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

The drug inhibits phosphodiesterase, increases accumulation in the tissues of cyclic adenosine monophosphate, 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 muscles of the bronchi, stops bronchospasm, increases mucociliary clearance, stimulates the 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 reduction in the severity and frequency of episodes of apnea. Normalizes the respiratory function, promotes the saturation of blood with oxygen and a decrease in the concentration of carbon dioxide. Strengthens lung ventilation in hypokalemia. Has a stimulating effect on the activity of the heart, increases the strength and heart rate, increases coronary blood flow and the need for myocardium in oxygen. Reduces the tone of blood vessels (mainly, the vessels of the brain, skin and kidneys). Has peripheral vasodilating effect, reduces pulmonary vascular resistance, lowers pressure in the "small" circle of blood circulation. Increases renal blood flow. Has a moderate diuretic effect. Expands extrahepatic biliary tract. It inhibits platelet aggregation (suppresses the platelet and prostaglandin E2 alpha activation factor), increases the resistance of erythrocytes to deformation (improves rheological properties of blood), reduces thrombus formation and normalizes microcirculation. Has tocolytic effect, increases the acidity of gastric juice.When used in large doses has an epileptogenic effect.

Pharmacokinetics:

Bioavailability for liquid dosage forms is 90-100%. The maximum concentration (7 μg / ml) with intravenous administration of 300 mg is achieved after 15 minutes.

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 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 blood serum), does not accumulate in adipose tissue. 90% 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 excretion of the drug, in particular among smokers this period is significantly reduced and ranges from 4 to 5 hours. Elimination of the drug is prolonged in patients with respiratory failure, with renal and heart failure, with viral infections and hyperthermia.

Indications:

Bronchoobstructive syndrome in bronchial asthma, bronchitis, pulmonary emphysema (mainly for relief of seizures); hypertension in the "small" circle of the circulation.

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

Left ventricular heart failure with bronchospasm and respiratory depression according to the Chain-Stokes type (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 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, acute porphyria.

Carefully:

Age over 55 years and uncontrolled hypothyroidism (the possibility of cumulation), widespread atherosclerosis of the vessels, sepsis,prolonged pyrexia, gastroesophageal reflux disease, peptic ulcer and duodenal ulcer (in history), prostatic hyperplasia.

The drug is administered with caution to patients with severe impairment of liver and kidney function.

Children under 14 years of age (due to possible side effects).

Pregnancy and lactation:

If necessary, use during pregnancy and lactation should be weighed against the expected benefit to the mother and the potential risk to the fetus or child.

If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Intravenously.

Adults administered slowly (within 4-6 min) 5-10 ml 24 mg / ml (0,12-0,24 g) which had been diluted in 10-20 ml of 0.9% sodium chloride solution. When palpitations, dizziness, nausea - injection speed or slow moving to a drip, which 10-20 ml of a solution of 24 mg / ml (0,24-0,48 g) was diluted in 100-150 ml of 0.9% solution sodium chloride; 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 aminophylline adults when administered intravenously: single - 0.25 g daily - 0.5 g

If necessary children injected eufillin intravenously drip from the calculation of a single dose of 2-3 mg / kg.

Higher doses for children with intravenous administration: 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 g, from 8 to 18 years - 0,25-0,5 g.

The procedure for working with a polymer ampoule:

1. Take an ampoule and shake it, holding it by the neck.

2. Press the ampoule with your hand, while the drug should not be isolated, and rotate and separate the valve with rotating movements.

3. Through the formed hole, immediately connect the syringe with the ampoule.

4. Turn the ampoule over and slowly put the contents into the syringe.

5. Put the needle on the syringe.

Side effects:

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

From the side of the cardiovascular system: palpitation, tachycardia (including the fetus when taking the pregnant woman in the III trimester), arrhythmias, lowering blood pressure right up to the collapse - with rapid intravenous injection, cardialgia, an increase in the frequency of angina attacks.

From the digestive system: gastroesophageal reflux, heartburn, exacerbation of peptic ulcer of the stomach and duodenum.

Allergic reactions: skin rash, itching of the skin, fever

OtherChest pain, tachypnea, a sense of "tide" to face, albuminuria, hematuria, hypoglycemia, increased diuresis, increased sweating.

Local Reactions: compaction, hyperemia, tenderness at the site of administration.

Overdose:

Symptoms: decreased appetite, gastralgia, diarrhea, nausea, vomiting (in m. hr. with blood), gastrointestinal bleeding, tachypnea, facial flushing, tachycardia, ventricular fibrillation, insomnia, motor agitation, anxiety, photophobia, tremors, 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: removal of the drug, diuresis, hemosorbtion, plasmasorption, hemodialysis (efficiency is low, peritoneal dialysis is ineffective), symptomatic therapy (r. h. metoclopramide and ondansetron - when vomiting).If seizures occur, maintain airway patency and conduct oxygen therapy. To stop the seizure - intravenously diazepam, 0.1-0.3 mg / kg (but not more than 10 mg). With severe nausea and vomiting - metoclopramide or ondansetron (intravenously).

Interaction:

The drug is incompatible with a solution of glucose, fructose.

The pH of the mixed solutions should be taken into account: pharmaceutically incompatible with acid solutions.

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

Doxapram, when used simultaneously with euphyllinum, increases the stimulation of the respiratory center in the central nervous system.

Euphyllin shows a synergistic toxicity with ephedrine and other sympathomimetics. With their joint application, the risk of arrhythmias increases.

The combined use of euphyllin and xanthine derivatives, including pentoxifylline, is contraindicated due to the risk of development of toxicity.

Enoxacin reduces excretion of euphyllin due to inhibition of cytochrome P4501A2; with the effect of euphyllin increased by 300%, which leads to an increased risk of seizures.

The combined use of euphyllin and fluvoxamine should be avoided. If their joint use is necessary, you should reduce the dose of euphyllin by half and carefully monitor the concentration of euphyllin in the blood plasma.

Rifampicin, phenobarbital, phenytoin, isoniazid, carbamazepine, sulfinpyrazone, aminoglutethimide, oral estrogen-containing contraceptives and moracisin, as inducers of microsomal oxidation, increase the clearance of euphyllin, which may require an increase in its dose.

With simultaneous use with antibiotics from the group of macrolides, lincomycin, with fluoroquinolones, small doses of ethanol, allopurinol, beta adrenoblockers, cimetidine, disulfiram, hormonal contraceptives for ingestion, recombinant interferon alpha, isoprenaline, viloxazine, methotrexate, propafenone, verapamil and for vaccination against influenza, the intensity of the action of euphyllin may increase, which may require a reduction in its dose.

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

Compatible with antispasmodics.

With caution appoint simultaneously with antiplatelet agents (ticlopidine) - suppresses platelet aggregation.

Special instructions:

Before parenteral administration, the solution must be heated to body temperature.

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.

Avoid the use of large quantities of caffeine-containing foods or beverages during the treatment period.

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

The drug may cause dizziness and other side effects. During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous administration, 24 mg / ml.

Packaging:

By 5 or 10 ml into ampoules of low-density polyethylene or polypropylene.

For 5 or 10 ampoules together with instructions for use in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003461

Date of registration:16.02.2016

Expiration Date:16.02.2021

The owner of the registration certificate:GROTEKS, LLC GROTEKS, LLC Russia

Manufacturer: & nbsp

GROTEKS, LLC Russia

Representation: & nbspGROTEKS, LLCGROTEKS, LLC

Information update date: & nbsp01.08.2016

Illustrated instructions

Instructions

Eufillin (Euphyllini )