Theophylline

Chemical name

1,3-demetilxantin

Gross

C7-H8-N4-O2

Characteristics

The white crystalline powder, Low in cold water (1:180), easily in hot (1:85), soluble in acid and scheloch.

Of drugs

Drugs, the skin, bronhodilatirtee, protiwastmaticescoe, sossoudorasshiratee, cardiotonicescoe, dioreticescoe. Links adenozinove receptors. Lock also fosfodiesterzu, Zamf stabilizes and reduces the concentration of intracellular calcium. Relaxes smooth muscles of internal organs (bronchi, stomach and cervix), suppresses degranulatia fat cells and reduces the mediators allergies (serotonin, histamine, etc.) in the blood (противоаллергически�� effect). Increases tone respiratory muscles (intercostals muscles and diaphragm); Expanding light vessels and improves blood oksigenatiu; Agregatia inhibits platelets (ingibiruet factor activated platelets and Pgf_2alfa) increases resistance cells to deformation (improves the flow properties of blood), reduces tromboobrazovanie and normalizes microcirculation. Antianginalny effect (increase oxygen delivery to miocardu) due to increased coronary Arteri.posle intake of fully absorbed (bioavailability over 90%). C_max blood achieved within 2 hours (the usual form), and 6900 (Form prolongirovannaya). In the blood by 40 to 60% related to the protein. Penetrates through gistogematicalkie barriers. Treated biotransformation in the liver with the formation of active metabolites. Excreted in the kidneys (up to 13% of adults and 50% of children in an unmodified form); Partly out of breast milk.

Indications

Bronchial asthma, asthma status obstruguy bronchitis, emphysema lung patients in the newborn (aid).

Contraindications

Hypersensitivity, incl. and other derivative xantina (caffeine, pentoksifillin, theobromin), haemorrhagic stroke, bleeding in the retina eyes, acute myocardial infarction, arteriosclerosis expressed coronary arteries, bleeding in the recent history, pregnancy, breast-feeding (at the end of treatment).

Side-Effects

The concerns of consciousness, convulsions, the disorder, scotoma, migraine pain, arrhythmia, tachycardia, hypotension, laringit, pershenie throat, grippopodobnyy syndrome, zalojennosti nose, xerostomia, anorexia, nausea, vomiting, flatulence, increased cholecystitis, holetsaticeski hepatitis, increasing the concentration of liver enzymes (AST, ALT, alkaline phosphatase, LDG), atony bowel lakopenia, gipofibrinogenemia, pancitopenia, thrombocytopenia, allergic reactions.

Patient interaction

Zimetidin, allopurinol, ciclosporin A makrolidnye antibiotics, oral contraceptives and anti-serum, diet low in protein and high-carbohydrate-Cl reduce and increase the risk of adverse Temeny.fenobarbital, phenytoin, xantina, smoking-speed biotransformatia (inducyruut mikrosomaiona liver enzymes). Beta-adrenoblokatora reduce bronholiticescuu activity. Adsorbents, obwolakiwate means antatsida, oxidants slow induction and reducyruut C_max and oschelacivate substance-increase. Do effects dioretikov reduces - NPVS (of the derivatives pirazolona) beta-adrenoblokatorov, probenecida.

Overdosing

Symptoms : ajitation, sputannosti consciousness, convulsions, tachycardia, irregular and hypotension, nausea, diarrhoea, vomiting, with some blood giperglikemia, gipokaliemia, metabolic Azidoz.lechenie : appointment of activated carbon, irrigation bowel combination poliatilenglikola and salts; With a development nausea and vomit-metoclopramide or ondansetron (in / in), convulsions, benzodiazepines, phenobarbital (or sodium thiopental), and peripheral muscle; if necessary gemoperfuzia.

Precautions

Treatment retardnami forms is carried out periodic monitoring of the drug in the blood (not to exceed 20 µ g / ml).

Dosing and Administration

Inside, after eating adult (neretardnye form) 0.1-0.2 g 2-4 times a day. Higher single and daily doses of 0.4 and 1.2 grams, respectively. Children : 2 to 4 years 0,01-0,04 g 5-6 years 0,04-0,06 g 7-9 years 0,05-0,075 g, 10-14 years 0.05-0.1 g per reception.

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