Salbutamol-Pharmstandart HF, inhalation aerosol 100 µg/dose, 200 doses

Composition

Active ingredient: salbutamol sulfate 0.1255 mg (based on salbutamol 0.100 mg)Excipients: ethanol (absolute ethanol) 1,9000 mg norflurane (1,1,1,2-tetrafluoroethane, chladon 134 a) 27,1600 mg

Pharmacological action

Pharmacotherapeutic group: bronchodilator-beta_-2-adrenomimetic selective.

ATX code: R03 AC 02

Pharmacological properties

Pharmacodynamics

Mechanism of action

Salbutamol is a selective beta_-2-adrenergic agonist. In therapeutic doses, it acts on beta_-2-adrenoreceptors of the smooth muscles of the bronchi and has a short (from 4 to 6 hours) bronchodilator effect on beta_-2-adrenoreceptors with a rapid onset of action (within 5 minutes) with reversible airway obstruction.

It has a pronounced bronchodilating effect, preventing or stopping bronchospasm, reduces resistance in the airways. Increases the vital capacity of the lungs. Increases mucociliary clearance (up to 36% in chronic bronchitis), stimulates mucus secretion, activates the functions of the ciliated epithelium.

In the recommended therapeutic doses, it does not have a negative effect on the cardiovascular system, does not cause an increase in blood pressure. To a lesser extent, compared with drugs of this group, it has a positive chrono – and inotropic effect. Causes dilation of the coronary arteries.

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

Pharmacokinetics

Suction

After inhalation,10-20% of the salbutamol dose reaches the lower respiratory tract. The remainder 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 is not metabolized in the lungs.

Distribution

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

Metabolism

When it enters the systemic circulation, salbutamol undergoes hepatic metabolism and is mainly excreted by the kidneys in unchanged form or in the form of phenolic sulfate.

The ingested portion of the inhaled dose is absorbed from the gastrointestinal tract and undergoes significant metabolism during the” first pass ” through the liver, turning into phenolic sulfate. Unchanged salbutamol and conjugate are mainly excreted by the kidneys.

Deduction

Intravenously administered salbutamol has a half-life of 4-6 hours. It is excreted partly by the kidneys and partly as a result of metabolism to 4’ – O-sulfate (phenolic sulfate), which is also mainly excreted by the kidneys. Only a small part of the administered dose of salbutamol is excreted through the intestine. Most of the dose of salbutamol administered intravenously, orally or by inhalation is excreted within 72 hours.

Indications

1. Bronchial asthma-relief of symptoms of bronchial asthma when they occur; – prevention of bronchospasm attacks associated with exposure to an allergen or caused by physical exertion; – use as one of the components in long-term maintenance therapy of bronchial asthma.

2. Other chronic lung diseases associated with reversible airway obstruction, including chronic obstructive disease (COPD), chronic bronchitis, and emphysema. Bronchodilators should not be the only or main component of treatment for unstable or severe asthma. In the absence of a response to salbutamol in patients with severe bronchial asthma, it is recommended to conduct therapy with glucocorticosteroids (corticosteroids) in order to achieve and maintain disease control. Failure to respond to salbutamol therapy may indicate an urgent need for medical advice or treatment.

Contraindications

• hypersensitivity to salbutamol or any other component that is part of the drug;
• children under 2 years of age;
• preterm birth management;
• threatened abortion.

With caution

Salbutamol-Pharmstandard HF should be used with caution in patients with tachyarrhythmia; ischemic heart disease; myocarditis; heart defects; aortic stenosis; severe chronic heart failure; arterial hypertension; thyrotoxicosis; pheochromocytoma; decompensated diabetes mellitus; glaucoma; as well as during pregnancy and lactation.

Side effects

The adverse reactions listed below are listed according to the lesion of organs and organ systems and frequency of occurrence. The frequency of occurrence is estimated as follows: very common (≥ 1/10), common (≥1/100 and < 1/10), uncommon (≥ 1/1000 and < 1/100), rare (≥1/10000 and < 1/1000), very rare ( Frequency categories were formed based on clinical studies of the drug and post-marketing surveillance.

Frequency of adverse reactions

Immune system disorders: very rarely – hypersensitivity reactions, including angioedema, urticaria, bronchospasm, decreased blood pressure and collapse.

Metabolic and nutritional disorders

Rare: hypokalemia. Beta_-2agonist therapy may result in clinically significant hypokalemia.

Nervous system disorders

are common: tremor, headache. Very rare: hyperactivity.

Disorders of the heart

Often: tachycardia. Infrequently: palpitation of the heart. Very rare: arrhythmias, including atrial fibrillation; supraventricular tachycardia and extrasystole.

Vascular disorders

Rare: peripheral vasodilation.

Respiratory, thoracic and mediastinal disorders

Very rare: paradoxical bronchospasm.

Disorders of the gastrointestinal tract

Infrequently: irritation of the oral and pharyngeal mucosa.

Musculoskeletal and connective tissue disorders

Infrequently: muscle cramps.

Interaction

It is not recommended to use salbutamol and non-selective beta-blockers, such as propranolol, at the same time.

Salbutamol is not contraindicated in patients receiving monoamine oxidase inhibitors (MAOIs).

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

Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias. Concomitant use with anticholinergic agents (including inhaled ones) may increase intraocular pressure. Diuretics and corticosteroids enhance the hypokalemic effect of salbutamol.

The interaction of salbutamol with levodopa, inhaled anesthetics, MAO inhibitors and tricyclic antidepressants, cardiac glycosides may lead to the risk of a sharp decrease in blood pressure.

How to take, course of use and dosage

Salbutamol-Pharmstandard HF is intended only for inhalation by inhalation through the mouth.

An increased need for the use of beta_-2-adrenergic agonists may be a sign of exacerbation of bronchial asthma. In such a situation, it may be necessary to re-evaluate the patient’s treatment regimen with consideration of the feasibility of prescribing simultaneous therapy with corticosteroids.

Since overdose can be accompanied by the development of undesirable reactions, the dose or frequency of use of the drug can be increased only on the recommendation of a doctor.

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

A spacer may be used in patients who have difficulty synchronizing their inhalation with the use of a pressurized metered-dose aerosol inhaler.

In children and children receiving the drugSalbutamol-Pharmaceutical Standard RF, it is advisable to use a pediatric spacer device with a face mask.

Relief of an attack of bronchospasm

Adults

The recommended dose is 100 or 200 mcg.

Children

100 mcg, if necessary, the dose can be increased to 200 mcg.

It is not recommended to use an inhalerSalbutamol-Farmstandart HF more than four times a day. The need for such frequent use of additional doses of the drugSalbutamol-Pharmstandard HF or a sharp increase in the dose indicates a worsening of the course of asthma (see the section ” Special instructions “).

Prevention of bronchospasm attacks related to allergen exposure or caused by physical exertion

Adults

200 mcg 10-15 minutes before exposure to the provoking factor or load.

Children

100 mcg 10-15 minutes before exposure to the provoking factor or load, if necessary, the dose can be increased to 200 mcg.

Long-term maintenance therapy

Adults

Up to 200 mcg 4 times a day.

Children

Up to 200 mcg 4 times a day.

Instructions for carrying out inhalations:

Preparation of the inhaler:

Before the first use of the drug, remove the protective cap from the mouthpiece of the inhaler nozzle, which is installed on the cylinder and valve stem. Then shake the balloon several times with vertical movements up and down, turn the balloon upside down with the inhaler nozzle and, pressing the bottom of the balloon with your index finger, make two sprays into the air to check the serviceability of the drug. After a break in the use of the drug for several days or longer, one spray into the air should be done in the same way.

Using the inhaler:

Press the outlet tube (mouthpiece) of the inhaler nozzle firmly with your lips. The balloon must be pointed upside down!

When performing actions in accordance with points 3 and 4, take your time. When releasing a dose of medication, it is important to inhale as slowly as possible. Before applying, practice in front of a mirror. If you notice “steam” coming out of the corners of your mouth, then start again from step 2. If you notice “steam” coming out of the top of the inhaler nozzle, then you must either carefully install the valve stem that seals the cylinder in the seat inside the inhaler nozzle, or clean the inhaler nozzle.

Cleaning the inhaler nozzle

The inhaler nozzle should be cleaned at least once a week. Remove the aluminum cylinder from the inhaler nozzle. Gently rinse the inhaler nozzle and protective cap with warm water. Do not use hot water! Shake the inhaler nozzle and protective cap to remove any remaining water and dry them without using heating devices. Do not allow the aluminum cylinder to come into contact with water!

The balloon is designed for 200 inhalations, after which the balloon should be replaced.

WARNING: The plastic mouthpiece is designed specifically for the drugSalbutamol is a high-frequency pharmaceutical standard and is used for accurate dosage of the drug. The mouthpiece should not be used with other metered-dose aerosols. You can also not use the drugSalbutamol-RF pharmaceutical standard with any other adapters, except for the mouthpiece supplied with the drug.

The contents of the cylinder are under pressure. The cylinder must not be opened or exposed to heat above 50 °C!

If you have any difficulties using your inhaler, please contact your doctor.

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

Special instructions

Use with caution for tachyarrhythmias and other heart rhythm disorders, arterial hypertension, myocarditis, heart defects, aortic stenosis, diabetes mellitus, thyrotoxicosis, glaucoma, acute heart failure (subject to careful monitoring by a doctor).

Increasing the dose or frequency of salbutamol should be done under the supervision of a doctor. Reducing the interval is possible only in exceptional cases and must be strictly justified.

When using salbutamol, there is a risk of hypokalemia, so during treatment in patients with severe bronchial asthma, the level of potassium in the blood should be monitored. The risk of hypokalemia increases with hypoxia.

Storage conditions

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

Shelf

life is 2 years. Do not use after the expiration date indicated on the package.

Active ingredient

Salbutamol

Conditions of release from pharmacies

By prescription

Dosage form

aerosol for inhalation