Euphyllinum

General characteristics. Structure:

Active ingredient: 24 mgaminofillin (Euphyllinum) in 1 ml of solution.

Excipients: water for injections.

Pharmacological properties:

Pharmacodynamics. Drug inhibits phosphodiesterase, increases accumulation in fabrics of cyclic adenosinemonophosphate, blocks adenosine (purine) receptors; reduces receipt of calcium ions via channels of cellular membranes, reduces sokratitelny activity of smooth muscles. Relaxes muscles of bronchial tubes, stops a bronchospasm, increases mukotsiliarny clearance, stimulates reduction of a diaphragm, improves function of respiratory and intercostal muscles, stimulates a respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation that finally leads to decrease in weight and frequency of episodes of an apnoea.

Normalizing respiratory function, promotes blood saturation by oxygen and to decrease in concentration of carbonic acid. Strengthens ventilation of the lungs in the conditions of a hypopotassemia. Exerts the stimulating impact on action of the heart, increases force and heart rate, raises a coronary blood stream and the need of a myocardium for oxygen. Reduces a tone of blood vessels (mainly vessels of a brain, skin and kidneys). Has peripheral venodilatiruyushchy effect, reduces pulmonary vascular resistance, lowers pressure in a "small" circle of blood circulation.

Increases a renal blood stream, renders moderate diuretic effect. Expands extrahepatic bilious ways. Slows down aggregation of thrombocytes (suppresses a factor of activation of thrombocytes and E2 prostaglandin an alpha), increases resistance of erythrocytes to deformation (improves rheological properties of blood), reduces a thrombogenesis and normalizes microcirculation. Possesses tokolitichesky action, increases acidity of a gastric juice. When using in high doses possesses epileptogenic action.

Pharmacokinetics. Bioavailability for liquid dosage forms - 90-100%. 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. Gets into breast milk (10% of the accepted dose), through a placental barrier (concentration in blood serum of a fruit is slightly higher, than in mother's serum).

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 release 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 kombinirovanyony therapy for reduction of intracranial pressure).

Left ventricular heart 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 intravenously slowly (within 4-6 minutes) 5-10 ml of solution of 24 mg/ml (0,12-0,24) which previously dissolve 0,9% of solution of sodium of chloride in 10-20 ml.

At emergence of heartbeat, dizziness, nausea rate of administering is slowed down or passed to drop introduction for what 10-20 ml of solution of 24 mg/ml (0,24-0,48) dissolve 0,9% of solution of sodium of chloride in 100-150 ml; enter with a speed of 30-50 thaws a minute. Parenterally enter an Euphyllinum to 3 times a day, no more than 14 days. 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 of an Euphyllinum for adults intravenously: one-time - 0,25 g, daily - 0,5 g 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, from 2 to 3 years - 0,09-0,12, from 4 to 7 years - 0,12-0,24, from 8 to 18 years - 0,25-0,5 g.

Features of use:

Pregnancy and lactation. In need of purpose of drug during pregnancy it is necessary to compare estimated advantage for mother and potential risk for a fruit.

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.

To be careful at the use of large numbers of kofeinsoderzhashchy products or drinks during treatment.

Before parenteral administration solution needs to be heated to body temperature.

Side effects:

From a nervous system: dizziness, a headache, sleeplessness, excitement, uneasiness, irritability, a tremor, is rare - spasms, nausea, vomiting.

From cardiovascular system: heartbeat, tachycardia (including at a fruit at reception of the pregnant woman in the III trimester), arrhythmias, a cardialgia, increase in frequency of attacks of stenocardia, a lowering of arterial pressure up to a collapse - at bystry in introduction.

From the alimentary system: gastroesophageal reflux, heartburn, aggravation of a peptic ulcer.

Allergic reactions: skin rash, skin itch, fever.

Others: a stethalgia, a tachypnea, feeling of inflows to the person, an albuminuria, a hamaturia, a hypoglycemia, strengthening of a diuresis, the increased sweating.

Local reactions: consolidation, a hyperemia, morbidity in an injection site.

Interaction with other medicines:

Pharmaceutical it is incompatible with solutions of acids. Increases probability of development of side effects of glucocorticosteroids, mineral of corticosteroids (hypernatremia), means for the general anesthesia (the risk of developing of ventricular arrhythmias increases), the means exciting the central nervous system (increases a neyrotokyosichnost).

Rifampicin, phenobarbital, Phenytoinum, isoniazid, carbamazepine, Sulfinpyrazonum, аминоглутетимид, oral estrogensoderzhashchy contraceptives and морацизин, being inductors of a microsomal oxidation, increase clearance of Aminophyllinum that can demand increase in its dose.

At simultaneous use with antibiotics of group of macroleads, lincomycin, Allopyrinolum, Cimetidinum, izoprenaliny, enoksatsiny, small doses of ethanol, Disulfiramum, ftorkhinolona, recombinant interferon the alpha, a methotrexate, meksiletiny, propafenony, thiabendazole, tiklopidiny, verapamil and at vaccination against flu intensity of action of Aminophyllinum can increase that can demand decrease in its dose.

Strengthens action beta адреностимуляторов and diuretics (including due to increase in glomerular filtering), reduces efficiency of drugs of lithium and beta adrenoblockers.

Let's combine with spasmolysants, do not apply together with other derivatives of xanthine.

With care appoint along with anticoagulants.

Contraindications:

Hypersensitivity to drug (including to other derivatives of xanthine: caffeine, пентоксифиллин, 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, hepatic and/or renal failure 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 gastroesophageal 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).

Overdose:

Symptoms: anorexia, gastralgia, diarrhea, nausea, vomiting, gastrointestinal bleeding, tachycardia, ventricular arrhythmias, tremor, generalized spasms, hyperventilation. At a serious poisoning epileptoidny attacks (especially at children without emergence of any harbingers), a hypoxia, a metabolic acidosis, a hyperglycemia, a hypopotassemia, a lowering of arterial pressure, a necrosis of skeletal muscles, confusion of consciousness, a renal failure with a myoglobinuria can develop.

Treatment: drug withdrawal, an artificial diuresis, hemosorption, a plazmosorbtion, a hemodialysis (peritoneal dialysis is inefficient), 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:

In the place protected from light at a temperature from 5 to 25 °C. To store in the place, unavailable to children. A period of validity - 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

On 10 ampoules with the application instruction, a knife ampoule or the scarificator ampoule in a pack or a box from a cardboard. When packaging the ampoules having a ring of a break or a point for opening the knife ampoule or the scarificator ampoule is not put. On 5 ampoules in cassette planimetric packaging. On 2 cassette planimetric packagings with the application instruction in a pack from a cardboard.