Euphyllinum

General characteristics. Structure:

Active ingredient: an Euphyllinum (Aminophyllinum) (in terms of dry matter) - 24 mg. Excipient: water for injections.

Pharmacological properties:

Pharmacodynamics. Drug inhibits phosphodiesterase, increases accumulation in tsAMF fabrics, blocks adenosine (purine) receptors; has ability to oppress transport of calcium ions via channels of cellular membranes, reduces sokratitelny activity of smooth muscles. Relaxes muscles of bronchial tubes, stops a bronchospasm. Has moderate inotropic and diuretic effect. The Euphyllinum lowers vascular resistance, reduces a tone of blood vessels (mainly, vessels of a brain, skin and kidneys), expands coronary vessels, lowers pressure in system of a pulmonary artery, improves reduction of a diaphragm, increases mukotsiliarny clearance, slows down release of mediators (a histamine and leukotrienes) from mast cells, stimulates a respiratory center, strengthens adrenaline emission by adrenal glands, slows down aggregation of thrombocytes, improves microcirculation.

Pharmacokinetics. 60% of an Euphyllinum (at healthy adults) and 36% (at newborn children) contact proteins of plasma and are distributed in blood, extracellular liquid and muscular tissue. The Euphyllinum gets through placental and hematoencephalic barriers, in fatty tissue does not collect. 90% of drug are metabolized in a liver. Metabolites are allocated with kidneys, 7-13% of drug are allocated in an invariable look. The elimination half-life makes at non-smoking adult from 5 to 10 hours, at children 10 months from 2,5 to 5 hours are more senior. Smoking and alcohol considerably influence metabolism and removal of drug, in particular at smokers this period is considerably reduced and makes from 4 to 5 hours. Removal of drug is extended at patients with respiratory insufficiency, at liver and heart failure, at viral infections and a hyperthermia.

Indications to use:

Bronkhoobstruktivny syndrome at bronchial asthma, bronchitis, emphysema of lungs, cardiac asthma (generally for stopping of attacks); hypertensia in a small circle of blood circulation. Disturbance of cerebral circulation on ischemic type (as a part of a combination therapy for reduction of intracranial pressure). A left ventricular failure with a bronchospasm and disturbance of breath as Cheyn-Stokes (as a part of complex therapy).

Route of administration and doses:

The adult enter into a vein slowly (within 4-6 minutes) 5-10 ml of drug (0,12 - 0,24) which is previously dissolved in 10-20 ml of isotonic solution of sodium of chloride. At emergence of heartbeat, dizziness, nausea rate of administering is slowed down or passed to drop introduction for what 10-20 ml of drug (0,24-0,48) part in 100-150 ml of isotonic solution of sodium of chloride; enter with a speed of 30-50 thaws a minute. Before parenteral administration solution needs to be heated to body temperature. Parenterally enter an Euphyllinum to 3 times a day, no more than 14 days. The highest doses of an Euphyllinum for adults in a vein: one-time - 0,25 g, daily - 0,5 g. Drug is not recommended to children up to 14 years because of side effects. However, if necessary to children enter an Euphyllinum intravenously at the rate of a single dose of 2-3 mg/kg preferably kapelno. The highest doses for children intravenously: one-time - 3 mg/kg, daily - aged up to 3 months - 0,03-0,06, from 4 to 12 months - 0,06-0,09 g, from 2 to 3 years - 0,09-0,12, from 4 to 7 years - 0,12-0,24 mg, from 8 to 18 years - 0,25-0,5 g.

Features of use:

Drug is appointed with care to patients with the expressed abnormal liver functions and kidneys, a peptic ulcer of a stomach and duodenum. Elderly patients are recommended to lower a drug dose because of the slowed-down removal it from an organism. The smoking patients are recommended to increase a dose in connection with the accelerated removal of drug from an organism.

Side effects:

From digestive tract: gastroezofagalny reflux (heartburn), aggravation of a peptic ulcer. From the central nervous system: headache, concern, uneasiness, irritability, dizziness, sleeplessness, tremor; seldom - spasms, nausea, vomiting. From cardiovascular system: heartbeat, tachycardia, a cardialgia, disturbances of a cordial rhythm, increase in frequency of attacks of stenocardia, a lowering of arterial pressure up to a collapse - at bystry intravenous administration. Allergic reactions: skin rash, skin itch, exfoliative dermatitis, feverish reaction. Local reactions: in an injection site - a hyperemia, morbidity, consolidation. Other: a stethalgia, a tachypnea, an albuminuria, a hamaturia, a hypoglycemia, perspiration, feeling of inflows to the person, strengthening of a diuresis.

Interaction with other medicines:

Ephedrine, beta адреностимуляторы, caffeine and furosemide strengthen effect of drug. Increases probability of development of side effects of glucocorticosteroids, mineralokortikosteroid (hypernatremia), means for the general anesthesia (the risk of developing of ventricular arrhythmias increases). In a combination with phenobarbital, Phenytoinum, rifampicin, an isoniazid, carbamazepine or Sulfinpyrazonum decrease in efficiency of an Euphyllinum is observed that increase in the applied drug doses can demand. Aminoglutetimid, морацизин, being inductors of a microsomal oxidation, increase clearance of an Euphyllinum that can demand increase in its dose. The clearance of drug decreases at appointment it in a combination with antibiotics of group of macroleads, lincomycin, Allopyrinolum, Cimetidinum, izoprenaliny, beta adrenoblockers that the dose decline can demand. Oral estrogensoderzhashchy contraceptives, antidiarrheal drugs, intestinal sorbents weaken, and H2-gistaminoblokatory, blockers of slow calcium channels, мексилетин strengthen action (contact enzymatic system of P450 cytochrome and change metabolism of Aminophyllinum). In case of use in a combination with enoksatsiny and other ftorkhinolina, small doses of ethanol, Disulfiramum, recombinant interferon the alpha, a methotrexate, propafenony, thiabendazole, tiklopidiny, verapamil and at vaccination against flu intensity of action of an Euphyllinum can increase that can demand decrease in its dose. Drug suppresses therapeutic effects of lithium carbonate and beta adrenoblockers. Purpose of beta adrenoblockers interferes with bronkhodilatiruyushchy action of an Euphyllinum and can cause a bronchospasm. The Euphyllinum exponentiates effect of diuretics due to increase in glomerular filtering and reduction of a canalicular reabsorption. With care the Euphyllinum is appointed along with anticoagulants, with other derivatives of theophylline or purine. It is not recommended to apply an Euphyllinum with the means exciting the central nervous system (increases a neurotoxicity). Drug cannot be used with dextrose solutions, it is not compatible to solution of glucose, fructose and levulose. It is necessary to take into account рН the mixed solutions: pharmaceutical it is incompatible with solutions of acids.

Contraindications:

Hypersensitivity to drug, and also to other derivatives of xanthine: to caffeine, pentoksifillin, theobromine. The expressed arterial hypotension or hypertensia, a Bouveret's disease, premature ventricular contraction, a myocardial infarction with disturbances of a cordial rhythm, epilepsy, the increased convulsive readiness, a hypertrophic subaortic stenosis, a thyrotoxicosis, a fluid lungs, heavy coronary insufficiency, a liver and/or renal failure, a hemorrhagic stroke, an eye retinal apoplexy, bleeding in the recent anamnesis, the lactation period. With care: pregnancy, the neonatality period, age is more senior than 55 years and an uncontrollable hypothyroidism (a possibility of cumulation), widespread atherosclerosis of vessels, sepsis, a long hyperthermia, a gastroezofagalny reflux, a peptic ulcer of a stomach and duodenum (in the anamnesis), prostate adenoma. Drug is not recommended for intravenous administration to children up to 14 years (because of possible by-effects). 
Use at pregnancy In need of purpose of drug during pregnancy should be compared estimated advantage for mother and potential risk for a fruit. In need of use of drug during the period in the period of a lactation feeding by a breast should be stopped.

Overdose:

At overdose the dermahemia of the person, sleeplessness, motive excitement, uneasiness, a photophobia, anorexia, diarrhea, nausea, vomiting, pains in epigastric area, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, a tremor, generalized spasms, a hyperventilation, sharp lowering of arterial pressure are observed. At a serious poisoning epileptoidny attacks (especially at children without emergence of any harbingers), a hypoxia, a metabolic acidosis, a hyperglycemia, a hypopotassemia, a necrosis of skeletal muscles, confusion of consciousness, a renal failure with a myoglobinuria can develop. Treatment of overdose depends on a clinical picture, includes drug withdrawal, stimulation of its removal from an organism (an artificial diuresis, hemosorption, a plazmosorbtion, a hemodialysis, peritoneal dialysis) and purpose of symptomatic means. Diazepam is applied to stopping of spasms (in injections). It is impossible to apply barbiturates. At the expressed intoxication (the maintenance of an Euphyllinum more than 50 g/l) the hemodialysis is recommended.

Storage conditions:

List B. In the place protected from light at a temperature from 10 to 25 °C. Freezing is inadmissible. To store in the places unavailable to children. 
Period of validity 3 years. Not to apply after the term specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution in/in введ. 24mg/ml amp. 5 ml No. 10.