Onbrez breezhaler® [Indacaterol]
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Onbrez Breezhaler - indacaterol is a selective agonist of long-acting β2-adrenoreceptors (for 24 hours) in a single dose. The pharmacological action of β2-adrenoreceptor agonists, including indacaterol, is associated with the stimulation of intracellular adenylate cyclase, an enzyme that catalyzes the conversion of ATP to cyclic 3 ', 5'-adenosine monophosphate (cyclic AMP). Increasing the content of cyclic AMP leads to relaxation of the smooth muscles of the bronchi. Indacaterol is a nearly complete β2-adrenoreceptor agonist; The stimulating effect of the drug on β2-adrenoreceptors is 24 times stronger than on β1-adrenoreceptors, and 20 times stronger than β3-adrenergic receptors.
After inhalation, the drug has a rapid and prolonged bronchodilatory effect.
Indacaterol provides a persistent, significant improvement in lung function (increased forced expiratory volume in the first second, FEV1) for 24 hours. The drug is characterized by a rapid onset of action (within 5 minutes after inhalation), comparable to the effect of salbutamol, a short-acting β2 adrenoreceptor agonist. The maximum effect of indacaterol is noted 2-4 hours after inhalation. In patients who received indacaterol for 1 year, there was no development of tachyphylaxis to the bronchodilatory effect of the drug. When using indacaterol, there was no dependence of the bronchodilating effect on the time of inhalation of the drug during the day (morning or evening).
Indacaterol reduces dynamic and static hyperinflation (an increase in lung volumes at the end of spontaneous expiration) in patients with moderate and severe COPD. When using the drug, there is a statistically significant increase in inspiratory capacity and FEV1, a decrease in shortness of breath, and an improvement in exercise tolerance. There is also a significant reduction in the risk of COPD exacerbations (an increase in time until the next exacerbation), a decrease in the need for short-acting β2-adrenoreceptor inhalation agonists and an improvement in the quality of life of patients (assessed using a certified questionnaire at St. George's Hospital).
Long-term maintenance therapy of bronchial obstruction in patients with COPD.
1 capsule contains indacaterol maleate 300 mcg.
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Dosage and Administration
For inhalation use only!
The drug is a capsule with powder for inhalation, which should be used only for inhalation through the mouth using a special device - Brizhalera, which is included in the kit. The drug can not be taken orally. Capsules with powder for inhalation should be stored in a blister and removed from it immediately before use. Inhalation of the drug is carried out daily 1 time / day at the same time. In the case of inhalation, the next day, the drug Onbrez breezhaler is used at the usual time.
The recommended dose of the drug is 150 mcg (content of 1 capsule 150 mcg) 1 time / day (1 inhalation per day). The dose of the drug can be increased only on the recommendation of a doctor.
Inhalation of the drug in a dose of 300 mcg (1 capsule 300 mcg contents) 1 time / day may provide additional clinical effect in some patients, for example, in patients with severe COPD.
The maximum dose - 300 mcg (contents of 1 capsule 300 mcg) 1 time / day (1 inhalation per day). The maximum allowed dose of the drug can not be exceeded.
No dose adjustment is required in patients aged 65 and older, patients with mild and moderate hepatic and renal dysfunction.
When using the drug in therapeutic doses, the following adverse events were most often noted: nasopharyngitis, cough, upper respiratory tract infections and muscle spasms. Most of the above adverse events were mild or moderate severity, the incidence of these adverse events decreased with further use.
Below are the undesirable effects observed with the use of the drug in doses of 150 and 300 mg 1 time / day. in patients with COPD. Undesirable reactions are distributed according to the frequency of occurrence. The following criteria were used to estimate the frequency: very often (≥1 / 10); often (≥1 / 100,
Infections and invasions: often - nasopharyngitis, upper respiratory tract infections, sinusitis.
On the part of the respiratory system: often - cough, sore throat, rhinorrhea.
On the part of the musculoskeletal system: often - muscle spasm, myalgia, bone pain.
On the part of the nervous system: infrequently - dizziness, paresthesia.
Since the cardiovascular system: often - IHD; infrequently - atrial fibrillation.
On the part of the digestive system: often - dry mouth.
Metabolic disorders: often - hyperglycemia / newly diagnosed diabetes mellitus.
General disorders: often - peripheral edema, pain in the chest (non-cardiogenic); infrequently - discomfort in the chest.
When using the drug in a dose of 600 mcg 1 time / day., The safety profile did not significantly differ from that during inhalation of therapeutic doses (150 and 300 mcg 1 time / day.). Additional adverse events were anemia and tremor. Muscle cramps and nasopharyngitis were also detected more frequently. In patients with COPD with inhalation at recommended doses, the drug does not have a clinically significant systemic β2-adrenomimetic effect. The average heart rate changed by no more than 1 beats / min. The incidence of tachycardia (noted in rare cases), a significant lengthening of the QTc interval (> 450 ms for men and> 470 ms for women) and hypokalemia was similar to placebo.
Plasma glucose concentrations were similar to those in the placebo group.
In clinical studies, within 15 seconds after inhalation of the drug in patients (in 17-20% of cases), sporadic cough development was observed with a duration of about 5 seconds. The occurrence of cough after inhalation of Onbrez Breezhaler slightly worried patients and did not require discontinuation of treatment with the drug (since cough is a symptom of COPD, and only in 6.6% of cases did patients cough with the use of the drug).There was no association between the cough observed immediately after the inhalation of the drug and the development of bronchospasm, exacerbation of COPD, worsening of the course of COPD and a decrease in the effectiveness of the drug.
- age up to 18 years (efficacy and safety have not been established);
- breastfeeding period;
- Hypersensitivity to any of the components of the drug.
Drugs that extend the QT interval
As with the use of other β2-adrenoreceptor agonists, prolongation of the QT interval is possible during drug therapy. Since this effect of indacaterol on the length of the QT interval can be potentiated by other drugs, Onbrez® Brizhaler® should be used with caution in patients receiving MAO inhibitors, tricyclic antidepressants, or other drugs that prolong the QT interval. Lengthening the QT interval increases the risk of developing ventricular arrhythmias.
The simultaneous use of indacaterol with sympathomimetics (both separately and as part of combination therapy) may increase the risk of developing adverse events.
The drug should not be used simultaneously with other long-acting β2-adrenoreceptor agonists or with drugs that include long-acting β2-adrenoreceptor agonists.
Concurrent use with methylxanthine derivatives, GCS, or potassium-infusing diuretics may enhance the potential hypokalemia caused by β2-adrenoreceptor agonists.
Since β2-adrenoreceptor blockers can weaken the effect or inhibit the action of β2-adrenoreceptor agonists, Onbrez® Bryzhaler® should not be used simultaneously with β2-adrenoreceptor blockers (including eye drops).
If necessary, the use of both classes of drugs, it is preferable to use cardioselective blockers of β2-adrenergic receptors, however, they must be used with caution.
Interaction at the level of isoenzyme CYP3A4 and membrane transporter P-glycoprotein
The interaction of indacaterol with specific inhibitors of the isoenzyme CYP3A4 and P-glycoprotein, such as ketoconazole, erythromycin and verapamil, has been studied.
The simultaneous use of indacaterol with verapamil resulted in a 1.4–2 fold increase in AUC and a 1.5 fold increase in Cmax. When indacaterol was administered with erythromycin, the AUC increased 1.4–1.6 times and Cmax increased 1.2 times. Combination therapy with indacaterol and ketoconazole caused a 2-fold and 1.4-fold increase in AUC and Cmax, respectively. This increase in exposure due to drug interactions did not change the safety profile.
When using indacaterol with other drugs, no drug interactions were observed. In vitro studies have shown that indacaterol has little potential for interaction with drugs at the metabolic level of enzymes or at the level of membrane transporters with systemic exposure achieved when prescribing therapeutic doses.
Due to the lack of data on the long-term use of indacaterol in patients with bronchial asthma, the drug should not be used in this category of patients.
Like any other inhalation therapy, the use of the drug can lead to the development of paradoxical bronchospasm, which represents a threat to the patient's life. In the event of a paradoxical bronchospasm treatment with the drug should be immediately discontinued and alternative therapy prescribed.
Deterioration of the underlying disease
The drug should not be used for the relief of acute bronchospasm, i.e. Do not use as emergency treatment.In the event of a deterioration in the course of COPD during treatment with a drug, it is necessary to reassess the patient’s condition and review the treatment regimen for the disease.
Effect on the cardiovascular system
In some patients, Onbrez® Brizhaler®, like other β2-adrenoreceptor agonists, may affect the cardiovascular system (increase heart rate, blood pressure). In the event of adverse events, it may be necessary to discontinue drug therapy. In addition, when using β2-adrenoreceptor agonists, the following electrocardiographic changes may occur: flattening of the T wave, lengthening of the QT interval and depression of the ST segment (however, the clinical significance of these changes has not been established).
When using the drug in clinical studies (at the recommended therapeutic doses), there was no significant lengthening of the QT interval compared with placebo.
In some patients, when using β2-adrenoreceptor agonists, significant hypokalemia may occur, leading to the development of adverse events on the part of the cardiovascular system. A decrease in serum potassium concentration is usually transient and does not require correction. In patients with severe COPD, hypokalemia may be enhanced by hypoxia and concomitant therapy, which, in turn, may increase the likelihood of developing arrhythmias.
When inhaling high doses of β2-adrenoreceptor agonists, plasma glucose levels may increase. When using the drug in patients with diabetes should regularly monitor the concentration of glucose in the blood plasma. In clinical studies in patients receiving the drug (in recommended doses), there was an increase in the incidence of clinically significant hyperglycemia by an average of 1-2% compared to placebo. The efficacy and safety of the drug in patients with uncompensated diabetes mellitus has not been studied.
Influence on ability to drive motor transport and control mechanisms
There is no data on the effect of the drug Onbrez breezhaler on the ability to drive vehicles and work with mechanisms.
Symptoms: After a single use of the drug Onbrez breezhaler in patients with COPD at a dose 10 times higher than the maximum therapeutic, there was a moderate increase in heart rate, increased blood pressure and lengthening of the QTc interval.
The most likely symptoms of drug overdose are tachycardia, tremor, heartbeat, headache, nausea, vomiting, drowsiness, ventricular arrhythmia, metabolic acidosis, hypokalemia and hyperglycemia (caused by increased systemic beta-2 adrenomimetic action).
Treatment: supportive and symptomatic therapy is indicated. In severe cases, patients should be hospitalized. If necessary, the use of cardioselective beta-blockers is possible. Cardioselective beta-blockers should be used with caution, only under strict medical supervision, because their use can provoke the development of bronchospasm.
- Brand name: Onbrez breezhaler
- Active ingredient: Indacaterol
- Dosage form: Capsules with powder for inhalation.
- Manufacturer: Novartis
- Country of Origin: Switzerland
- Characterization of the bronchodilatory dose response to indacaterol in patients with chronic obstructive pulmonary disease using model-based approaches
- Cardiac safety of indacaterol in healthy subjects: a randomized, multidose, placebo- and positive-controlled, parallel-group thorough QT study
- Indacaterol, a novel inhaled, once-daily, long-acting beta2-agonist for the treatment of obstructive airways diseases
- Erratum to: Indacaterol, a novel inhaled, once-daily, long-acting beta2-agonist for the treatment of obstructive airways diseases
- Indacaterol provides sustained 24 h bronchodilation on once-daily dosing in asthma: a 7-day dose-ranging study
- The long-acting β-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells
- Pharmacogenetic characterization of indacaterol, a novel β2-adrenoceptor agonist
- Indacaterol : a new long-acting β2-agonist in the management of chronic obstructive pulmonary disease
- Indacaterol: A Novel Long-Acting β2-Agonist
- Indacaterol: a long-acting beta2- agonist taken once daily
- Efficacy and Tolerability of Indacaterol 75 μg Once Daily in Patients Aged ≥40 Years With Chronic Obstructive Pulmonary Disease: Results From 2 Double-Blind, Placebo-Controlled 12-Week Studies
- Lipid membrane interactions of indacaterol and salmeterol: Do they influence their pharmacological properties?
- Validation of an on-line solid-phase extraction method coupled to liquid chromatography–tandem mass spectrometry detection for the determination of Indacaterol in human serum
- Indacatérol en 1 prise/j : méthodologie d’une analyse par classes d’âge (données poolées) et caractéristiques des patients
- Efficacité de l’indacatérol en 1 prise/j chez le sujet âgé de 65 ans et plus (données poolées)
- Tolérance de l’indacatérol en 1 prise/j chez le sujet âgé de 65 ans et plus (données poolées)
- Indacaterol provides 24-hour bronchodilation in COPD: a placebo-controlled blinded comparison with tiotropium
- Efficacy and safety of indacaterol 150 and 300 µg in chronic obstructive pulmonary disease patients from six Asian areas including Japan: A 12-week, placebo-controlled study
- Safety, tolerability and efficacy of indacaterol, a novel once-daily β2-agonist, in patients with COPD: A 28-day randomised, placebo controlled clinical trial
- Bronchodilator effects of indacaterol and formoterol in patients with COPD
- Integrating indacaterol dose selection in a clinical study in COPD using an adaptive seamless design
- Sustained 24-hour efficacy of once daily indacaterol (300 μg) in patients with chronic obstructive pulmonary disease: A randomized, crossover study
- Safety and tolerability of indacaterol in asthma: A randomized, placebo-controlled 28-day study
- A dose-ranging study of indacaterol in obstructive airways disease, with a tiotropium comparison