Salbutamol-Teva (Aerosol) Instructions for Use

Marketing Authorization Holder

Teva Pharmaceutical Industries, Ltd. (Israel)

Manufactured By

Norton (Waterford) Limited T/A IVAX Pharmaceuticals Ireland T/A Teva Pharmaceuticals Ireland (Ireland)

ATC Code

R03AC02 (Salbutamol)

Active Substance

Salbutamol (Rec.INN registered by WHO)

Dosage Form

Salbutamol-Teva

Metered-dose inhalation aerosol 100 mcg/1 dose: 200-dose canister with a dosing device

Dosage Form, Packaging, and Composition

Metered-dose inhalation aerosol, when sprayed onto glass, leaves a white spot.

Excipients: hydrofluoroalkane (HFA-134a) – 30.36 mg, ethanol – 3.93 mg.

200 doses – aluminum canisters (1) with a metering valve, with an inhalation device and a protective cap – cardboard packs^×.

^× protective stickers may additionally be applied.

Clinical-Pharmacological Group

Bronchodilator drug – selective beta₂-adrenergic agonist

Pharmacotherapeutic Group

Bronchodilator agent – selective beta2-adrenomimetic

Pharmacological Action

Salbutamol is a stimulator of β₂-adrenergic receptors. In therapeutic doses, it acts on β₂-adrenergic receptors of bronchial smooth muscle, exerting a pronounced bronchodilatory effect, prevents and relieves bronchospasm, and increases vital lung capacity. It prevents the release of histamine, slow-reacting substance from mast cells, and neutrophil chemotaxis factors. It causes a slight positive chronotropic and inotropic effect, dilates coronary arteries, and practically does not reduce blood pressure. It has a tocolytic effect: it lowers the tone and contractile activity of the myometrium.

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

The drug’s action begins 5 minutes after inhalation and lasts for 4-6 hours.

Pharmacokinetics

After inhalation, 10 to 20% of the dose reaches the airways. The remainder is retained in the device or deposited in the oropharynx and then swallowed. The part of the dose that remains in the airways is absorbed by the lung tissues without undergoing metabolism in the lungs and enters the bloodstream. Upon entering the systemic circulation, it can be metabolized in the liver and is excreted mainly in the urine unchanged or as a phenolic sulfate. The degree of binding of salbutamol to plasma proteins is 10%. C_max in blood plasma is 30 ng/ml. The part of the dose that enters the gastrointestinal tract is absorbed and undergoes intensive metabolism during the “first pass” through the liver, turning into phenolic sulfate. The unchanged drug and conjugate are excreted mainly in the urine. Most of the salbutamol dose administered intravenously, orally, or by inhalation is excreted within 72 hours. T_1/2 is 3.7-5 hours.

Indications

• Prevention and relief of bronchospasm in bronchial asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis, pulmonary emphysema.

ICD codes

Dosage Regimen

Adults and children over 12 years: 100-200 mcg (1-2 inhalation doses) to relieve asthma attacks. For controlling the course of mild asthma – 1-2 doses 1-4 times/day and moderate severity of the disease – in the same dosage in combination with other anti-asthmatic drugs. For prevention of exercise-induced asthma – 20-30 minutes before exercise, 1-2 doses per administration.

Children from 2 to 12 years for the development of a bronchial asthma attack, as well as to prevent bronchial asthma attacks associated with allergen exposure or caused by physical exertion, the recommended dose is 100-200 mcg (1 or 2 inhalations).

The daily dose should not exceed 800 mcg (8 inhalations).

Instructions for using the inhaler

Check the operation of the inhaler before first use, and also if you have not used it for some time.

1. Remove the cap from the inhaler. Make sure there is no dust or dirt in the outlet tube.
2. Hold the canister upright, with your thumb on the bottom and your index finger on the top of the canister.
3. Vigorously shake the canister up and down.
4. Take as deep an exhale as possible (without straining). Clamp the outlet tube of the canister tightly with your lips.
5. Take a slow, deep breath. At the moment of inhalation, press the canister valve with your index finger, releasing a dose of the medicine. Continue to inhale slowly.
6. Remove the inhaler tube from your mouth and hold your breath for 10 seconds or as long as you can without straining. Exhale slowly.

If more than one dose of medicine is required, wait about a minute and then repeat the steps starting from step 2. Put the cap back on the inhaler.

Do not rush when performing steps 3 and 4. It is important to inhale as slowly as possible at the moment the dose of medicine is released. Practice in front of a mirror at first. If you notice vapor coming out of the top of the canister or the corners of your mouth, start again from step 2.

Cleaning the inhaler

The inhaler should be cleaned at least once a week. Remove the metal canister from the plastic case and rinse the case and cap with warm water. Do not use hot water. Dry thoroughly, but do not use heating devices for this. Place the canister back into the case and put on the cap. Do not immerse the metal canister in water.

Adverse Reactions

Salbutamol-Teva may cause finger tremor, which is a typical side effect for all β₂-adrenergic receptor agonists. Headache, dizziness, increased excitability, anxiety, sleep disturbance, insomnia, peripheral vasodilation (facial skin flushing), slight compensatory increase in heart rate, increased blood pressure, chest pain, arthralgia may be noted.

Hypersensitivity reactions may develop (including angioedema, urticaria, erythema, nasal congestion, bronchospasm, arterial hypotension, and collapse); muscle cramps, nausea, vomiting, dyspepsia.

Inhalation drugs can cause paradoxical bronchospasm. Inhalation drugs can cause irritation of the oral and pharyngeal mucosa (pharyngitis), cough.

Salbutamol therapy can cause hypokalemia, which can pose a serious danger to the patient, as well as reversible metabolic disorders, for example, an increase in blood glucose concentration.

The drug can cause agitation and increased motor activity in children. The occurrence of arrhythmias (including atrial fibrillation, supraventricular tachycardia, and extrasystole) is possible.

Contraindications

• Rhythm disorders (paroxysmal tachycardia, multifocal ventricular extrasystole);
• Myocarditis;
• Heart defects;
• Aortic stenosis;
• Coronary artery disease;
• Tachyarrhythmia;
• Thyrotoxicosis;
• Decompensated diabetes mellitus;
• Glaucoma;
• Epileptic seizures;
• Pyloroduodenal stenosis;
• Renal or hepatic failure;
• Concomitant use of non-selective beta-blockers;
• Pregnancy;
• Children under 2 years of age;
• Hypersensitivity to any component of the drug.

With caution – chronic heart failure, hyperthyroidism, arterial hypertension, pheochromocytoma.

Use in Pregnancy and Lactation

Contraindicated in pregnancy.

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

Use in Hepatic Impairment

Contraindicated in hepatic failure.

Use in Renal Impairment

Contraindicated in renal failure.

Pediatric Use

Children from 2 to 12 years for the development of a bronchial asthma attack, as well as to prevent bronchial asthma attacks associated with allergen exposure or caused by physical exertion, the recommended dose is 100-200 mcg (1 or 2 inhalations).

Special Precautions

In patients with severe or unstable bronchial asthma, the use of bronchodilators should not be the main or only method of therapy. If the effect of the usual dose of Salbutamol-Teva becomes less effective or less prolonged (the effect of the drug should last at least 3 hours), the patient should consult a doctor.

Frequent use of salbutamol can lead to increased bronchospasm, sudden death, therefore, breaks of several hours should be taken between doses of the drug.

An increased need for the use of inhaled short-acting β₂-adrenergic receptor agonists to control the symptoms of bronchial asthma indicates an exacerbation of the disease. In such cases, the patient’s treatment plan should be reviewed and the issue of prescribing or increasing the dose of inhaled or systemic corticosteroids should be decided.

Therapy with β₂-adrenergic receptor agonists can lead to hypokalemia. Particular caution is recommended when treating severe attacks of bronchial asthma, 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 necessary to monitor the level of potassium in the blood serum.

The Salbutamol-Teva canister must not be pierced, disassembled, or thrown into fire, even if it is empty. Like most other inhalation agents in aerosol packaging, Salbutamol-Teva may be less effective at low temperatures. If the canister is cooled, it is recommended to remove it from the plastic case and warm it with your hands for several minutes.

Overdose

Symptoms: nausea, vomiting, increased excitability, hallucinations, tachycardia, ventricular flutter, peripheral vasodilation, decreased blood pressure, hypoxia, acidosis, hypokalemia, hyperglycemia, muscle tremor, headache.

Treatment: drug withdrawal, cardioselective beta-blockers; symptomatic therapy. If an overdose is suspected, the serum potassium level should be monitored.

Drug Interactions

Theophylline and other xanthines, when used concomitantly with salbutamol, increase the likelihood of tachyarrhythmias; inhalation anesthetics, levodopa – severe ventricular arrhythmias.

It is not recommended to use Salbutamol-Teva and non-selective beta-adrenergic receptor blockers, such as propranolol, simultaneously.

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

Salbutamol enhances the effect of CNS stimulants, the side effects of thyroid hormones, and cardiac glycosides.

Reduces the effectiveness of antihypertensive drugs, nitrates.

Hypokalemia may be enhanced by the simultaneous use of xanthine derivatives, corticosteroids, and diuretics.

Concomitant administration with anticholinergic agents (including inhaled ones) may contribute to an increase in intraocular pressure.

Storage Conditions

Keep out of reach of children, at a temperature not exceeding 30°C (86°F), protected from direct sunlight. Do not freeze.

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

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.