2010/12/12

Atimos

Release form, composition and packing

Aerosol inhalation dose in the form of colorless or slightly yellow transparent solution. 1 dose of formoterol fumarate 12 mcg Excipients: ethanol, hydrochloric acid, norfluran (1,1,1,2-tetrafluoroethane).

Clinico-pharmacological group: bronchodilator medication - beta 2-adrenoceptor agonists.

Pharmacological action

Bronchodilatory drug, a selective agonist of β2-adrenoretsepterov with low affinity for the β1-adrenoreceptors.

The mechanism of action is associated with activation of adenylyl cyclase, which leads to an increase in cyclic AMP (cAMP), which causes the activation of protein kinase A. Activated protein kinase A inhibits the phosphorylation of key proteins responsible for the control of smooth muscle tone.

Increasing intracellular cAMP also leads to suppression of release of calcium ions from the depot. The totality of these processes leads to a bronchodilator effect.

Effect of the drug occurs quickly and persists for a long time.

Formoterol effective in preventing bronchospasm caused by inhaled allergens, exercise, cold air, histamine or methacholine.

Pharmacokinetics

Absorption and distribution

About 90% of the drug after inhalation application can swallow. After oral administration, rapidly absorbed from the gastrointestinal tract. Cmax formoterol in blood plasma is 60% after 15 minutes after application and decreased to 10% at 24 h after application.

Distribution

The binding of formoterol from plasma proteins is 50-65%.

Metabolism and Elimination

Formoterol being metabolized by the direct connection of the balance of glucuronic acid and O-demethylation. The active substance and its metabolites are completely eliminated from the body: 36-45% is excreted in urine, 50-56% - in the feces within 72 hours after application. T1 / 2 at 4 h after iv injection and 6 h - after ingestion.

Statement
Prevention and treatment of bronchospasm in patients with asthma;
Prevention and treatment of bronchospasm caused by allergens, exercise or cold air;
Prevention and treatment of bronchial obstruction in patients with COPD.

Dosing regimen

Adults, including elderly patients for treatment and prevention of asthma appoint 12-24 mg (1-2 doses), 2 times per day. If required, for relief of symptoms can enter 1 or 2 additional doses throughout the day. The need for more frequent use of the drug for additional doses (eg, more than 2 days per week) is indicative of worsening asthma. In this case, the patient should consult a doctor to review treatment.

Children aged 6 years and older prescribed to 12 mg (1 dose) 2 times / day.

For the prevention of bronchospasm caused by exercise or unavoidable exposure to known allergens appointed to 12 mg (1 dose) 15 minutes before provocation. Patients with severe asthma may require 2 doses of 12 micrograms.

Method of application

Before the first application (or if the inhaler is not used within 3 days or more) should remove the protective cap from the mouthpiece and make spray 1 time into the air to make sure that the inhaler works.
Get inhaler thumb and forefinger, remove the cap from the inhaler mouthpiece.
Take the mouthpiece in your mouth, tightly clasping his lips, and exhale completely through your nose.
Slowly and deeply inhale while pushing on the end of the balloon forefinger. After inhalation should be as long as possible to hold your breath. To maintain the purity of the mouthpiece is recommended to wash it with warm water from pollution.

Use of the drug in children should be supervised by adults. It is recommended to prevent inhaling through the nose during inhalation pinch the nostrils of the child.

Side effect

Estimate the incidence of side effects: sometimes - 0.1-1%, rare - 0.01-0.1%.
From the musculoskeletal system: sometimes - tremor, rarely - muscle aches, muscle cramps.
With the cardiovascular system: sometimes - palpitations, rarely - tachycardia, decreased blood pressure.
CNS and peripheral nervous system: sometimes - headache, rarely - excitement, dizziness, anxiety, nervousness, insomnia.
Part of the respiratory system: sometimes - cough, rarely - paradoxical bronchospasm.

Local reactions: seldom - irritation of the oropharynx.

Allergic reactions: itching, urticaria, angioedema.
From the digestive system: nausea, dry mouth, taste changes.

Other: Sometimes - weakness, possibly a rash, hypokalemia. Risk of side effects may be reduced if strict adherence to dosing regimen.

Contraindications
tachyarrhythmia;
AV-block III degree;
idiopathic subaortalny stenosis;
hypertrophic obstructive cardiomyopathy;
hyperthyroidism;
lengthening the interval QT (QTc> 0.44 sec);
Children under the age of 6 years;
lactation;
Hypersensitivity to formoterol or other ingredients.

Precautions should be used in the preparation for coronary artery disease, exacerbation of hypertension, cardiac arrhythmias, congestive heart failure at the stage of decompensation, diabetes, prostate enlargement, glaucoma, pregnancy.

Pregnancy and lactation

Health & Safety Atimosa during pregnancy and lactation has not been established. Use of the drug during pregnancy only in cases where the expected benefits of therapy to the mother justifies the potential risk to the fetus. No data on the allocation of formoterol with breast milk in humans. If necessary, use during lactation breastfeeding should be discontinued.

Cautions

If you need regular treatment with inhaled adrenomimetikami, patients with asthma should receive systemic anti-inflammatory treatment. Consequently, if the prescribed treatment Atimosom should evaluate the need for the appointment of anti-inflammatory therapy.

When patients are already receiving this treatment (inhaled or oral corticosteroids), it must continue without any change, even if there is improvement in symptoms. Preservation of asthma symptoms or the need to increase the dose Atimosa may indicate a worsening of bronchial asthma and the need for revision of treatment.

Special caution is required when selecting the dose Atimosa to treat patients with such comorbidities as coronary artery disease, myocardial infarction, exacerbation of hypertension, cardiac arrhythmia, chronic heart failure, diabetes, prostatic hyperplasia, glaucoma. Due to glucagon action of beta2-agonists in patients with diabetes need additional control over the content of glucose in the blood. Potentially treated beta2-adrenomimetikami may cause hypokalemia. This action can be enhanced by hypoxia and concomitant treatment, so extreme caution should be exercised in patients suffering from bronchial asthma. Under these conditions, it is recommended to monitor potassium levels in blood plasma.

In applying Atimosa (as well as during other inhalation therapy) may develop paradoxical bronchospasm. In this case, you should immediately remove the drug and to appoint an alternate treatment.

It is recommended to strictly follow the recommended dosing regimen to avoid serious side effects, primarily from the cardiovascular system. Atimos contains a small amount of ethanol - less than 100 mg / 1 dose.

Using the drug is not for medical purposes is regarded as doping: the drug causes the doping effect and gives a positive reaction to a doping test. Effects on ability to drive vehicles and management mechanisms Adverse effects, in the case of their occurrence, may affect the ability to drive vehicles or operate machinery.

Overdose

Symptoms: nausea, vomiting, headache, tremor, drowsiness, feeling of palpitation, tachycardia, ventricular fibrillation, low / high blood pressure, metabolic acidosis, hypokalemia, hyperglycemia.

Treatment: it is shown holding a symptomatic therapy, in severe cases - hospitalization. Can be considered the use of cardioselective beta-blockers, subject to extreme caution, because these funds can cause bronchospasm.

Drug Interactions

I antiarrhythmic drugs of class A (quinidine, disopyramide, novokainamid) and class III (sotalol, amiodarone), phenothiazines, antihistamines, MAO inhibitors, tricyclic antidepressants, erythromycin for iv injection, pentamidine, sultoprid, vancomycin, galofantrin, bepridil may lengthen QT interval and increase the risk of ventricular arrhythmias (including arrhythmias such as "pirouette"). The simultaneous use of other adrenergic agents may exacerbate the side effects Atimosa.

Simultaneous treatment with xanthine derivatives, corticosteroids or diuretics may increase the potential gipokaliemicheskoe effect of beta2-agonists.