Salbutamol-MCPA - instructions for use, dose, side effects, contraindications

active substance: salbutamol sulfate micronized (in terms of 100% anhydrous substance) - 0.030125 g (equivalent to 0.025 grams of salbutamol) / 120.5 μg (equivalent to 100 μg of salbutamol);

Excipients: rectified ethyl alcohol * 0.340 g / 1.36 mg, propellant HFC-134 a (1,1,1,2-tetrafluoroethane) -

14.630 g / 58.52 mg.

* Volume fraction of ethyl alcohol - not less than 96.3%.

Description:The preparation is a white or almost white suspension, which is under pressure in an aluminum monoblock tank with a metering valve, equipped with a nozzle-inhaler with a protective cap; The drug is sprayed out of the balloon as an aerosol spray.

Pharmacotherapeutic group:Bronchodilator - β-2-adrenomimetic is selective.

ATX: & nbsp

R.03.A.C Selective beta-2-adrenomimetics

R.03.A.C.02 Salbutamol

Pharmacodynamics:Salbutamol is a selective β 2 -adrenoreceptor agonist. In therapeutic doses, it acts on β2-adrenergic receptors of the smooth muscles of the bronchi, with little or no effect on myocardial β1 receptors.Has a pronounced bronchodilator effect, preventing or reducing spasm of the bronchi, reduces resistance in the airways. Increases the vital capacity of the lungs. Increases mucociliary clearance (with chronic bronchitis to 36%), stimulates the secretion of mucus, activates the functions of ciliated epithelium.

In recommended therapeutic doses does not have a negative effect on the cardiovascular system, does not cause an increase in blood pressure. To a lesser degree, in comparison with the drugs of this group, it has a positive chrono- and inotropic effect. Causes the enlargement of the coronary arteries. It has a number of metabolic effects: it reduces the concentration of potassium in the plasma, affects glycogenolysis and insulin secretion, has hyperglycemic (especially in patients with bronchial asthma) and a lipolytic effect, increasing the risk of acidosis.

After the application of inhalation forms, the effect develops rapidly, the onset of the effect is 5 minutes, the maximum after 30-90 minutes (75% of the maximum effect is achieved within 5 minutes), the duration is 4-6 hours.

Pharmacokinetics:

After inhalation, 10-20% of the dose of salbutamol reaches the lower respiratory tract. The rest of the dose remains in the inhaler or is deposited in the oropharynx and then swallowed. The fraction deposited in the respiratory tract is absorbed into the lung tissue and blood, but not metabolized in the lungs.

The degree of binding of salbutamol with plasma proteins is about 10%.

Once in the blood, salbutamol metabolized in the liver and excreted mainly with urine in unchanged form and in the form of phenolic sulfate. The swallowed portion of the inhalation dose is absorbed from the gastrointestinal tract and is subjected to active metabolism during "first passage through the liver", turning into phenolic sulfate. Unchanged salbutamol and the conjugate is excreted mainly in the urine.

Introduced intravenously salbutamol has a half-life of 4-6 hours. It is excreted by the kidneys partly in unmodified form and partly as an inactive metabolite of 4'-O-sulfate (phenolic sulfate). With feces only a small part of the administered dose of salbutamol is excreted. Most of the dose of salbutamol administered intravenously, orally or by inhalation is excreted within 72 hours.

Indications:

1. Bronchial asthma:

- relief of attacks of bronchial asthma, including with exacerbation of severe bronchial asthma;

- prevention of attacks of bronchospasm associated with exposure to an allergen or caused by physical exertion;

- application as one of the components with prolonged maintenance therapy of bronchial asthma.

2. Chronic obstructive pulmonary disease (COPD), accompanied by reversible airway obstruction, chronic bronchitis.

Contraindications:

- Hypersensitivity to any component of the drug.

- Management of preterm labor.

- Threatening abortion.

- Children up to 2 years.

- Pregnancy

Carefully:Be wary of medication if patients have a history of tachyarrhythmia, myocarditis, valvular heart disease, aortic stenosis, coronary heart disease, severe chronic heart failure, hypertension, hyperthyroidism, pheochromocytoma, decompensated diabetes, glaucoma, epipripadki, renal or hepatic failure, simultaneous reception of non-selective β-adrenoblockers, lactation period.

Pregnancy and lactation:

Contraindicated during pregnancy.

During lactation, it is prescribed only in cases where the expected benefit to the mother exceeds any possible risk to the child.

Dosing and Administration:

Salbutamol-MHPP aerosol for inhalations dosed with 100 mcg / dose is intended only for inhalation.

Solve the issue of increasing the dose or frequency of the drug can only be a doctor.

It is not recommended to use the drug more than 4 times a day. The need for frequent use of maximum doses of the drug or in a sudden increase in dose indicates a worsening of the course of the disease.

Adults and children over 12 years.

Causing an attack of bronchospasm: the recommended dose is 100-200 mcg (1-2 inhalations).

Prevention of attacks of bronchospasm associated with exposure to allergens or caused by physical exertion: the recommended dose is 200 mcg (2 inhalations) for 10-15 minutes before the effect of the provoking factor.

Long-term maintenance therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

The maximum daily dose: 1200 mcg (12 inhalations).

Children up to 12 years.

Causing an attack of bronchospasm: the recommended dose is 100-200 mcg (1-2 inhalations).

Prevention of attacks of bronchospasm associated with exposure to an allergen or caused by physical exertion: the recommended dose is 100-200 μg (1-2 inhalations) for 10-15 minutes before the impact of the provoking factor.

Long-term maintenance therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

The maximum daily dose: 800 mcg (8 inhalations).

Application rules:

Preparation for first use:

Before the first use of the drug should: put on the balloon and the valve stem nozzle-inhaler, equipped with a protective cap, remove the protective cap from the nozzle-inhaler. Then vigorously shake the balloon with vertical movements, turn the balloon with the inhaler downward and make two sprays into the air to make sure the valve works adequately. If the product is interrupted for several days, one spray should be made into the air after a thorough shaking of the balloon.

Application:

1. Remove the protective cap from the nozzle-inhaler. Make sure the inner and outer surfaces of the nozzle-inhaler are clean.

2. Vigorously shake the balloon with vertical movements.

3. Turn the balloon with the inhaler downward, hold the balloon vertically between the thumb and the middle and index fingers so that the thumb is under the inhaler.

4. Make the deepest exhalation, then put the inhaler in the mouth between your teeth and grasp it with your lips, without biting at the same time.

5. Starting the inspiration through the mouth, press on the top of the balloon to produce a dose of the drug, while continuing to slowly and deeply inhale.

6. Hold your breath, remove the inhaler from your mouth and lift your finger from the top of the bottle. Continue to hold your breath as much as possible.

7. If you need to perform the next inhalation, you should wait about 30 seconds, keeping the balloon upright. After this, perform inhalation in accordance with the instructions in paragraphs 2-6.

Close the nozzle-inhaler with a protective cap. IMPORTANT:

Perform actions in accordance with paragraphs 4, 5 and 6, slowly. It is important to start inhaling as soon as possible before giving out the dose. The first few times should be practiced in front of the mirror. If there is a "cloud" on each side of the mouth, start again with step 2.

Cleaning:

The nozzle-inhaler should be cleaned at least once a week.

1. Remove the protective cap from the nozzle-inhaler, and remove the nozzle-inhaler from the balloon.

2. Thoroughly flush the nozzle-inhaler and the protective cap under the warm flow-

3. Carefully dry the nozzle-inhaler and protective cap inside and out.

4. To put the nozzle-inhaler on the balloon and the valve stem, close the free aperture of the nozzle-inhaler protective cap.

Do not put the cylinder in water!

Side effects:

By frequency, side effects can be divided into the following categories: very frequent (> 1/10), frequent (> 1/100 and <1/10), infrequent (> 1/1000 and <1/100), the rare (> 1/10 000 and <1/100), very rare (<1/10 000).

From the immune system: very rarely - hypersensitivity reactions, including angioedema, rash, bronchospasm.

On the part of metabolic processes: rarely - hypokalemia, an increase in the blood of free fatty acids. Severe hypokalemia can potentially result from β2-agonist therapy.

From the nervous system: often - a tremor, a headache; very rarely - hyperactivity.

From the cardiovascular system: often - tachycardia; rarely - heart palpitations; very rarely - arrhythmia, including atrial fibrillation,supraventricular tachycardia, extrasystole, arterial hypotension and collapse; rarely - the expansion of peripheral vessels.

From the respiratory system: very rarely - a paradoxical bronchospasm.

From the gastrointestinal tract: rarely - irritation of the mucous membrane of the oral cavity and pharynx.

From the musculoskeletal system: rarely convulsions.

Overdose:Symptoms: more frequent - hypokalemia, lowering blood pressure, tachycardia, muscle tremor, nausea, vomiting; less frequent - agitation, hyperglycemia, respiratory alkalosis, hypoxemia, headache; rare - hallucinations, convulsions, tachyarrhythmias, fluttering of the ventricles, widening of the peripheral vessels.

Treatment:

In case of an overdose of salbutamol, the best antidotes are cardioselective β-adrenoblockers. However, β-adrenoreceptor blockers should be used with caution in patients with a history of bronchospasm.

The use of large doses of salbutamol can cause hypokalemia, so if you suspect an overdose, you should monitor the potassium level in the blood serum.

Interaction:

It is not recommended to apply simultaneously salbutamol and non-selective β-adrenergic receptor blockers, such as propranolol.

Salbutamol is not contraindicated in patients who receive monoamine-sidase inhibitors (MAOI).

In patients with thyrotoxicosis, the effect of stimulants of the central nervous system, tachycardia, increases the likelihood of developing extrasystole against the background of cardiac glycosides.

Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias; means for inhalation anesthesia, levodopa - severe ventricular arrhythmias.

Simultaneous administration with anticholinergics (including inhalation) may help increase intraocular pressure.

Diuretics and glucocorticosteroids increase the hypokalemic effect of salbutamol.

Special instructions:

Patients should be instructed about the correct use of the drug Salbutamol-MCPA aerosol for inhalation dosed with 100 μg / dose (200 doses). It is necessary to use the drug correctly and strictly follow the instructions in order to ensure that salbutamol enters the bronchi.At the beginning of treatment, the drug should be administered under the supervision of medical personnel and after training in front of the mirror.

As with the use of other inhalants, the therapeutic effect may decrease with cooling of the balloon. Therefore, before using the balloon with the drug should be warmed to room temperature (warm the balloon with your hands for several minutes, you can not use other methods!).

The contents of the cylinders are under pressure, so cylinders can not be heated, broken, punctured or burned, even when they are empty.

In case of unpleasant sensations in the mouth and perspiration in the throat after inhalation, the mouth should be rinsed with water.

Bronchodilators should not be the only or main component of asthma therapy for unstable or severe flow.

If the effect of the usual dose of the drug becomes less effective or less prolonged (the drug should last at least 3 hours), the patient should consult a doctor. Increasing the dose or frequency of salbutamol should be done only under the supervision of a doctor.Reduction of the interval between the intake of the following doses is possible only in exceptional cases and must be strictly justified. The increased need for the use of inhaled β2-adrenoreceptor agonists with short duration of action for the treatment of bronchial asthma indicates an exacerbation of the disease. In such cases, the patient's treatment plan should be reviewed. Taking high doses of salbutamol with exacerbation of asthma can cause the syndrome "rebound" (each subsequent attack becomes more intense). In case of a severe attack of suffocation, the interval between inhalations should be at least 20 minutes.

The risk of complications increases both with a considerable duration of treatment, and with a sharp withdrawal of the drug. Long-term use of salbutamol should be accompanied by the use of anti-inflammatory drugs for basic therapy.

Sudden and progressive deterioration of bronchial asthma can pose a threat to the life of the patient, so in such cases, it is urgent to decide whether to prescribe or increase the dose of glucocorticosteroids. In such patients it is recommended to monitor the peak exhalation rate daily.

Salbutamol should be used with caution in patients with thyrotoxicosis.

Therapy agonists (β2-adrenergic receptors, particularly when administered parenterally or by application via a nebulizer may result in hypokalemia. Particular caution is advised to exercise in the treatment of severe attacks of asthma, since in these cases, hypokalemia may be enhanced by the simultaneous use of xanthine derivatives, glucocorticoids , diuretics, and also due to hypoxia.In such cases, it is necessary to monitor the potassium level in the blood serum.

Effect on the ability to drive transp. cf. and fur:There is no information in the reference literature on the effect of salbutamol inhalation on a patient's ability to drive and / or other mechanisms. The content of the drug in a single dose of 1.36 mg rectified ethyl alcohol is so small that it can not influence the ability to drive and / or other mechanisms.

Form release / dosage:Aerosol for inhalation dosed with 100 μg / dose (200 doses).

Packaging:For 200 doses in cylinders, aluminum monoblock with internal protection, sealed by a metering valve and equipped with a nozzle-inhaler with a protective cap. Each cylinder, together with a nozzle-inhaler and a protective cap, as well as instruction for medical use, is placed in a pack.

Storage conditions:

At a temperature of no higher than 25 ° C. Do not freeze.

Keep out of the reach of children!

Protect from falls, shocks and direct sunlight.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002064

Date of registration:LP-002064

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp18.08.2015

Illustrated instructions

Instructions

Salbutamol-MCPP (Salbutamole-MHFP)