Eufillin solution instructions for use. Instructions for the use of aminophylline in ampoules for intravenous administration. It's time to sound the alarm! In your case, the likelihood of developing asthma is huge

One tablet contains 150 mg of active substance, as well as calcium stearate and potato starch.

Part injection solution aminophylline included in a concentration of 24 mg/ml. Water is used as an auxiliary component.

Release form

Tablets 150 mg (packaging No. 10 and No. 30).

Injection solution 2.40% in ampoules of 5 ml (packaging No. 10, No. 50 and No. 100) and 10 ml (packing No. 10).

pharmachologic effect

Bronchodilator , tocolytic , antispasmodic ,diuretic . Belongs to a group of drugs for systemic use in diseases that are accompanied by obstruction (obstruction syndrome) of the respiratory tract.

Clinical and pharmacological group (according to the Vidal reference book): bronchodilator - PDE inhibitor. Pharmaceutical subgroup - xanthines.

Pharmacodynamics and pharmacokinetics

Mechanism of action aminophylline (in Latin - aminophylline) is associated with its ability to block purine (adenosine) A2-type receptors of bronchial smooth muscle cells, increase the accumulation of cyclic AMP in tissues, suppress PDE, reduce the flow of Ca ions through plasma membrane channels (cell membranes), reduce the contractile activity of smooth muscles .

The effects of the drug manifest themselves as:

• relaxation of the bronchial muscles;
• stimulation of diaphragm contractions;
• increasing mucociliary clearance;
• improving the function of intercostal and respiratory muscles;
• stimulation of the respiratory center and increasing its sensitivity to CO2;
• improving alveolar ventilation.

All this helps to reduce the severity and frequency of episodes of respiratory arrest ( ).

By normalizing breathing, it ensures better oxygen saturation of the blood and helps reduce CO2 concentration. Stimulates the activity of the heart muscle, increases the number and strength of its contractions, improves blood circulation through the blood vessels of the heart and increases the myocardial need for oxygen.

Reduces tension in the vascular walls, promotes dilation of peripheral vessels, reduces vascular resistance in the lungs, and reduces pressure in the pulmonary circulation.

Is diuretic moderate strength of action, increases the volume of blood flow in the kidneys, promotes the expansion of the bile ducts, inhibits platelet aggregation, increases the resistance of red blood cells to deformation (improves blood rheology), normalizes microcirculation and reduces thrombus formation.

Reduces the excitability and contractility of the myometrium (tocolytic effect), in high doses it has epileptogenic effect .

Absorption from the gastrointestinal tract when taken orally is rapid. Food does not change its magnitude, but reduces its speed. The degree of absorption also depends on the dose: the higher it is, the slower it is absorbed aminophylline .

In a healthy adult, about 60% of the dose taken aminophylline binds to plasma proteins, in the patient - about 35%, in infants during the newborn period - 36%.

TSmax for regular tablets is 60-120 minutes.

In the liver, part of the dose taken aminophylline biotransforms into caffeine . T1/2 caffeine in children under 3 years of age it is longer than in adults. The concentration of the substance in a child can reach 30% of the concentration aminophylline .

In patients older than three years of age, the phenomenon of cumulation caffeine not visible.

The T1/2 indicator is influenced by concomitant diseases and the patient’s age. In children under six months of age, as well as in adult patients with heart failure , COPD and pulmonary heart disease it is more than 24 hours, in children over six months of age - 3.7, in non-asthmatic adults - 8.7, in people who smoke more than 20 cigarettes per day - 4-5 hours. After quitting smoking, it takes at least 3 months for the pharmacokinetics of the drug to normalize.

Eliminated by the kidneys, about 10% is excreted in pure form in adults, and about half of the taken dose of aminophylline is excreted in children.

Indications for use of Eufillin

Eufillin - what are these pills for?

Indications for use of Eufillin tablets:

• (BA);
• Pickwick's syndrome (night paroxysmal apnea);
• chronic obstructive (COB);
• chronic “pulmonary heart” ;
• lungs .

Eufillin is the drug of choice for exercise-induced asthma; for other forms of the disease it is used in combination with other drugs.

When is Euphyllin in ampoules prescribed?

Indications for Eufillin in ampoules are:

• broncho-obstructive syndrome at bronchitis , BA, cardiac asthma (mainly to relieve attacks) or emphysema ;
• cerebrovascular insufficiency of the brain (the solution is used in combination with other drugs to reduce intracranial pressure);
• hypertension in the pulmonary circulation;
• left ventricular failure , accompanied by periodic breathing of the Cheyne-Stokes type and bronchospasm (in combination with other drugs).

Contraindications for Eufillin solution and tablets

Contraindications to the use of tablets:

• intolerance aminophylline or any other derivatives xanthine ;
• (MI) in the acute stage;
• hypertrophic cardiomyopathy with obstruction;
• tachyarrhythmia ;
• exacerbation of symptoms ulcers of the stomach/duodenum ;
• severe functional impairment of the kidneys/liver;

In pediatrics, it is not prescribed to children under six years of age, or in combination with .

Injection of the drug is contraindicated in:

• hypersensitivity in aminophylline and other derivatives xanthine ;
• MI in the acute stage;
• extrasystoles ;
• paroxysmal ;
• severe arterial hypotension/hypertension ;
• pulmonary edema ;
• hemorrhagic stroke ;
• there is an indication of any spontaneous bleeding in the anamnesis;
• hemorrhage into the retinal tissue;
• in the acute stage;
• increased threshold of convulsive readiness;
• gastroesophageal reflux (GER);
• uncontrolled hypothyroidism ;
• thyrotoxicosis ;
• hyperthyroidism ;
• porphyria ;
• sepsis ;
• kidney and/or liver dysfunction .

Due to the likelihood of side effects, it is not recommended to use the solution in children under 14 years of age. Children under three years of age are contraindicated to administer Eufillin intravenously; in children over three years of age, the medicine can be used for health reasons and for no more than 14 days.

Side effects

Side effects of using Eufillin tablets:

• sleep disturbances, anxiety, dizziness, convulsions, tremor;
• irregular heart rhythm, palpitations;
• hematuria , albuminuria ;
• hypoglycemia (rarely).

Against the background of injection therapy, the following are possible:

• headache, anxiety, dizziness, agitation, irritability, tremor, ;
• , (including in the fetus, if the woman took the drug in the 3rd trimester of pregnancy), palpitations, decreased blood pressure, unstable ;
• nausea, , heartburn, gastralgia , vomiting, worsening symptoms peptic ulcer , GER, with long-term use - loss of appetite;
• itching of the skin, skin rashes, fever;
• tachypnea , chest pain, hypoglycemia ,albuminuria , increased diuresis, hematuria , increased sweating, feeling of heat in the face.

Side effects are dose-dependent, that is, to relieve them, it is often enough to reduce the dose of the drug.

Local reactions to the injection of the solution manifest themselves in the form of skin hyperemia, pain and the formation of a seal at the injection site.

Instructions for use of Eufillin

Eufillin tablets: instructions for use

The Vidal reference book states that the tablets should be taken orally after meals with plenty of liquid. The dosage of the drug is selected individually, taking into account different rates of elimination aminophylline in different patients.

If necessary, the dose is increased every three days until the desired effect is achieved.

For patients weighing more than 50 kg (including adolescents) Eufillin with bronchitis and others accompanied bronchial obstruction , conditions are prescribed to take 450-900 mg/day; if necessary, the dose can be increased to 1.2 g with a frequency of use of 4 times/day. with an interval of 6 hours.

For patients weighing less than 50 kg and adolescents whose weight is in the range of 45-55 kg, Eufillin tablets are prescribed to take 450-600 mg/day.

Children 6-17 years old bronchitis and others broncho-obstructive conditions tablets are given at the rate of 13 mg/kg, usually 1 tablet 3 times a day.

For COPD in the acute phase, treatment begins with a dose of 5-6 mg/kg (for adults) with further increases. Serum concentration should not exceed 0.02 mg/ml. An increase in the dose for every 0.5 mg/kg leads to an increase in the concentration of the drug in the blood by 0.001 mg/ml.

Outside of an exacerbation, the initial dose of Eufillin for an adult with COPD is 6-8 mg/kg/day, the highest (in the initial stages of treatment) is 400 mg/day. It is recommended to divide it into 3-4 doses.

If used during pregnancy, the dosage (as well as the method of administration) is determined by the doctor. It should be borne in mind that for the mother, an overdose is associated with the risk of cardiac dysfunction (and sometimes cardiac arrest), and for the fetus, high doses of Eufillin are dangerous due to the likelihood of hypoxia and antenatal death.

Eufillin ampoules: instructions for use

For conditions that require emergency care, adult patients are advised to use an infusion with a loading dose of the drug: Eufillin is administered intravenously over half an hour at a dose of 5.6 mg/kg. To prepare a dropper, 10-20 ml of solution is combined with a similar volume of 0.9% aqueous NaCl solution and then the medicine is diluted in 0.25-0.5 liters of physiological solution.

During maintenance therapy, Eufillin is infused into the patient intravenously for 1-3.5 times at a dose of 0.9 mg/kg.

If the patient has previously taken , dose should be reduced by at least half.

At status asthmaticus 720 to 750 mg is injected into the bloodstream by drip aminophylline .

The permissible upper limit of the daily dose for an adult is 0.4-0.5 ml/kg.

Children up to 3 months are administered intravenously from 30 to 60 mg aminophylline per day, for older children and adolescents the dose varies from 60 to 500 mg/day.

Intravenous injections of Eufillin in emergency conditions are performed for at least five minutes. A single dose for an adult is 6 mg/kg. Before giving the injection, the drug is diluted in 10-20 ml of a 0.9% aqueous solution of NaCl.

The daily dose for intramuscular administration is from 0.1 to 0.5 mg.

For children with COPD, Eufillin is administered at a dose of 5-6 mg/kg (initial dose); during maintenance therapy for children under six months of age, the drug is administered every 8 hours at a dose calculated by the formula: child’s age in weeks * 0.07 + 1, 7.

For children aged six months to one year, the maintenance dose is calculated using the formula: child’s age in weeks * 0.05 + 1.25. The interval between injections is 6 hours.

Children from one to 9 years old are administered 5 mg/kg, children 9-12 years old - 4 mg/kg, children 12-16 years old - 3 mg/kg every 6 hours.

Outside of exacerbation, the initial dose for a child is 16 mg/kg/day, the highest dose is 400 mg/day. It should be divided into 3-4 injections.

If necessary and if Eufillin is well tolerated, the dose is increased every couple of days by 25% to the highest daily dose, which for children under one year old is calculated using the formula “age in weeks * 0.3 +8”, for children under 9 years old it is 22, for children up to 12 years old - 20, for adolescents under 16 years old - 18, for patients over 16 years old - 13 mg/kg.

Eufillin is administered intramuscularly to children at a dose of 15 mg/kg/day. The maximum duration of parenteral use in children is 14 days.

At apnea in children of the first year of life (accompanied bradycardia And cyanotic condition , in which the child has periods of no breathing for 15 seconds), the starting dose is 5 mg/kg (the medicine is administered through a nasogastric tube). When carrying out maintenance therapy, the child is recommended to use 2 mg/kg in two doses.

Treatment can last up to several months (usually several weeks).

Electrophoresis with Eufillin

Euphylline for electrophoresis in adults is used to treat arthrosis And . For electrophoresis, it is prescribed to children when , and also when it is necessary to remove muscle hypertonicity or reduce intracranial pressure .

In case of cerebrovascular insufficiency or intracranial hypertension it is carried out on the cervical vertebrae, with hypertonicity the child's legs - in the lumbar region.

Electrophoresis with Eufillin is a procedure that allows you to create the desired concentration of the active substance directly in the affected tissues. Acting locally, the medicine does not cause systemic side effects, so it can be used in infants older than one month.

The doctor places a gauze cloth soaked in Eufillin solution on the sore spot and secures the electrodes. Exposure time is 15 minutes. This is enough for the drug to penetrate deep into the tissue. The course of treatment is designed for ten sessions.

To restore organ function after birth injuries in newborns, cerebral circulation during pathologies of the cervical spine , and also when cerebral palsy Electrophoresis according to Ratner is recommended.

The essence of this method is that the patient is placed on two pads impregnated with different drugs: the first (with a solution of Eufillin 0.5%) - on the cervical vertebrae, the second (with a solution 1%) - on the ribs, to the right of the sternum. Exposure time is 15 minutes. Current strength is 1-2 mA.

It should be noted that both children and adults tolerate the procedure equally well, so in the absence of contraindications, it can be performed without any fear.

Electrophoresis is contraindicated for any skin diseases, arterial hypertension ,arrhythmias , heart failure , the presence of neoplasms in the patient (any location).

Inhalations with Eufillin for children - effective or inappropriate?

Prescription for children with cough and bronchial obstruction Eufillina allows you to expand the bronchi, relieve spasm and facilitate the discharge of sputum. However, the drug has these effects only when it enters the systemic circulation.

The use of Eufillin for inhalation belongs to the “off-label” prescribing category. Despite the lack of instructions in the manufacturer's instructions regarding the possibility of using the drug in this way, many people often prescribe this treatment for themselves and, moreover, treat their children in this way.

Most doctors unanimously believe that the effectiveness of inhalations with Eufillin is extremely low, since when inhaling vapors, the drug settles on the mucous membrane and, therefore, does not enter the systemic bloodstream in a therapeutically effective concentration.

The positive effect on the bronchi (their relaxation and improvement of sputum discharge) is due to the fact that during inhalation water vapor enters them. This means that the effectiveness of the drug when used in inhalation is comparable to the effectiveness of ordinary water.

Eufillin for cellulite

One of the properties aminophylline is the ability to expand peripheral vessels and restore the functioning of the circulatory system, which in turn cannot. But cellulite, as is known, occurs when blood circulation is impaired, and cells begin to suffer from a lack of oxygen. The use of Eufillin allows you to tighten the upper layers of the skin, remove excess fluid and reduce swelling.

For weight loss and getting rid of orange peel, the product is used in the form of creams, masks and wraps. Massage with Eufillin also gives a good effect.

To prepare the composition, the medicine should be mixed with any massage cream, and then add a small amount to it Dimexide , which in this case will act as a transporter (thanks to him aminophylline can penetrate very deeply into tissue).

For wraps, you can use a mixture of regular baby cream, Dimexide , Euphyllin and essential oil of tangerine or lemon (6-8 drops). The composition is applied to the skin cleansed with a scrub and covered with cling film. While it “works” (impact time is usually about 30 minutes), it is recommended to move intensively to enhance the effect.

To prepare anti-cellulite cream based on Eufillin, use the following recipe:

• petrolatum;
• moisturizing cream;
• 1 powdered tablet or the contents of 1 ampoule (5 ml) of Eufillin (this dose of the drug is suitable for women weighing less than 75 kg);
• Dimexide (for one five-milliliter ampoule of solution, take 2 ml of Dimexide concentrate).

You can also add the drug to a ready-made pharmaceutical anti-cellulite product. The optimal proportion of ingredients is 1:5.

Reviews about Eufillin for cellulite can be found very different - some are completely dissatisfied with the result, others claim that the result exceeded all expectations. Based on this, we can draw the following conclusion - if the remedy works, then definitely not from the first procedure.

Overdose

The annotation states that overdose symptoms develop when the plasma concentration aminophylline exceeds 0.02 mg/ml. Characteristic are:

• diarrhea ;
• prolonged vomiting;
• facial hyperemia;
• excitation;
• arrhythmia ;
• photophobia;
• convulsions.

When the blood concentration exceeds 0.04 mg/ml, the patient falls into a coma.

Helpful measures include stopping the administration of Eufillin to the patient and enhancing natural detoxification by stimulating kidney function (forced diuresis).

If the level aminophylline exceeds 0.05 mg/ml, indicated plasmapheresis , hemosorption , peritoneal dialysis or , respiratory support (ventilation and oxygen supply), monitoring of hemodynamic parameters.

For cupping convulsive syndrome the patient is injected (intramuscular). Application barbiturates contraindicated!

Interaction

Strengthening the action aminophylline promotes use in combination with , viloxazine , , , β-blockers , influenza vaccines leads to slower elimination aminophylline , an increase in its plasma concentration and, consequently, a decrease in the applied dose of Eufillin.

If the drug is prescribed in combination with drugs fluoroquinolone group the dose of Eufillin is reduced to 25% of the usually recommended one.

Aminophylline weakens the therapeutic effect of Li drugs and β-blockers. β-blockers, in turn, weaken bronchodilator effect of aminophylline .

When taking Eufillin together with GCS (for example, with dexamethasone ), diuretics And β-adrenergic agonists the risk of developing hypoglycemia .

Aminophylline may cause side effects from fluorinated derivatives of general anesthesia ( ventricular arrhythmias ), mineracorticosteroids (hypernatremia), CNS stimulating drugs ( neurotoxicity ).

May enhance the effect anticoagulants .

The solution is incompatible with solutions of acids, fructose, glucose and levulose. When preparing for intravenous infusion of an infusion solution, it is necessary to take into account the pH of the solutions used.

Should be used with caution in combination with purine derivatives , theophylline derivatives , anticoagulants . During the treatment period, it is prohibited to take substances that contain xanthines (including tea and coffee).

In one syringe, Eufillin solution can only be mixed with isotonic NaCl solution.

Terms of sale

On prescription.

Recipe in Latin (parenteral administration to a ten-year-old child):

Rp: Sol. Euphyllini 2.4% - 10.0

D.t.d. N 3 in amp.

S. 5-10 ml IV drip or slow stream, on physical. solution (0.15 mg/kg or 1.0 ml/year of life).

Storage conditions

List B. Store in a light and moisture protected place at room temperature.

Best before date

Two years.

special instructions

Bronchodilator effect The drug appears when the concentration of the active substance reaches 0.01-0.02 mg/ml. A concentration exceeding 0.02 mg/ml is toxic.

The stimulating effect on the respiratory center is realized when the content aminophylline in the blood is in the range from 0.005 to 0.01 mg/ml.

In newborn infants and people over 55 years of age, the medicine is used with caution due to the insufficient activity of those involved in biotransformation aminophylline liver enzymatic systems.

Eufillin during pregnancy

The manufacturer, in the instructions for Eufillin, warns that the use of solution/tablets during pregnancy may create concentrations that are potentially hazardous to the health of the fetus/newborn. aminophylline and caffeine.

Children whose mothers received the drug during pregnancy (especially in the third trimester) should be under medical supervision during the neonatal period to monitor possible symptoms of intoxication with methyl xanthine derivatives.

Prescription of Eufillin during pregnancy and lactation is possible only for extreme health reasons and requires an assessment of possible risks to the fetus/child.

Why can Eufillin be prescribed during pregnancy?

Gynecologists recommend the use of Eufillin for edema during pregnancy, for placental insufficiency, and in complex therapy gestosis , as well as for other conditions requiring urgent use of this medicine due to a threat to the life of the mother.

There is no clear treatment regimen for Eufillin during pregnancy, since the manufacturer’s instructions list pregnancy as one of the contraindications for use. The doctor makes all appointments depending on the condition of a particular patient.

For effective treatment of acute stage osteochondrosis, a whole range of medications and procedures is used. Vasodilator drugs are an essential component of treatment. Most often, doctors prescribe the old, time-tested Eufillin.

Description and pharmacological action of the drug

The course of spinal osteochondrosis is always accompanied by severe vascular spasm and myalgia.

In the acute stage, when sympathetic innervation is involved in inflammation, impulse flows weaken, provoking spasms in blood vessels.

Advanced stage, inadequate drug therapy leads to further damage to nearby tissues. To completely eliminate such severe consequences, complex drug treatment is prescribed.

How do drugs with vasodilating effects work?:

1. relieving spasms, eliminating stagnant processes;
2. stabilize the transmission of impulses through the central and peripheral nervous system;
3. promote better blood supply with microcirculation in the area of ​​the pathological focus.

For vasodilator therapy, the drug Eufillin is most often used. According to clinical and pharmacological affiliation, the drug Eufillin is included in the bronchodilator group.

The drug has a wide range of effects on the body:

• stimulates the contractility of the diaphragm;
• stimulates respiratory, intercostal muscle contraction;
• has a relaxing effect on the spasmodic muscles of the bronchi;
• influencing the respiratory center, stimulates respiratory function;
• increases the strength and frequency of contractions in the myocardium;
• dilates blood vessels of brain tissue, skin, kidneys.

The main active component of the drug Eufillin is aminophylline. It is a synthetic derivative of theophylline and ethylenediamine.

Theophylline is a plant alkaloid. Theophylline is present in tea leaves, mate, cocoa beans. It is a natural antispasmodic and bronchodilator. In Euphylline, ethylenediamine acts as an auxiliary component, which allows theophylline to dissolve and be absorbed faster.

The drug Euphyllin has a high absorption rate and bioavailability of 95-100%. Excreted from the body by the liver. Time of elimination of the drug: 22-24 hours.

Composition and release form

The drug Eufillin is available in solid and liquid dosage forms.

The solid form of Euphyllin is tablets with the main active ingredient aminophylline 150 mg.

The liquid dosage form of Eufillin is represented by injection solutions of two types:

• 24% solutions of Euphyllin for intramuscular administration (1 ml), with the amount of the main active ingredient aminophylline 240 mg;
• 2.4% solutions of Eufillin for intravenous infusion (5 ml, 10 ml), with the amount of the main active ingredient per 1 ml of 24 mg.

Important: injection solutions of the drug are not interchangeable!

Indications for use

Eufillin is a drug with a wide spectrum of therapeutic action.

The drug is prescribed to relieve bronchospasm, pain syndrome of a spastic nature, in the acute period of cholecystitis, and other diseases of the biliary system.

The drug Eufillin is prescribed to normalize blood microcirculation.

The drug Eufillin is used in physiotherapy for osteochondrosis. Electrophoresis procedures with Eufillin normalize trophic processes at the level of intervertebral cartilage.

Contraindications and side effects

The drug Eufillin is not used in treatment if the patient suffers from hypersensitivity to the active ingredients.

Eufillin is not prescribed to patients with ulcerative pathology of the gastrointestinal tract in an aggravated period, with severe hypertension and hypotension.

In pediatric practice, the drug Eufillin is used only for children over 3 years of age.

Treatment with Euphyllin with caution, prescribed for special indications:

1. at the acute stage of myocardial infarction;
2. with extensive atherosclerosis;
3. patients with increased convulsive readiness;
4. patients with ventricular extrasystole;
5. at elevated temperatures;
6. patients with prostate hyperplasia;
7. for hypothyroidism and thyrotoxicosis.

With extreme caution, with individual selection of dosages, the drug Eufillin is prescribed to pregnant and lactating women, as well as children and the elderly.

Application of Eufillin for electrophoresis

In complex treatment, a course of electrophoresis procedures with Eufillin - from 10 to 20 sessions

The ability of the drug Eufillin to reduce is used in physiotherapy.

The electrophoresis procedure uses a 2% Eufillin solution.

Electrophoresis with Eufillin ensures deep penetration of the drug through the skin with an additional warming effect.

Electrophoresis with Eufillin is prescribed for pulmonary, vascular and neurological pathologies.

The effect of weakening muscle spasms and pain relief is used to treat osteochondrosis, intervertebral hernias, arthrosis, and arthritis.

Advantages of the electrophoresis procedure with Eufillin for pathologies of the spine and joints:

1. A low therapeutic dose with maximum therapeutic effect, directed directly to the area of ​​the pathological focus.
2. During the procedure, the main part of the drug is retained by the skin and subcutaneous fat. This allows Eufillin to gradually enter the bloodstream (prolonged action).
3. “Targeted action” on the pathological focus gives a concentration greater than when administering Eufillin by injection or orally.
4. Eufillin does not pass through the gastrointestinal tract, and therefore does not have side effects on the body.

Instructions for use

Eufillin belongs to group B (potent) drugs, therefore the dosage, course of treatment, and dosage form of the drug are prescribed exclusively by the attending physician.

Typically, the dosage of Eufillin tablets for adults: 1 or 2 pcs. two or three times a day.

The medicine is taken after meals with a small amount of water. The course of treatment with Eufillin tablets is from 2 to 3 weeks.

In pediatrics, the dosage of the drug is calculated according to the following scheme: from 7 to 10 mg per 1 kg of child’s body weight.

Intravenous procedures with the drug are prescribed only in case of emergency conditions. An intravenous procedure with Eufillin should be carried out on a patient who is only in a horizontal position, under medical supervision of breathing and blood pressure indicators.

Patients taking Eufillin should not consume foods and drinks with caffeine and refrain from driving vehicles and machinery.

Price

Analogues substitutes

The drug is produced at almost every pharmaceutical enterprise, with the main active ingredient and under one name - Eufillin.

But some enterprises register their own, original names:

• Eufillin Darnitsa (produced by the Ukrainian pharmaceutical company “Darnitsa Drug Company”);
• Eufillin-UBF (produced in Russia by OJSC Uralbiopharm);
• Euphylong in capsules, rectal capsules, retard capsules (Manufacturer: Bick Gulden GmbH, Germany);
• Etiphylline (tablets only). Manufacturers: Russian companies ICN Oktyabr, Dalkhimfarm, Irbitsky HFZ, Lekform, Purin, Tatkhimfarmpreparat, Tyumen HFZ, Urabbiofarm.

All drugs with the main active ingredient theophylline, with indications and contraindications identical to Euphyllin.

Bronchodilator, phosphodiesterase inhibitor (PDE). It is the ethylenediamine salt of theophylline (which facilitates solubility and increases absorption). It has a bronchodilator effect, apparently due to a direct relaxing effect on the smooth muscles of the respiratory tract and blood vessels of the lungs. It is believed that this effect is caused by selective inhibition of the activity of specific PDEs, which leads to an increase in the intracellular concentration of cAMP. The results of in vitro experimental studies show that the main role appears to be played by type III and IV isoenzymes. Suppression of the activity of these isoenzymes may also cause some side effects of aminophylline (theophylline), including. vomiting, arterial hypotension and tachycardia. Blocks adenosine (purine) receptors, which may be one of the factors affecting the bronchi.

Reduces airway hyperresponsiveness associated with the late phase response caused by inhaled allergens through an unknown mechanism that is not due to PDE inhibition or blockade of adenosine. There are reports that aminophylline increases the number and activity of T-suppressor cells in peripheral blood.

Increases mucociliary clearance, stimulates contraction of the diaphragm, 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. By normalizing respiratory function, it helps saturate the blood with oxygen and reduce 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 strength and heart rate, increases coronary blood flow and increases the 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 PgE 2α), 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. In high doses it has an epileptogenic effect.

Pharmacokinetics

In the body, aminophylline is metabolized at physiological pH values ​​to release free theophylline. Bronchodilating properties appear at plasma theophylline 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 concentration - 5-10 mcg/ml.

Theophylline binding to plasma proteins is approximately 40%; in newborns, as well as in adults with diseases, binding decreases. Plasma protein binding in adults is about 60%, in newborns - 36%, in patients with liver cirrhosis - 36%. Penetrates the placental barrier (the concentration in the fetal blood serum is slightly higher than in the maternal serum). Excreted in breast milk.

Theophylline is metabolized in the liver with the participation of several cytochrome P450 isoenzymes, the most important of which is CYP1A2. During metabolism, 1,3-dimethyluric acid, 1-methyluric acid and 3-methylxanthine are formed. These metabolites are excreted in the urine. 10% is excreted unchanged in adults. In newborns, a significant portion is excreted in the form of caffeine (due to the immaturity of the pathways for its further metabolism), unchanged - 50%.

Significant individual differences in the rate of hepatic metabolism of theophylline are the cause of pronounced variability in clearance values, plasma concentrations, and half-life. Hepatic metabolism is influenced by factors such as age, addiction to tobacco smoking, diet, diseases, and concurrent drug therapy.

T1/2 of theophylline in non-smoking patients with bronchial asthma with virtually no pathological changes in other organs and systems is 6-12 hours, in smokers - 4-5 hours, in children - 1-5 hours, in newborns and premature babies - 10 -45 hours

T1/2 of theophylline increases in the elderly and in patients with heart failure or liver disease.

Clearance decreases with heart failure, liver dysfunction, chronic alcoholism, pulmonary edema, chronic obstructive pulmonary disease.

Ethylenediamine does not affect the pharmacokinetics of theophylline.

Indications

For parenteral use: status asthmaticus (additional therapy), neonatal apnea, ischemic cerebrovascular accident (as part of combination therapy), left ventricular failure with bronchospasm and Cheyne-Stokes type breathing disorder, edematous syndrome of renal origin (as part of complex therapy) ; acute and chronic heart failure (as part of combination therapy).

For oral administration: broncho-obstructive syndrome of various origins (including bronchial asthma, COPD, including emphysema, chronic obstructive bronchitis), hypertension in the pulmonary circulation, cor pulmonale, sleep apnea; acute and chronic heart failure (as part of combination therapy).

Instructions for use / dosage

Individual, depending on the indications, age, clinical situation, route and schedule of administration, nicotine addiction.

Side effect

From the side of the central nervous system: dizziness, sleep disturbances, anxiety, tremors, convulsions.

From the cardiovascular system: palpitations, heart rhythm disturbances; with rapid intravenous administration - the appearance of pain in the heart, decreased blood pressure, tachycardia (including in the fetus when taken in the third trimester of pregnancy), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks.

From the digestive system: nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea; with prolonged ingestion - anorexia.

From the urinary system: albuminuria, hematuria.

Allergic reactions: skin rash, itching, fever.

From the side of metabolism: rarely - hypoglycemia.

Local reactions: compaction, hyperemia, pain at the injection site; when used rectally, irritation of the rectal mucosa, proctitis.

Others: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Contraindications

Severe arterial hyper- or hypotension, tachyarrhythmias, peptic ulcer of the stomach and duodenum in the acute phase, hyperacid gastritis, severe dysfunction of the liver and/or kidneys, epilepsy, hemorrhagic stroke, hemorrhage in the retina, simultaneous use with ephedrine in children, childhood (up to 3 years, for prolonged oral forms - up to 12 years), hypersensitivity to aminophylline and theophylline.

Use during pregnancy and breastfeeding

Theophylline penetrates the placental barrier. The use of aminophylline during pregnancy may result in potentially dangerous concentrations of theophylline and caffeine in the blood plasma of the newborn. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) require medical supervision to monitor possible symptoms of theophylline intoxication.

Theophylline is excreted in breast milk. When using aminophylline in a nursing mother during lactation, irritability may occur in the child.

Thus, the use of aminophylline during pregnancy and lactation (breastfeeding) is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk for the fetus or child.

special instructions

Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystoles, increased convulsive readiness, liver and/or renal failure, gastric and duodenal ulcers (history), with recent bleeding from the gastrointestinal tract, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, with prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, in elderly patients, in children (especially orally).

Correction of the aminophylline dosage regimen may be required for heart failure, liver dysfunction, chronic alcoholism, fever, and acute respiratory infections.

In elderly patients, a dose reduction may be required.

When replacing the used dosage form of aminophylline with another, clinical observation and monitoring of the concentration of theophylline in the blood plasma is necessary.

Aminophylline is not used simultaneously with other xanthine derivatives. During the treatment period, you should avoid eating foods containing xanthine derivatives (strong coffee, tea).

Use with caution simultaneously with anticoagulants, with other theophylline or purine derivatives.

Concomitant use with beta-blockers should be avoided.

Aminophylline should not be used simultaneously with glucose solution.

Do not use rectally in children.

Drug interactions

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

Xanthine derivatives can potentiate hypokalemia caused by the action of β 2 -adrenergic receptor stimulants, corticosteroids and diuretics.

Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.

Pharmaceutically incompatible with acid solutions.

Aminophylline (aminophylline)

Composition and release form of the drug

Solution for intravenous administration in the form of a colorless or slightly colored transparent liquid.

Excipients: water for injection - up to 1 ml.

5 ml - ampoules (5) - cardboard packs.
5 ml - ampoules (10) - cardboard packs.
10 ml - ampoules (5) - cardboard packs.
10 ml - ampoules (10) - cardboard packs.

pharmachologic effect

Bronchodilator, PDE inhibitor. It is an ethylenediamine salt (which facilitates solubility and increases absorption). It has a bronchodilator effect, apparently due to a direct relaxing effect on the smooth muscles of the respiratory tract and blood vessels of the lungs. It is believed that this effect is caused by selective inhibition of the activity of specific PDEs, which leads to an increase in the intracellular concentration of cAMP. The results of in vitro experimental studies show that the main role appears to be played by type III and IV isoenzymes. Suppression of the activity of these isoenzymes may also cause some side effects of aminophylline (theophylline), including. vomiting, arterial hypotension and tachycardia. Blocks adenosine (purine) receptors, which may be one of the factors affecting the bronchi.

Reduces airway hyperresponsiveness associated with the late phase inhalation response through an unknown mechanism that is not due to PDE inhibition or blockade of adenosine action. There are reports that aminophylline increases the number and activity of T-suppressor cells in peripheral blood.

Increases mucociliary clearance, stimulates contraction of the diaphragm, 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. By normalizing respiratory function, it helps saturate the blood with oxygen and reduce 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 strength and heart rate, increases coronary blood flow and increases the 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 PgE 2α), 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. In high doses it has an epileptogenic effect.

Pharmacokinetics

In the body, aminophylline is metabolized at physiological pH values ​​to release free theophylline. Bronchodilating properties appear at concentrations of theophylline in the blood of 10-20 mcg/ml. Concentrations above 20 mg/ml are toxic. The stimulating effect on the respiratory center is realized at a lower concentration - 5-10 mcg/ml.

Theophylline binding to plasma proteins is approximately 40%; in newborns, as well as in adults with diseases, binding decreases. Plasma protein binding in adults is about 60%, in newborns - 36%, in patients with liver cirrhosis - 36%. Penetrates the placental barrier (the concentration in the fetal blood serum is slightly higher than in the maternal serum). Excreted in breast milk.

Theophylline is metabolized in the liver with the participation of several cytochrome P450 isoenzymes, the most important of which is CYP1A2. During metabolism, 1,3-dimethyluric acid, 1-methyluric acid and 3-methylxanthine are formed. These metabolites are excreted in the urine. 10% is excreted unchanged in adults. In newborns, a significant portion is excreted in the form of caffeine (due to the immaturity of the pathways for its further metabolism), unchanged - 50%.

Significant individual differences in the rate of hepatic metabolism of theophylline are the cause of pronounced variability in clearance values, plasma concentrations, and half-life. Hepatic metabolism is influenced by factors such as age, addiction to tobacco smoking, diet, diseases, and concurrent drug therapy.

T1/2 of theophylline in non-smoking patients with bronchial asthma with virtually no pathological changes in other organs and systems is 6-12 hours, in smokers - 4-5 hours, in children - 1-5 hours, in newborns and premature babies - 10 -45 hours

T1/2 of theophylline increases in the elderly and in patients with heart failure or liver disease.

Clearance decreases with heart failure, liver dysfunction, chronic alcoholism, pulmonary edema, COPD.

Ethylenediamine does not affect the pharmacokinetics of theophylline.

Indications

For parenteral use: status asthmaticus (additional therapy), neonatal apnea, ischemic cerebrovascular accident (as part of combination therapy), left ventricular failure with bronchospasm and Cheyne-Stokes type breathing disorder, edematous syndrome of renal origin (as part of complex therapy) ; acute and chronic failure (as part of combination therapy).

For oral administration: broncho-obstructive syndrome of various origins (including bronchial asthma, COPD, including emphysema, chronic obstructive bronchitis), hypertension in the pulmonary circulation, cor pulmonale, sleep apnea; acute and chronic heart failure (as part of combination therapy).

Contraindications

Severe arterial hyper- or hypotension, tachyarrhythmias, peptic ulcer of the stomach and duodenum in the acute phase, hyperacid gastritis, severe dysfunction of the liver and/or kidneys, epilepsy, hemorrhagic stroke, hemorrhage in the retina, simultaneous use with children, childhood ( up to 3 years, for prolonged oral forms - up to 12 years), increased sensitivity to aminophylline and theophylline.

Dosage

Individual, depending on the indications, age, clinical situation, route and schedule of administration, nicotine addiction.

Side effects

From the nervous system: dizziness, sleep disturbances, anxiety, tremors, convulsions.

From the cardiovascular system: feeling of palpitations, heart rhythm disturbances; with rapid intravenous administration - the appearance of pain in the heart, decreased blood pressure, tachycardia (including in the fetus when taken in the third trimester of pregnancy), arrhythmias, decreased blood pressure, cardialgia, increased frequency of angina attacks.

From the digestive system: nausea, vomiting, gastroesophageal reflux, heartburn, exacerbation of peptic ulcer, diarrhea; with prolonged ingestion - anorexia.

From the urinary system: albuminuria, hematuria.

Allergic reactions: skin rash, itching, fever.

From the side of metabolism: rarely - hypoglycemia.

Local reactions: compaction, hyperemia, pain at the injection site; when used rectally, irritation of the rectal mucosa, proctitis.

Others: chest pain, tachypnea, flushing, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Drug interactions

When used simultaneously with sympathomimetics, a mutual enhancement of action occurs; with 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, 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

Xanthine derivatives can potentiate hypokalemia caused by the action of β 2 -adrenergic receptor stimulants, corticosteroids and diuretics.

Antidiarrheal drugs and enterosorbents reduce the absorption of aminophylline.

Pharmaceutically incompatible with acid solutions.

special instructions

Use with caution in severe coronary insufficiency (acute phase of myocardial infarction, angina pectoris), widespread atherosclerosis, hypertrophic obstructive cardiomyopathy, frequent ventricular extrasystoles, increased convulsive readiness, liver and/or renal failure, gastric and duodenal ulcers (history), with recent bleeding from the gastrointestinal tract, uncontrolled hypothyroidism (possibility of cumulation) or thyrotoxicosis, with prolonged hyperthermia, gastroesophageal reflux, prostatic hypertrophy, in elderly patients, in children (especially orally).

Correction of the aminophylline dosage regimen may be required for heart failure, liver dysfunction, chronic alcoholism, fever, and acute respiratory infections.

In elderly patients, a dose reduction may be required.

When replacing the used dosage form of aminophylline with another, clinical observation and monitoring of the concentration of theophylline in the blood plasma is necessary.

Aminophylline is not used simultaneously with other xanthine derivatives. During the treatment period, you should avoid eating foods containing xanthine derivatives (strong coffee, tea).

Use with caution simultaneously with anticoagulants, with other theophylline or purine derivatives.

Concomitant use with beta-blockers should be avoided.

Aminophylline should not be used simultaneously with glucose solution.

Do not use rectally in children.

Pregnancy and lactation

Theophylline penetrates the placental barrier. The use of aminophylline during pregnancy may result in potentially dangerous concentrations of theophylline and caffeine in the blood plasma of the newborn. Newborns whose mothers received aminophylline during pregnancy (especially in the third trimester) require medical supervision to monitor possible symptoms of theophylline intoxication.

Theophylline is excreted in breast milk. When using aminophylline in a nursing mother during lactation, irritability may occur in the child.

Thus, the use of aminophylline during pregnancy and lactation (breastfeeding) is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk for the fetus or child.

Use in old age

With caution: elderly patients (dose reduction may be required).

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 case 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.