In the article, we will consider in which cases “Eufillin” is used intramuscularly.
This is a bronchodilator drug. The medicine is available in the form of solutions and tablets, but in which case and in what dosages to use it is a difficult question. It depends on the severity of the pathological condition, the patient’s diagnosis, his age, indications and contraindications. Many people are interested in: is it possible to inject “Eufillin” intramuscularly or intravenously or is it better to use a tablet form? Experts are of the opinion that through an intramuscular injection, the drug quickly penetrates into the blood and the therapeutic effect occurs within a few minutes. This is indicated in emergency situations and in severe forms of the disease. In the case of moderate and mild severity of the pathology, the medication is prescribed orally.
Pharmacological properties
Bronchodilator drug is an inhibitor of PDE. The active substance is the theophylline ethylene diamine salt (which increases absorption and facilitates solubility). It has a pronounced bronchodilator effect, which is due to a direct relaxing effect on the smooth muscles of blood vessels in the lungs and respiratory tract. It is believed that this effect is caused by selective inhibition of the activity of specific PDE, which contributes to an increase in intracellular cAMP concentrations. The results of experimental tests conducted by invitro showed that the main role is played by isoenzymes of the 3rd and 4th types. Suppression of the functionality of these isoenzymes can also provoke some adverse reactions of aminophylline (theophylline), in particular vomiting, tachycardia and arterial hypotension. Blocks purine (adenosine) receptors, which may be one of the factors affecting the bronchi.
Many people wonder if you can use “Eufillin” intramuscularly. About this - below.
It reduces the hyperresponsiveness of the respiratory canals, which is associated with the late phase of the reaction, provoked by inhalation of allergens, through a mechanism of unknown etiology, which is not related to the suppression of PDE or to the blockade of adenosine exposure. There is also information that aminophylline increases the number and activity of T-suppressors in peripheral blood.
The medication increases mucociliary clearance, improves the functioning of the intercostal and respiratory muscles, activates the contraction of the diaphragm and the respiratory center, increases its sensitivity to carbon dioxide molecules and normalizes alveolar ventilation, which ultimately leads to a decrease in the frequency and severity of apnea attacks. By normalizing respiratory functions, this medication helps to saturate the blood with oxygen and reduce the concentration of carbon dioxide. Increases lung ventilation with hypokalemia.
In addition, this medication has a stimulating effect on the activity of the heart, increases the frequency of contractions of the heart, increases blood flow in the coronary vessels and increases the oxygen demand of the heart muscle. It reduces the tone of the vascular walls (mainly the skin, blood vessels of the brain and kidneys), has a venodilating peripheral effect, reduces vascular resistance in the lungs, lowers blood pressure in the pulmonary circulation. Enhances renal blood flow, has a light diuretic effect.
It expands bile extrahepatic pathways, stabilizes mast cell membrane structures, slows down the release of mediators that provoke the development of allergic reactions and platelet aggregation (inhibits the activation factor of PgE2α and platelets), increases the resistance of red blood cells to structural changes (normalizes the rheological properties of blood), and reduces the likelihood of thrombosis and normal microcirculation, has a tocolytic property, increases the acidity of the juice of the stomach. In high doses, it has an epileptogenic effect.
The instruction for use of "Eufillin" intramuscularly confirms this.
Pharmacokinetic properties
Aminophylline is metabolized in the human body at physiological pH values with the release of free theophylline. The bronchodilating property is manifested at theophylline concentrations in the blood in the range of 10-20 μg / ml. A concentration of more than 20 mg / ml is considered toxic. The exciting effect on the respiratory center is realized at lower concentrations - 5-10 μg / ml.
The binding of the main element to plasma proteins is approximately 40%; in newborns, as well as in adults with certain pathologies, the level of binding decreases. In adult patients, plasma protein binding is approximately 60%, in newborns - 36%, in people with cirrhosis - 36%. The substance crosses the placenta (the level in the fetal blood is slightly higher than in the mother’s blood) and into mother’s milk.
Theophylline undergoes metabolic processes in the liver with the participation of some isoenzymes of cytochrome P450, the most important of which is considered CYP1A2. With metabolic changes, 1,3-dimethyl uric acid is formed, as well as 3-methylxanthine and 1-methyl uric acid. These metabolites are excreted through the urinary system. In adult patients, approximately 10% of the main component is excreted unchanged. In newborns, a significant part is excreted in the form of caffeine (due to the immaturity of the pathways of its subsequent metabolism), in unchanged form - about 50%.
Serious individual differences in the rate of hepatic metabolism of theophylline are considered the main reason for the pronounced variability of indicators of clearance, blood concentration, elimination half-life. The process of hepatic metabolism is influenced by factors such as addiction to smoking, age, dietary preferences, diseases, combined drug therapy.
Theophylline half-life in non-smoking patients with bronchial asthma with almost no pathological changes from other systems and organs is 6-12 hours, in people with an addiction to smoking - 4-5 hours, in children - 1-5 hours, during the neonatal period and in premature infants - 10-45 hours. This interval increases in the elderly and in people suffering from liver disease or heart failure.
Ground clearance is reduced with impaired liver function, heart failure, pulmonary edema, chronic alcoholism, COPD. Ethylenediamine does not affect the pharmacokinetic properties of theophylline.
Is it possible to use "Eufillin" intramuscularly, it is important to find out in advance.
Composition and form of release
The main active ingredient of the drug is aminophylline. It is thanks to him that all pharmacological actions of the drug are achieved. For intramuscular administration, it is released in the form of ampoules. The composition of the solution (concentration of 24 mg / ml) includes the main substance and an auxiliary component - water for injection. Ampoules contain 5 or 10 ml of medical solution.
Indications for appointment
The medicinal product "Eufillin" is intramuscularly prescribed for the following pathological conditions:
- Asthmatic status (as an additional treatment).
- Apnea in the neonatal period.
- Left ventricular insufficiency with bronchospasm and impaired respiratory function according to the Cheyne-Stokes type (as part of complex treatment).
- Edematous syndrome of renal origin.
- Ischemic cerebrovascular accident (as part of complex therapy), acute and chronic heart failure (as part of combined treatment).
- Bronchial obstructive syndrome of various etiologies (including COPD, bronchial asthma, pulmonary emphysema, chronic obstructive bronchitis), increased pressure in the pulmonary circulation, apnea, pulmonary heart.
Instructions for use
How to apply according to the instructions "Amyfillin" in ampoules - intramuscularly or intravenously?
The dosage selection regimen for this drug is individual, depending on age, indications, clinical situation, the presence of nicotine addiction.
In conditions requiring emergency care, adults are shown to use "Eufillina" intramuscularly in a loading dose. If the patient has previously taken theophylline, the dosage of aminophylline should be halved.
What else does the instruction for the use of “Eufillin” in ampoules intramuscularly tell us?
Contraindications
Injection of the drug is contraindicated in the following cases:
- hypersensitivity to aminophylline and other xanthine derivatives;
- angina pectoris;
- acute myocardial infarction;
- acute heart failure;
- extrasystole;
- paroxysmal tachycardia;
- pulmonary edema;
- severe arterial hypertension / hypotension;
- atherosclerosis of blood vessels;
- hemorrhagic stroke;
- the presence of a history of any sudden bleeding;
- retinal hemorrhage;
- peptic ulcer at the stage of exacerbation;
- epilepsy;
- increased threshold of convulsive readiness;
- gastroesophageal reflux (GER);
- uncontrolled hypothyroidism;
- thyrotoxicosis;
- porphyria;
- sepsis;
- impaired functioning of the liver or kidneys.
Can everyone use Eufillin to inject intramuscularly?
Due to the likelihood of side effects, it is not recommended to use the solution in children under 14 years of age. In children older than 3 years, this medicine can be used exclusively for emergency indications, for a period of not more than 14 days.
Adverse reactions
According to the instructions for use, "Eufillin" intramuscularly can provoke the occurrence of a number of adverse reactions, which include the following:
- Nervous system: anxiety, dizziness, tremors, sleep disturbances, cramps.
- Cardiovascular system: heart rhythm disturbance, palpitations, pain in the heart, tachycardia, decreased blood pressure, arrhythmias of various kinds, cardialgia, increased symptoms of angina pectoris.
- Digestive system: gastroesophageal reflux, nausea, heartburn, vomiting, diarrhea, exacerbation of peptic ulcer; with prolonged use, anorexia may develop.
- Urinary system: hematuria, albuminuria.
- Allergic manifestations: skin rash and itching, febrile syndrome.
- Metabolism: hypoglycemia (rare cases).
- Local reactions: hyperemia, induration, tenderness at the injection site.
- Other side effects: tachypnea, chest pain, sensation of hot flashes in the face, albuminuria, hematuria, increased diuresis, excessive sweating.
Can Amyfillin in ampoules be used intramuscularly during pregnancy and lactation? We will clarify further.
Use during pregnancy and lactation
The medicinal substance of the drug crosses the placenta, and therefore the use of aminophylline during pregnancy can lead to the creation of potentially dangerous levels of the active substance and caffeine in the blood of a newborn baby. Children whose mothers received aminophylline during pregnancy need medical monitoring of possible signs of intoxication in the first days of life.
Theophylline is excreted in breast milk. When using the drug during lactation, excessive agitation and irritability in the child may occur. In this regard, the use of this drug in pregnancy and lactation can be prescribed only in cases where the benefit of therapy for the mother is higher than the potential risk to the child.
Special recommendations
With caution, the Eufillin medicine is administered intramuscularly according to the instructions for severe coronary artery insufficiency (angina pectoris, acute infarction), obstructive hypertrophic cardiomyopathy, common atherosclerosis, rapid ventricular extrasystole, high convulsive readiness, liver or kidney failure, recent digestive organs path, with peptic ulcer, uncontrolled hypothyroidism or thyrotoxicosis, with a prolonged increase in t mperatury body, prostatic hypertrophy, gastroesophageal reflux disease, in elderly patients and in children.
Correction of the dosage of aminophylline may be necessary for heart failure, impaired liver function, fever, prolonged alcoholism, SARS. In elderly patients, a dosage reduction may be required.
Aminophylline is not used concurrently with other xanthine derivatives. During the period of therapy, the use of products that contain xanthine derivatives should be avoided. With caution, a medication is used simultaneously with purine derivatives and anticoagulants. The combined use with glucose and beta-blockers should be avoided.
Is it possible to inject “Eufillin” intramuscularly, now it is known.
Reviews
There are few reviews about this drug, since most often it is used only in stationary conditions. Nevertheless, patients indicate some cases of prescribing the medication for use at home with bronchial asthma, in particular when an attack of this disease occurs.
In the reviews, it is noted that the medicine has a very high efficiency, quickly eliminates the signs of a serious condition in patients, facilitates breathing and is prescribed for obstructive bronchitis and some cardiac pathologies.
There are a lot of side effects from using the “Eufillin” instructions for injections intramuscularly. Patients to whom the medication was administered note that approximately 15 minutes after administration, they experienced severe nausea, and sometimes even vomiting. There are also indications of severe dizziness, disturbances in the nervous system.
We reviewed the instructions for "Eufillin." Intramuscularly, it is administered in severe forms of pathologies.