TEOFILLIN (Theophyllinum). 1, 3-Dimetilksantin.

     Synonyms : Aqualin, Asmafil, Lanophyllin, Optiphyllin, Oralphyllin, Teolix, Theocin, Theofin and others.

     Alkaloid contained in the tea leaves and coffee. There is also a synthetic way.

     The white crystalline powder. Malorastvorim in cold water (1 : 180), easy-to hot (1 : 85), soluble in acid and alkali.

     Theophylline affect various body functions. He has a catalytic effect on the central nervous system, but expressed less than caffeine; Increases Oxytocics of attack. Several expands peripheral, coronary and renal vessels, providing moderate diureticheskoe act ingibiruet aggregation of platelets, inhibits the release of fat cells mediators allergies. Particularly important is the ability to provide teofillina bronhorasshiryayuschy effect.

     In teofillina mechanism of action (as well as other metilksantinov) play a role inhibition fosfodiesterazy and accumulation in the tissues of cyclic 3 ', 5'- adenozinmonofosfata (tsAMF). Among metilksantinov Theophylline is one of the most powerful inhibitors fosfodiesterazy.

     The accumulation in the cells tsAMF slowing connection with miozina aktinom that reduces Oxytocics activity smooth muscles and promotes, among other things, to relax bronchial and lifting bronhiolospazma.

     To relax muscles has the ability to oppress teofillina transport calcium ions through "slow" channels of cellular membranes (See Antagonisty calcium ions.) .

     Of particular importance to the molecular mechanism of action teofillina has recently identified its ability to block adenozinovye (purinovye) receptors.

     Adenosine is an endogenous purinovym nukleozidom, derivative adenina treated as a natural ligand, with specific svyazyvayuschiysya adenozinovymi (purinovymi) receptors located in the peripheral organs, heart muscle, bronchus, in the central nervous system (See also Caffeine, Heart glycosides.) . Currently, there are various subgroups adenozinovyh receptors (A 1 A 2, etc.).

     Enlisting adenozinovyh muscle receptors is bronhiolospazm bronchi. It was found that adenosine and its analogues are strong bronhokonstriktorami in bronchial asthma.

     Theophylline, caffeine and other relatives of metilksantiny serve as exogenous ligands adenozinovyh receptors and blocking of adenosine. This is facilitated by structural relatedness of adenosine and metilksantinov.

     I think that this biochemical mechanism (molecular) is mainly due to bronhorelaksiruyuschee teofillina.

     It is also possible that Theophylline inhibits release of endogenous adenosine.

     The central catalytic effect caffeine, and other teofillina metilksantinov be explained by the fact that adenosine has phosphabenzide effect on synaptic transmission in the central nervous system, a central adenozinovye metilksantiny blocking receptors.

     Theophylline in "Clean" as used currently limited. The preparation of rapidly absorbed. Peak concentrations in plasma observation is about 2 h after administration of the interior, but it relatively quickly, with different rates for different patients metabolized in the liver with the formation of inactive metabolites.

     A urine unchanged for around 10% of the interior of the drug. The effectiveness and duration of the drugs vary for different patients.

     Basically Theophylline used as a bronchodilatory and as a moderate force kardiotonicheskoe and diureticheskoe means stagnation in the heart and renal origin.

     Sometimes nominated along with other inflammatory and Bronchiodialator drugs.

     Is the inside of 0.1 - 0.2 g (adults), 2 to 4 times a day after meals. The best effect is often observed in the employment preparation in the form of rectum candles, as Theophylline least be in the way of metabolism in the liver. Rectally introduce adults and 1 candle 1 - 2 times a day.

     Length of teofillina depends on the nature of the disease and provided a therapeutic effect.

     Children 2 to 4 years 0,01 - 0,04 designate g, 5-to 6 - 0.04-0.06 g, 7-9-0.05 - 0.075 g, 10 - 14-0, 05-0.1 g per reception. Children under the age of 2 years is not appointed.

     Higher doses for adults inside and rectally : single 0.4 g daily 1, 2 grams.

     In some cases, there are side effects : indigestion, nausea, vomiting, diarrhea, headache. When using candles burning in a sense perhaps rectum. When bad endurance drug overturned.

     In teofillina overdose may arise epileptoidnye seizures. To prevent such side effects is not recommended Theophylline long.

     Theophylline and products containing it can not receive in individual intolerances, hyperthyroidism, severe heart attack, subaortalnom stenoses, arrythmia, epilepsy and other conditions of convulsions, pregnancy. Caution should be observed in stomach ulcer and duodenal ulcer. Furthermore, it should be borne in mind that drugs cause "induction" liver enzymes (barbiturates, etc.; Phenobarbital, Benzonal), reduce its concentration in the blood. For smokers, in patients with liver cirrhosis, with congestive heart failure, for teofillina increased. Furosemide, tsimetidin, verapamil, propranolol (Inderal), Lincomycin, antibiotics, macrolides (see), Fluoroquinolones (see), hormonal contraceptives reduce elimination teofillina increase its concentration in the blood and may increase its side effects.

     Method of issuance : powder; Candles 0.2 g (Suppositoria cum T h eor hyllino 0.2).

     Storage : List B. The well ukuporennoy packaging keeps from the world.

     Theophylline is a fundamental part eufillina (see). Included in some combined pills (Teofedrin etc.). Sometimes prepare ex tempore combination with teofillina dimedrol, ephedrine, and other inflammatory drugs. Recently there have been combined with modern Theophylline bronhorasshiryayuschimi drugs. Thus, the drug "Teo- Asthalin (T h eo- A sthalin, India), a 1 pill, and 0.1 g teofillina 0,002 (2 mg) one (see), and" Teo- Asthalin forte "- respectively 0.2 teofillina grams and 0,004 grams (4 mg) declaration.

     R p. : T h h eor from 0.1 llini

     Dimedroli 0,025

     M.f. p ulv.

     D.t.d. N 20

     S. On January powder 2 - 3 times a day (at tomography)

     R p. : Supp. with um T heophyllino 0.2 N. 10

     D.S. On one candle 2 times a day (at stagnation cardiac origin)

     Pills "Teofedrin (Ta bulettae" T h e drinum eor h) contain 0.05 grams teofillina, teobromina and caffeine; On 0.2 g amidopirina and fenatsetina; 0.02 grams of ephedrine hydrochloride and phenobarbital, 0,004 g herb extract thick and 0 , 0001 g tsitizina.

     Applied as a treatment and preventative tool in bronchial asthma. Adults appoint one pill (with strong attacks two tablets) one time (and, if necessary 2 - 3 times) a day; Children between 2 and 5 years for the 1 / 4 to 1 / 2 tablets, from 6 to 12 years - 1 / 2 - 3 / 4 pills. In order to sleep at night, teofedrin should take the morning or afternoon.

     Contraindications : glaucoma, a violation of coronary circulation, Ray.

     Storage : List B.

     Note. 1. Due to the limited number of amidopirina (see) can release tablets teofedrina without one of the drugs. It bronchodilatory effect has not changed. 2. In terms of composition and actions "Teofedrin" close to the foreign drug "Antastman" (A ntasthman); No currently wide application.

     Recently developed drugs are being Theophile am acting with the benefits of "clean" fillinom theories. Teofillina slow release of these products ensures its smooth flow in the current blood (with ingestion), a slow increase in plasma concentrations and longer productive effect (up to 12 hours or more), better portability. Because of the long lead perf was an important indication for the use of a warning night and pre bronhiolospazma phenomena.

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