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. Eufillin lowers the vascular resistance, lowers the tone of 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 platelet aggregation, improves microcirculation.

Pharmacokinetics:

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. Eufillin penetrates through the placental and blood-brain barrier, in adipose tissue does not accumulate. 90 % the drug is metabolized in the liver. Metabolites are excreted by the kidneys, 7-13 % of the drug is released 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 in bronchial asthma, bronchitis, pulmonary emphysema, cardiac asthma (mainly for relief of seizures); hypertension in a small circle of blood 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 hypotension or hypertension, paroxysmal tachycardia, arrythmia, myocardial infarction with cardiac arrhythmia, epilepsy, increased convulsive readiness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and / or renal failure, hemorrhagic stroke, bleeding into the retina eyes, bleeding in a recent medical history, hypersensitivity to the drug (including other xanthine derivatives: caffeine, pentoxifyli well, theobromine), the period of lactation.

Carefully:

With caution: pregnancy, neonatal period, age over 55 years and uncontrolled hypothyroidism (the possibility of cumulation),sepsis, prolonged hyperthermia, gastroesophageal reflux, prostate adenoma.

The drug is not recommended for intravenous administration to children under 14 years of age (due to possible side effects).

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.

Dosing and Administration:

In the vein, adults are slowly injected (for 4-6 minutes) with 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 gastrointestinal tract: gastroesophageal reflux (heartburn), exacerbation of peptic ulcer.

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

From the cardiovascular system: palpitations, tachycardia (including the fetus in pregnant while taking III trimester) cardialgia, increasing the frequency of attacks of angina, cardiac arrhythmias, blood pressure decline until collapsing - under rapid on / in .

From the digestive system: gastralgia, diarrhea.

Allergic reactions: exfoliative dermatitis, febrile reaction.

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

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

Overdose:

When an overdose occurs, anorexia, diarrhea, nausea, vomiting, epigastric pain, gastrointestinal bleeding, tachycardia,ventricular arrhythmias, tremor, generalized convulsions, hyperventilation, a sharp drop in blood pressure.

Treatment of overdose depends on the clinical picture, includes the abolition of the drug, stimulation of its removal from the body (forced diuresis, hemosorption, plasmosorption, hemodialysis, peritoneal dialysis) and the appointment of symptomatic agents. For cramping seizures applied diazepam (in injections). Do not use barbiturates. At the expressed intoxication (the maintenance of an eufillina more than 50 g / l) the hemodialysis is recommended.

Interaction:

In combination with phenobarbital, diphenin, rifampicin, isoniazid, carbamazepine or sulfinpyrazone, a decrease in the efficacy of euphyllin is observed, which may require an increase in the applied doses of the drug. The clearance of the drug is reduced when it is administered 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. With simultaneous use with small doses of ethanol, disulfiram, fluoroquinolones,recombinant interferon alpha, methotrexate, mexiletine, propafenone, thiabendazole, ticlopidine, verapamil, and with influenza vaccination, the intensity 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-histamine blockers, slow calcium channel blockers increase the effect (bind to the enzymatic system of cytochrome P450 and slow the metabolism) of aminophylline. The administration of beta-blockers inhibits the bronchodilating action of euphyllin and can cause bronchospasm. Euphyllin potentiates the action of diuretics funds due to increased glomerular filtration and reduced tubular reabsorption, reduces the effectiveness of lithium preparations. With caution, euphyllin is prescribed concomitantly with anticoagulants, with other theophylline derivatives or purine. It is not recommended to use eufillin with agents that excite the central nervous system (increases neurotoxicity).Increases the likelihood of side effects of 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.

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

Form release / dosage:

Solution for intravenous administration is 24 mg / ml.

Packaging:5 ml, 10 ml of the drug into neutral glass ampoules with a notch marked with a dot (paint).

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

1 circuit cell pack together with instructions for use, a scarifier or an ampoule knife is placed in a cardboard box.

Storage conditions:

Store in a dry, 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:LSR-000055

Date of registration:27.04.2007

The owner of the registration certificate: Mapichem AG Mapichem AG Switzerland

Manufacturer: & nbsp

SHANDONG SHENGLU PHARMACEUTICAL, Co.Ltd China

Representation: & nbspMapichem AGMapichem AG

Information update date: & nbsp08.11.2010

Illustrated instructions

Instructions

Eufillin (Euphyllini)