Neophyllinum

General characteristics. Structure:

1 tablet contains theophylline (in terms of 100% substance) - 100 mg or 300 mg;
excipients: lactoses monohydrate, talc, magnesium stearate, 30% dispersion of methacrylic acid-ethyl acrylate of a kopolimer (1:1), 30% dispersion ammonium methacrylate of a kopolimer, type A.

Pharmacological properties:

Pharmacodynamics. Theophylline - a natural compound, alkaloid. The mechanism of effect of theophylline is caused, preferential, by blocking of adenosine receptors, oppression of phosphodiesterases, increase in maintenance of intracellular tsAMF, decrease in intracellular concentration of calcium ions. Owing to what smooth muscles of bronchial tubes, digestive tract, biliary tract, a uterus, coronary, cerebral and pulmonary vessels relax, coronary arteries extend, peripheric vascular resistance decreases. Drug raises a tone of respiratory muscles (intercostal muscles and a diaphragm), reduces resistance of pulmonary vessels and improves blood oxygenation, activates a respiratory center of a myelencephalon, increases its sensitivity to carbon dioxide, improves alveolar ventilation that leads to decrease in weight and frequency of episodes of an apnoea. Theophylline eliminates a vasomotor spasm, raises a collateral blood stream and saturation of blood oxygen, reduces perifocal and general wet brain, reduces likvorny and, respectively, intracranial pressure. Improves rheological properties of blood, reduces a thrombogenesis, slows down aggregation of thrombocytes (oppressing a factor of activation of thrombocytes and F2alfa prostaglandin), normalizes microcirculation. Renders antiallergic effect, suppressing degranulation of mast cells and reducing the level of mediators of an allergy (serotonin, a histamine, leukotrienes). Strengthens a renal blood stream, has the diuretic effect caused by decrease in a canalicular reabsorption, increases removal of water, ions of chlorine, sodium, etc.
The effect of drug completely develops in 3-4 days from an initiation of treatment.

Pharmacokinetics. At intake theophylline is completely soaked up in digestive tract, bioavailability makes about 90%. At reception of theophylline in the form of tablets of the prolonged action the maximum concentration is reached in 6 hours. Linkng with proteins of a blood plasma makes: healthy adults have about 60%, patients with cirrhosis have 35%. Gets through gistogematichesky barriers, being distributed in fabric. About 90% of theophylline are metabolized in a liver with the participation of several isoenzymes of P450 cytochrome to inactive metabolites - 1,3-dimethyl uric acid, 1-methyl-uric acid and 3 methylxanthines. It is excreted generally by kidneys in the form of metabolites; in not changed look it is removed at adults to 13%, at children - to 50% of drug. It is partially allocated with breast milk. The elimination half-life of theophylline depends on age and existence of associated diseases and makes: adult patients with bronchial asthma have 6-12 hours, at children 6 months - are more senior 3-4 hours, the smoking persons have 4-5 hours, at elderly people and at heart failure, an abnormal liver function, a fluid lungs, chronic obstructive pulmonary diseases and bronchitis - more than 24 hours that demands the corresponding correction of an interval between administrations of drug.
Therapeutic concentration of theophylline in blood make: for achievement of broncholitic effect - 10-20 mkg/ml, for exciting effect on a respiratory center - 5-10 mkg/ml. Toxic concentration - it is higher than 20 mkg/ml.

Indications to use:

Bronchial asthma, the asthmatic status, chronic obstructive bronchitis and diseases of lungs with the bronkhoobstruktion phenomena, pulmonary hypertensia, night an apnoea.

Route of administration and doses:

The dose of drug is selected individually depending on disease severity, by body weights of the patient, age, features of metabolism at smokers.
At adults the initial dose usually makes 0,3 g of 1 times a day. In 3 days in the absence of serious side effects it is possible to increase a dose to supporting - 0,6 g (on 0,3 g 2 times a day), in case of preferential night and morning attacks - 0,6 g once in the evening.
At the smoking patients the initial dose makes 0,3 g of 1 times a day which at good tolerance is gradually increased by each 2 days by 0,3 g to supporting - 0,9-1,2 g (0,6 g in the evening, 0,3-0,6 g in the morning).
Persons with body weight have less than 60 kg: the daily dose makes 0,3 g (1 time a day or distributing a dose: 0,2 g in the evening, 0,1 g in the morning); at body weight less than 40 kg: the initial dose makes 0,2 g of 1 times a day, supporting - 0,4 g (on 0,2 g 2 times a day).
Children have 12-16 years (at the body weight of 40-60 kg): the initial dose makes 0,3 g of 1 times a day. In 3 days at good tolerance it is possible to increase a dose to supporting - 0,6 g (on 0,3 g 2 times a day).
Children have 6-12 years (at the body weight of 20-40 kg): the initial dose makes 0,2 g of 1 times a day. In 3 days at good tolerance it is possible to increase a dose to supporting - 0,4 g (on 0,2 g 2 times a day).
Children have 3-6 years (at body weight to 20 kg): the initial dose makes 0,1 g of 1 times a day. In 3 days at good tolerance it is possible to increase a dose to supporting - 0,2 g (on 0,1 g 2 times a day).

Features of use:

At a serious illness of cardiovascular system, a liver, a viral infection, elderly people should reduce and apply a dose of drug with care. At the smoking persons efficiency of drug can be lowered.

Side effects:

From the central nervous system: headache, dizziness, excitement, tremor, concern, sleeplessness, spasms.
From cardiovascular system: tachycardia, arrhythmia, lowering of arterial pressure.
From digestive tract: discomfort and pains in epigastric area, vomiting, heartburn, an exacerbation of cholecystitis, cholestatic hepatitis, increase in concentration of ALT, nuclear heating plant in blood.
Allergic reactions: skin rash, itch, grippopodobny syndrome, difficulty of nasal breath.

Interaction with other medicines:

At simultaneous use of drugs of theophylline to sympathomimetics and diuretic means there is mutual strengthening of their action; with β-adrenoblockers and drugs of lithium - their action mutually decreases. Pharmakoterapevtichesky effects of theophylline can decrease (owing to increase in its clearance by induction of microsomal enzymes of a liver) at simultaneous use with xanthines, carbamazepine, dipheninum, rifampicin, an isoniazid, terbutaliny. Allopyrinolum, Cimetidinum, изопреналин, cyclosporine A, makrolidny antibiotics (erythromycin, Oleandomycinum), lincomycin, oral contraceptives (estrogen) and anti-influenza serum increase risk of development of by-effects of theophylline (owing to reduction of its clearance) that causes need of correction of its dose. The risk of development of side effects of glucocorticoids, mineralokortikoid, anesthetics (the risk of developing of ventricular arrhythmias increases), the xanthines and means exciting the central nervous system (the neurotoxicity increases), ephedrine and efedrinsoderzhashchy drugs, beta-adrenergic agonists increases.

Contraindications:

Hypersensitivity to components of drug and derivatives of xanthine (caffeine, пентоксифиллин), epilepsy, a peptic ulcer of a stomach or duodenum in an aggravation stage, glaucoma, a concomitant use of Oleandomycinum or erythromycin, a hemorrhagic stroke, an eye retinal apoplexy, an acute myocardial infarction, the expressed atherosclerosis of coronary arteries, the previous internal bleeding, pregnancy, a lactation, children's age up to 3 years, heavy arterial hypertension, a tachyarrhythmia, a hypertrophic subaortic stenosis, a hyperthyroidism.

Overdose:

Symptoms at adults: spasms, fervescence, disturbances of cordial activity (tachycardia, ventricular arrhythmias, hypotension).
Symptoms at children: hyperexcitability, disturbances of mentality, fervescence, nausea, spasms, tachycardia, hypotension, диспноэ.
Treatment. Termination of administration of drug, gastric lavage, irrigation of intestines combination of polyethyleneglycol and salts, reception of absorbent carbon, stimulation of removal of theophylline from an organism (artificial diuresis, hemosorption, plazmosorbtion, hemodialysis, peritoneal dialysis) and purpose of symptomatic means: at the expressed nausea and vomiting - Metoclopramidum or ондансетрон, at spasms - diazepam.

Storage conditions:

To store in original packaging at a temperature no more than 25 °C. To store in the place, unavailable to children.
Period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging; on 5 blister strip packagings in a pack.