmal tachycardia, extrasystole, myocardial infarction with heart rhythm disturbances, epilepsy, increased convulsive alertness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and / or renal insufficiency, hemorrhagic stroke, retinal hemorrhage eyes, bleeding in a recent anamnesis.

Carefully:

Sepsis, gastric and duodenal ulcer (in the anamnesis), elderly age (over 55 years), uncontrolled hypothyroidism (possibility of cumulation), widespread atherosclerosis of the vessels, prostatic hyperplasia, children under 14 years of age (due to possible side effects).

Pregnancy and lactation:

If you need to use the drug during pregnancy, you should compare the expected benefit to the mother and the potential risk to the fetus.

If you need to use the drug during breastfeeding, breast-feeding should be discontinued.

Dosing and Administration:

Method of administration: intravenously.

Adults inject slowly (within 4-6 minutes) for 5-10 ml of the drug (0.12-0.24 g), which is previously diluted in 10-20 ml of 0.9% sodium chloride solution.

When there is a palpitation, dizziness, nausea, the speed of administration slows down or goes to a drip introduction, for which 10-20 ml of the drug (0.24-0.48 g) is diluted in 100-150 ml of 0.9 % solution of sodium chloride; injected at a rate of 30-50 drops per minute.

Before parenteral administration, the solution must be heated to body temperature. Parenterally administered aminophylline up to 3 times a day, no more than 14 days. Higher doses of aminophylline for adults with intravenous administration: single dose - 0.25 g, daily - 0.5 g.

If necessary, children are injected aminophylline intravenously drip from the calculation of a single dose of 2-3 mg / kg. Higher doses for children with intravenous administration: 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.

From the cardiovascular system: a feeling of palpitations,tachycardia (including the fetus when taking a pregnant woman in the 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, peptic ulcer, diarrhea, with prolonged admission - a decrease in appetite.

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

Other: pain in the chest, tachypnea, a sensation of "hot flashes" to the face, albuminuria, hematuria, hypoglycaemia, increased diuresis, increased sweating.

Side effects decrease with a decrease in the dose of the drug, with the replacement of the method of administration (from the jet to the drip).

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

Overdose:

Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial flushing, tachycardia, ventricular arrhythmia, insomnia, motor agitation, anxiety, photophobia, tremors, convulsions. In severe poisoning, epileptic seizures may develop (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia,reduction in blood pressure, necrosis of skeletal muscles, confusion, renal failure with myoglobinuria.

Treatment: drug withdrawal, forced diuresis, hemosorption, plasmosorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (including intravenously metoclopramide - when vomiting). If seizures occur, maintain airway patency and conduct oxygen therapy. For cramping seizures, intravenously inject diazepam 0.1-0.3 mg / kg (but not more than 10 mg).

Interaction:

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 oral estrogen-containing contraceptives weaken the effect of aminophylline (bind to the enzymatic system of cytochrome P450 and alter the metabolism of aminophylline).

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine and moracizin, being inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.

While the use of macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and influenza vaccination intensity aminophylline steps may 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.

Special instructions:

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

Before use, the drug solution must be heated to 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.

Effect on the ability to drive transp. cf. and fur:During drug treatment it is not recommended to drive vehicles, mechanisms, and also engage in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous administration is 24 mg / ml.

Packaging:

5 or 10 ml into neutral glass ampoules. For 10 ampoules together with instructions for use and scarifier ampoule in a box of cardboard.

5 ampoules per contour cell pack. 2 contour packs with instructions for use and a scapegrator in a pack of cardboard. When using ampoules with a notch, dot or ring fracture, the scarifier is not inserted.

Storage conditions:

In the dark place at a temperature of 2 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001268

Date of registration:22.08.2011

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp17.12.2013

Illustrated instructions

Instructions

Eufillin (Euphyllini)