2010/06/22

Ventolin



Composition, structure and packing

Aerosol metered dose for inhalation as a suspension of white or nearly white. 1 dose of salbutamol sulphate 120.5 mg which corresponds to the content of salbutamol 100 micrograms. Excipients: propellant 1,1,1,2-tetrafluoroethane (HFA 134a) does not contain chlorofluorocarbons. .

Clinico-pharmacological group: bronchodilators product - beta2-adrenomimetics.

Pharmacological action

Selective beta2-adrenomimetics. At therapeutic doses, acts on the β2-adrenergic receptors of smooth muscles of the bronchi, providing little effect on β1-adrenergic receptors infarction. Salbutamol inhibits the release of mast cell histamine, leukotrienes, prostaglandin D2, and other biologically active substances for a long time. Inhibits early and late bronchial reactivity. Has pronounced bronchodilatory effect, preventing or kupiruya bronchospasm, reduces the resistance in the airways. Increases vital capacity.

Increases mucociliary clearance (with chronic bronchitis and 36%), stimulates mucus secretion, activates the function of ciliated epithelium. Hinders release of inflammatory mediators from mast cells and basophils, in particular the release of histamine induced by antibodies to immunoglobulin E, eliminates the suppression of antigen mucocilliary transport and separation factor of chemotaxis of neutrophils.

Prevents the development of allergen-induced bronchospasm. Can lead to a decrease in the number of β1-adrenergic receptors, including on lymphocytes. It has a number of metabolic effects: reduces the concentration of potassium in the plasma affects glycogenolysis and insulin release, has a hyperglycemic (especially in patients with bronchial asthma) and the lipolytic effect, increases the risk of acidosis.

Pharmacokinetics

Absorption and metabolism

After inhalation of salbutamol 10-20% of the dose reaches the lower respiratory tract. The remainder of the dose remains in the inhaler, or deposited in the oropharynx and then swallowed.

The fraction deposited in the airways, absorbed in the lung tissue and blood, but is not metabolized in the lungs. Swallowed portion of an inhalation dose is absorbed from the gastrointestinal tract and is subjected to intensive metabolism in the "first pass" through the liver, becoming inactive 4'-O-sulphate (phenolic sulphate).

Distribution

Linking calbutamola to plasma proteins is 10%.

Withdrawal

When i / in the introduction of T1 / 2 of salbutamol is 4-6 hours Unchanged salbutamol and conjugate are excreted primarily in urine. Since feces displayed only a fraction of the administered dose of salbutamol. Most of the dose of salbutamol, introduced in the body in / in, inside, or by inhalation displayed within 72 hours

Statement

Asthma:
relief of asthma attacks, including during exacerbation of asthma severe course;
preventing attacks of bronchospasm associated with exposure to an allergen or due to physical activity;
used as a component for long-term maintenance treatment of bronchial asthma.

Chronic obstructive pulmonary disease (COPD), accompanied by reversible airway obstruction, including chronic bronchitis and emphysema of the lungs.

Dosage regimen

Metered Aerosol Ventolin is intended only for inhalation. To solve the issue of increasing the dose or frequency of use of the drug can only be a doctor. Not recommended for use Ventolin often 4 times / day. The need for frequent use Ventolin in the maximum doses or in a sudden increase in dose indicates deteriorating course of the disease. Adults (including elderly patients). Cupping bronchospasm: the recommended dose is 100-200 mcg (1-2 inhalations).

Preventing attacks of bronchospasm associated with exposure to an allergen or caused by physical stress: the recommended dose is 200 mcg (2 inhalations) for 10-15 minutes before exposure to a provoking factor. Long-term maintenance therapy: The recommended dose is 200 mcg (2 inhalations) 4 times / day. Ventolin, you can enter through the spacer Volyumatik.

Children cupping bronchospasm: the recommended dose is 100-200 mcg (1-2 inhalations). Preventing attacks of bronchospasm associated with exposure to an allergen or caused by physical stress: the recommended dose is 100-200 mcg (1-2 inhalations) for 10-15 minutes before exposure to a provoking factor. Long-term maintenance therapy: The recommended dose is 200 mg (2 inhalations) 4 times / day. Ventolin, you can enter through the spacer Bebihaler or Volyumatik.

Side effect

Allergic reactions: seldom - angioedema, urticaria.
From the side of the central nervous system: often - tremor, headache, and very rarely - hyperactivity.
Since the cardiovascular system: often - tachycardia is very rare - arrhythmia, supraventricular tachycardia, extrasystoles, increased peripheral vascular diseases.
On the part of the respiratory system: very rarely - bronchospasm.
On the part of the digestive system: rarely - irritation of the mucous membrane of the oral cavity and pharynx.
On the part of the musculoskeletal system: rarely - muscle cramps.
On the part of metabolism: rarely - hypokalemia.

Contraindications
management of preterm labor;
threatened abortion;
Children under 2 years
Hypersensitivity to any component of the drug.

Pregnancy and lactation

During pregnancy and lactation drug prescribed only in cases where the expected benefit to the mother than any possible risk to the fetus. Salbutamol is likely to penetrate into breast milk.

Data to know whether present in breast milk salbutamol harmful effect on the newborn, no. Cautions should instruct the patient about the proper use of inhaler Ventolin. Bronchodilators should not be the sole or main component of bronchial asthma or severe unstable flow.

If the action is the usual dose of Ventolin becomes less effective or less long (drug effect persists at least 3 h), the patient should consult a doctor. Increasing demand for use of inhaled β2-adrenoceptor agonist with a short duration of action for the control of asthma symptoms reflecting the worsening of the disease. In such cases, should review the treatment plan.

Sudden and progressive deterioration of bronchial asthma may pose a threat to the patient's life, so in these situations need to urgently address the issue of the appointment or increasing the dose of GCS. In such patients is recommended for daily monitoring of peak velocity of exhalation. With careful use the drug in patients with thyrotoxicosis. Therapy β2-adrenoceptor agonists, especially when they are introduced parenterally or by nebulizer, can lead to hypokalaemia.

Particular caution should be exercised when treating severe asthma attacks, because in these cases, the hypokalemia may be exacerbated by the simultaneous application of xanthine derivatives, SCS, diuretics, and also due to hypoxia. In such situations need to monitor potassium levels in blood serum.

Effects on ability to drive vehicles and management mechanisms

Data on the effect on the ability to drive motor vehicles and / or other mechanisms are absent.

Overdose

Symptoms: possible hypokalemia.

Treatment: for suspected overdose should monitor the level of potassium in the blood serum. Antidotes are cardioselective beta-blockers. However, β-adrenoceptor blockers should be used with caution in patients with a history of attacks of bronchospasm.

Drug Interactions

It is not recommended to use both salbutamol and nonselective β-adrenoceptor blockers such as propranolol. Salbutamol is not contraindicated in patients who are receiving MAO inhibitors.

Terms and conditions of storage

The drug should be stored at a temperature below 30 ° C. Shelf life - 2 years. Inhaler should not be frozen and exposed to direct sunlight.