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

Active substance:
Salbutamol Sulfate	0.120 mg
(in terms of salbutamol)	(0.100 mg)
Excipients:
Ethanol (absolute ethyl alcohol)	5.905 mg
Oleic acid	0.009 mg
Propellant R 134a of pharmacopoeial quality (1,1,1,2-tetrafluoroethane)	67.966 mg

Description:

A suspension of white or almost white color, under pressure in a stainless steel tank with a dosing valve and a spray nozzle; The drug is sprayed out of the balloon as an aerosol spray.

Pharmacotherapeutic group:bronchodilator - beta2-adrenergic selective

ATX: & nbsp

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

R.03.A.C.02 Salbutamol

Pharmacodynamics:

Salbutamol is a selective β agonist₂β-adrenoreceptors (β₂adrenomimetic). In therapeutic doses, it acts on β₂-adrenoceptors of smooth muscles of the bronchi, having little or no effect on the β₁-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. 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 extent compared with the drugs of this group has a positive chrono-inotropic effect. Causes the enlargement of the coronary arteries.

It has a number of metabolic effects: reduces the concentration of potassium in the blood plasma, affects glycogenolysis and insulin secretion, has hyperglycemic (especially in patients with bronchial asthma) and lipolytic effects, increases the risk of acidosis.

After applying the inhalation dose of salbutamol, the effect develops rapidly, the beginning of the effect in 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:

Suction

After the 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. A fraction that gets into the respiratory tract is absorbed into the lung tissue and blood, but not metabolized in the lungs.

Distribution

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

Metabolism

When entering the systemic circulation salbutamol is exposed to hepatic metabolism. 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.

Excretion

Introduced intravenously salbutamol has a half-life of 4-6 hours. Salbutamol is excreted mainly by the kidneys in the form of a conjugate - inactive 4'-O-sulfate (phenolic sulfate) and partially unchanged, and an insignificant part of salbutamol is excreted through the intestine. 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 the active substance or any other component included in the preparation.

- Management of preterm labor.

- Threatening abortion.

- Children under 2 years.

Carefully:

Salbutamol aeronaut should be used with caution in patients with thyrotoxicosis, tachyarrhythmia, myocarditis, heart defects, aortic stenosis, coronary heart disease, severe chronic heart failure, arterial hypertension, pheochromocytoma, decompensated diabetes mellitus, glaucoma, and during pregnancy and during breastfeeding.

Pregnancy and lactation:

Fertility

There is no data on the effects of salbutamol on human fertility.

Pregnancy

Pregnant women salbutamol appointed only if the expected benefit for the patient exceeds the potential risk to the fetus.

There are data on rare cases of various developmental malformations in children, including the formation of "wolf mouth" and developmental limbs, against the background of salbutamol intake by mothers during pregnancy. In some of these cases, mothers took several concomitant medications during pregnancy. In view of the absence of a permanent nature of defects and the background frequency of congenital anomalies, ranging from 2 to 3%, a causal relationship with the administration of salbutamol has not been established.

Breastfeeding period

Salbutamol probably penetrates into breast milk, and therefore it is not recommended to prescribe it to nursing women, except when the expected benefit for the mother herself exceeds the potential risk for the child. There is no evidence as to whether the person present in breast milk salbutamol harmful effect on the newborn.

Dosing and Administration:

Salbutamol aeronaut is only for inhalation use.

The increased need for agonists (β₂-adrenoreceptors may be a sign of aggravation of bronchial asthma. In such a situation, a reassessment of the patient's treatment regimen may be required, with consideration of the advisability of prescribing concurrent glucocorticosteroid therapy (GCS).

The dose or the multiplicity of salbutamol can be increased only on the advice of a doctor, since an overdose can be accompanied by the development of unwanted reactions.

The duration of action of salbutamol in most patients is from 4 to 6 hours.

In patients experiencing difficulty in inspiratory synchronization using a metered aerosol inhaler under pressure, a spacer can be used.

In children and infants receiving salbutamol, it is advisable to use a pediatric spacer device with a facial mask.

In case of unpleasant sensations in the mouth and throat swelling after inhalation, rinse the mouth with water.

Curbing an attack of bronchospasm

Adults

The recommended dose is 100 or 200 μg (1 or 2 inhalations).

Children

The recommended dose is 100 mcg (1 inhalation), if necessary, the dose may be increased to 200 mcg (2 inhalations).

It is not recommended to apply the drug Salbutamol aeronaut more often 4 times a day. The need for frequent use of maximum doses of the drug Salbutamol aeronaut or a sudden increase in the dose indicates a worsening of the course of bronchial asthma (see section "Special instructions").

Prevention of attacks of bronchospasm associated with exposure to an allergen or caused by physical exertion

Adults

The recommended dose is 200 mcg (2 inhalations) for 10-15 minutes before exposure to a provoking factor or load.

Children

The recommended dose is 100 μg (1 inhalation) 10-15 minutes before the effect of the provoking factor or load, if necessary, the dose may be increased to 200 μg (2 inhalations).

Prolonged maintenance therapy

Adults

The recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

Children

The recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

Instructions for inhalation

Checking the inhaler

Before using the inhaler for the first time, or if the inhaler has not been used for 5 days or more, check its operation. To do this, remove the protective cap from the mouthpiece of the inhaler, shake the inhaler well and press the balloon, releasing one jet of the drug into the air.

Use of an inhaler

War 1. Remove the protective cap from the inhaler mouthpiece, as shown in figure 1.

Step 2. Vigorously shake the inhaler to evenly mix the contents of the inhaler.

Step 3. Make a slow, full exhalation. Do not exhale into the inhaler!

Step 4. Holding the balloon, as shown in Figure 2, tightly grasp the mouthpiece with your lips, without grasping your teeth. The balloon should be pointed upside down!

Step 5. Execute the deepest inhalation through the mouth, while simultaneously press the bottom of the balloon to release one inhalation dose.

Step 6. Hold the breath for a few seconds, then remove the mouthpiece from the mouth and slowly exhale through the nose.

Step 7. Put the protective cap on the inhaler mouthpiece. Wait 30 seconds and repeat steps 2-6 to get a second inhalation dose, if necessary.

Cleaning the inhaler

Regularly (at least once a week), you should clean the mouthpiece of the inhaler, as shown in Figure 3.

Remove the metal can from the plastic case and rinse the case and cap with warm water. Do not use hot water. Thoroughly dry, but do not use heating devices. Place the metal can back into the case and put on the cap. Do not immerse the metal can into the water.

The cylinder is designed for 200 inhalations. After this, the cylinder should be replaced.

WARNING: a plastic mouthpiece designed specifically for the preparation Salbutamol aeronaut and serves for accurate dosing of the drug. The mouthpiece should not be used with other metered aerosols. Also You can not use the drug Salbutamol aeronaut with any other adapters, except the mouthpiece supplied with the drug.

The contents of the cylinder are under pressure. The cylinder should not be opened and subjected to heating above 50 ° C!

If you have difficulty using the inhaler, contact your doctor.

Young children need to use the inhaler under the supervision or with the help of adults.

Side effects:

The undesirable reactions presented below are listed in accordance with the damage to organs and organ systems. Frequency of occurrence is estimated as follows: Often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10000 and <1/1000), rarely (< 1/10000).

Immune system disorders: rarely - reactions hypersensitivity, including angioedema, hives, bronchospasm, lowering blood pressure and collapse.

Disorders from the metabolism and nutrition: rarely hyperglycemia, hypokalemia.

Therapy with agonists β₂-adrenoceptor can lead to clinically significant hypokalemia.

Disturbances from the nervous system: often - tremor, headache; rarely - hyperactivity.

Heart Disease: often - tachycardia; infrequently - myocardial ischemia, severe palpitation (palpitation); rarely - Arrhythmias, including atrial fibrillation; supraventricular tachycardia and extrasystole.

Vascular disorders: rarely peripheral vasodilation.

Disturbances from the respiratory system, chest and mediastinal organs: rarely - Paradoxical bronchospasm.

Disorders from the gastrointestinal tract: infrequently - irritation of the mucous membrane of the oral cavity and pharynx.

Disturbances from musculoskeletal and connective tissue: infrequently - muscle cramps.

If any of the above at instructions for adverse reactions are aggravated, or you notice any other undesirable reactions not indicated at instructions, inform the doctor about it.

Overdose:

Symptoms

Signs and symptoms of an overdose of salbutamol are transient phenomena pharmacologically caused by stimulation β-adrenergic receptors, such as lowering blood pressure, tachycardia, muscle tremor, nausea, vomiting, hyperglycemia, lactic acidosis. When using high doses, as well as with short-acting beta-agonists, development of lactic acidosis was observed, therefore, in case of overdose, control over the increase of serum lactate and the possibility of metabolic acidosis development (especially with preservation or deterioration of tachypnea, despite the elimination of other signs of bronchospasm, such like wheezing) (see "Special instructions" and "Side effect" sections). The use of high doses of salbutamol can cause hypokalemia, so it is necessary to monitor the concentration of potassium in the blood plasma.

Treatment

It should be canceled salbutamol and prescribe appropriate symptomatic therapy. Cardioselective (β-adrenoblockers in patients with cardiac symptoms (eg, tachycardia, palpitation) should be used with caution because of the risk of bronchospasm.

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 (iMAO).

In patients with thyrotoxicosis salbutamol enhances the effect of stimulants of the central nervous system and tachycardia.

Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias.

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

Diuretics and GCS increase the hypokalemic effect of salbutamol.

The interaction of Salbutamol with levodopa, the means for inhalation anesthesia, MAO inhibitors and tricyclic antidepressants, cardiac glycosides can lead to the risk of a sharp drop in blood pressure.

Special instructions:

Treatment of bronchial asthma is recommended to be carried out step by step, monitoring the patient's clinical response to treatment and lung function.

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

The increased need for the use of short-acting bronchodilators, in particular agonists β₂-adrenoreceptors, to control the symptoms of bronchial asthma indicates a worsening of the course of the disease. In such cases, the patient's treatment plan should be reviewed.

Sudden and progressive deterioration of bronchial asthma can pose a potential threat to the life of the patient, so in such situations, the desirability of prescribing or increasing the dose of GCS should be considered. In patients at risk, daily monitoring of peak expiratory flow is recommended.

Therapy with agonists β₂-adrenoceptors, especially when administered parenterally or 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 may be exacerbated by the simultaneous use of xanthine derivatives, GCS, diuretics, and also due to hypoxia. In such situations it is recommended to monitor the concentration of potassium in the blood plasma.

If there is no effect on the previously effective dose of inhaled salbutamol for at least three hours, the patient should consult a physician for any additional measures.

Patients should be instructed about the correct use of the inhaler Salbutamol aeronaut.

Immediately after the administration of salbutamol, paradoxical bronchospasm may develop with increased wheezing. This condition requires immediate treatment using another high-speed inhaled bronchodilator. A drug Salbutamol aeronaut should immediately cancel, assess the patient's condition and, if necessary, prescribe an alternative therapy.

Frequent use of salbutamol can lead to an increase in bronchospasm, sudden death, therefore, between the doses of regular doses of the drug, breaks must be taken in a few hours; with a severe attack of suffocation, the interval between inhalations should be at least 20 minutes.

When cooling the balloon, the therapeutic effect of the drug may decrease, so before using the balloon should be warmed to room temperature (warm hands for several minutes, other methods are unacceptable!).

The contents of the cylinder are under pressure, so even empty cylinders can not be damaged, heated, or burned.

Effect on the ability to drive transp. cf. and fur:

Data on the effect of the drug Salbutamol aeronaut there is no ability to control vehicles and mechanisms. In case of development of such undesirable reactions as muscle cramps or bronchospasm, it is necessary to refrain from controlling vehicles and mechanisms, as well as from engaging in other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Aerosol for inhalation dosed, 100 mcg / dose.

Packaging:

For 200 doses of the drug in a stainless steel balloon with a dosing valve and a spray nozzle.

Each cylinder is accompanied with instructions for use in a cardboard bundle.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C, away from heating appliances. Do not freeze.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-003899