Fenoterol-nativ

General characteristics. Structure:

Active ingredient: 1 mg of Fenoterolum of hydrobromide.

Excipients: Natrium benzoicum, dinatrium of an edetat a dihydrate (corresponds dinatrium to an edetat), citric acid monohydrate (corresponds to citric acid anhydrous), water for injections.

Pharmacological properties:

Pharmacodynamics. Fenoterol-nativ is effective broncholitic remedy for the prevention and stopping of attacks of a bronchospasm at the bronchial asthma and other diseases which are followed by reversible obstruction of respiratory tracts, such as a chronic obstructive pulmonary disease, chronic bronchitis, emphysema of lungs.

Fenoterolum - the selection stimulator β2-адренорецепторов. At use of drug in higher doses there is a stimulation β1-адренорецепторов (for example, at appointment for tokolitichesky therapy). The mechanism of action is connected with activation of adenylatecyclase through stimulyatorny GS protein with the subsequent increase in formation of cyclic adenosinemonophosphate (tsAMF) which activates a protein kinase And, the last deprives a myosin of ability to connect to actin that interferes with reduction of smooth muscles and promotes broncholitic action and elimination of a bronchospasm.

Besides, Fenoterolum inhibits release from mast cells of mediators of an inflammation, thereby having protective action from influence of such bronchoconstrictors as a histamine, metasincaline, cold air and allergens. Reception of Fenoterolum in doses of 0,6 mg increases activity of a ciliary epithelium of bronchial tubes and accelerates mukotsiliarny transport.

Due to the stimulating influence on β-adrenoceptors, Fenoterolum can have effect on a myocardium (especially in the doses exceeding therapeutic), causing increase and strengthening of cordial reductions.

Fenoterolum warns and quickly stops a bronchospasm of various genesis. The beginning of action after inhalation - in 5 min., at most - 30 - 90 min., action duration - 3 - 5 hour.
 
Pharmacokinetics. Absorption. 10-30% of the active agent released from aerosol drug after inhalation reach the lower respiratory tracts depending on a method of inhalation and the used inhalation system, and other part is deposited in upper respiratory tracts and swallowed. As a result a quantity of the inhalated Fenoterolum gets into digestive tract. After inhalation of one dose of drug extent of absorption makes 17% of the entered dose. Absorption has two-phase character - 30% of Fenoterolum of hydrobromide are quickly soaked up with an elimination half-life of 11 min., and 70% are soaked up slowly with an elimination half-life of 120 min. There is no correlation between the concentration of Fenoterolum in a blood plasma reached after inhalation and a pharmakodinamichesky curve "time - effect". Long (3-5 hour) the bronchodilatory effect of drug after inhalation, comparable with the corresponding effect reached after intravenous administration is not supported by high concentration of active agent in a system blood-groove.

Distribution. Linkng with proteins of plasma - 40-55%. In not changed look Fenoterolum can get through a placental barrier and get to breast milk.

Metabolism. At a proglatyvaniye active substance is exposed to biotransformation owing to effect of "primary passing" through a liver. It is metabolized in a liver. Thus, the swallowed amount of drug does not exert impact on the concentration of active agent in a blood plasma reached after inhalation. Fenoterolum biotransformation at the person proceeds only by conjugation with sulfates preferential in an intestines wall.

Removal. It is removed by kidneys and with bile in the form of inactive sulphatic conjugates. Allocation of Fenoterolum with urine (0,27 l/min) corresponds to about 15% of average general clearance systemically of an available dose. The volume of renal clearance demonstrates tubular secretion of Fenoterolum in addition to glomerular filtering.

Indications to use:

• attacks of bronchial asthma or other states with reversible obstruction of respiratory tracts, such, as, a chronic obstructive pulmonary disease, obstructive bronchitis, emphysema of lungs;
• prevention of attacks of bronchial asthma owing to physical tension;
• as bronchodilatory means before inhalation of other medicines (antibiotics, mucolytic means, glucocorticosteroids);
• carrying out bronkhodilatatsionny tests at a research of function of external respiration.

Route of administration and doses:

The drug "Fenoterol-nativ" is intended only for inhalation introduction. 20 drops = 1 ml. 1 drop = 50 mkg of Fenoterolum of hydrobromide.

Doses should be selected according to individual needs of the patient; besides, during treatment of the patient has to be under observation of the doctor. The attacks of bronchial asthma and other states which are followed by reversible obstruction of respiratory tracts. It is inhalation.
• 0,5 ml (10 drops = 0,5 mg of Fenoterolum of hydrobromide) in most cases are enough for immediate stopping of an attack;
• in need of repeated purpose of drug inhalate on 0,5 ml (10 drops = 0,5 mg of Fenoterolum of hydrobromide) to 4 times a day, however reduction of an individual dose depending on efficiency of treatment is possible;
• in hard cases if the dose of 1 ml (20 drops) is inefficient, higher doses from 1 to 1,25 ml can be required (20 - 25 drops = 1 - 1,25 mg of Fenoterolum of hydrobromide);
• in exclusively hard cases if the dose to 2,0 ml (40 drops) is inefficient, inhalate under observation of the doctor 2 ml (40 drops = 2 mg of Fenoterolum of hydrobromide).

Prevention of attacks of bronchial asthma owing to physical tension. It is inhalation.
• 0,5 ml (10 drops = 0,5 mg of Fenoterolum of hydrobromide) to an exercise stress. Treatment is begun, as a rule, with the smallest recommended dose. The recommended dose is parted by 0,9% with chloride sodium solution up to the final volume of 3 - 4 ml, spray and inhalate before full consumption of the received cultivation.

Fenoterol-nativ it is impossible to part with the distilled water. Solution part every time again before use; the remains of divorced solution pour out. Fenoterol-nativ it is recommended to apply with use of the inhalation device - the nebulizer. In the presence of the oxygen and respiratory equipment solution is the best of all to inhalate 6 - 8 l/min at a flow rate.

Fenoterol-nativ it is possible to inhalate along with well-cared and mucolytic
means. It concerns, first of all, drugs an ipratropiya bromide and Ambroxol in the form of solutions for inhalation.

Features of use:

Use at pregnancy and during breastfeeding. Negative influence of drug on the course of pregnancy was not revealed. Nevertheless, to pregnant women (especially in the first trimester) drug is appointed only in those cases if the potential advantage for mother exceeds potential risk for a fruit. It is necessary to consider a possibility of the inhibiting effect of Fenoterolum on a sokratitelny uterine activity.

Fenoterolum gets into breast milk. Safety of use of drug in the period of a lactation is not studied. Use of drug during a lactation is possible only in cases when the potential advantage for mother exceeds potential risk for the child.

Other sympathomimetic bronchodilators can be applied along with Fenoterolom-nativ only under observation of the doctor. At the acute, quickly amplifying asthma (the complicated breath) it is necessary to see a doctor immediately. At prolonged use of drug:
• stopping of attacks of bronchial asthma can be more preferable
regular use of drug (symptomatic treatment);
• it is necessary to conduct regular examination of patients for detection of need of additional or more intensive antiinflammatory treatment (for example, inhalations of glucocorticosteroids) for the purpose of control of an inflammation of respiratory tracts and the prevention of long exacerbations of bronchial asthma.

In case of strengthening of obstruction of bronchial tubes it is considered unacceptable and there can be even risky an increase in frequency rate of reception β2-агонистов, contained in such drugs as Fenoterol-nativ, over the recommended doses. In such situation it is necessary to reconsider treatment planning and, especially, adequacy of antiinflammatory therapy.

At treatment β2-агонистами development of the expressed hypopotassemia is possible. Extra care should be shown at heavy bronchial asthma as this effect can be strengthened by the accompanying use of derivatives of xanthine, glucocorticosteroids and diuretics. At a hypoxia strengthening of influence of a hypopotassemia on a cordial rhythm is possible. In such situations it is recommended to carry out regular control of potassium concentration in blood serum.

The myocardium ischemia connected with β2-агонистами was in rare instances observed.

Use of Fenoterolum for patients with a hypopotassemia who receive cordial glycosides can cause arrhythmia.

At patients with a diabetes mellitus during treatment it is necessary to carry out regular control of content of glucose in plasma.

Drug contains the dinatrium stabilizer эдетат which can cause a bronchospasm in some patients.

Use of Fenoterolum can lead to positive takes of tests for abuse of psychoactive drugs on not medical indications, and also on dope at athletes.

Influence on ability to driving and other vehicles, for work with moving mechanisms. Researches on studying of influence of drug on ability to driving of motor transport and control of mechanisms were not conducted. In case of development of side effects at use of drug it is necessary to refrain from driving of motor transport and control of mechanisms.

Side effects:

Determination of frequency: very often (> 1/10), it is frequent (from 1/100 to 1/10), infrequently (from 1/1000 to 1/100), is rare (from 1/10000 to 1/1000), is very rare (<1/10000).

From a nervous system: very often - nervousness, uneasiness, a tremor, a headache, dizziness; very seldom - excitement.

From cardiovascular system: often - tachycardia, a heart consciousness; very seldom - arrhythmia, increase in systolic pressure of blood, decrease in diastolic pressure of blood, myocardium ischemia.

From metabolism and food: often - a hypopotassemia, a hyperglycemia.

From respiratory system: infrequently - cough, irritation of a throat and throat; seldom - a paradoxical bronchospasm.

From the alimentary system: infrequently - nausea, vomiting.

Skin and hypodermic cellulose: infrequently - allergic skin reactions, such as rash, an itch, urticaria; seldom – a hyperhidrosis.

Musculoskeletal system and related diseases of fabrics: infrequently - muscular weakness, a spasm of muscles, a mialgiya.

From immune system: seldom - hypersensitivity.

Interaction with other medicines:

Glucocorticosteroids, anticholinergics, ksantinovy derivatives (for example, theophylline), kromoglitsiyevy acid can strengthen action of Fenoterolum.

β-adrenergic means, glucocorticosteroids and diuretics can strengthen side effects of Fenoterolum.

Perhaps considerable decrease in bronchodilatory action of Fenoterola-nativ at co-administration of β-adrenoblockers..........

It is necessary to appoint with care β-agonists to the patients receiving inhibitors of a monoaminooxidase or tricyclic antidepressants as these drugs are capable to strengthen action of Fenoterolum.

Inhalations of the halogenated hydrocarbon anesthetics (a halothane, trichloroethylene, энфлуран) can strengthen action of Fenoterolum on cardiovascular system. The halothane promotes development of arrhythmia.

Co-administration of bronchial spasmolytics with the similar mechanism of action results in the additive effect and the phenomena of overdose.

Contraindications:

- hypersensitivity to Fenoterolum or any component of drug;
- hypertrophic subaortic stenosis;
- tachyarrhythmia;
- age up to 18 years.
 
With care a hyperthyroidism, arterial hypotension, arterial hypertension, an intestines atony, a hypopotassemia, a diabetes mellitus, recently postponed myocardial infarction (within the last 3 months), a heart disease, vessels, such as chronic heart failure, coronary heart disease, diseases of coronary arteries, heart diseases (including an aortal stenosis), the expressed damages of cerebral and peripheral arteries, a pheochromocytoma, glaucoma.

Overdose:

Symptoms: tachycardia, the strengthened heartbeat, decrease or increase in arterial pressure, increase in pulse pressure, pain behind a breast, arrhythmias, feeling of rushes of blood to the person, a tremor, a metabolic acidosis, a headache, dizziness, concern, excitement, a hypopotassemia.

Treatment: sedatives, tranquilizers, in hard cases carry out intensive symptomatic care. As specific antidotes it is possible to appoint β-adrenoblockers ((((((((((preferably the selection β1-адреноблокаторы); it is necessary to consider a possibility of strengthening of obstruction of bronchial tubes and to carefully select doses of these drugs at the patients having bronchial asthma.

Storage conditions:

In the place protected from light, at a temperature not above 25 °C. Not to freeze. To store in the place, unavailable to children. A period of validity - 3 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for inhalations of 1 mg/ml. On 20 ml of drug in bottles of dark glass with a polyethylene dropper and the screwing-up polypropylene cover or a polyethylene cover. On 1 bottle with the application instruction place in a cardboard pack.