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Pharmacodynamics
Euphylline is a complex of theophylline and ethylenediamine. Thanks to the presence of ethylenediamine, the solubility of the drug in water and the possibility of intravenous administration are achieved.
Theophylline is a bronchodilator from the methylxanthine group. The mechanism of action is primarily due to the blocking of adenosine receptors, inhibition of phosphodiesterase, an increase in the content of intracellular cAMP, a decrease in the intracellular concentration of calcium ions, as a result of which the smooth muscles of the bronchi, biliary tract, coronary, cerebral and pulmonary vessels relax, and peripheral vascular resistance decreases. By reducing vascular resistance in the pulmonary artery, it reduces pressure in the vessels of the pulmonary circulation and normalizes perfusion processes in the lungs. Improves contractility of the intercostal muscles and diaphragm, activates the respiratory center, improves alveolar ventilation and blood oxygen saturation, accelerates mucociliary transport. Prevents the release of inflammatory mediators, inhibits platelet aggregation. It increases renal blood flow and has a diuretic effect due to a decrease in tubular reabsorption of water and electrolytes. Increases the frequency and strength of heart contractions, increases coronary blood flow and myocardial oxygen demand.
Pharmacokinetics
Chemical binding to ethylenediamine does not affect the pharmacokinetics and bioavailability of theophylline. In adults, about 60% of theophylline is bound to plasma proteins. The volume of distribution of theophylline is about 0.5 l/kg. Theophylline is distributed in the blood, extracellular fluid and muscle tissue.
Penetrates through the placental barrier and into breast milk.
The clearance of theophylline depends on age, body weight, diet, smoking habit, and concomitant use of other medications. In patients with cardiac or respiratory failure, impaired liver function, or viral infection, the half-life is prolonged.

Indications for use

Broncho-obstructive syndrome in bronchial asthma and chronic obstructive pulmonary disease.

Contraindications

Hypersensitivity to ethylenediamine or allergy to theophyllines, caffeine and theobromine,
- simultaneous use with other xanthine-containing drugs. When therapeutic doses of aminophylline and/or theophylline are administered simultaneously, by more than one route of administration, or in more than one drug product, the risk of serious toxicity increases,
- children up to 6 months of age,
- acute porphyria,
- acute period of myocardial infarction,
- paroxysmal tachycardia.

Precautionary measures

To reduce the undesirable stimulating effects of aminophylline on the central nervous and cardiovascular systems, intravenous administration of the drug should be slow and the rate should not exceed 25 mg/min.
Eufillin has a narrow therapeutic index and serum concentrations should be monitored regularly, especially during initiation of therapy.
The drug should be administered with caution in patients over 55 years of age.
Elderly patients with cardiac or hepatic disease should be closely monitored for signs of theophylline toxicity.
Children are particularly susceptible to the effects of theophylline and caution is required when prescribing the drug to children.
There have been reports of seizures in children who were prescribed theophylline at plasma concentrations within the accepted therapeutic range. Alternative treatment should be considered in patients with a history of seizure activity, and if Eufillin, intravenous solution 24 mg/ml is used in such patients, they should be carefully monitored for possible signs of CNS hyperstimulation.
Due to the fact that the average half-life of theophylline is shorter in smokers than in non-smokers, the former group may require larger doses of aminophylline.
Caution should be exercised in patients who have received influenza immunization, those with influenza infection, or those with acute febrile illnesses.
Eufillin should be prescribed with caution to patients with heart failure, chronic obstructive pulmonary disease, renal or hepatic dysfunction and chronic alcoholism, since the clearance of aminophylline is reduced.
Serum potassium levels should be monitored during regular therapy. This is very important when combined therapy with beta-2 agonists, corticosteroids or diuretics, or in the presence of hypoxia.
The drug should be used with caution in patients with peptic ulcer disease, hyperthyroidism, glaucoma, diabetes mellitus, severe hypoxemia, hypertension and impaired cardiac function or circulation, as these conditions may be aggravated.
Methylxanthines may increase gastric acidity and appropriate precautions should be taken if used in patients with a history of peptic ulcers.
The drug Eufillin, solution for intravenous administration 24 mg/ml should not be prescribed simultaneously with other xanthine-containing drugs.
Theophylline should be used only after assessing the benefit/risk ratio in patients with unstable angina, hypertrophic obstructive cardiomyopathy, cardiac arrhythmias (tachycardia, extrasystole), hemorrhagic stroke, retinal hemorrhage.

Interaction with other drugs

The following drugs may decrease the clearance of aminophylline, resulting in theophylline concentration increases in plasma and creates the potential for increased toxicity:
- fluvoxamine (concomitant use of theophylline and fluvoxamine should generally be avoided. Where possible, patients should receive their theophylline dose (possibly reduced by half) and plasma theophylline levels should be closely monitored);
- cimetidine;
- macrolides (for example, erythromycin, clarithromycin);
- quinolones (for example, ciprofloxacin, norfloxacin);
- fluconazole;
- isoniazid;
- propranolol;
- allopurinol (for example, high doses 600 mg per day);
- oral contraceptives;
- mexiletine, propafenone;
- calcium channel blockers, diltiazem, verapamil;
- medicines based on St. John's wort;
- disulfiram;
- interferon alpha, influenza vaccines;
- methotrexate;
- zafirlukast;
- tacrine;
- thiabendazole;
- thyroid hormones.
The following medicines may reduce concentrationtheophylline in plasma:
- rifampicin;
- antiepileptics (for example, carbamazepine, phenytoin, primidone, phenobarbital);
- ritonavir;
- aminoglutethimide;
- sulfpyrazone.
Other interactions:
- xanthines (concomitant use of other xanthine derivatives, including theophylline and pentoxifylline, is contraindicated due to the risk of toxicity);
- lithium (aminophylline increases the excretion of lithium and may reduce its therapeutic effectiveness);
- benzodiazepines (theophylline can reduce the effect of benzodiazepines);
- quinolones (increased risk of seizures);
- general anesthetics (increased risk of seizures with ketamine, increased risk of arrhythmia with halothane);
- pancuronium (resistance to neuromuscular block with pancuronium has been reported in patients receiving aminophylline);
- sympathomimetics (aminophylline may exhibit synergistic toxicity with ephedrine and other sympathomimetics when used together and may lead to cardiac arrhythmia);
- β2-agonists (increased risk of cardiac arrhythmia (see also hypokalemia);
- β-blockers (antagonism with the bronchodilator effect of aminophylline);
- cardiac glycosides (the direct stimulating effect of aminophylline on the myocardium can increase the sensitivity and toxic potential of cardiac glycosides);
- adenosine (antagonism of the antiarrhythmic effect of adenosine with theophylline);
- leukotriene antagonists (in clinical studies, coadministration with theophylline resulted in a decrease in plasma levels of zafirlukast by approximately 30%, but did not affect plasma concentrations of theophylline. However, during post-marketing surveillance, there were rare cases of increased theophylline levels in patients using zafirlukast (see above));
- doxapram (increased stimulation of the central nervous system);
- hypokalemia (the hypokalemic effect of beta-2 agonists may be enhanced by concomitant treatment with aminophylline. There is an increased risk of hypokalemia when theophylline derivatives are prescribed together with corticosteroids and diuretics (see Precautions)).

Pregnancy and lactation

Studies of the effect on reproductive function in animals have not been conducted. It is not known whether theophylline can cause fetal harm when administered to pregnant women. Although the safe use of theophylline during pregnancy has not been established regarding potential risk to the fetus, theophylline has been used during pregnancy without teratogenicity or other adverse effects on the fetus. Due to the risk of uncontrolled bronchial asthma, safety during pregnancy, when the administration of aminophylline is really necessary, is usually not questioned. The question of using aminophylline during pregnancy is decided by the doctor. Theophylline crosses the placenta.
Theophylline is distributed into breast milk and may occasionally cause irritation or other signs of toxicity in nursing infants and therefore should not be used by nursing mothers.

Impact on the ability to drive vehicles and operate machinery

The medicine may cause dizziness and other side effects. During the treatment period, you must refrain from driving vehicles and operating machinery.

Directions for use and dosage

The drug is intended for slow intravenous administration.
The solution should be administered very slowly over 4-6 minutes, 5-10 ml of the drug (0.12-0.24 g), which is pre-diluted with a small volume (5-10 ml) of 5% dextrose or 0.9% solution sodium chloride for injection.
Before administration, the solution must be warmed to body temperature. Eufillin is administered parenterally up to 3 times a day, for no more than 14 days. Higher doses of aminophylline for adults when administered intravenously: single - 0.25 g, daily - 0.5 g.
Maintenance therapy can be provided by administering large volumes of infusion solutions, the rate of administration is adjusted to provide the required amount of drug every hour.
Typically, when administered by drip, 10-20 ml of the drug (0.24-0.48 g) is diluted in 100-150 ml of 0.9% sodium chloride solution and administered at a rate of 30-50 drops per minute.
Theophylline therapeutic plasma concentrations are considered to range from 5 to 20 mcg/mL, and levels above 20 mcg/mL are most likely associated with toxicity. There is also individual patient variation in the dosage required to achieve plasma theophylline concentrations within the desired therapeutic range.
During therapy, patients should be closely monitored for toxicity and, where possible, theophylline levels should also be monitored; doses should be based on ideal body weight; the drug is not recommended for children under 6 months of age due to significant fluctuations in the metabolism of theophylline in young children.
Patients not receiving drugs containing theophylline
A. A loading dose of aminophylline 6 mg/kg body weight can be administered intravenously slowly at a rate not exceeding 25 mg/min.
B. Depending on the patient's condition, the maintenance dose for the next 12 hours can be calculated as follows:
- children aged 6 months to 9 years: 1.2 mg/kg/hour (decrease to 1 mg/kg/hour after 12 hours);
- children aged 9 to 16 years and young adult smokers: 1 mg/kg/hour (reduced to 0.8 mg/kg/hour after 12 hours);
- healthy non-smoking adults: 0.7 mg/kg/hour (decrease to 0.5 mg/kg/hour after 12 hours);
- elderly patients and persons with cor pulmonale: 0.6 mg/kg/hour (decrease to 0.3 mg/kg/hour after 12 hours);
- patients with congestive heart failure or liver disease: 0.5 mg/kg/hour (reduction to 0.1-0.2 mg/kg/hour after 12 hours).
Patients already receiving theophylline
The loading dose can be calculated on the basis that every 0.5 mg/kg of theophylline administered as a loading dose would result in a 1 mcg/mL increase in serum theophylline concentration.
Ideally, administration should be delayed until serum theophylline is determined. If this is not possible and if the clinical situation requires that the drug be administered, then administer 3.1 mg/kg aminophylline (equivalent to 2.5 mg/kg theophylline anhydrous) on the basis that this may result in increased serum theophylline concentrations approximately 5 mcg/ml when administered as a loading dose.
In the future, the maintenance dose is recommended to be the same as described above.

Overdose

Eufillin has a narrow therapeutic index. Theophylline toxicity is most likely to occur at serum concentrations greater than 20 mcg/mL and becomes increasingly severe at higher serum concentrations.
Doses greater than 3 g may have serious effects in adults (40 mg/kg in a child). The lethal dose may be as low as 4.5 g in adults (60 mg/kg in children), but is usually higher.
When aminophylline is administered intravenously in large doses in patients with renal, liver failure or cardiovascular complications, or if the injection is given quickly, death is possible.
Symptoms: tachycardia, in the absence of hypoxia, fever, or during coadministration of sympathomimetic drugs, may be a sign of theophylline toxicity.
Gastrointestinal symptoms: anorexia, nausea, vomiting, diarrhea, vomiting blood.
Neurological symptoms: anxiety, insomnia, irritability, headache, agitation, hallucinations, extreme thirst, slight fever, dilated pupils and tinnitus. Seizures can occur even without previous symptoms of toxicity and often lead to death. In very severe cases, coma may develop.
Cardiovascular symptoms: palpitations, arrhythmias, arterial hypotension, supraventricular and ventricular arrhythmias.
Metabolic symptoms: Hypokalemia can develop quickly and can be severe. Hyperglycemia, albuminuria, hyperthermia, hypomagnesemia, hypophosphatemia, hypercalcemia, respiratory alkalosis, metabolic acidosis, and rhabdomyolysis may also develop.
Treatment: Treatment of overdose is supportive and symptomatic.
Serum theophylline and potassium levels should be checked. Repeated oral administration of activated charcoal promotes the removal of theophylline from the body, even after intravenous administration. Aggressive antiemetic therapy may be required to allow oral administration of activated charcoal.
Convulsions can be stopped by intravenous administration of diazepam 0.1-0.3 mg/kg to 10 mg/kg. Restoring fluid and electrolyte balance is essential. Hypokalemia should be corrected by intravenous infusion of potassium chloride. Sedation with diazepam may be required in agitated patients.
Propranolol can be administered intravenously to correct tachycardia, hypokalemia and hyperglycemia, provided that the patient does not suffer from asthma.
In general, theophylline is metabolized quickly and hemodialysis is not warranted. In patients with congestive heart failure or liver disease, hemodialysis may increase the clearance of theophylline by 2-fold.
Hemosorption should be considered if:
- intestinal obstruction prevents the administration of several doses of activated carbon;
- plasma concentrations of theophylline >80 mg/l (acute) or >60 mg/l (chronic). In the elderly, hemosorption should be considered at theophylline concentrations >40 mg/L. Clinical signs, rather than theophylline concentration, are the best guide for treatment.

Active substance

Aminophylline

Dosage form

solution for infusion

Manufacturer

Dalkhimfarm, Russia

Compound

1 ml of solution for intramuscular administration contains:
active ingredient: aminophylline 24 mg.

pharmachologic effect

Pharmaceutical group: bronchodilator.
Pharmaceutical action: Bronchodilator, methylxanthine derivative; inhibits PDE, increases the accumulation of cAMP in tissues, blocks adenosine (purine) receptors; reduces the flow of Ca2+ through the channels of cell membranes, reduces the contractile activity of smooth muscles.
Relaxes the bronchial muscles, stimulates the respiratory center and improves alveolar ventilation, which ultimately leads to a reduction in the severity and frequency of apnea episodes.
It has a stimulating effect on the activity of the heart, increases strength and heart rate, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly those of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, and lowers pressure in the pulmonary circulation. Increases renal blood flow and has a moderate diuretic effect. Expands extrahepatic bile ducts.
Stabilizes mast cell membranes, inhibits the release of mediators of allergic reactions.
Inhibits platelet aggregation (suppresses platelet activating factor and PgE2 alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation.
It has a tocolytic effect, increases the acidity of gastric juice. When used in large doses, it has an epileptogenic effect.
Pharmacokinetics: After oral administration, it is quickly and completely absorbed, however, the bioavailability and kinetics of absorption depend on the dosage form of the drug. Bioavailability for tablet forms with rapid release of the active substance and liquid dosage forms is 90-100%. When using prolonged dosage forms, absorption parameters and bioavailability may vary. Food reduces the rate of absorption without affecting its magnitude (large volumes of liquid and proteins speed up the process). The higher the dose taken, the lower the absorption rate. TCmax with intravenous administration of 0.3 g - 15 min, Cmax value - 7 μg/ml. TCmax for conventional dosage forms - 1-2 hours, for extended-release forms - 4-7 hours, for enteric-coated tablets - 5 hours. The volume of distribution is in the range of 0.3-0.7 l/kg (30-70% of the “ideal” weight body), on average 0.45 l/kg. Communication with plasma proteins in adults - 60%, in newborns - 36%, in patients with liver cirrhosis - 36%. 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 maternal serum).
Aminophylline exhibits bronchodilating properties in concentrations of 10-20 mcg/ml. Concentrations above 20 mg/ml are toxic. The stimulating effect on the respiratory center is realized at a lower content of the drug in the blood - 5-10 mcg/ml.
Metabolized at physiological pH values ​​with the release of free theophylline, which is further metabolized in the liver with the participation of several cytochrome P450 isoenzymes. As a result, 1,3-dimethyluric acid (45-55%) is formed, which has pharmacological activity, but is 1-5 times inferior to theophylline. Caffeine is an active metabolite and is formed in small quantities, with the exception of premature newborns and children under 6 months, in whom, due to the extremely long half-life of caffeine, its significant accumulation occurs in the body (up to 30% of that for aminophylline).
In children over 3 years of age and in adults, the phenomenon of caffeine accumulation is absent.
T1/2 in newborns and children under 6 months - more than 24 hours; in children over 6 months - 3.7 hours; in adults - 8.7 hours; for “smokers” (20-40 cigarettes per day) - 4-5 hours (after quitting smoking, pharmacokinetics normalize after 3-4 months); in adults with COPD, pulmonary heart disease and pulmonary heart failure - over 24 hours. Excreted by the kidneys. In newborns, about 50% of theophylline is excreted unchanged in the urine versus 10% in adults, which is associated with insufficient activity of liver enzymes.

Indications

• Broncho-obstructive syndrome (mainly to relieve attacks) with:
  • Bronchial asthma.
  • Bronchitis.
  • Pulmonary emphysema.
  • Cardiac asthma.
• Hypertension in the pulmonary circulation.
• Relief of cerebral vascular crises of atherosclerotic origin.
• As part of combination therapy for ischemic strokes and chronic cerebrovascular insufficiency to reduce intracranial pressure and cerebral edema.

Contraindications

Hypersensitivity (including to other xanthine derivatives: caffeine, pentoxifylline, theobromine), epilepsy, peptic ulcer of the stomach and duodenum (in the acute stage - for oral forms, especially non-extended-release tablets), gastritis with high acidity, severe arterial hyper- or hypotension, severe tachyarrhythmias, hemorrhagic stroke, retinal hemorrhage, children's age (up to 3 years, for prolonged oral forms - up to 12 years).
Carefully. Severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread vascular atherosclerosis, HOCM, frequent ventricular extrasystole, increased convulsive readiness, liver and/or renal failure, peptic ulcer of the stomach and duodenum (history), bleeding from the gastrointestinal tract in recent history, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy. pregnancy, lactation, old age, childhood (especially for oral forms).

Side effects

From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.
From the cardiovascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks.
From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with long-term use - loss of appetite.
Allergic reactions: skin rash, skin itching, fever.
Other: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.
Side effects decrease with decreasing dosage of the drug.
Local reactions: compaction, hyperemia, pain at the injection site.
When administered rectally - proctitis, irritation of the rectal mucosa.

Interaction

When used simultaneously with sympathomimetics, a mutual enhancement of action occurs; with beta-blockers and lithium preparations - the effect is mutually reduced. The intensity of action of aminophylline may decrease (due to an increase in its clearance) when used simultaneously with phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazone, phenytoin, as well as in smokers.

The intensity of action of aminophylline may increase (due to a decrease in its clearance) when used simultaneously with macrolide antibiotics, lincomycin, quinolones, allopurinol, beta-blockers, cimetidine, disulfiram, fluvoxamine, hormonal contraceptives for oral administration, isoprenaline, viloxazine and when vaccinated against flu
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Xanthine derivatives can potentiate hypokalemia caused by the action of β2-adrenergic receptor stimulants, corticosteroids and diuretics.

Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.
Pharmaceutically incompatible with acid solutions.

How to take, course of administration and dosage

Eufillin is prescribed intramuscularly, 1 ml (240 mg) of solution deep into the upper quadrant of the gluteal muscle.

Eufillin is administered parenterally up to 3 times a day, for no more than 14 days. The concentration of aminophylline in blood serum should not exceed 20 mcg/ml.

• Higher doses of aminophylline for intramuscular administration
  • For adults: single dose - 0.5 g, daily - 1.5 g.
  • For children: single dose - 7 mg/kg, daily dose - 15 mg/kg.

Correction of the dosage regimen may be required for heart failure, liver dysfunction, and chronic alcoholism.

In elderly patients, a dose reduction may be required (single dose - 0.3 g).

from 1 year to 9 years - 22 mg/kg;
from 9 to 12 years - 20 mg/kg;
from 12 to 16 years - 18 mg/kg;
over 16 years old - 13 mg/kg.
Children are prescribed intramuscularly at a dose of 15 mg/kg/day. IV at the age of up to 3 months - 30-60 mg/day, 4-12 months - 60-90 mg/day, 2-3 years - 90-120 mg, 4-7 years - 120-240 mg, 8- 18 years old - 250-500 mg/day. The duration of parenteral administration is no more than 14 days.
For neonatal apnea, the initial dose (a condition characterized by periods of absence of breathing for 15 seconds and accompanied by cyanosis and bradycardia) is 5 mg/kg (by nasogastric tube), maintenance dose is 2 mg/kg in 2 divided doses. The duration of treatment is several weeks, in rare cases - months.
Can be administered rectally in the form of microenemas. Dose for adults - 0.24-0.48 g in 20-25 ml of warm water; for children - less, according to age.
Higher doses for adults orally, intramuscularly and rectally - single 0.5 g, daily 1.5 g; IV - single dose 0.25 g, daily 0.5 g.
Higher doses for children orally, intramuscularly and rectally - single 7 mg/kg, daily 15 mg/kg; IV - single dose 3 mg/kg.

Overdose

Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, flushing of the facial skin, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions . In severe poisoning, epileptoid seizures may develop (especially in children without any warning signs), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, decreased blood pressure, skeletal muscle necrosis, confusion, renal failure with myoglobinuria.
Treatment: drug withdrawal, gastric lavage, administration of activated charcoal, laxatives, intestinal lavage with a combination of polyethylene glycol and electrolytes, forced diuresis, hemosorption, plasma sorption, hemodialysis (low efficiency, peritoneal dialysis is ineffective), symptomatic therapy (including metoclopramide and ondansetron - when vomiting). If convulsions occur, maintain airway patency and administer oxygen therapy. To stop a seizure - intravenous diazepam, 0.1-0.3 mg/kg (but not more than 10 mg). For severe nausea and vomiting, use metoclopramide or ondansetron (iv).

Instructions for use:

Eufillin is a bronchodilator.

Pharmacological properties

Euphyllin belongs to the group of xanthines. It contains the main active ingredient - theophylline. The drug has a dilating effect on the bronchi, relaxing their smooth muscles and eliminating spasms. In addition, it improves the functioning of the cilia of the respiratory tract epithelium, improves the contractions of the diaphragmatic, intercostal and other respiratory muscles. Eufillin stimulates the respiratory center in the medulla oblongata, improves pulmonary ventilation, oxygen saturation of the blood and reduces the carbon dioxide content in it, that is, normalizes respiratory function.

The mechanism of action of Eufillin is the inhibition of the phosphodiesterase enzyme, due to which cAMP accumulates in the tissues, the flow of calcium ions into the cells, which are responsible for muscle contraction, is reduced, and this relaxes the bronchial muscles.

According to the instructions, aminophylline stimulates cardiac activity, increasing the frequency and force of myocardial contraction. It can reduce the tone of blood vessels, mainly the skin, kidneys and brain. By having a relaxing effect on the venous walls in the pulmonary circulation, the drug reduces pressure in it.

The use of Eufillin improves blood supply to the kidneys, thereby increasing the formation and excretion of urine.

The drug slows down platelet aggregation and makes red blood cells more resistant to damage, that is, it improves the rheological properties of blood.

Eufillin is known to have a tocolytic effect on the uterus; it also increases the acidity of gastric juice.

The product is well absorbed from the digestive tract, its bioavailability reaches 100%. When taken simultaneously with food, absorption slows down somewhat. It passes into breast milk and through the placenta. Euphyllin metabolism occurs in the liver, and it is excreted from the body in the urine.

Release form

Eufillin according to the instructions is produced in tablets of 150 mg, in ampoules in the form of 2.4% and 24% solution.

Indications

The drug is used to relieve attacks of bronchial asthma, heart failure, angina pectoris, pulmonary edema and other conditions associated with congestion. According to reviews, Eufillin effectively reduces blood pressure during hypertensive crises. It is used in the complex treatment of stroke and other ischemic conditions of the brain, and in the treatment of neonatal apnea.

Contraindications

The use of Eufillin is contraindicated in cases of intolerance, during the acute period of myocardial infarction, collapse, paroxysmal tachycardia, extrasystole, epilepsy, hyperthyroidism, peptic ulcer, disorders of the liver and kidneys, prostate adenoma, diarrhea. The use of the drug in tablets is not recommended for children under 6 years of age.

Instructions for use of Eufillin

In the form of a solution, the drug is administered intravenously and intramuscularly; parenteral use is justified in the treatment of emergency conditions. In this case, the dosage is calculated individually, depending on the severity of the condition and the patient’s weight.

For adults in emergency situations, the dose of Eufillin according to the instructions is selected at the rate of 6 mg/kg, it is diluted in 20 ml of physiological sodium chloride solution, and administered intravenously slowly over at least 5 minutes.

Asthmatic status requires infusion administration of the drug in the amount of 720 - 750 mg. Parenteral administration of Eufillin is not recommended for longer than 14 days.

To alleviate the condition of chronic obstructive pulmonary diseases in the acute phase, start with a dose of 5–6 mg/kg of the drug. If necessary, it should be increased very carefully, under control of its content in the blood.

Eufillin tablets are taken 0.15 g 1 to 3 times a day, after meals. The course of treatment can last from several days to several months.

For apnea of ​​newborns, when breathing stops last for 15 seconds with a simultaneous decrease in heartbeat, the initial dose of this drug for newborns is 5 mg/kg/day in 2 divided doses. The drug is administered through a nasogastric tube. When the condition stabilizes, switch to a maintenance dose of 2 mg/kg/day in 2 divided doses. The duration of use can range from several weeks to several months.

Depending on the severity of the condition and indications for Eufillin in children, the daily dose varies from 6 to 15 mg/kg.

For elderly patients, caution should be exercised when treating with the drug. According to reviews, Eufillin enhances the side effects of glucocorticoids, mineralocorticoids and adrenergic stimulants. Do not use this product simultaneously with other xanthine derivatives.

Side effects of Eufillin

According to reviews, Eufillin can cause such undesirable effects as insomnia, dizziness, agitation, headaches, tremors, increased heart rate, arrhythmias, heart pain, decreased blood pressure, abdominal pain, nausea, heartburn, vomiting, diarrhea, allergic reactions, increased sweating, decreased blood glucose, changes in urine tests.

Catad_pgroup Antiasthmatic drugs

Eufillin solution - instructions for use

INSTRUCTIONS for medical use of the drug

Registration number:

Tradename:

Eufillin

INN:

Aminophylline

Dosage form:

solution for intravenous administration

Compound:

1 ml contains:

Active substance:
aminophylline for injection (aminophylline) - 24.0 mg;

Excipient:
water for injection - up to 1 ml

Description:

clear, colorless or slightly colored liquid

Pharmacotherapeutic group:

bronchodilator

ATX code:

R03DA05

Pharmacological properties

Smart Eating
The drug inhibits phosphodiesterase, increases the accumulation of cyclic adenosine monophosphate in tissues, blocks adenosine (purine) receptors, reduces the flow of calcium ions through cell membrane channels, and reduces the contractile activity of smooth muscles.

Relaxes the bronchial muscles, stimulates the respiratory center and improves alveolar ventilation, which ultimately leads to a reduction in the severity and frequency of apnea episodes.

It has a stimulating effect on the activity of the heart, increases the strength and frequency of heart contractions, increases coronary blood flow and myocardial oxygen demand. Reduces the tone of blood vessels (mainly those of the brain, skin and kidneys). It has a peripheral venodilating effect, reduces pulmonary vascular resistance, and lowers pressure in the pulmonary circulation. Increases renal blood flow, enhances the release of adrenaline by the adrenal glands. Has a moderate diuretic effect. Expands extrahepatic bile ducts. Inhibits platelet aggregation (suppresses platelet activating factor and prostaglandin E2 alpha), increases the resistance of red blood cells to deformation (improves the rheological properties of blood), reduces thrombus formation and normalizes microcirculation.

It has a tocolytic effect, increases the acidity of gastric juice. When used in large doses, it has an epileptogenic effect.

Theophylline is a bronchodilator from the methylxanthine group. The mechanism of action is primarily due to the blocking of adenosine receptors, inhibition of phosphodiesterase, an increase in the content of intracellular cAMP, a decrease in the intracellular concentration of calcium ions, as a result of which the smooth muscles of the bronchi, biliary tract, coronary, cerebral and pulmonary vessels relax, and peripheral vascular resistance decreases. By reducing vascular resistance in the pulmonary artery, it reduces pressure in the vessels of the pulmonary circulation and normalizes perfusion processes in the lungs. Improves contractility of the intercostal muscles and diaphragm, activates the respiratory center, improves alveolar ventilation and blood oxygen saturation, accelerates mucociliary transport. Prevents the release of inflammatory mediators, inhibits platelet aggregation. It increases renal blood flow and has a diuretic effect due to a decrease in tubular reabsorption of water and electrolytes. Increases the frequency and strength of heart contractions, increases coronary blood flow and myocardial oxygen demand.
Bioavailability of the drug is 90-100%.

The maximum concentration (7 mcg/ml) with intravenous administration of 300 mg is achieved after 15 minutes.

The volume of distribution is in the range of 300-700 ml/kg (30-70% of “ideal” body weight), with an average of 450 ml/kg.

Communication with plasma proteins in adults - 60%, in newborns - 36%, in patients with liver cirrhosis - 36%. 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 maternal blood serum).

Aminophylline exhibits bronchodilating properties in concentrations of 10-20 mcg/ml. Concentrations above 20 mg/ml are toxic. The stimulating effect on the respiratory center is realized at a lower content of the drug in the blood - 5-10 mcg/ml.

Metabolized at physiological pH values ​​with the release of free theophylline, which is further metabolized in the liver with the participation of several cytochrome P450 isoenzymes. As a result, 1,3-dimethyluric acid (45-55%) is formed, which has pharmacological activity, but is 1-5 times inferior to theophylline. Caffeine is an active metabolite and is formed in small quantities, with the exception of premature newborns and children under 6 months, in whom, due to the extremely long half-life of caffeine, its significant accumulation in the body occurs (up to 30% of that for aminophylline).

In children over 3 years of age and in adults, the phenomenon of caffeine accumulation is absent.

The half-life in newborns and children under 6 months is more than 24 hours; in children over 6 months - 3.7 hours; in adults - 8.7 hours; for smokers (20-40 cigarettes per day) - 4-5 hours (after quitting smoking, normalization of pharmacokinetics occurs for 3-4 months); in adults with chronic obstructive pulmonary disease (COPD), pulmonary heart failure - over 24 hours.

Excreted by the kidneys. In newborns, about 50% of theophylline is excreted unchanged in the urine versus 10% in adults, which is associated with insufficient activity of liver enzymes.

Indications for use:

Broncho-obstructive syndrome of any origin: bronchial asthma (the drug of choice in patients with bronchial asthma of physical exertion and as an additional remedy for other forms), chronic obstructive pulmonary disease, emphysema, chronic obstructive bronchitis, hypertension in the pulmonary circulation, night apnea. Ischemic cerebrovascular accident (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 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 eyes, recent history of bleeding.

Carefully

Sepsis, peptic ulcer of the stomach and duodenum (history), old age (over 55 years), uncontrolled hypothyroidism (possibility of cumulation), widespread vascular atherosclerosis, prostatic hyperplasia, children under 14 years of age (due to possible side effects).

Pregnancy and lactation

If it is necessary to use the drug during pregnancy, the expected benefit to the mother should be compared with the potential risk to the fetus.

If it is necessary to use the drug during breastfeeding, breastfeeding should be discontinued.

Directions for use and doses

Method of administration: intravenously.

Adults are administered slowly (over 4-6 minutes) 5-10 ml of the drug (0.12-0.24 g), which is pre-diluted in 10-20 ml of 0.9% sodium chloride solution.

If a feeling of palpitations, dizziness, or nausea occurs, the rate of administration is slowed down or switched to drip administration, for which 10-20 ml of the drug (0.24-0.48 g) is diluted in 100-150 ml of 0.9% sodium chloride solution; administered at a rate of 30-50 drops per minute.

Before parenteral administration, the solution must be warmed to body temperature. Aminophylline is administered parenterally up to 3 times a day, for no more than 14 days. Higher doses of aminophylline for adults when administered intravenously: single - 0.25 g, daily - 0.5 g.

If necessary, children are administered aminophylline intravenously by drip at a single dose of 2-3 mg/kg. Higher doses for children with intravenous administration: single - 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 effect

From the nervous system: dizziness, headache, insomnia, agitation, anxiety, irritability, tremor.

From the cardiovascular system: palpitations, tachycardia (including in the fetus when taken by a pregnant woman in the third trimester), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks.

From the digestive system: gastralgia, nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea, with long-term use - decreased appetite.

Allergic reactions: skin rash, skin itching, exfoliative dermatitis, fever.

Other: chest pain, tachypnea, feeling of “hot flashes” in the face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Side effects decrease when the dose of the drug is reduced, when the method of administration is changed (from jet to drip).

Local reactions: compaction, hyperemia, pain at the injection site.

Overdose

Symptoms: loss of appetite, gastralgia, diarrhea, nausea, vomiting (including blood). gastrointestinal bleeding, tachypnea, facial skin flushing, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia. tremor, convulsions. In severe poisoning, epileptoid convulsions may develop (especially in children without any warning signs), 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 intravenous metoclopramide for vomiting). If convulsions occur, maintain airway patency and administer oxygen therapy. To relieve seizures, administer diazepam 0.1-0.3 mg/kg intravenously (but not more than 10 mg).

Interaction with other drugs

Pharmaceutically incompatible with acid solutions.

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

Antidiarrheal drugs and oral estrogen-containing contraceptives weaken the effect of aminophylline (they bind to the cytochrome P450 enzymatic system and change the metabolism of aminophylline).

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine and moracizine, being inducers of microsomal oxidation, increase the clearance of aminophylline, which may require an increase in its dose.

When used simultaneously with macrolide antibiotics, lincomycin, allopurinol, cimetidine, isoprenaline, small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil and with influenza vaccination, the intensity of the action of aminophylline may increase, which may require a reduction in its dose.

Enhances the effect of beta-adrenergic stimulants and diuretics (including by increasing glomerular filtration), reduces the effectiveness of lithium preparations and beta-blockers.

Compatible with antispasmodics, do not use in combination with other xanthine derivatives.

Prescribe with caution simultaneously with anticoagulants.

special instructions

Use caution when consuming large amounts of caffeine-containing foods or drinks during treatment.

Before use, the drug solution must be warmed to body temperature.

Impact on the ability to drive vehicles, operate machinery and engage in other activities that require concentration and speed of psychomotor reactions.
During treatment with the drug, it is not recommended to drive vehicles, machinery, or engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Release form:

Solution for intravenous administration 24 mg/ml.
5 or 10 ml in neutral glass ampoules. 10 ampoules each along with instructions for use and an ampoule scarifier in a cardboard box.
5 ampoules per blister pack. 2 blister packs each, along with instructions for use and an ampoule scarifier in a cardboard pack.
When using ampoules with a notch, a point or a break ring, do not insert a scarifier.

Storage conditions:

In a place protected from light at a temperature of 2 to 25 ° C.
Keep out of the reach of children.

Best before date:

3 years.
Do not use after the expiration date stated on the package.

Vacation conditions

Prescription release.

Manufacturer's address/
Organization accepting complaints:

st. Bolshiye Kamenschiki, 9, Moscow, 115172

Place of production

JSC "Moskhimfarmpreparaty" named after. N.A. Semashko"
1. st. Sergius of Radonezh, 15-17, Moscow. 107120;
2. st. B. Kamenshchiki, 9, Moscow. 115172.

Many of us have encountered illnesses where breathing was difficult, shortness of breath was excruciating, and it was impossible to clear our throat. Often, the doctor prescribed a remedy such as Eufillin, which brought instant relief. Asthmatics know about this drug firsthand: it is their constant companion, a savior during asthmatic attacks. Possessing powerful vasodilator and bronchodilator effects, the medicine quickly relieves unpleasant symptoms caused by bronchial obstruction and bronchospasm. It is most effective to use Eufillin intravenously.

pharmachologic effect

The drug Eufillin is a bronchodilator, antispasmodic, vasodilator and bronchodilator. The active substance of the drug aminophylline has a relaxing effect. By expanding the bronchi, it helps to reduce the tone of their muscles and eliminate spasms. The drug has a beneficial effect on respiratory function, saturating the blood with oxygen and reducing the content of carbon dioxide in it. At the same time, the medicine relieves pressure on the blood vessels, improving the functioning of the cardiovascular system, in particular the functioning of the myocardium.

Eufillin stimulates the renal blood supply, due to which the formation and outflow of urine from the body increases, that is, it has a mild diuretic effect.

Providing a tocolytic effect, the drug increases the acidity of gastric juice. By slowing platelet aggregation, the drug has a beneficial effect on red blood cells, making them more invulnerable to damage, as well as thinning the blood.

The drug, entering the digestive tract, quickly spreads through the bloodstream throughout the body. The onset of the effect slows down when consuming food simultaneously with Eufillin. Easily penetrates the placenta and is excreted in breast milk.

The medicine is processed in the liver and leaves the body in the urine.

Release forms and composition

The drug is released in tablet form with a dosage of 150 mg.

The most common injection solution is produced in ampoules. The content of the active substance in the solution can be 2.4 mg/ml or 240 mg/ml. The first option is used for intravenous administration, the second - for intramuscular administration. A cardboard box contains 5 or 10 ampoules of 5 or 10 ml.

Eufillin, injections, contains:

• aminophylline, active substance - 24 or 240 mg;
• water for injections - 1 ml.

Indications for use

The medicine is prescribed in the case of:

• bronchial asthma;
• asthmatic bronchitis;
• chronic obstructive pulmonary disease;
• emphysema;
• the presence of a “pulmonary” heart;
• Pickwick's syndrome (apnea);
• increased intracranial pressure.

Parenteral solution for internal administration is used:

• to relieve asthmatic attacks;
• in case of acute cerebrovascular accident (stroke) and cerebral edema;
• in the presence of left ventricular failure with bronchospasm of the Cheyne-Stokes type;
• in cases of apnea in newborns;
• if there is acute or chronic heart failure;
• to relieve intracranial pressure, as well as pressure in the pulmonary vessels;
• for edema caused by kidney pathologies;
• for neuralgia.

Contraindications

The drug, like any other drug of synthetic origin, has a number of contraindications. Eufillin is not used for:

• some heart diseases (myocardial infarction) and heart rhythm disturbances (arrhythmias, extrasystoles, tachycardia);
• coronary insufficiency;
• epileptic disease;
• gastric and duodenal ulcers in the acute phase;
• exacerbation of gastritis;
• severe pathologies of the liver and kidneys;
• the presence of hemorrhage in the retina of the eye;
• allergies to aminophylline.

For the treatment of neuralgia and osteochondrosis, a dropper of Eufillin with Dexamethasone is used.

Children under 14 years of age, pregnant and lactating women, elderly people, patients with vascular atherosclerosis and prostatic hyperplasia are treated with caution.

Eufillin, instructions for use in ampoules

The drug is prescribed by a doctor for each patient individually. This takes into account the diagnosis, the patient’s age and weight.

If it is necessary to relieve bronchospasm, intravenous administration of the drug in large quantities is indicated. The medicine is administered through a dropper, the solution for which contains:

• 10-20 ml Euphyllin;
• 10-20 ml of 9% sodium chloride solution;
• 0.5 l of saline solution.

The drug is administered over 30 minutes. For 1 kg of patient weight, 5-6 mg of medication is needed. When introducing a drip, it is necessary to monitor the patient's blood pressure and heart rate.

In order to relieve an attack of bronchial asthma, it is necessary to administer 750 ml of medication using a dropper.

For intravenous administration, Eufillin is mixed with a solution of sodium chloride. The intravenous injection is given slowly, over 6 minutes. With simultaneous treatment with Euphylline and Theophylline, the dosage of the former is reduced by half.

An injection of Eufillin intramuscularly is quite painful. For injections, exclusively thick needles are used. Dosage: single dose - 7 mg/kg, daily dose - 13 mg/kg. The drug is used more than three times a day. The duration of treatment is 14 days.

The medicine is also used for inhalation, which is carried out for bronchospasms and asthmatic attacks in children. To prepare the solution you need:

• Euphyllin ampoule 2.4%;
• three ampoules of Diphenhydramine;
• 150 ml saline solution.

The dosage of the solution is prescribed by the pediatrician, depending on the diagnosis and body weight of the child. A nebulizer is used as an inhaler.

Side effects

The drug can cause numerous side effects. They appear:

• headaches and dizziness;
• excited state, insomnia, anxiety, tremor, flushing, fever;
• a sharp decrease in blood pressure, heart rhythm disturbances (tachycardia, arrhythmia, palpitations), exacerbation of angina pectoris;
• nausea, vomiting, heartburn, exacerbations of gastritis and ulcers, diarrhea and loss of appetite;
• allergic manifestations (itching, rash and other skin rashes, swelling, etc.), increased sweating;
• increased shallow breathing and chest pain;
• a drop in blood sugar below normal;
• an increase in the daily volume of urine, the presence of blood in the urine, and the release of protein in the urine;
• convulsions;
• compaction and pain at the injection site.

If side effects occur, you should stop treatment and seek advice from your doctor.

Overdose

An overdose of Eufillin can manifest itself:

• intestinal or stomach bleeding;
• anxiety and sleep disorders;
• nausea and vomiting with blood discharge;
• tachycardia;
• decreased blood pressure;
• swelling of the face;
• ventricular arrhythmia;
• photophobia;
• cramps.

If poisoned by the drug, a person may fall into a coma.

In case of drug overdose, you must immediately call an ambulance.

Eufillin during pregnancy

Often, pregnant women experience edema, which sometimes cannot be eliminated using conventional methods, that is, the use of diuretics. In this case, Eufillin is prescribed, which, by dilating blood vessels, stimulates the kidneys, helping them remove excess fluid from the body.

The drug is taken during pregnancy with extreme caution and only under the supervision of the attending physician, since in the first two trimesters the internal organs of the unborn baby are formed, and the medicine has the ability to penetrate the placental barrier. The product is used only when absolutely necessary. Start using it with small doses, gradually increasing the amount. Therapy with the drug is prescribed in short courses, no more than a few days. In rare cases, the dose is increased to 1 month.

Alcohol compatibility

Most medications are incompatible with alcohol consumption. Eufillin is one of these medications. Aminophylline can enhance the effect of many chemicals, in particular alcohol. When used simultaneously with alcohol, the drug may cause:

• a sharp decrease in blood pressure, up to collapse;
• symptoms of suffocation;
• disturbance of heart rhythms (arrhythmia, tachycardia, palpitations);
• relaxation of the lung muscles, which may impair respiratory function;
• bleeding in the brain if the blood vessels are weakened.

Rarely, simultaneous use of alcohol and Eufillin can be fatal.

Interaction with other drugs

The drug is incompatible with medications containing any acids. Combined use with certain types of antibiotics may enhance the effect of Eufillin, therefore, the dosage of the latter will need to be reduced. If you take the drug with Dexamethasone or Prednisolone, side effects may increase.

Medicines such as Carbamazepine, Diphenin, Sulfinpyrazone, Phenytoin, Phenobarbital, etc., reduce the effect of aminophylline, therefore, its dosage is increased when taken simultaneously with these drugs.

The simultaneous use of Eufillin with diuretics and beta-agonists enhances the effect of the latter. The drug reduces the effectiveness of beta-blockers and lithium preparations.

Features of the use of Eufillin

Intravenous administration of the drug is carried out subject to certain conditions:

• before use, the medicine must be heated to human body temperature;
• begin administration with a minimum dosage, gradually increasing it;
• the drug is not diluted with glucose solution;
• During administration, strict monitoring of the patient's blood pressure and pulse is necessary. If they change, it is necessary to reduce the rate of administration;
• when administering large doses, monitor the content of Euphyllin in the blood. If necessary, the dosage of the medication is reduced.

During drug therapy, you should refrain from carrying out work that requires maximum concentration of attention, as well as from driving vehicles.

Price for the drug in the pharmacy chain

The price may vary depending on the pharmacy chain and its location.

Eufillin's analogs

Analogs of the drug that have an identical effect:

• Aminophylline;
• Prednisolone;
• Tizol;
• Berodual et al.