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

Inhibits phosphodiesterase, increases accumulation in tissues of cyclic adenosine monophosphate, 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 musculature of the bronchi, it relieves bronchospasm. Has a moderate inotropic and diuretic effect. Aminophylline lowers vascular resistance,reduces the tonus of blood vessels (mainly the brain, skin and kidney), dilates coronary vessels, lowers blood pressure in the pulmonary artery, improves contraction of the diaphragm, increases mucociliary clearance, inhibits the release of mediators (histamine and leukotrienes) from mast cells, stimulates the respiratory center , emission increases adrenal glands, inhibits platelet aggregation (inhibits platelet activating factor alpha and prostaglandin E2), increases the resistance to deformation of the erythrocyte (improves rheology and blood properties), reduces thrombogenesis and normalizes microcirculation.

Pharmacokinetics:

Bioavailability of the drug is 90-100%. The time required to reach the maximum concentration for intravenous administration of 0.3 g is 15 minutes, the maximum concentration is 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.

60% of the aminophylline (healthy adults) and 36% (in newborns) binds to plasma proteins and is distributed in the blood, extracellular fluid, and muscle tissue. Aminophylline penetrates the placental and blood-brain barrier, does not accumulate in adipose tissue. 90 % the drug is metabolized in the liver. Metabolites are excreted by the kidneys, 7-13% of the drug is excreted unchanged. The half-life is for non-smokers from 5 to 10 hours, for children over 10 months from 2.5 to 5 hours. Smoking alcohol significantly affect the metabolism and excretion of the drug, in particular among smokers this period is significantly reduced and ranges from 4 to 5 hours. Elimination of the drug is prolonged in patients with respiratory failure, with renal and heart failure, with viral infections and hyperthermia.

Indications:

Bronchoobstructive syndrome in bronchial asthma, bronchitis, pulmonary emphysema, cardiac asthma (mainly for relief of seizures); 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 heart failure (as part of complex therapy).

Contraindications:

Hypersensitivity to the drug, as well as to other xanthine derivatives: 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, haemorrhage in the retina of the eye, bleeding in a recent history, lactation.

If you have any of the listed diseases, always consult a doctor before using the drug.

Carefully:

Pregnancy, the period of newborns, the age of over 55 years and uncontrolled hypothyroidism (the possibility of cumulation), widespread atherosclerosis of the vessels, sepsis, prolonged hyperthermia, gastroesophageal reflux, peptic ulcer of the stomach and duodenum (in the anamnesis), prostatic hyperplasia.

The drug is not recommended for intravenous administration to children under 14 years of age (due to possible side effects).

If you have any of the listed diseases, always consult a doctor before using the drug.

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.

Dosing and Administration:

In the vein, adults are slowly injected (for 4-6 minutes) with 5-10 ml of the drug (0.12-0.24 g), which is previously diluted in 10-20 ml of 0.9 % solution of sodium chloride. 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 in the vein: single - 0.25 g, daily - 0.5 g. The drug is not recommended for children under 14 years due to side effects.

However, if necessary, children are aminophylline intravenously from the calculation of a single 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 gastrointestinal tract: gastroesophageal reflux (heartburn), nausea, vomiting, exacerbation of peptic ulcer.

From the central nervous system: headache, anxiety, anxiety, irritability, dizziness, insomnia, tremor; rarely - a cramp.

From the cardiovascular system: palpitations, tachycardia, cardialgia, cardiac rhythm disturbances, increased frequency of angina attacks, lowering of arterial pressure up to collapse - with rapid intravenous injection.

Allergic reactions: skin rash, skin itching, exfoliative dermatitis, febrile reaction.

Local reactions: at the injection site - hyperemia, tenderness, denseness. Other: pain in the chest, tachypnea, albuminuria, hematuria, hypoglycemia, increased sweating, a sensation of "hot flashes" to the face, increased diuresis.

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: hyperemia of the facial skin, insomnia, motor excitement, anxiety, photophobia, anorexia, diarrhea, nausea, vomiting, epigastric pain,gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized seizure, hyperventilation, a sharp drop in blood pressure. In severe poisoning, epileptonic seizures may develop (especially in children without the appearance of any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria.

Treatment: drug cancellation, forced diuresis, hemosorption, plasmosorption, hemodialysis, symptomatic therapy. For cramping seizures applied diazepam (in injections). Do not use barbiturates. At the expressed intoxication (the maintenance of an aminophylline more than 50 g / l) the hemodialysis is recommended.

Interaction:

Ephedrine, beta-adrenomimetics, caffeine and furosemide increase the effect of the drug.

Increases the likelihood of side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), funds for general anesthesin (the risk of ventricular arrhythmias increases). In combination with phenobarbital, phenytoin, rifampicin, isoniazid,carbamazepine or sulfinpyrazone, a decrease in the efficacy of aminophylline is observed, which may require an increase in the doses used. Aminoglutethimide, moracizin, being inducers of microsomal enzymes of the liver, increase the clearance of aminophylline, which may require an increase in its dose. The clearance of the drug decreases when it is administered in combination with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, which may require a dose reduction.

Oral estrogen-containing contraceptives, antidiarrheal drugs, intestinal sorbents weaken, and H2-gnastnonblokatory, blockers of slow calcium channels, mexiletine intensify the action (bind to the enzymatic system of cytochrome P450 and alter the metabolism of aminophylline). When used in combination with enoxacin and other fluoroquinolones, small doses of ethanol, disulfiram, recombinant interferon alpha, methotrexate, propafenone, thiabendazole, ticlopidine, verapamil, and when vaccinated against influenza, the intensity of aminophylline may increase, which may require a reduction in its dose.The drug inhibits the therapeutic effects of lithium carbonate and beta-blockers. The appointment of beta-adrenoblockers interferes with bronchodilating action of aminophylline and can cause bronchospasm. Aminophylline potentiates the action of diuretics by increasing the glomerular filtration and reducing tubular reabsorption. Carefully aminophylline appoint simultaneously with anticoagulants, with other derivatives of theophylline or purine. It is not recommended to apply aminophylline with agents that excite the central nervous system (increases neurotoxicity). The drug can not be used with solutions of dextrose, is not compatible with a solution of glucose, fructose and levulose. The pH of the mixed solutions should be taken into account: pharmaceutically incompatible with acid solutions.

Special instructions:

The drug is administered with caution to patients with severe impairment of liver and kidney function, peptic ulcer of the stomach and duodenum. 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.

Avoid the use of large quantities of caffeine-containing foods or beverages during the treatment period.

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

Influence on the ability to drive vehicles and mechanisms. During the treatment period, 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:

Solution for internal administration 24 mg / ml.

Packaging:

5 or 10 ml into neutral glass ampoules.

10 ampoules per box of cardboard.

5 ampoules per circuit cell box made of polyvinyl chloride film and foil of aluminum printed lacquered or foil-free.

1 or 2 contour squares are placed in a pack of cardboard.

In each pack, the box is attached instructions for use, the ampullar scarifier.

When using ampoules with a kink ring or with a notch and a dot the ampoule scaper is not inserted.

Storage conditions:

In the dark place at a temperature of 10 to 25 ° C.Do not freeze. Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-002194

Date of registration:20.01.2011

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp20.01.2011

Illustrated instructions

Instructions

Eufillin (Euphyllini)