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 Euphyllinum (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% 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 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 arterial hypotension or hypertension, paroxysmal tachycardia, extrasystole, myocardial infarction with heart rhythm disturbances, epilepsy, increased convulsive alertness, hypertrophic obstructive cardiomyopathy, thyrotoxicosis, pulmonary edema, severe coronary insufficiency, hepatic and / or renal insufficiency, hemorrhagic stroke, retinal hemorrhage eyes, bleeding in a recent medical history, hypersensitivity to the drug (including other xanthine derivatives: caffeine, pentoxifyli well, theobromine).

Carefully:

Carefully: pregnancy, lactation period, newborn 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, Euphyllin is administered up to 3 times a day, no more than 14 days.

Higher doses of Eufillina 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 given Eufillin intravenously 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 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, diarrhea, gastralgia, nausea, vomiting, with prolonged admission - decreased appetite.

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

On the part of the cardiovascular system: tachycardia, cardialgia, an increase in the frequency of angina attacks, cardiac rhythm disturbances, lowering blood pressure right up to collapse - with a rapid IV injection.

Allergic reactions: exfoliative dermatitis, febrile reaction, skin rash, itching. Local reactions: at the injection site - hyperemia, soreness.

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

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 or contents of Eufillina more than 50 g / l) the hemodialysis is recommended.

Interaction:

Ephedrine, beta-adrenostimulators, caffeine and furosemide increase the effect of the drug. In combination with phenobarbital, diphenin, rifampicin, isoniazid, carbamazepine or sulfinpyrazone, a decrease in the efficacy of Eufillin is observed, which may require an increase in the applied doses of the drug.

The clearance of the drug decreases when it is administered in combination with antibiotics of the macrolide group, lincomycin, allopurinol, cimetidine, isoprenaline, beta-blockers, which may require a dose reduction.

Oral estrogen-containing contraceptives, antidiarrheal drugs, intestinal sorbents weaken, and H2-histaminoblockers, slow calcium channel blockers, mexiletine increase the effect (bind to the enzymatic system of cytochrome P450 and slow the metabolism of aminophylline).

When used in combination with enoxacin and other fluoroquinolines, the dose of Eufillin is reduced.

The drug inhibits the therapeutic effects of lithium carbonate and beta-blockers. The administration of beta-blockers inhibits the bronchodilating effect of Euphyllin and can cause bronchospasm.

Eufillin potentiates the action of diuretics by increasing the glomerular filtration and reducing tubular reabsorption.

It is not recommended to use Euphyllinum simultaneously with anticoagulants, with other derivatives of theophylline or purine.

With simultaneous administration with agents that excite the central nervous system, neurotoxicity increases.

The drug can not be used with solutions of dextrose, is not compatible 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:

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:Solution for intravenous administration of 24 mg / ml in ampoules of 5 ml or 10 ml. For 10 ampoules together with instructions for use, ampoule scraper or knife for opening ampoules in a box or a pack of cardboard with partitions or liner.

Storage conditions:

List B. Store at a temperature of no higher than 30 ° C in a place protected from light and inaccessible to children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N000808 / 01

Date of registration:15.08.2007

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp15.08.2007

Illustrated instructions

Instructions

Eufillin (Euphyllini)