Eufillin-Zdorovye, 2%r-r 5 ml No. 10

General characteristics. Structure:

International and chemical names: aminophyline (Aminophyllinum), 3,7-дигидро-1,3-диметил-1Н-пурин-2,6-дион-1,2-этандиамин; main physical and chemical properties: the transparent colourless or slightly painted liquid; structure: 1 ml of solution contains theophylline 0,0192 g, ethylene diamine of 0,0048 g; excipients: water for injections.

Pharmacological properties:

Pharmacodynamics. The Euphyllinum relaxes muscles of bronchial tubes, expands coronary vessels, expands vessels of a small circle of blood circulation, reduces resistance of blood vessels, lowers pressure in system of a pulmonary artery, increases a renal blood stream, has the diuretic effect caused by decrease in a canalicular reabsorption, increases removal of water, ions of chlorine, sodium, etc., slows down aggregation of thrombocytes. The Euphyllinum renders a positive inotropic effect against the background of relative tachycardia, increases electric instability of a myocardium. The cardiopromoting effect of the Euphyllinum is caused by braking of activity of phosphodiesterase and accumulation of tsAMF in a myocardium that leads to strengthening of a glycogenolysis and stimulates a metabolism. At the same time the Euphyllinum increases the need of a myocardium for oxygen. Besides, blocks adenosine receptors, suppresses effects of prostaglandins on unstriated muscles, reduces emission of a histamine and leukotrienes from mast cells. Intravenous administration of the Euphyllinum removes a vasomotor spasm, increases collateral circulation and saturation of blood oxygen, reduces perifocal and general hypostasis of brain fabric, lowers likvorny and, respectively, intracranial pressure.
Activates a respiratory center of a myelencephalon, increases its sensitivity to carbon dioxide and improves alveolar ventilation that finally leads to decrease in weight and frequency of episodes of an apnoea.

Pharmacokinetics. In blood about 60% contact proteins of plasma (at healthy adults), newborns have 36%, and patients with cirrhosis have about 35%. The volume of distribution is in range of 0,3 - 0,7 l/kg. In a liver with the participation of P 450 cytochrome partially turns into caffeine. The elimination half-life of an Euphyllinum depends on age, and also from existence of associated diseases and makes at newborns and children up to 6 months – more than 24 h; at children 6 months – 3,7 h are more senior; at the adults who do not have asthma – 8,7 h; at adults with obstructive diseases of lungs, a pulmonary heart and heart failure – exceeds 24 h.
It is allocated with kidneys, including adults have 10% and children have 50%, in not changed look.
Bronkhodilatiruyushchy action of an Euphyllinum is shown at its concentration in blood of 10-20 mkg/ml. Concentration over 20 mkg/ml is toxic. The exciting effect on a respiratory center is implemented at concentration of an Euphyllinum in blood of 5-10 mkg/ml.

Indications to use:

The Euphyllinum is applied at bronchial asthma and bronchospasms of different genesis (to stopping of attacks), hypertensia in a small circle of blood circulation, at the cardiac asthma (which is especially followed by a bronchospasm and Cheyn-Stokes's breath), to improvement of a renal blood-groove, to stopping of cerebral vascular crises of an atherosclerotic origin and improvement of cerebral circulation, reduction of intracranial pressure and wet brain at ischemic strokes, at chronic insufficiency of cerebral circulation.

Route of administration and doses:

The Euphyllinum is appointed intravenously at bad attacks of bronchial asthma and strokes.
Intravenously the Euphyllinum is entered struyno slowly, within 4-6 minutes in a dose of 0,12 - 0,24 (5-10 ml of 2,4% of solution which is previously dissolved in 10-20 ml of isotonic solution of sodium of chloride). At emergence of heartbeat, dizziness, nausea introduction is slowed down or passed to drop administration of drug. For this purpose 10-20 ml of 2,4% of solution of an Euphyllinum (0,24-0,48) part in 100-150 ml of isotonic solution of sodium of chloride and enter with a speed of 30-50 thaws a minute. To children intravenously enter in a single dose 2-3 mg/kg (preferably kapelno). Because of emergence of side effects the Euphyllinum is not recommended to be entered this way to children up to 14 years.
For rectal administration in microclysters of 10-20 ml of 2,4% of solution part in 20-25 ml of warm water.
In a vein the drug is administered under control of arterial pressure, number of cordial reductions, a respiration rate and overall health.
The highest doses of an Euphyllinum for adults in a vein: one-time - 0,25 g, daily - 0,5 g. In exclusively hard cases, especially in the conditions of resuscitation, doses can be increased.
The highest doses for children intramusculary and rektalno – 7 mg/kg, daily – 15 mg/kg; intravenously single dose of 3 mg/kg.
Because the Euphyllinum possesses exciting action, it should not be applied just before a dream. At purpose of drug for the night it is reasonable to combine the Euphyllinum with hypnotic drugs.

Features of use:

At pregnancy and a lactation use of drug is possible only according to vital indications.
Because of insufficient activity of biotransfarmatsionny enzymatic systems of a liver (and possibilities of cumulation) at newborns and persons 55 years an Euphyllinum are more senior appoint with care.
Intravenous administration is contraindicated to children up to 14 years.

Side effects:

At bystry introduction to a vein - dizziness, a headache, the heartbeat which sometimes is followed by disturbance of a rhythm, nausea, vomiting, spasms, a sharp lowering of arterial pressure. At rectal administration the irritation of a mucous membrane of a rectum is possible. At hypersensitivity to ethylene diamine exfoliative dermatitis, fever are possible.

Interaction with other medicines:

Pharmaceutical it is incompatible with solutions of acids. It is impossible to apply with the glucose solution, substances containing xanthine derivatives, indirect anticoagulants with other derivatives of theophylline or purine.
The ephedrine and means supporting him increase risk of development of side effects. Propranolol weakens influence on heart rate and a tone of bronchial tubes.
Let's combine with spasmolysants.
Pharmaceutical it is incompatible with Calcii chloridum, alkaloid salts, Dibazolum. Inactivates sodium benzylpenicillin. The Euphyllinum exponentiates effect of diuretics due to increase in glomerular filtering and reduction of a canalicular reabsorption.

Contraindications:

Hypersensitivity, acute cardiovascular insufficiency, stenocardia, Bouveret's disease (especially intravenous administration), premature ventricular contraction, sharp hypotonia, epilepsy, liver and/or renal failure, myocardial infarction, pregnancy, lactation, for intravenous administration – children's age up to 14 years.

Overdose:

Symptoms: anorexia, diarrhea, nausea, vomiting, tachypnea, hyperemia of the person, tachycardia, ventricular arrhythmias, sleeplessness, photophobia, generalized spasms.
Treatment: drug withdrawal, stimulation of its removal from an organism (artificial diuresis, hemosorption, plazmosorbtion, hemodialysis, peritoneal dialysis) and purpose of symptomatic means.

Storage conditions:

To store in protected from light and the place, unavailable to children, at a temperature not above +25 °C.
Lines of the validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 2,4% on 5 ml in ampoules, No. 10.