Eufillin - instructions for use, dose, side effects, contraindications

The drug inhibits phosphodiesterase, increases accumulation in the tissues of cAMP, blocks adenosine (purine) receptors; has the ability to inhibit the transport of calcium ions through the channels of cell membranes, reduces the contractile activity of smooth muscles. Relaxes the musculature of the bronchi, it relieves bronchospasm. Has a moderate inotropic and diuretic effect.Euphyllin lowers vascular resistance, reduces the tone of the blood vessels (mainly the vessels of the brain, skin and kidneys), dilates the coronary vessels, lowers the pressure in the pulmonary artery system, improves the contraction of the diaphragm, increases mucociliary clearance, inhibits the release of mediators (histamine and leukotrienes) from the mast cells, stimulates the respiratory center, increases the adrenaline release of the adrenal glands, inhibits the aggregation of platelets, improves microcirculation.

Pharmacokinetics:

Bioavailability for liquid dosage forms is 90 - 100%. Time to reach the maximum concentration in blood plasma with intravenous administration of 0.3 g - 15 minutes, the maximum concentration in blood plasma - 7 μg / ml. 60% of euphillin (in healthy adults) and 36% (in newborns) binds to plasma proteins and is distributed in the blood, extracellular fluid and muscle tissue. Euphyllin penetrates into breast milk (10% of the dose), through the placental barrier (the concentration in the fetal serum is slightly higher than in the mother's serum), does not accumulate in adipose tissue. 90% of the drug is metabolized in the liver. Metabolites are excreted by the kidneys, 7-13% of the drug is excreted unchanged.The half-life is for non-smokers from 5 to 10 hours, for children over 10 months from 2.5 to 5 hours. Smoking and alcohol significantly affect the metabolism and release of the drug, particularly among smokers, this period is significantly reduced and ranges from 4 to 5 hours. Removal of the drug is prolonged in patients with respiratory failure, with hepatic and cardiac failure, with viral infections and hyperthermia.

Indications:

Bronchoobstructive syndrome with bronchial asthma, bronchitis, emphysema, hypertension in the "small" circulation.

Violation of cerebral circulation by ischemic type (as part of combination therapy to reduce intracranial pressure).

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

Contraindications:

Severe arterial hypotension or hypertension, paroxysmal tachycardia, extrasystole, myocardial infarction with cardiac rhythm disturbances, epilepsy, increased convulsive alertness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency,hepatic and / or renal failure, hemorrhagic stroke, bleeding in the retina, bleeding in a recent medical history, Hypersensitivity to the drug (including other derivatives of xanthine: caffeine, pentoxifylline, theobromine).

Carefully:

pregnancy, newborn, age over 55 years, and uncontrolled hypothyroidism (possibility of cumulation), sepsis, prolonged pyrexia, gastroesophageal reflux disease, prostatic hyperplasia, widespread atherosclerosis, patients with severe liver and kidney, gastric ulcer and 12 duodenal ulcer (in the anamnesis).

Be careful when consuming large quantities of caffeine-containing foods or drinks during the treatment period.

Pregnancy and lactation:

If it is necessary to prescribe the drug during pregnancy and lactation, it is necessary to compare the expected benefit to the mother and the potential risk to the fetus or newborn. If you need to use the drug during lactation, breast-feeding should be discontinued.

Dosing and Administration:

Intravenously.

In the vein, adults are slowly administered (for 4-6 minutes) 5-10 ml of a 2.4% solution (0.12-0.24 g), which is previously diluted in 10-20 ml of isotonic sodium chloride solution. With the appearance of palpitations, dizziness, nausea, the rate of administration slows down or changes to drop introduction, for which 10-20 ml of a 2.4% solution (0.24-0.48 g) is diluted in 100-150 ml of isotonic sodium chloride solution; injected at a rate of 30-50 drops per minute. Parenterally enter euphyllin up to 3 times a day, no more than 14 days.

Higher doses of euphyllin for adults in the vein: single-dose 0.25 g, daily - 0.5 g.

The drug is not recommended for children under 14 years due to side effects.

However, if necessary, children are administered intravenous eufillin at a single dose of 2-3 mg / kg, preferably drip.

Higher doses for children intravenously: single dose - 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 mg, from 8 to 18 years - 0,25-0,5 g.

Side effects:

From the digestive system: gastroesophageal reflux, heartburn, exacerbation of peptic ulcer and duodenal ulcer, gastralgia, diarrhea.

From the side of the central nervous system: anxiety, anxiety, irritability, dizziness, rarely - convulsions, nausea, vomiting, insomnia, tremor.

From the cardiovascular system: a feeling of palpitations, tachycardia (incl.the fetus when taking the pregnant woman in the third trimester), cardialgia, an increase in the frequency of angina attacks, cardiac arrhythmias, lowering blood pressure right up to collapse - with a rapid IV injection.

Allergic reactions: exfoliative dermatitis, fever.

Local reactions: compaction at the injection site - hyperemia, tenderness.

Other: sensation of "hot flashes" to the face, increased diuresis, chest pain, tachypnea, albuminuria, hematuria, hypoglycemia, increased sweating, skin rash, itching of the skin.

Overdose:

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (including blood), gastrointestinal bleeding, tachypnea, facial skin hyperemia, tachycardia, ventricular arrhythmias, insomnia, motor agitation, anxiety, photophobia, tremor, convulsions . In severe poisoning, epileptic seizures may develop (especially in children without any precursors), hypoxia, metabolic acidosis, hyperglycemia, hypokalemia, lowering blood pressure, necrosis of skeletal muscles, confusion, renal insufficiency with myoglobinuria.

Treatment: drug withdrawal, forced diuresis, hemosorption, plasmosorption, hemodialysis (efficacy is low, peritoneal dialysis is ineffective), symptomatic therapy (incl. metoclopramide and ondansetron - when vomiting). If seizures occur, maintain airway patency and conduct oxygen therapy. For seizure seizure - in / in diazepam, 0.1-0.3 mg / kg (but not more than 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (w / w).

Interaction:

In combination with phenobarbital, phenytoin, rifampicin, isoniazid, carbamazepine or sulphinpyrazone, a decrease in the effectiveness of euphyllin is observed, which may require an increase in the doses used. The clearance of the drug is reduced when used in combination with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, enoxacin, beta-blockers, which may require a dose reduction. Ephedrine and caffeine increase the effect of the drug. When used simultaneously with small doses of ethanol, disulfiram, fluoroquinolones, recombinant interferon alpha, methotrexate, mexiletine, propafenone, tiabendazole, ticlopidine, verapamil, and when vaccinated against influenza, the intensity the action of aminophylline may increase, which may require a reduction in its dose. Enhances the action of beta-adrenostimulyatorov.

Oral estrogen-containing contraceptives, antidiarrhoeal drugs, intestinal sorbents weaken, and H2-histaminoblockers, blockers of "slow" calcium channels increase the effect (bind to the enzymatic system of cytochrome P450 and slow the metabolism) of aminophylline. The use of beta-adrenoblockers interferes with the bronchodilating effect of euphyllin and can cause bronchospasm. Eufillin potentiates the action of diuretics by increasing glomerular filtration and reducing tubular reabsorption, decreases the effectiveness of lithium preparations. With caution, euphyllin is used concomitantly with anticoagulants, with other theophylline derivatives or purine.

Increases the likelihood of side effects of drugs that excite the central nervous system (increases neurotoxicity), glucocorticosteroids, mineralocorticosteroids (hypernatremia), funds for general anesthesia (the risk of ventricular arrhythmias increases).Compatible with antispasmodics. The drug is incompatible with a solution of glucose, fructose and levulose. The pH of the mixed solutions should be taken into account: pharmaceutically incompatible with acid solutions.

Special instructions:

Before parenteral administration, the solution must be heated to body temperature. The drug is administered with caution to patients with severe impairment of liver and kidney function, peptic ulcer of the stomach and duodenum.

Elderly patients are advised to reduce the dose of the drug due to delayed excretion of it from the body. Smoking patients are advised to increase the dose due to accelerated removal of the drug from the body.

Effect on the ability to drive transp. cf. and fur:

The drug may cause dizziness and other side effects that may affect the ability to drive vehicles and perform other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous administration is 24 mg / ml.

Packaging:

5 ml or 10 ml into neutral glass ampoules with a notch.

5 or 10 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

1 circuit cell pack together with the instruction for use is placed in a cardboard box pack.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002546

Date of registration:25.07.2014

The owner of the registration certificate:MARCH, LTD.MARCH, LTD.

Manufacturer: & nbsp

ANHUI CHENGSHI MANUFACTURE MEDICINE, Co. Ltd. China

Information update date: & nbsp25.07.2014

Illustrated instructions

Instructions

Eufillin (Euphyllini)