Aminophylline

Chemical name

3,7-Дигидро-1,3-диметил-1��-пурин-2,6-дион 1,2-etandiamin (2:1)

Gross

C16-H24-N10-O4

Characteristics

It is a mixture of 80% theofillina (1,3-demetilxantin), and 20% etilendiamina (1,2-etilendiamin). White or white with a yellow-brown crystalline powder with weak smell ammonia. Rat in the water, aqueous solutions have pH 9,0-9,7.

Of drugs

The drugs-bronhodilatirtee, tokoliticescoe, dioreticescoe, skin. Ingibiruet fosfodiesterzu and stabilizes Zamf reduces intrazellliarnogo concentration of calcium. In addition, the blocks adenozinove receptors suppresses the effects of GHGs in the smooth muscle, reduces emissions and gistamina lakotrienov of fat Kletok.bystro drawn from the blood after oral introduction. Food reduces the absorption without affecting the value (large volumes of liquid and protein Speeds). This also depends on the dosage aminofillina : the higher the dose adopted, the lower the rate of removals. The blood plasma protein binds to 60% (healthy adults), in newborn children, the figure is 36% and in patients with cirrhosis of the liver, approximately 35%. The distribution is in the range of injection l / kg (30-70% of the ideal body mass index), average 0.45 l / kg C_max is depending on the drug forms in 1-2 hours for ordinary through 4-7 h for extended forms and five hours for pills kishechnorastvorimam surface. In the liver, with the participation of zitohroma P450 part, into caffeine. Children up to three years T_1/2 caffeine longer than in adults, and the concentration can be up to 30% of one-aminofillina. Children over three years and in adults phenomenon cumulation caffeine is not available. T_1/2 drug depends on the age, as well as the availability of opportunistic diseases, ranging from infants and children up to six months, more than 24 hours; For children older than 6 months, 3.7 hours; Adults without asthma 8.7 hours; Smokers (40 cigarettes a day), 4-5 hrs (and, after stopping smoking farmakokinetika aminofillina returned to the category of patients in 3-4 months). The adults with COPD lung disease, heart disease and heart failure T_1/2 exceed 24 hours Provided news, including 10% of the adults and 50% of children in destination Vide.aminofillin relaxation of smooth muscles bronchi, coronary, cerebral and pulmonary pressure, stomach, a pun; increases airway skeletal muscles (including breathing). Increased pressure kidney clubockov by filtration rate and the increase in diureza. Activates breathing centre oblong brain increases sensitivity to carbon dioxide and improves alveoljarnuu ventilation, which ultimately led to a decline in severity and frequency of episodes of apnoea. Suppress rhythm of the pregnant uterus; Ingibiruet agregatia platelets; Increases acidity gastric juice. When used in high doses has противоэпилептически м �ействием.Бронходилат ирующие aminofillina properties are when its concentration in the blood of 10 to 20 µ g / J The concentration of more than 20 mg / ml was toxic. Exciting effect on the respiratory center implemented with a lower content of the drug in the blood, 5-10 µ g / Ml.iz-za not biotransformaih activity of the enzyme liver (and the rules) in newborns and persons over 55 years of age shall aminofillin with caution.

Indications

Obstruguy chronic bronchitis, bronchial asthma (drug of choice in patients with asthma physical stress, and as an additional means to other forms), asthma status (additional therapy), emphysema lung patients newborns (a condition characterized by periods of breathing for 15 seconds, followed cianosis and bradikardiei), breathing Chein-Stokes.

Contraindications

Hypersensitivity, adults, arterial hypertension, heart disease, myocardial infarction, heart failure, acute and chronic (acute phase), gastritis, saying disease stomach and duodenal ulcers, prostate adenoma cancer, diarrhoea, kistosno-fibrosnaya mastopatia, alcoholism, heart lung, fever, gipoksemia, respiratory infections, disruption of the liver, gipertireoidizm, chronic and acute renal failure, otechny syndrome, gipernatriemia, rectal diseases, breast-feeding (at the time of treatment needs to be reversed).

Side-Effects

Gastro-ezofagealny reflux (heartburn, vomiting), the pain in the chest, palpitations, hypotension, dizziness, tahipnoe, tidal sense to a person, headache, allergic reactions (sweating, fever), the reaction on the ground of (soil compaction, hyperemia, pain).

Patient interaction

It increases the likelihood of the side effects of glucocorticoids, mineralokortikoidov (gipernatriemia), of narcosis (increased risk of arrhythmias jeludockovh) xantinov and means of central nervous system stimulants (increases neurotoxicity), beta-adrainomimetikov. Decreases specific activity lithium salts. Oral contraceptives (estrogensoderjaschie) antidiareynye preparations intestinal sorbents weaken and H_2-gistaminoblokatora, ftorhinolona, BAC, beta-adrenoblokatora, mexiletin, erythromycin increase Effects (associated with the enzyme zitohroma P450 and slow biotransformatia aminofillina).

Overdosing

Symptoms : anorexia, diarrhoea, nausea, vomiting, pain in epigastralna area jeludern-kisherne bleeding tahipnoe, hyperemia person tachycardia, jeludockove adults, insomnia, anxiety, refers, Generalized Sudorogi.lechenie includes lifting drug stimulation of diversion from the body (flush stomach, big diurez, gemosorbece, plazmosorbece, Hepatology, peritonealny dialysis), and the appointment of symptomatic funds.

Dosing and Administration

Obstructive lung diseases. The acute phase of adults : initial dose of 5-6 mg / kg (with the further increase drug dosages for every 0.5 mg / kg was increased aminofillina concentration in the blood of 1 µ g / ml); It should be borne in mind that aminofillina concentration in the serum must not exceed 20 µ g / ml (possibly the side effects); supporting dose for smokers 4 mg / kg every 6 h; for non-smokers, and patients with liver disease, 2 mg / kg every 8 hours; children initial dose-5-6 mg / kg supporting (in mg / kg), calculated by the formula : children under 6 months-0.07 x age in weeks + 1.7 every 8 hours, children of 6 months to 1 year, 0.05 x age in weeks +1.25 every six hours, from 1 to 9 years old, 5 mg / kg every 6 h, from 9 to 12 years, 4 mg / kg every 6 h, from 12 to 16 to 3 mg / kg every 6 C.vne worsening adults initial dose of 6-8 mg / kg / day (maximum 400 mg / day) divided by the reception 3-4; with good endurance may further increase dose by 25% every 2-3 days to a maximum of 13 mg / kg / day (900 mg / kg / day); children : initial dose of 16 mg / kg / day (maximum 400 mg / day) divided by the reception 3-4; with good endurance may increase dose by 25% every 2-3 days to a maximum daily, which amounts to age 1 year - 0.3 x age in weeks + 8.0, from 1 to 9 years old-22 mg / kg, from 9 to 12 years, 20 mg / kg, from 12 to 16 - 18 mg / kg, above the age of 16-13 mg / Kg.pri patients newborn initial dose of 5 mg / kg (introduced on nazogastralnomu DigiTrak), which supports the dose to 2 mg / kg, 2 reception. The course of treatment lasts for a few weeks, in rare cases, months.

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