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

Excipients: oleyl alcohol 0.0625 mg, ethanol (rectified ethyl alcohol) 2.02 mg, propellant R 134a (1,1,1,2-tetrafluoroethane, HFA 134a) 56.91 mg. The drug does not contain chlorofluorocarbon propellants.

1 bottle of the drug contains:

Active substance: salbutamol sulfate in terms of 100% substance) 0.029 g (equivalent to 0.024 grams of salbutamol).

Excipients: oleyl alcohol 0.015 g, ethanol (rectified ethyl alcohol) 0.485 g, propellant R 134a (1,1,1,2-tetrafluoroethane, HFA 134a) 13.659 g (up to 12.00 ml). The drug does not contain chlorofluorocarbon propellants.

Description:

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

Pharmacotherapeutic group:Bronchodilator - beta2-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, exerting an insignificant effect on the β 1 -adrenoceptors of the myocardium. Has a pronounced bronchodilator effect, preventing or reducing spasm of the bronchi, reduces resistance in the airways. Increases the vital capacity of the lungs. 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 potassium concentration 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 settles on the mucous membrane of the oropharynx and then is swallowed. Fraction, settled on the mucosa of 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%.

Salbutamol is 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. The half-life of salbutamol is 4-6 hours. It is excreted by the kidneys partly in unmodified form and partly in the form of the inactive metabolite 4'-0-sulfate (phenolic sulfate). A small part is excreted with bile (4%), with feces. Most of the dose of salbutamol 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.

- Children up to 2 years.

Carefully:If there is a history of tachyarrhythmia, myocarditis, heart defects, aortic stenosis, ischemic heart disease, severe chronic heart failure, arterial hypertension, thyrotoxicosis, pheochromocytoma, decompensated diabetes mellitus, glaucoma, epimetiopathy, renal or hepatic insufficiency, simultaneous reception of non-selective β-adrenergic blockers , pregnancy, lactation.

Pregnancy and lactation:Pregnant women salbutamol can be prescribed only if the expected benefit for the patient exceeds the potential risk to the fetus.The likelihood of salbutamol penetrating into breast milk is not ruled out, so it is not recommended to administer it to nursing women, unless the expected benefit for the patient exceeds the potential risk for the baby. There is no evidence as to whether the person present in breast milk salbutamol harmful effect on the newborn.

Dosing and Administration:

Salbutamol aerosol for inhalations dosed with 100 μg / 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 (including elderly patients). Long-term maintenance therapy for bronchial asthma and COPD in the complex therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

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

Preventing bronchospasm attacks,associated with the effect of an allergen or caused by physical exertion: the recommended dose is 200 mcg (2 inhalations) for 10-15 minutes before the impact of the provoking factor.

Children. Long-term maintenance therapy for bronchial asthma and COPD in the complex therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

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.

Application rules:

Preparation for first use:

Before the first use of the drug, 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 off the top of the balloon. Continue to hold your breath as far as possible.

7. If necessary, perform the following inhalation. To do this, wait about 30 seconds, keeping the cylinder 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 you should apply the drug after training in front of the mirror. If a "cloud" appears on the sides of the mouth, then it is necessary to start again from point 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 inhaler and protective cap under warm running water.

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 often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10 000 and <1/100), very rarely (<1 / 10,000) occurring.

From the immune system: rarely - dermatitis; very rarely - hypersensitivity reactions, including angioedema, skin rash; On the part of metabolic processes: rarely - hypokalemia.

From the nervous system: often - tremor, headache, anxiety; rarely - dizziness, drowsiness, fatigue; very rarely - hyperactivity.

From the cardiovascular system: often tachycardia, palpitation; rarely - the expansion of peripheral vessels with skin flushing, discomfort or chest pain; very rarely - arrhythmia, including atrial fibrillation, supraventricular tachycardia, extrasystole, lowering blood pressure and collapse.

From the respiratory system: rarely - cough, irritation of the respiratory tract; very rarely - bronchospasm (paradoxical or caused by hypersensitivity to the drug).

From the gastrointestinal tract: rarely - dryness and irritation of the mucous membrane of the mouth and throat, changes in taste, nausea, vomiting.

From the musculoskeletal system: rarely - muscle cramps.

Overdose:Symptoms of overdose: 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.In case of an overdose of salbutamol, the best antidotes are cardioselective β-adrenoblockers. However, β-adrenoreceptor blockers should be used with caution (risk of developing bronchospasm).

The use of large doses of salbutamol can cause hypokalemia, so if you suspect an overdose, you should monitor the potassium concentration 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 oxidase inhibitors (MAOIs).

Enhances the effect of stimulants of the central nervous system.

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

Simultaneous use with m-holinoblokatorami (including inhalation) can 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. Proper use of the drug and strict compliance with the instructions are necessary 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 β-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 in case of exacerbation of bronchial asthma can cause a syndrome of "ricochet" (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 with β 2 -adrenoreceptor agonists, especially when administered by parenteral administration or when used with a nebulizer, can lead to hypokalemia. Particular caution should be exercised in the treatment of severe attacks of bronchial asthma, because in these cases, hypokalemia can be exacerbated by the simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics, and also due to hypoxia. In such cases, it is necessary to monitor the potassium concentration in the blood serum.

Effect on the ability to drive transp. cf. and fur:Because the Salbutamol can cause such side effects as convulsions and dizziness, it is recommended at the first receptions to exercise increased caution or refuse to drive vehicles and engage in other potentially hazardous activities.

Form release / dosage:Aerosol for inhalation dosed with 100 μg / dose.

Packaging:200 doses (12 ml each) in cylinders of aluminum monoblock with internal protection, hermetically sealed by a metering valve and equipped with a nozzle-inhaler with a protective cap. Each cylinder, together with a nozzle and protective cap, as well as instruction for use, is placed in a bundle.

Storage conditions:

Store at a temperature not exceeding 25 ° C. Do not freeze. Keep out of the reach of children!

Keep away from heating system and direct sunlight. Protect from falls and shocks.

Shelf life:3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-006937/10

Date of registration:LSR-006937/10

The owner of the registration certificate:BINNOFARM, CJSC BINNOFARM, CJSC Russia

Manufacturer: & nbsp

BINNOFARM, CJSC Russia

Representation: & nbspBINNOFARM CJSC BINNOFARM CJSC Russia

Information update date: & nbsp22.08.2015

Illustrated instructions

Instructions

Salbutamol (Salbutamol)