Euphyllin solution for intravenous administration 24 mg / ml, 5 ml No. 10

• Broncho-obstructive syndrome in bronchial asthma, bronchitis, pulmonary emphysema (mainly for relief of attacks);

• Hypertension in the 'small' circle of blood circulation.

• Impaired cerebral circulation of the ischemic type (as part of combination therapy to reduce intracranial pressure).

• Left ventricular heart failure with bronchospasm and respiratory failure of the Cheyne-Stokes type (as part of complex therapy).

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen. Individual, depending on indications, age, clinical situation, route and scheme of administration, nicotine addiction.

1 ml of the drug contains:

Active ingredient: aminophylline (aminophylline) - 24 mg

Excipient: water for injection - up to 1 ml

• Hypersensitivity to the drug, as well as to xanthine derivatives: caffeine, pentoxifylline, theobromine.

• Severe arterial hypotension or hypertension,

• paroxysmal tachycardia,

• extrasystole,

• myocardial infarction with cardiac arrhythmias,

• epilepsy,

• increased convulsive readiness,

• hypertrophic obstructive cardiomyopathy,

• thyrotoxicosis,

• pulmonary edema,

• severe coronary insufficiency,

• hepatic and / or renal failure,

• hemorrhagic stroke,

• retinal hemorrhage,

• recent history of bleeding

• acute porphyria.

Carefully

Age over 55 years and uncontrolled hypothyroidism (the possibility of cumulation), widespread atherosclerosis of the vessels, sepsis, prolonged hyperthermia, gastroesophageal reflux, gastric ulcer and duodenal ulcer (in history), prostatic hyperplasia. The drug is prescribed with caution to patients with severe impaired liver and kidney function.
Children under 14 years of age (due to possible side effects).

Trade name:

Euphyllin

International non-proprietary or group name:

Aminophylline

Dosage form:

Intravenous solution

Composition

1 ml of the drug contains:

Active ingredient: aminophylline (aminophylline) - 24 mg

Excipient: water for injection - up to 1 ml

Description

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group

Bronchodilating agent.

ATX code:

R03DA05.

Pharmacological properties

Pharmacodynamics
The drug inhibits phosphodiesterase, increases the accumulation of cyclic adenosine monophosphate in tissues, blocks adenosine (purine) receptors; has the ability to inhibit the transport of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles.

It relaxes the bronchial muscles, relieves bronchospasm, increases mucociliary clearance, stimulates diaphragm contraction, improves the function of the respiratory and intercostal muscles, stimulates the respiratory center, increases its sensitivity to carbon dioxide and improves alveolar ventilation, which ultimately leads to a decrease in the severity and frequency of apnea episodes. It normalizes the respiratory function, contributes to the saturation of blood with oxygen and a decrease in the concentration of carbon dioxide. Strengthens ventilation of the lungs in conditions of hypokalemia. It has a stimulating effect on the activity of the heart, increases the strength and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly the vessels of the brain, skin and kidneys). Has a peripheral vasodilating effect,reduces pulmonary vascular resistance, lowers pressure in the 'small' circle of blood circulation. Increases renal blood flow. Has a moderate diuretic effect. Expands the extrahepatic biliary tract. Inhibits platelet aggregation (inhibits platelet activation factor and prostaglandin E2 alpha), increases the resistance of erythrocytes to deformation (improves blood rheological properties), reduces thrombus formation and normalizes microcirculation. Has a tocolytic effect, increases the acidity of gastric juice. When used in large doses, it has an epileptogenic effect.Inhibits platelet aggregation (inhibits platelet activation factor and prostaglandin E2 alpha), increases the resistance of erythrocytes to deformation (improves blood rheological properties), reduces thrombus formation and normalizes microcirculation. Has a tocolytic effect, increases the acidity of gastric juice. When used in large doses, it has an epileptogenic effect.Inhibits platelet aggregation (inhibits platelet activation factor and prostaglandin E2 alpha), increases the resistance of erythrocytes to deformation (improves blood rheological properties), reduces thrombus formation and normalizes microcirculation. Has a tocolytic effect, increases the acidity of gastric juice. When used in large doses, it has an epileptogenic effect.

Pharmacokinetics
Bioavailability for liquid dosage forms is 90-100%. The maximum concentration (7 ?g / ml) with intravenous administration of 300 mg is achieved after 15 minutes. 60% of aminophylline (in healthy adults) and 36% (in newborns) binds to plasma proteins and is distributed in the blood, extracellular fluid and muscle tissue. Eufillin penetrates into breast milk (10% of the dose taken), through the placental barrier (the concentration in the fetal blood serum is slightly higher than in the mother's blood serum), does not accumulate in the adipose tissue. 90% of the drug is metabolized in the liver. Metabolites are excreted by the kidneys, 7-13% of the drug is excreted unchanged. The half-life in nonsmoking adults is from 5 to 10 hours, in children over 10 months from 2.5 to 5 hours. Smoking and alcohol significantly affect the metabolism and excretion of the drug,in particular, for smokers, this period is significantly reduced and ranges from 4 to 5 hours. Excretion of the drug is prolonged in patients with respiratory failure, with renal and heart failure, with viral infections and hyperthermia.

Indications for use

• Broncho-obstructive syndrome in bronchial asthma, bronchitis, pulmonary emphysema (mainly for relief of attacks);

• Hypertension in the 'small' circle of blood circulation.

• Impaired cerebral circulation of the ischemic type (as part of combination therapy to reduce intracranial pressure).

• Left ventricular heart failure with bronchospasm and respiratory failure of the Cheyne-Stokes type (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 cardiac arrhythmias,

• epilepsy,

• increased convulsive readiness,

• hypertrophic obstructive cardiomyopathy,

• thyrotoxicosis,

• pulmonary edema,

• severe coronary insufficiency,

• hepatic and / or renal failure,

• hemorrhagic stroke,

• retinal hemorrhage,

• recent history of bleeding

• acute porphyria.

Carefully

Age over 55 years and uncontrolled hypothyroidism (the possibility of cumulation), widespread atherosclerosis of the vessels, sepsis, prolonged hyperthermia, gastroesophageal reflux, gastric ulcer and duodenal ulcer (in history), prostatic hyperplasia. The drug is prescribed with caution to patients with severe impaired liver and kidney function.
Children under 14 years of age (due to possible side effects).

Application during pregnancy and during breastfeeding

If it is necessary to use the drug during pregnancy and lactation, the intended benefit to the mother should be weighed against the potential risk to the fetus or child. If necessary, the use of the drug during lactation, breastfeeding should be discontinued.

Method of administration and dosage

Intravenously.
Adults are injected slowly (over 4-6 minutes) in 5-10 ml of a solution of 24 mg / ml (0.12-0.24 g), which is previously diluted in 10-20 ml of 0.9% sodium chloride solution. When a feeling of palpitations, dizziness, nausea appears, the rate of administration is slowed down or switched to drip, for which 10-20 ml of a solution of 24 mg / ml (0.24-0.48 g) is diluted in 100-150 ml of a 0.9% solution sodium chloride; injected at a rate of 30-50 drops per minute.

Eufillin is parenterally administered up to 3 times a day, no more than 14 days.
Higher doses of aminophylline for adults with intravenous administration: single - 0.25 g, daily - 0.5 g.

If necessary, children are injected intravenously with aminophylline at the rate of a single dose of 2-3 mg / kg. Higher doses for children with intravenous administration: single - 3 mg / kg, daily - at the age of 3 months - 0.03-0.06 g, from 4 to 12 months - 0.06-0.09 g, from 2 to 3 years old - 0.09-0.12 g, from 4 to 7 years old - 0.12-0.24 g, from 8 to 18 years old - 0.25-0.5 g.

Side effect

From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremors, convulsions, nausea, vomiting.

From the side of the cardiovascular system: palpitations, tachycardia (including in the fetus when taking a pregnant woman in the third trimester), arrhythmias, a decrease in blood pressure up to collapse - with rapid intravenous administration, cardialgia, an increase in the frequency of angina attacks.

From the digestive system: gastroesophageal reflux, heartburn, exacerbation of gastric ulcer and duodenal ulcer.

Allergic reactions: skin rash, itching of the skin, fever.

Others: chest pain, tachypnea, a feeling of 'hot flashes' to the face, albuminuria, hematuria, hypoglycemia, increased urine output, increased sweating.

Local reactions: induration, hyperemia, soreness at the injection site.

Overdose

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

Treatment: drug withdrawal, forced diuresis, hemosorption, plasma sorption, hemodialysis (low efficiency, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide and ondansetron - with vomiting). If seizures occur, maintain airway patency and oxygen therapy. To stop the seizure - intravenous diazepam, 0.1-0.3 mg / kg (but not more than 10 mg). For severe nausea and vomiting, metoclopramide or ondansetron (intravenously).

Interaction with other medicinal products

The drug is incompatible with glucose, fructose solution. The pH of the mixed solutions should be taken into account: it is pharmaceutically incompatible with acid solutions.

Increases the likelihood of developing side effects of glucocorticosteroids, mineralocorticosteroids (hypernatremia), agents for general anesthesia (the risk of ventricular arrhythmias increases), agents that excite the central nervous system (increases neurotoxicity).

Doxapram, when used simultaneously with euphyllin, increases the stimulation of the respiratory center in the central nervous system.

Euphyllin exhibits synergistic toxicity with ephedrine and other sympatomimetics. When used together, the risk of arrhythmias increases. The combined use of aminophylline and xanthine derivatives, including pentoxifylline, is contraindicated due to the risk of toxicity.

Enoxacin reduces the excretion of aminophylline due to inhibition of cytochrome P4501A2; the effect of aminophylline increases by 300%, which leads to an increased risk of seizures.

The combined use of aminophylline and fluvoxamine should be avoided. If their combined use is necessary, the dose of aminophylline should be halved and the concentration of aminophylline in the blood plasma should be closely monitored.

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracizin, being inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.

With simultaneous use with antibiotics from the macrolide group, lincomycin, with fluoroquinolones, small doses of ethanol, allopurinol, beta-blockers, cimetidine, disulfiram, hormonal contraceptives for oral administration, recombinant interferon alfa, isoprenaline, viloxazatomine, vaphotrechenone, and methotrechenone against influenza, the intensity of action of aminophylline may increase, which may require a decrease in its dose.

It enhances the effect of diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium preparations and beta-blockers. Compatible with antispasmodics. With caution, it is prescribed simultaneously with antiplatelet agents (ticlopidine) - it suppresses platelet aggregation.

special instructions

Before parenteral administration, the solution must be heated to body temperature.
Elderly patients are advised to reduce the dose of the drug due to the slow elimination of it from the body. Smoking patients are advised to increase the dose due to the accelerated elimination of the drug from the body.
Avoid consuming large amounts of caffeinated foods or drinks during treatment.

Influence on the ability to drive vehicles and mechanisms

The drug may cause dizziness and other side effects. During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Release form

Solution for intravenous administration 24 mg / ml.
5 or 10 ml in ampoules made of polyethylene of low density or polypropylene (Politvist) with a twisting cap for needleless collection of the drug.
5, 10, 20, 50 or 100 ampoules with instructions for use in a carton box.

Storage conditions

Store at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life

3 years.
Do not use after the expiration date!

Vacation conditions

Dispensed by prescription.