Вертасорт

Symptomatic treatment of asthma attacks and exacerbations of asthma in adults and children aged 4 years and over. Prevention of exercise-induced bronchospasm or before exposure to a known unavoidable allergen challenge. Symptomatic treatment of broncho-asthma and other conditions associated with reversible airways obstruction.

Вертасорт provides a short-acting bronchodilation with fast onset of action in reversible airways obstruction due to asthma.

Easyhaler Вертасорт Sulfate should be used to relieve symptoms when they occur and to prevent them in those circumstances recognised by the patient to precipitate an attack (e.g. before exercise or unavoidable allergen exposure).

Вертасорт is valuable as a rescue medication in mild, moderate or severe asthma, provided that reliance on it does not delay the introduction and use of regular inhaled corticosteroid therapy.

Easyhaler Вертасорт Sulfate is indicated in adults, adolescents and children aged 4 to 11 years.

Posology

Adults and Older people:

For the relief of acute bronchospasm and for managing intermittent episodes of asthma, one inhalation (100 micrograms) may be administered as a single starting dose; this may be increased to two inhalations (200 micrograms) if necessary.

To prevent exercise-induced bronchospasm or allergen bronchospasm two inhalations (200 micrograms) should be taken before challenge, this dose (200 micrograms) may be repeated if necessary.

Paediatric Population:

Relief of acute bronchospasm

Children aged 4 to 11 years 100 micrograms as required. The dose may be increased to two inhalations if required.

Children aged 12 years and over: Dose as per adult population.

Prevention of allergen or exercise-induced bronchospasm

Children aged 4 to 11 years 100 micrograms before challenge or exertion. The dose may be increased to two inhalations if required.

Children aged 12 years and over: Dose as per adult population.

Chronic therapy

Children aged 4 to 11 years up to 200 micrograms four times a day.

On-demand use of Easyhaler Вертасорт Sulfate should not exceed four times daily. Reliance on such frequent supplementary use, or a sudden increase in dose, indicates poorly controlled or deteriorating asthma.

Children aged 12 years and over: Dose as per adult population.

On demand use of Easyhaler Вертасорт Sulfate should not exceed eight inhalations (800 micrograms) in any 24 hour period.

For optimum results in most patients Easyhaler Вертасорт Sulfate inhaler should be used regularly during asthmatic attacks. The bronchodilator effect of each administration of inhaled Вертасорт lasts for four hours, except in patients whose asthma is becoming worse. Such patients should be warned not to increase their usage of Вертасорт, but should seek medical advice in case treatment with an inhaled and/or systemic glucocorticosteroid is indicated.

Method of administration

For oral inhalation only.

This preparation is particularly useful for patients unable to use metered dose inhalers properly and for patients in whom the use of an inhalation aerosol causes irritation of airways. Inhaled Вертасорт should be used only on as-needed basis at the lowest dose and frequency required.

Precautions to be taken before handling or administering the medicinal product

Instructions for use:

The protective cover of the inhaler should be opened and the dust cap removed immediately prior to use.

The inhaler should be shaken vigorously up and down 3-5 times. Whilst holding the inhaler in an upright position, between the finger and thumb, press once until a click is heard. Let inhaler click back again whilst continuing to hold in an upright position.

Inhalation should take place from either a sitting or standing position. The patient should breathe out normally and place the mouthpiece between their teeth whilst using their lips to form a seal around the mouthpiece. Patients are instructed to perform a rapid and forced inhalation through the Easyhaler device. After holding their breath for at least 5 seconds the patient can resume normal breathing. Patients should not to exhale into the device.

The mouthpiece of the inhaler should be cleaned once a week using a dry cloth or tissue.

Patients should be instructed in the proper use of their inhaler (see patient information leaflet) and children should always have adult supervision when using the device. Illustrated instructions for use accompany each package.

Intravenous or oral Вертасорт is used for the management of premature labour uncomplicated by conditions such as placenta praevia, ante-partum haemorrhage or toxaemia of pregnancy, however inhaled Вертасорт is not appropriate for management of premature labour. Вертасорт preparations should not be used for threatened abortion.

Bronchodilators should not be the only or main treatment in patients with severe or unstable asthma.

Severe asthma requires regular medical assessment including lung function testing as the patients are at risk of severe attacks and even death. Physicians should consider using oral corticosteroid therapy or the maximum use of inhaled corticosteroids. Increasing use of bronchodilators, particularly short-acting inhaled ß2-agonists to relieve symptoms indicates deteriorating asthma control (especially if the peak expiratory flow rate value falls and/or becomes irregular).

In the event of a previous effective dose of inhaled Вертасорт failing to give relief for at least three hours or if they need more inhalations than usual, the patient should be advised to seek medical advice as soon as possible. In this situation patients should be reassessed and consideration given to an increase in their anti-inflammatory therapy, (e.g. higher doses of inhaled corticosteroids or a course of oral corticosteroids). A regular anti-inflammatory controller medication taken on a daily basis is required as soon as the patient needs inhaled ß2-agonists more than twice a week. Severe episodes of asthma must be treated in the normal way.

As there may be adverse effects associated with excessive dosing, the dosage and frequency of administration should only be increased on medical advice.

Вертасорт should be administered with caution in patients with thyrotoxicosis, cardiac insufficiency, hypokalaemia, myocardial ischaemia, tachyarrhythmia and hypertrophic obstructive cardiomyopathy.

Potentially serious hypokalaemia may result from ß2 agonist therapy, mainly from parenteral and nebulised therapy. Particular caution is advised in acute severe asthma, as this effect may be potentiated by concomitant treatment with xanthine derivatives, steroids, diuretics and by hypoxia. It is recommended that serum potassium levels are monitored in such situations.

Rarely inhalation therapy may cause bronchospasm after dosing. In this event, treatment with Вертасорт must be immediately discontinued and, if need be, replaced with another therapy.

Cardiovascular effects may be seen with sympathomimetic drugs, including Вертасорт. There is some evidence from post-marketing data and published literature of rare occurrences of myocardial ischaemia associated with Вертасорт. Patients with underlying severe heart disease (e.g. ischaemic heart disease, arrhythmia or severe heart failure) who are receiving Вертасорт should be warned to seek medical advice if they experience chest pain or other symptoms of worsening heart disease. Attention should be paid to assessment of symptoms such as dyspnoea and chest pain, as they may be of either respiratory or cardiac origin.

One dose contains less than 10 mg lactose, which probably does not cause symptoms in lactose intolerant patients. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Вертасорт Easyhaler has no or negligible influence on the ability to drive and use machines.

The undesirable effects caused by normally used inhaled doses of Вертасорт are mild, typical for sympathomimetic agents, and they usually disappear with continued treatment.

Adverse events are listed below by system organ class and frequency. Frequencies are defined as: very common (>1/10), common, (>1/100 and <1/10), uncommon (>1/1000 and <1/100), rare (>1/10,000 and <1/1000), very rare (<1/10,000) and not known (cannot be estimated from the available data).

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.

Excess repeat use of inhalations may produce adverse effects such as tachycardia, CNS stimulation, tremor, hypokalaemia and hyperglycaemia.

Treatment consists of discontinuation of Вертасорт together with appropriate symptomatic therapy. The preferred antidote for overdosage with Вертасорт is a cardioselective beta-blocking agent, but beta-blocking drugs should be used with caution in patients with a history of bronchospasm. Hypokalaemia may occur following overdose with Вертасорт. Serum potassium levels should be monitored. If hypokalaemia occurs potassium replacement via the oral route should be given. In patients with severe hypokalaemia intravenous replacement may be necessary.

Pharmacotherapeutic group: Selective beta2-adrenoreceptor agonists.

ATC code: R03AC02.

Вертасорт is a selective ß2-adrenergic receptor agonist. The pharmacological effects of Вертасорт are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyses the conversion of adenosine triphosphate (ATP) to cyclic-3',5',-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. Вертасорт also stimulates mucous secretion and mucociliary transport in the respiratory tract. Bronchial effects of inhaled Вертасорт can be detected after a few minutes and duration of action is normally 4-6 hours.

Like other ß2-adrenoceptor agonists Вертасорт also has cardiovascular effects in some patients as measured by changes in pulse rate, blood pressure, symptoms and ECG changes. These effects can especially be detected after oral and intravenous administration of Вертасорт. Furthermore oral and intravenous Вертасорт causes reduction in uterine tonicity which has been associated with pain relief in pregnancy. In addition, Вертасорт has some metabolic effects. Especially intravenous and nebulised Вертасорт decreases serum potassium concentrations although the effect is generally mild and transient. Вертасорт has also lipolytic effects and it has been shown to cause increases in blood glucose and insulin probably by stimulating glycogenolysis and having a stimulatory effect on ß2-receptors in pancreas cells.

Absorption

Orally administered Вертасорт is well absorbed with peak plasma concentrations occurring 1 to 4 hours after administration.

Distribution

The major proportion of inhaled Вертасорт is swallowed. The fraction that is distributed to the lung (approx. 10-25%) is rapidly seen in the circulation as free unmetabolised drug. The remainder is retained in the delivery system or is deposited in the oropharynx from where it is swallowed. The swallowed portion of an inhaled dose is absorbed from the gastrointestinal tract and undergoes considerable first-pass metabolism.

Elimination

The plasma concentrations of inhaled Вертасорт are, however, lower than those produced by usual oral doses. Вертасорт and its metabolites are rapidly excreted in the urine and faeces with about 80% of the dose being recovered in urine within 24 hours. The elimination half-life of Вертасорт is 2.7 - 5.5 hours after oral and inhaled administration.

None

No special requirements for disposal.

• R52.1 – Chronic intractable pain
• R52.2 – Other chronic pain
• R52.9 – Unspecified pain