Ventolin - instructions for use, dose, side effects, contraindications

Name of components	Quantity in one dose	Quantity in 1 inhaler
Active substance
Salbutamol sulfate (micronized)¹	120.5 μg²	28.92 mg
Excipient
Propellant (1,1,1,2-tetrafluoroethane)	up to 75.0 mg	up to 18,0 g

Notes:

1. To provide an output of 200 doses when using the inhaler, each inhaler contains an amount of suspension equivalent to 240 doses.

2. 120.5 μg of salbutamol sulfate (micronized) are equivalent to 100.0 μg of salbutamol.

3. Depending on the equipment used in the manufacture of the preparation, up to 10% excess of the active substance may be included in the production formula.

Description:An aluminum inhaler equipped with a plastic dispenser with a protective cap containing a suspension of white or almost white color.

Pharmacotherapeutic group:Bronchodilator beta2-adrenomimetic is selective

ATX: & nbsp

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

R.03.A.C.02 Salbutamol

Pharmacodynamics:Mechanism of action

Salbutamol is a selective beta agonist₂adrenoreceptors. In therapeutic doses, it acts on beta₂-adrenoceptors of smooth muscles of the bronchi, having little or no effect on beta₂-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 degree, in comparison with the drugs of this group, it has a positive chrono- and inotropic effect. Causes the enlargement of the coronary arteries.

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

After the application of inhalation forms, the effect develops rapidly, the onset of the effect after 5 minutes, maximum after 30-90 minutes (75% of the maximum effect is achieved within 5 minutes), duration - 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. The fraction deposited in 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

Once in the blood, salbutamol is subjected to hepatic metabolism and excreted mainly with urine in unchanged form or in the form of phenolic sulfate.

The swallowed portion of the inhalation dose is absorbed from the gastrointestinal tract and subjected to significant metabolism during the "first passage" through the liver, turning into phenolic sulfate. Unchanged salbutamol and the conjugate is excreted mainly in the urine.

Excretion

Introduced intravenously salbutamol has a half-life of 4-6 hours.It is excreted partially by the kidneys and partly by metabolism to the inactive 4'-O-sulfate (phenolic sulfate), which is also excreted mainly in the urine. Only a small part of the administered dose of salbutamol is excreted with feces. Most of the dose of salbutamol administered intravenously, orally or by inhalation, is excreted within 72 hours.

Indications:1. Bronchial asthma:

- the purchase of attacks of bronchial asthma, including with exacerbation of bronchial asthma severe course;

- Preventing attacks of bronchospasm associated with exposure to an allergen or caused by physical exertion;

- use 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; preterm delivery; threatening abortion.

Carefully:Salbutamol 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.

Pregnancy and lactation:Fertility

Not studied.

Pregnancy

Pregnant women are prescribed a drug only if the expected benefit for the patient exceeds the potential risk to the fetus.

During post-registration observation, rare cases of various developmental malformations in children, including the formation of "wolf mouth" and developmental limbs, were detected, against the background of the intake of salbutamol by mothers during pregnancy. In some of these cases, mothers took several concomitant medications during pregnancy. Due to the lack of a permanent nature of defects and the background frequency of congenital anomalies, ranging from 2 to 3%, the cause-and-effect relationship with taking the drug has not been established.

Breastfeeding period

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

Dosing and Administration:The drug Ventolin is intended only for inhalation.

Increased need for beta agonists_2-adrenergic receptors 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 concurrent glucocorticosteroid therapy.

Since an overdose can be accompanied by the development of adverse events, the dose or multiplicity of the drug may be increased only on the advice of a doctor.

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 who receive the drug Ventolin, it is advisable to use a pediatric spacer device with a facial mask.

Curbing an attack of bronchospasm

Adults

The recommended dose is 100 or 200 μg.

Children

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

It is not recommended to use Ventolin inhaler more than four times a day. The need for frequent use of maximum doses of the drug Ventolin or in a sudden increase in dose indicates a worsening of the course of asthma (see section "Special instructions and precautions for use").

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

Adults

200 mcg for 10-15 min before exposure to a provoking factor or load.

Children

100 mcg for 10-15 min before exposure to a provoking factor or load, if necessary, the dose may be increased to 200 mcg.

Prolonged maintenance therapy

Adults

Up to 200 mcg 4 times a day.

Children

Up to 200 mcg 4 times a day.

INSTRUCTION FOR USE OF THE INHIBITOR

Checking the inhaler

Before the first use of the inhaler or,if the inhaler has not been used for 5 days or more, remove the cap from the mouthpiece, lightly squeezing the cap off the sides, shake the inhaler well and spray two into the air to ensure that the inhaler is working.

Use of an inhaler

1. Remove the cap from the mouthpiece by slightly squeezing the cap from the sides.

2. Inspect the inhaler inside and outside, including the mouthpiece, for any foreign objects.

3. Shake the inhaler thoroughly to remove any foreign objects and to evenly mix the contents of the inhaler.

4. Hold the inhaler between the index and thumb in an upright position with the bottom facing up, with the thumb on the base under the mouthpiece.

5. Exhale as deeply as you can, then place the mouthpiece in your mouth between your teeth and grasp it with your lips, without grasping your teeth.

6. While making the deepest inhalation through the mouth, simultaneously press the upper part of the inhaler to release one inhalation dose of the drug Ventolin.

7. Hold your breath, take the inhaler out of your mouth and remove your finger from the top of the inhaler, continue to hold your breath for as long as you can.

8.If you need to re-spray the drug, keep the inhaler in an upright position, wait about 30 seconds and then repeat steps 3-7.

9. Close the mouthpiece firmly with a protective cap.

IMPORTANT

Performing stages 5, 6 and 7 you can not hurry. It is important that you begin to inhale as slowly as possible immediately before pressing the inhaler. In the first few times it is recommended to practice before the mirror. If you see a "fog" coming from the top of the inhaler or from the corners of the mouth, then you should start all over again from stage 2.

If the doctor gave you other instructions for using the inhaler, then strictly observe them. Contact your doctor if you have difficulty using the inhaler.

Cleaning the inhaler

The inhaler should be cleaned at least once a week.

1. Remove the metal can from the plastic housing of the inhaler and remove the cover from the mouthpiece.

2. Thoroughly flush the valve under a stream of warm water.

3. Dry the valve thoroughly inside and out.

4. Place the metal can in the plastic casing and put the lid on the mouthpiece.

Do not put a metal can in the water.

Side effects:The adverse events presented below are listed in accordance with the damage to organs and organ systems and frequency of occurrence. Frequency of occurrence is defined as follows: very often (≥ 1/10), often (≥ 1/100 and <1/10), infrequently (≥ 1/1 000 and <1/100), rarely (≥ 1/10 000 and <1/1 000), very rarely (<1/10 000, including individual cases). Frequency categories were formed on the basis of clinical studies of the drug and post-registration surveillance.

Frequency of occurrence of undesirable phenomena

Immune system disorders

Very rarely: hypersensitivity reactions, including angioedema, hives, bronchospasm, hypotension and collapse.

Disorders from the metabolism and nutrition

Rarely: hypokalemia. Therapy beta₂ agonists can lead to clinically significant hypokalemia.

Disturbances from the nervous system

Often: tremor, headache. Very rarely: hyperactivity.

Heart Disease

Often: tachycardia. Infrequent: palpitation. Very rarely: arrhythmias, including atrial fibrillation; supraventricular tachycardia and extrasystole.

Vascular disorders

Rarely: peripheral vasodilation.

Disturbances from the respiratory system, chest and mediastinal organs

Very rarely: paradoxical bronchospasm. As with other agents for inhalation therapy, paradoxical bronchospasm may occur with increased wheezing immediately after treatment. This condition requires immediate treatment with the use of alternative forms of production, or other high-speed inhaled bronchodilator. Ventolin drug should be lifted immediately, assess the condition of the patient and, if necessary, appoint an alternative therapy.

Disorders from the gastrointestinal tract

Infrequent: irritation of the mucous membrane of the oral cavity and pharynx.

Disturbances from musculoskeletal and connective tissue

Infrequently: muscle cramps.

Overdose:Symptoms

Signs and symptoms of salbutamol overdose are transient phenomena, pharmacologically mediated stimulation of beta-adrenergic receptors (see. Sections "Special instructions and precautions for the use of" and "Side Effects"), such as lowering blood pressure, tachycardia, muscle tremors, nausea, vomiting .

The use of large doses of salbutamol can cause hypokalemia, it is necessary to monitor the potassium level in the serum.

Treatment

It is necessary to cancel the drug and prescribe appropriate symptomatic therapy, such as the use of cardioselective beta-adrenergic blockers in patients with cardiac symptoms (eg, tachycardia, palpitation). Blockers of beta-adrenergic receptors should be used with caution in patients with bronchospasm in the anamnesis.

Interaction:It is not recommended to apply simultaneously salbutamol and nonselective beta-adrenergic receptor blockers, such as propranolol.

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

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

Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias. Simultaneous administration with anticholinergics (including inhalation) may help increase intraocular pressure. Diuretics and glucocorticosteroids increase the hypokalemic effect of salbutamol.

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.

Increased demand for bronchodilators with short duration of action, in particular beta agonists₂-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 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 beta agonists₂-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 increase as a result of the simultaneous use of xanthine derivatives, corticosteroids, diuretics, and also due to hypoxia. In such situations it is recommended to monitor the potassium level in the blood serum.

If there is no effect of using an earlier effective dose of inhaled salbutamol for at least three hours, the patient should consult a doctor for any additional measures.

Patients should be instructed about the proper use of the Ventolin inhaler.

Effect on the ability to drive transp. cf. and fur:No data.

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

Packaging:For 200 doses in an aluminum inhaler equipped with a plastic dosing device with a protective cap. The inhaler and the metering device are assembled together with the instructions for use in a cardboard box.

Storage conditions:Store at a temperature of no higher than 30 ° C, do not freeze, do not expose to direct sunlight.

Keep out of the reach of children.

Shelf life:2 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014212 / 01

Date of registration:01.06.2010 / 20.04.2016

Expiration Date:Unlimited

The owner of the registration certificate:GlaxoSmithKline Trading, ZAO GlaxoSmithKline Trading, ZAO Russia

Manufacturer: & nbsp

GLAXO WELLCOME, S.A. Spain

GLAXO WELLCOME PRODUCTION France

GlaxoSmithKline Pharmaceuticals, S.A. Poland

Representation: & nbspGlaxoSmithKline Trading, ZAOGlaxoSmithKline Trading, ZAO

Information update date: & nbsp26.01.2017

Illustrated instructions

Instructions

Ventolin® (Ventolin®)