Salbutamol-Pharmstandart HF, aerosol 100 mcg/dose 200 doses

Pharmacotherapeutic group: bronchodilator – β₂-adrenomimetic selective.

ATX code: R03AC02

Pharmacological properties

Pharmacodynamics

Mechanism of action

Salbutamol is a selective beta₂-adrenoreceptor agonist. In therapeutic doses, it acts on beta₂-adrenoceptors of bronchial smooth muscle and has a short-term (4 to 6 hours) bronchodilator effect on beta₂-adrenoceptors with rapid onset of action (within 5 minutes) in reversible airway obstruction.

It has a pronounced bronchodilator effect, preventing or relieving bronchial spasm, reduces airway resistance. Increases the vital capacity of the lungs. Increases mucociliary clearance (in chronic bronchitis up to 36%), stimulates mucus secretion, activates the functions of the atrial epithelium.

In the recommended therapeutic doses does not have negative effects on the cardiovascular system, does not cause increase in arterial pressure. To a lesser extent compared to the drugs of this group, it has positive chrono- and inotropic effects. It causes dilation of the coronary arteries.

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

Pharmacokinetics

absorption

After inhalation, 10-20% of the dose of salbutamol reaches the lower airways. 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 lung tissue and blood, but is not metabolized in the lungs.

Distribution

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

Metabolism

In the systemic bloodstream, salbutamol undergoes hepatic metabolism and is excreted mainly by the kidneys unchanged or as phenolic sulfate.

The swallowed portion of the inhaled dose is absorbed from the gastrointestinal tract and undergoes significant metabolism during “first passage” through the liver, being converted to phenolic sulfate. The unchanged salbutamol and the conjugate are excreted primarily by the kidneys.

Elimation

Intravenously administered salbutamol has a half-life of 4-6 hours. It is excreted partly by the kidneys and partly by metabolism to 4′-O-sulfate (phenol sulfate), which is also excreted mainly 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 by intravenous, oral or inhalation routes is excreted within 72 hours.

Indications

Bronchial asthma
-relief of bronchial asthma symptoms when they occur;
prevention of bronchospasm attacks associated with exposure to an allergen or caused by physical activity;
-use as a component in long-term maintenance therapy of bronchial asthma.

2. Other chronic lung diseases with reversible airway obstruction, including chronic obstructive pulmonary disease (COPD), chronic bronchitis, and pulmonary emphysema.
Bronchodilators should not be the sole or main component of therapy for unstable or severe bronchial asthma. If there is no response to salbutamol in patients with severe bronchial asthma, glucocorticosteroid (GCS) therapy is recommended to achieve and maintain disease control. Lack of response to salbutamol therapy may indicate the need for urgent medical consultation or treatment.

Active ingredient

Salbutamol

Composition

Active substance:
salbutamol sulfate 0.1205 mg
(in terms of salbutamol 0.100 mg)
Supplements:
ethanol (ethanol absolute) 1.9000 mg
norflurane (1,1,1,1,2-tetrafluoroethane, chladone 134a) 27.1600 mg

Mineral sulfate.

How to take, the dosage

Salbutamol-Farmstandart HF is for inhalation only inhalation by mouth.

The increased need for beta_2- adrenoreceptor agonists may be a sign of worsening bronchial asthma. In this situation a reassessment of the patient’s regimen may be necessary to consider the appropriateness of concomitant GKS therapy.

As overdose may be accompanied by adverse reactions, the dose or the frequency of use of the drug may be increased only on the recommendation of the physician.

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

In patients who have difficulty timing their breath when using a pressurized metered dose aerosol inhaler, a spacer can be used.

In children and infants receiving Salbutamol-Farmstandart HF, a pediatric spacer device with a face mask may be appropriate.

Cure an attack of bronchospasm

Adults

The recommended dose is 100 or 200 mcg.

Children

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

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

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

Adults

200 mcg 10-15 minutes before exposure to a provocateur or exercise.

Children

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

Long-term maintenance therapy

Adults

Up to 200 mcg 4 times daily.

Children

Up to 200 mcg 4 times daily.

Inhalation instructions:

Preparing the inhaler:

Before using the drug for the first time, remove the protective cap from the mouthpiece of the inhaler nozzle, which is mounted on the cylinder and valve stem. Then shake the balloon vertically several times up and down, invert the balloon with the inhaler nozzle down and press the base of the balloon with your index finger and spray two times in the air to confirm that the product is in good condition. If you have not used the product for several days or longer, do the same for one spray in the air.

Use an inhaler:

1. Remove the protective cap from the inhaler nozzle and make sure the outlet tube (mouthpiece) of the inhaler nozzle is clean. Hold the cylinder with the inhaler nozzle vertically between your thumb and index finger with your thumb under the base of the inhaler nozzle and your index finger over the bottom of the cylinder.
2. Shake the aluminium balloon with its inhaler head vigorously up and down. Do not exhale into the inhaler!

Grip the outlet tube (mouthpiece) of the inhaler nozzle firmly with your lips.The balloon must point upwards!

4. Just take slow, deep breaths. As you inhale, use your index finger to push down on the bottom of the bottle releasing the dose of Salbutamol-Farmstandart HF and continue slowly inhaling.
5. Remove the mouthpiece of the inhaler nozzle from your mouth and hold your breath for 10 seconds or as long as you are comfortable. Slowly exhale.
6. After inhalation, rinse your mouth with water to wash away the medicine that got into your oral mucosa during inhalation. You should not swallow with your saliva the medicine that got into the oral mucosa during inhalation and the water with which you wash it off.
7. If another dose of medicine is required, wait for 1 minute and repeat all steps, starting with Step 2 and ending with Step 6.
8. Close the inhaler nozzle with the protective cap.

When you proceed to point 3 and 4, take your time. It is important to breathe in as slowly as possible as you release the dose of medicine. Practice in front of a mirror before application. If you notice “steam” coming out of the corners of your mouth, start the steps again from step 2. If you notice steam coming from the top of the inhaler nozzle, either carefully insert the valve stem that seals the balloon into 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 canister from the inhaler head. Gently rinse the inhaler head and the protective cap with warm water. Do not use hot water! Shake the inhaler nozzle and protective cap to remove any residual water and dry them without using heating devices. The aluminum water bottle should never come in contact with water!

The bottle is designed for 200 inhalations, after this time it needs to be replaced.

WARNING: The plastic mouthpiece is designed specifically for the product Salbutamol-Farmstandart HF and is used for precise dosing of the product. The mouthpiece must not be used with other metered-dose aerosols. You must also not use Salbutamol-Farmstandart HF with any adapter other than the mouthpiece supplied with the product.

The contents of the cylinder are under pressure. The bottle should never be opened or heated above 50°C!

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

In young children, the inhaler should be used under adult supervision or guidance.

Interaction

It is not recommended to use salbutamol and non-selective β-adrenoreceptor blockers such as propranolol simultaneously.

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

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

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

Interaction of salbutamol with levodopa, agents for inhalation anesthesia, MAO inhibitors and tricyclic antidepressants, cardiac glycosides may lead to a risk of sharp reduction of blood pressure.

Special Instructions

With caution, use in tachyarrhythmias and other heart rhythm disorders, arterial hypertension, myocarditis, heart defects, aortic stenosis, diabetes, thyrotoxicosis, glaucoma, acute heart failure (subject to close medical supervision).

An increase in the dose or frequency of administration of salbutamol should be performed under the supervision of a physician. Decreasing the interval is only possible in exceptional cases and must be strictly justified.

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

Contraindications

• hypersensitivity to salbutamol or any other component of the drug;
• children under 2 years of age;
• Preterm birth;
• Threatened abortion.

Cautions

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

Side effects

The adverse reactions presented below are listed according to organ and organ system involvement and frequency of occurrence. The incidence is rated as follows: very common (≥1/10), common (≥1/100 and < 1/10), infrequent (≥1/1000 and < 1/100), rare (≥1/10000 and < 1/1000), very rare (< 1/10000, including individual cases). Frequency categories were formed based on clinical studies of the drug and post-registration surveillance.

Frequency of adverse reactions

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

Metabolic and nutritional disorders

Rarely: hypokalemia. Therapy with beta₂ agonists may lead to clinically significant hypokalemia.

Nervous system disorders

Frequently: tremor, headache. Very rarely: hyperactivity.

Cardiac disorders

Frequently: tachycardia. Infrequent: feeling of palpitations. Very rare: arrhythmias, including atrial fibrillation; supraventricular tachycardia and extrasystole.

vascular disorders

Rarely: peripheral vasodilation.

Disorders of the respiratory system, thorax and mediastinum

Very rare: paradoxical bronchospasm.

Gastrointestinal tract disorders

Infrequent: irritation of the oral mucosa and pharynx.

Muscular and connective tissue disorders

Infrequent: muscle cramps.

Similarities

Salbutamol, Salbutamol-MCFP, Salbutamol-Pharmstandart, Novatron