Medication

Aminophylline

Structure

In 1 ml of an aminophylline solution for intravenous administration contains 24 mg of the same active substance.

There are also numerous forms of release in the form of an ointment or cream with aminophylline.

Release form

  • 5 ml of a solution of the drug in an ampoule, five ampoules in a blister pack, two or one packs in a pack of cardboard;
  • 5 ml of a solution of the drug in an ampoule, ten ampoules in a blister pack, two or one packs in a pack of cardboard;
  • 10 ml of a solution of the drug in an ampoule, five ampoules in a blister pack, two or one packs in a pack of cardboard;
  • 10 ml of a solution of the drug in an ampoule, ten ampoules in a blister pack, two or one packs in a pack of cardboard.

Pharmachologic effect

Vasodilating, diuretic, antispasmodic, bronchodilating.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Bronchodilator drug. Chemically - theophylline ethylenediamine salt. It has a bronchodilating effect due to the direct relaxing effect on the smooth muscle fibers of the respiratory tract and blood vessels. This is caused by selective suppression of activity. phosphodiesterase, which leads to an increase in intracellular content cAMP.

Reduces respiratory tract hyperreactivity through a mechanism that is still unknown. There is evidence that aminophylline increases the amount and activity T-suppressors in blood.

Is increasing mucociliary clearance, enhances the contraction of the diaphragm, stimulates the work of intercostal respiratory and muscles, activates the respiratory center, improves its sensitivity and enhances alveolar ventilation, which leads to a decrease in the severity and multiplicity of episodes apnea. By regulating respiratory function, it improves blood oxygen saturation and lowers the concentration of carbon dioxide. Stimulates lung ventilation in the background hypokalemia.

It has an activating effect on the work of the heart, increases the strength and heart rate, increases cardiac blood flow and increases the heart's oxygen demand. Reduces the tone of the vessels of the brain, skin, kidneys. Has peripheral venostasis act, reduces the resistance of the vessels of the lungs, reduces the pressure in the pulmonary circle of blood circulation. Stimulates renal blood flow, has a moderate diuretic effect. Expands bile ducts outside the liver.

Stabilizes mast cell walls, slows down the release of mediators of reactions hypersensitivity. It inhibits platelet adhesion, increases the stability of red blood cells, lowers thrombosis and regulates microcirculation.

Shows epileptogenic act in large doses.

Pharmacokinetics

In the human body, aminophylline is metabolized to release unbound theophylline.

Binding theophylline with plasma proteins is 40%. The drug crosses the placental barrier and is excreted in breast milk.

Theophylline transforms in the liver with the participation of a number of important enzymes cytochrome P450, the main one is isoenzyme CYP1A2. In the process of chemical transformations are formed 1-methyl uric acid, 1,3-dimethyl uric acid and 3-methylxanthine. These derivatives are excreted in the urine. In its original form, about 10% is excreted.

Significant individual features of the rate of hepatic transformation theophylline are the reason for the strong variability of clearance, plasma content, elimination half-life.

Half-life in non-smoking patients suffering from bronchial asthmareaches 12 hours, in smokers - 4 hours, in children it ranges from 1 to 5 hours, in newborns it can last up to two days.

Indications for use

  • Parenteral administration is used for: asthmatic status, apnea newborns, ischemic cerebrovascular accident, left ventricular failure (complicated with bronchospasm and respiratory distress), edema of renal origin, acute or chronic heart failure.
  • Oral administration is used for: bronchial obstructive syndrome diverse etiologies (e.g. bronchial asthma, pulmonary emphysema, COPD, obstructive bronchitis), pulmonary heartan increase in pressure in the pulmonary circle of blood circulation, sleep apnea, heart failure acute or chronic type.

Contraindications

Pronounced arterial hyper or hypotension, stomach ulcer or duodenum, tachyarrhythmiasevere liver or kidney damage, hyperacid gastritis, epilepsyretinal hemorrhage, hemorrhagic strokesharing with ephedrine in children, age up to 3 years, for extended oral forms, age limit up to 12 years, sensitization to aminophylline and theophylline.

Side effects

  • Reactions from CNS: sleep disorders, dizziness, tremor, anxiety, cramps.
  • Reactions from circulatory system: heart rhythm disturbances; with rapid intravenous administration - the occurrence of pain in the heart, a decrease in pressure, tachycardia, cardialgiaaggravation of the course angina pectoris.
  • Reactions from digestive systems: gastroesophageal reflux, nausea, vomiting, heartburn, diarrheaaggravation peptic ulcer, anorexia.
  • Reactions from genitourinary system: hematuria, albuminuria.
  • Allergic reactions: itching, rashfever.
  • Reactions from metabolism: hypoglycemia.
  • Local reactions: hyperemia, tightening, pain in the injection area.
  • Other reactions: tachypnea, chest pain, hot flashes, albuminuria, hypoglycemia, hematuriadaily gain diuresisincreased sweating.

Instructions for use of Aminophylline (Method and dosage)

The dosage regimen is often individual, developed depending on age, clinical presentation, indications, and nicotine addiction.

Perhaps intravenous or intramuscular administration. Adults are injected slowly intravenously - 240 mg once or twice a day. Children are administered intravenously or intramuscularly: up to 3 months of age - 30-60 mg, 4-12 months - 60-90 mg, 1-3 years old - 90-120 mg, 4-7 years old - 120-240 mg, 8-18 years - 240-480 mg per day in two to three injections.

Overdose

There are no reports of cases of overdose. If such a condition does occur, it is recommended to stop taking the drug and begin symptomatic therapy.

Interaction

When combined with sympathomimetic means mutual activation of pharmacological action occurs. With drugs lithium and beta blockers - the opposite is mutually weakened.

The intensity of the effect of aminophylline decreases with the simultaneous use of Rifampicin, Phenobarbital, Isoniazid, Sulfinpyrazone, Carbamazepine, Phenytoinas well as smokers.

The strength of aminophylline may increase while using Lincomicin, quinolones, macrolides, allopurinol, cimetidine, beta-blockers, isoprenaline, fluvoxamine, disulfiram, oral contraceptives, ATiloxazine and with influenza vaccination.

Derivatives xanthine potentiate hypokalemiacaused by action corticosteroids, beta-2 adrenergic agonists and diuretics.

Antidiarrheal drugs and enterosorbents lower the adsorption of aminophylline.

Terms of sale

On prescription.

Storage conditions

  • keep away from children;
  • store at temperatures up to 25 degrees.

Shelf life

Three years.

Special instructions

Use the drug with caution in severe forms coronary insufficiencywidespread atherosclerosisfrequent paroxysms ventricular extrasystolehypertrophic obstructive cardiomyopathy, cramps, stomach ulcer or duodenal ulcer or renal failurewith bleeding from the digestive tract, gastroesophageal reflux, hypothyroidism or thyrotoxicosiswith long hyperthermia, prostatic hypertrophy, in elderly people and children.

Analogs

Matches for ATX Level 4 code:AerofillinEufillinTheotardTheopecTheophyllineNeophylline

Aminophylline-Eskom, Eufillina pills, Eufillin-Darnitsa, Eufillin for injection.

For children

Children under 3 years of age (for extended oral forms for children under 12 years of age) are not allowed to take the drug. Do not use aminophylline rectally in children.

For weight loss

Aminophylline against cellulite is used very often. It enhances blood circulation in tissues, improves drainage function.

Here is just a short list of creams containing Aminophylline for cellulite: Turboslim, Reflexe Minceur (Lancome), Shape-up(Oriflame), Phyto-complexe (Sisley), Celluli-Zone (Biotherm), Draine minceur (Biotherm), Gel Silhouette Refining (Thalgo), Phyto-gel minceur (Sysley), Body lift (Lierac). Schemes for using Aminophylline cream depend on the manufacturer and composition.

During pregnancy and lactation

It is possible to use as prescribed by the doctor and the presence of strict indications.

Reviews about Aminophylline

Aminophylline solution is an old and proven remedy, whose effectiveness is beyond doubt, especially with seizures bronchial asthma.

Reviews for the cream with aminophylline are controversial. Some patients claim that the effect of the drug is absent, and some, on the contrary, share impressive results after using Aminophylline from cellulite. Reviews are characterized by a very large amplitude of ratings.

Aminophylline price, where to buy

Buy Aminophylline 10 ml No. 10 in Ukraine will cost 15-18 hryvnia. In Russia, the price of Aminophylline in ampoules of 10 ml No. 10 is 42-47 rubles. And the price of a cream with Aminophylline from cellulite or a similar ointment ranges from 280-400 rubles.

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