Salben^® (Powder) Instructions for Use

Marketing Authorization Holder

Pulmomed, CJS (Russia)

ATC Code

R03AC02 (Salbutamol)

Active Substance

Salbutamol (Rec.INN registered by WHO)

Dosage Form

Salben®

Inhalation powder 200 mcg/1 dose: “Cyclohaler” inhalers 100 doses or 200 doses

Dosage Form, Packaging, and Composition

100 doses – “Cyclohaler” inhalers (1) – polyethylene bags (1) – cardboard packs.
200 doses – “Cyclohaler” inhalers (1) – polyethylene bags (1) – cardboard packs.

Clinical-Pharmacological Group

Bronchodilator drug – beta₂-adrenergic agonist

Pharmacotherapeutic Group

Selective beta2-adrenomimetic

Pharmacological Action

Beta-adrenomimetic with a predominant effect on β₂-adrenergic receptors. In therapeutic doses, Salbutamol acts on β₂-adrenergic receptors of bronchial smooth muscles and exerts a short-acting (from 4 to 6 hours) bronchodilatory effect on β₂-adrenergic receptors with a rapid onset of action (within 5 minutes) in reversible airway obstruction.

It prevents and relieves bronchospasm; reduces airway resistance, increases vital lung capacity. It prevents the release of histamine, slow-reacting substance from mast cells and neutrophil chemotaxis factors. It increases mucociliary clearance (in chronic bronchitis up to 36%), stimulates mucus secretion, and activates ciliary epithelium functions.

In recommended therapeutic doses, it does not have a negative effect on the cardiovascular system and does not cause an increase in blood pressure. To a lesser extent, compared to other drugs in this group, it exerts a positive chronotropic and inotropic effect on the myocardium. It causes dilation of the coronary arteries.

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

Pharmacokinetics

During inhalation, 10-20% of the dose reaches the small bronchi, the remainder is deposited in the upper airways. The fraction deposited in the airways is absorbed into the lung tissue and blood but is not metabolized in the lungs. After inhalation, systemic absorption is rapid but low. The C_max of salbutamol in blood plasma is observed after 3 hours.

When taken orally, Salbutamol is well absorbed from the gastrointestinal tract.

Plasma protein binding is 10%.

It is metabolized during the “first pass” through the liver and possibly in the intestinal wall; the main metabolite is an inactive sulfate conjugate. Salbutamol is not metabolized in the lungs, thus its final metabolism and excretion after inhalation depends on the method of administration, which determines the ratio between inhaled and unintentionally swallowed salbutamol.

The T_1/2 from plasma is 3-7 hours. It is excreted by the kidneys, mainly unchanged (about 90%) and as an inactive phenol sulfate metabolite (about 60%) within 72 hours, and with bile.

Salbutamol penetrates the blood-brain barrier, creating concentrations approximately equal to 5% of the concentration in blood plasma.

Indications

Bronchial asthma: relief of bronchial asthma symptoms as they occur; prevention of bronchospasm attacks associated with allergen exposure or caused by physical exertion; use as one of the components in long-term maintenance therapy of bronchial asthma. Other chronic lung diseases accompanied by reversible airway obstruction, including COPD, chronic bronchitis, pulmonary emphysema.

ICD codes

Dosage Regimen

Use Salben^® inhalation powder only via the oral inhalation route with the provided Cyclohaler device.

For relief of acute bronchospasm in adults and adolescents (12 years and older), administer a single dose of 200 mcg (one inhalation) as needed.

For prevention of exercise-induced bronchospasm, administer 200 mcg (one inhalation) 15 minutes prior to physical exertion.

The maximum recommended daily dosage is 4 inhalations (800 mcg) for intermittent symptom relief.

Do not exceed the prescribed frequency. Increasing the need for rapid-acting bronchodilators indicates worsening asthma control and requires medical re-evaluation.

For long-term maintenance therapy, the dosage is individualized. The typical regimen is one to two inhalations up to four times daily.

If a previously effective dose fails to provide relief for at least 3 hours, seek immediate medical attention.

Ensure proper inhaler technique. Exhale fully before placing the mouthpiece between lips. Inhale deeply and forcefully through the device. Hold breath for 10 seconds if possible.

Rinse mouth with water after each use to reduce local irritation and systemic absorption.

Monitor the dose counter. Do not use the inhaler after the final dose. Do not attempt to disassemble the device.

Adverse Reactions

From the immune system very rarely – hypersensitivity reactions, including urticaria, skin rash, angioedema, paradoxical bronchospasm, erythema multiforme, Stevens-Johnson syndrome, decreased blood pressure and collapse.

From metabolism rarely – hypokalemia.

From the nervous system often – tremor, headache; very rarely – hyperactivity; when taken orally – psychoneurological disorders, including psychomotor agitation, disorientation, sleep disturbance, memory impairment, aggressiveness, panic state, hallucinations, suicide attempts, schizophrenia-like disorders.

From the cardiovascular system: often – tachycardia; infrequently – palpitations; rarely – peripheral vasodilation; very rarely – arrhythmias, including atrial fibrillation; supraventricular tachycardia and extrasystole.

From the respiratory system very rarely – paradoxical bronchospasm.

From the digestive system infrequently – irritation of the oral and pharyngeal mucosa.

From the musculoskeletal system infrequently – muscle cramps.

Other chest pain, urinary retention.

Contraindications

Hypersensitivity to salbutamol; childhood – depending on the dosage form.

For inhalation use: management of preterm labor; threatened abortion.

With caution in patients with thyrotoxicosis, tachyarrhythmia, myocarditis, heart defects, aortic stenosis, coronary artery disease, severe chronic heart failure, arterial hypertension, pheochromocytoma, decompensated diabetes mellitus, glaucoma.

For oral administration: coronary artery disease, severe heart failure, arrhythmia (paroxysmal tachycardia, multifocal ventricular extrasystole); myocarditis, heart defects, aortic stenosis, decompensated diabetes mellitus, hyperthyroidism, pheochromocytoma, glaucoma, epileptic seizures, pyloroduodenal stenosis, kidney and liver diseases with impaired function, first trimester of pregnancy, simultaneous use of non-selective beta-blockers.

With caution: mild to moderate chronic heart failure, arterial hypertension, pheochromocytoma.

Use in Pregnancy and Lactation

During pregnancy and breastfeeding, use is possible according to indications in cases where the expected benefit for the mother outweighs the potential risk for the fetus or infant.

Salbutamol may cause tachycardia and hyperglycemia in the mother (especially in the presence of diabetes mellitus) and the fetus, and may also cause delayed labor in the mother. There are reports of rare cases of various malformations in children, including the formation of cleft palate and limb deformities, against the background of mothers taking salbutamol during pregnancy.

Salbutamol is excreted in breast milk, so if it is necessary to use during lactation, the expected benefit of treatment for the mother and the possible risk for the child should also be assessed.

Use in Hepatic Impairment

Should be used with caution in liver diseases.

Use in Renal Impairment

Should be used with caution in kidney diseases.

Pediatric Use

Can be used in children of appropriate age categories strictly according to indications, in recommended doses and dosage forms. It is necessary to strictly follow the instructions in the salbutamol drug leaflets regarding contraindications for the use of specific salbutamol dosage forms in children of different ages.

Special Precautions

Treatment of bronchial asthma is recommended to be carried out in stages, controlling the patient’s clinical response to treatment and lung function.

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

An increased need for the use of short-acting bronchodilators, in particular β₂-adrenergic receptor agonists, to relieve bronchial asthma symptoms indicates a worsening of the disease. In such cases, the patient’s treatment plan should be reviewed.

Sudden and progressive worsening of bronchial asthma may pose a potential threat to the patient’s life, so in such situations, the advisability of prescribing or increasing the dose of corticosteroids should be considered. In patients at risk, daily monitoring of peak expiratory flow is recommended. Therapy with β₂-adrenergic receptor agonists, especially when administered parenterally or via nebulizer, can lead to hypokalemia.

Particular caution should be exercised in the treatment of severe asthma attacks, since in these cases hypokalemia may be enhanced by the simultaneous use of xanthine derivatives, corticosteroids, diuretics, and also due to hypoxia. In such situations, it is recommended to monitor plasma potassium concentration.

As with the use of other means for inhalation therapy, paradoxical bronchospasm with increased wheezing may develop immediately after the use of salbutamol. In such cases, Salbutamol must be immediately discontinued, the patient’s condition assessed, and alternative therapy prescribed if necessary.

Drug Interactions

With simultaneous use of salbutamol with theophylline and other xanthines, the likelihood of tachyarrhythmias increases.

With simultaneous use of salbutamol with agents for inhalation anesthesia, levodopa, the likelihood of developing severe ventricular arrhythmias increases.

With simultaneous use, MAO inhibitors and tricyclic antidepressants enhance the effect of salbutamol, which can lead to a sharp decrease in blood pressure.

With simultaneous use of salbutamol and non-selective beta-blockers (such as propranolol), the risk of developing severe bronchospasm increases.

Prescribing salbutamol simultaneously with anticholinergic agents may contribute to increased intraocular pressure.

With simultaneous use, diuretics and corticosteroids enhance the hypokalemic effect of salbutamol.

With simultaneous use, Salbutamol enhances the effect of CNS stimulants and aggravates the side effects of thyroid hormones on the heart.

Increases the likelihood of glycoside intoxication.

With simultaneous use, Salbutamol reduces the antianginal efficacy of nitrates and the hypotensive activity of antihypertensive agents.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.