Aminophylline
Aminophylline: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Aminophyllin
ATX code: R03DA05
Active ingredient: aminophylline (aminophylline)
Producer: Krakow Pharmaceutical Plant (Poland), Remedica Ltd (Cyprus), Borisov Plant of Medical Products, JSC (Republic of Belarus)
Description and photo updated: 2019-27-08
Aminophylline is an anti-asthmatic agent, antispasmodic, bronchodilating and vasodilating action.
Release form and composition
Dosage forms of release:
- tablets (10 pcs. in a package);
- solution for intravenous administration 2.4% (in ampoules of 5 or 10 ml, 10 ampoules in a contour package, 1 or 2 packages in a cardboard box);
- rectal suppositories (6 pcs. in a blister strip, 2 packs in a cardboard box).
Each pack also contains instructions for the use of Aminophylline.
Pharmacological properties
Pharmacodynamics
Aminophylline is a bronchodilator, PDE (phosphodiesterase) inhibitor. The substance is the ethylenediamine salt of theophylline, which facilitates solubility and helps to increase absorption.
It has a bronchodilatory effect, which is most likely due to a direct relaxing effect on the smooth muscles of the blood vessels of the lungs and respiratory tract. There is an assumption that this effect is associated with the selective suppression of the activity of specific PDEs. This leads to an increase in the intracellular concentration of cAMP (cyclic adenosine monophosphate). As a result of the studies carried out, it was found that the main role probably belongs to type III and IV isoenzymes. When the activity of these isoenzymes is suppressed, some side reactions of aminophylline (theophylline) can be observed, including vomiting, tachycardia and arterial hypotension. The substance blocks purine (adenosine) receptors, which may be one of the factors affecting the bronchi.
Reduces airway hyperresponsiveness, which is associated with the late phase of the reaction due to inhalation of allergens. There is evidence that aminophylline in the peripheral blood increases the activity and number of T-suppressors.
The substance stimulates the respiratory center and diaphragm contraction, increases mucociliary clearance, improves the function of the intercostal and respiratory muscles, and alveolar ventilation. Together, these effects lead to a decrease in the frequency and severity of apnea episodes. Due to the normalization of the respiratory function, the blood is saturated with oxygen and the concentration of carbon dioxide decreases. In conditions of hypokalemia, it enhances ventilation.
Aminophylline has a stimulating effect on the activity of the heart, increases the strength and heart rate, coronary blood flow and myocardial oxygen demand. At the same time, there is a decrease in the tone of the blood vessels (mainly the vessels of the brain, kidneys and skin).
It has a peripheral venodilating effect, reduces pressure in the pulmonary circulation and pulmonary vascular resistance. In high doses, it has an epileptogenic effect.
Other effects of aminophylline:
- expansion of the extrahepatic biliary tract;
- stabilization of the mast cell membrane, inhibition of the release of mediators of allergic reactions;
- increased renal blood flow (has a mild diuretic property);
- inhibition of platelet aggregation, increasing the resistance of erythrocytes to deformation (improving the rheological properties of blood), reducing thrombus formation and normalizing microcirculation;
- increased acidity of gastric juice (tocolytic effect).
Pharmacokinetics
Aminophylline in the body is metabolized at physiological pH values, with the release of free theophylline. Bronchodilating effect develops at plasma concentrations of theophylline in the range of 0.01-0.02 mg / ml. A concentration of more than 20 mg / ml is considered toxic. At a lower concentration (0.005–0.01 mg / ml), an exciting effect on the respiratory center is realized.
The level of binding of theophylline to plasma proteins is approximately 40%. In adults, this figure is ~ 60%, in newborns and patients with liver cirrhosis ~ 36%. Penetrates through the placental barrier (serum concentration in the blood of the fetus is slightly higher than that of the mother). The substance is excreted in breast milk.
Theophylline metabolism occurs in the liver. Several isoenzymes of cytochrome P 450 are involved in the process, the most important is CYP1A2. The result is 1-methyl-uric acid, 1,3-dimethyl-uric acid, and 3-methylxanthine. The excretion of these metabolites occurs in the urine. In adults, 10% of the substance is excreted unchanged. In newborns, due to the immaturity of the pathways of its further metabolism, most of it is excreted in the form of caffeine, 50% - unchanged.
Significant individual variability in the rate of hepatic metabolism of theophylline is the cause of pronounced differences in the values of clearance, T 1/2 (half-life), plasma concentration. Hepatic metabolism is influenced by the following factors: age, addiction to tobacco smoking, dietary intake, and concomitant medications.
In nonsmokers with bronchial asthma without significant pathological changes in other systems and organs, T 1/2 of theophylline is 6-12 hours, in smokers - from 4 to 5 hours, in children - from 1 to 5 hours, in newborns and premature infants - within 10–45 hours. In elderly patients and patients with heart failure or liver disease, the T 1/2 value of theophylline increases.
In heart failure, chronic alcoholism, liver dysfunction, pulmonary edema, chronic obstructive pulmonary disease, clearance decreases.
Ethylenediamine has no effect on the theophylline pharmacokinetic parameters.
Indications for use
Aminophylline injection solution is used as a monotherapy agent or an additional agent in combination therapy in the treatment of the following diseases:
- Apnea of newborns;
- Status asthmaticus;
- Ischemic cerebral circulation disorders;
- Edematous syndrome of renal origin;
- Left ventricular failure, accompanied by a Cheyne-Stokes-type breathing disorder and bronchospasm;
- Acute and chronic heart failure.
Suppositories and tablets Aminophylline are prescribed for the treatment of:
- Sleep apnea;
- Hypertension in the pulmonary circulation;
- Broncho-obstructive syndrome of various origins, including bronchial asthma, chronic obstructive pulmonary disease;
- Chronic and acute heart failure (as part of combination therapy).
Contraindications
The use of Aminophylline is contraindicated:
- With severe arterial hyper- or hypotension;
- With tachyarrhythmias;
- Against the background of gastric ulcer and duodenal ulcer in the acute phase;
- With hyperacid gastritis;
- Against the background of severe violations of the liver and kidneys;
- With epilepsy;
- With hemorrhagic stroke;
- With retinal hemorrhage;
- Simultaneously with ephedrine in children;
- With hypersensitivity to the components of the drug, as well as to other xanthine derivatives: caffeine, pentoxifylline, theobromine.
In the treatment of neonatal apnea, the drug is given through a nasogastric tube.
The appointment of Aminophylline solution to children under the age of 3 years, prolonged oral forms - up to 12 years is contraindicated. The drug in the form of rectal suppositories is not prescribed for children.
Relative contraindications (Aminophylline is used with caution, under medical supervision):
- renal and hepatic impairment;
- pregnancy and lactation;
- elderly age.
Aminophylline, instructions for use: method and dosage
The dosage regimen of Aminophylline is set by the doctor individually, depending on age, indications, clinical situation, scheme and routes of administration, as well as nicotine addiction.
Intravenous aminophylline is administered slowly (2 ml / minute) 1-3 times a day at 4-6 mg / kg.
For oral administration, the initial dosage is 1 tablet per day, divided into 2 parts (interval between doses - 12 hours). The dose is increased every 3 days until the optimal therapeutic effect is achieved. Reduced dosages are used against the background of chronic heart and liver failure, acute pneumonia, viral infections, as well as in the elderly.
Adults are rectally prescribed 1 suppository up to 2 times a day, for children at the rate of 7 mg / kg one time, a maximum of 15 mg / kg per day.
Side effects
The use of Aminophylline can lead to the development of disorders on the part of some body systems, manifested in most cases as:
- Tachycardia, palpitations, arrhythmias, cardialgia, decreased blood pressure, increased frequency of angina attacks;
- Insomnia, dizziness, anxiety, irritability, headache, agitation, tremor;
- Itchy skin, skin rash, fever;
- Vomiting, gastralgia, diarrhea, nausea, heartburn, gastroesophageal reflux, exacerbation of peptic ulcer disease;
- Increased urine output, chest pain, flushing, tachypnea, hematuria, albuminuria, hypoglycemia, increased sweating.
With rectal administration of Aminophylline, proctitis and irritation of the rectal mucosa may develop.
With long-term therapy, there may be a decrease in appetite.
The severity of side effects depends on the dosage taken.
Overdose
The main symptoms: ventricular arrhythmias, insomnia, photophobia, anxiety, generalized convulsions, tachypnea, epigastric pain, anorexia, diarrhea, vomiting, nausea, gastrointestinal bleeding, tachycardia, facial flushing.
Therapy: cancellation of Aminophylline, stimulation of the excretion of the substance from the body (prescribe gastric lavage, forced diuresis, hemosorption, plasma sorption, peritoneal dialysis, hemodialysis); symptomatic treatment.
special instructions
Caution should be exercised when used simultaneously with anticoagulants, as well as with other derivatives of purine or theophylline.
During treatment, it is not recommended to consume large amounts of caffeinated drinks or foods.
Combined use with beta-blockers and glucose solution should be avoided.
Application during pregnancy and lactation
Aminophylline during pregnancy / lactation can be used only in cases where the expected benefit from therapy outweighs the possible risk.
Theophylline crosses the placental barrier. Aminophylline therapy in pregnant women can result in potentially harmful plasma concentrations of theophylline and caffeine in the newborn's blood. The condition of newborns whose mothers received aminophylline during pregnancy (especially during the third trimester) should be monitored in order to control possible symptoms of theophylline intoxication.
Theophylline is excreted in breast milk. The use of the drug by a nursing mother can cause irritability in the child.
Pediatric use
It is contraindicated to prescribe Aminophylline injections to children under the age of 3 years, prolonged oral forms - up to 12 years. In the form of rectal suppositories, the drug is not prescribed to children.
With impaired renal function
- severe renal dysfunction: therapy is contraindicated;
- renal impairment: Aminophylline should be used with caution.
For violations of liver function
- severe liver dysfunction: therapy is contraindicated;
- hepatic impairment: Aminophylline should be used with caution.
Use in the elderly
Elderly patients Aminophylline is prescribed under medical supervision. Dose reduction may be required.
Drug interactions
The effect of drugs / substances on the intensity of action of Aminophylline:
- decrease (due to increased clearance of aminophylline): phenobarbital, rifampicin, isoniazid, carbamazepine, sulfinpyrazones, phenytoin; intensity also decreases in smoking patients;
- an increase (due to a decrease in aminophylline clearance): antibiotics from the macrolide group, lincomycin, quinolones, allopurinol, beta-blockers, cimetidine, disulfiram, fluvoxamine, hormonal contraceptives for oral administration, isoprenaline, viloxazine; intensity also increases when used concurrently with influenza vaccination.
Other possible interactions:
- beta-blockers, lithium preparations: mutual decrease in action;
- sympathomimetics: mutual enhancement of action;
- enterosorbents, drugs with antidiarrheal action: decreased absorption of aminophylline;
- xanthine derivatives: mutual potentiation of hypokalemia due to the action of β 2 -adrenoreceptor stimulants, diuretics and corticosteroids;
- acid solutions: pharmaceutical incompatibility.
Analogs
Aminophylline analogs are:
- According to the active substance - Eufillin and Aminophyllin-Eskom;
- By the mechanism of action - Theobiolong, Theotard, Teopek, Theobromine, Diprofillin, Neo-Teofedrin.
Terms and conditions of storage
The drug in the form of a solution for injection is stored for 3 years at a temperature of 5-20 ° C, and tablets for 5 years at a temperature not exceeding 30 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Aminophylline
There are no reviews of Aminophylline, which is due to the lack of the drug in pharmacies.
Price for Aminophylline in pharmacies
The price of Aminophylline is unknown, since it is not available in pharmacy chains.
An analogue of the drug - Euphyllin, its cost is: tablets of 150 mg (in a package of 30 pcs.) - 11–21 rubles, solution for intramuscular administration of 24 mg / ml (in a package of 10 ampoules of 10 ml) - 41–52 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
