Onbrez Breezhaler
Onbrez Breezhaler: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Onbrez Breezhaler
ATX code: R03AC18
Active ingredient: indacaterol (Indacaterol)
Producer: Novartis Pharma Stein, AG (Novartis Pharma Stein, AG) (Switzerland)
Description and photo update: 2019-09-07
Prices in pharmacies: from 1362 rubles.
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Onbrez Breezhaler is a bronchodilator.
Release form and composition
Dosage form - capsules with powder for inhalation: size No. 3, hard, gelatinous, with a colorless transparent body and lid, the lid has the inscription "IDL 150" in black ink and a black strip (capsules of 150 mcg) or the inscription "IDL 300" in blue ink and a strip of blue color (capsules of 300 μg), under the strip there is a marking in the form of a company logo; the contents of the capsules are white or almost white powder [10 pcs. in a blister complete with a device for inhalation (breezhaler), in a cardboard box of 1, 3 or 9 blisters and instructions for use Onbrez Breezhaler].
Composition of 1 capsule:
- active substance: indacaterol maleate - 150 or 300 mcg (in terms of indacaterol base);
- auxiliary component: lactose monohydrate;
- the composition of the capsule shell: gelatin; capsules at a dosage of 150 mcg - black ink [purified water, propylene glycol (E1520), iron dye black oxide (E172), black ink (shellac (E904)]; capsules at a dosage of 300 mcg - blue ink [purified water, titanium dioxide (E171), propylene glycol (E1520), aluminum varnish, shellac (E904), iron oxide black dye (E172), brilliant blue dye (E133)].
Pharmacological properties
Pharmacodynamics
The active ingredient Onbrez Breezhaler is indacaterol - a selective, almost complete long-acting β 2 -adrenoceptor agonist (24 hours). The mechanism of its action is due to the ability to stimulate intracellular adenylate cyclase - an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) into cyclic 3 ', 5'-adenosine monophosphate (cyclic AMP). Due to an increase in the content of cyclic AMP, the smooth muscles of the bronchi relax. The stimulating effect of indacaterol in relation to β 2 -adrenergic receptors is 24 times stronger than β 1 -adrenoreceptors, and 20 times stronger than β 3 -adrenergic receptors.
When administered by inhalation, Onbrez Breezhaler has a quick and long-lasting bronchodilating effect.
The use of the drug allows you to achieve a significant lasting improvement in lung function [increase in forced expiratory volume in the first second (FEV1)] within 24 hours.
The onset of action of indacaterol is noted already approximately 5 minutes after inhalation, which is comparable to the action of salbutamol, which is a short-acting agonist of β 2 -adrenergic receptors. The maximum effect of the drug develops within 2-4 hours after inhalation.
In the case of the use of Onbrez Breezhaler for 1 year, the development of tachyphylaxis to its bronchodilatory effect was not noted. Also, no dependence of the bronchodilating effect on the time of drug administration (morning or evening) was found.
In patients with moderate and severe chronic obstructive pulmonary disease (COPD), indacaterol reduces dynamic and static hyperinflation (increase in lung volume at the end of spontaneous expiration), and also increases inspiratory capacity and FEV1, reduces shortness of breath, reduces the need for inhaled β 2 -adrenoreceptor agonists actions, improves exercise tolerance and quality of life of patients (assessed through the certified questionnaire of the Hospital of St. George). There was a significant decrease in the risk of exacerbation of episodes of the disease (an increase in the intervals between exacerbations).
Pharmacokinetics
The maximum concentration (C max) of indacaterol in the blood serum is reached on average within 15 minutes. The systemic exposure of the drug increases with increasing dose (in the range from 150 to 600 μg) and is dose-dependent.
The absolute bioavailability after a single inhalation is approximately 43%. Systemic exposure results from absorption of indacaterol in the lungs and intestines. With repeated use, the concentration of the drug in the blood serum increases. Equilibrium concentration (C ss) is achieved within 12-15 days of treatment. When using the drug once a day (in the dose range from 75 to 600 mcg) for 14 days, the cumulation coefficient of indacaterol, estimated by the exposure of the drug on the 1st and 14th or 15th days (AUC 0-24), is 2, 9-3.8.
The volume of distribution (Vd) of the drug after intravenous administration was 2.361-2.557 liters, which indicates a good distribution of the substance. Plasma protein binding is 95.1–96.2%, and serum protein binding - 94.1–95.3%.
In studies with oral administration of radiolabeled indacaterol, unchanged substance was the main component of serum and accounted for about ⅓ of the total AUC 0-24 associated with the drug. Of the metabolites in the blood serum, the hydroxylated derivative of indacaterol predominates; phenolic O-glucuronide of indacaterol and hydroxylated indacaterol are also determined. Later, C- and N-dealkylated products, diastereomers of the hydroxylated derivative, N-glucuronide of indacaterol are revealed.
Indacaterol is biotransformed to phenolic O-glucuronide only with the isoenzyme UDP-glucuronosyl transferase (UGT1A1). Hydroxylation of the active substance of the drug occurs mainly with the participation of the CYP3A4 isoenzyme. Despite the fact that indacaterol has a low affinity, it is a substrate for the membrane transporter of P-glycoprotein (P-gp) molecules.
No more than 2% of the received dose of indacaterol is excreted unchanged in the urine. The renal clearance of the drug is 0.46–1.2 l / h. Serum clearance - 18.8-23.3 l / h. This indicates an insignificant excretion of the drug through the kidneys (approximately 2–5% of the systemic clearance).
In the case of oral administration, indacaterol is excreted mainly (90% of the dose) through the intestines, including 54% - unchanged, 23% - in the form of hydroxylated metabolites.
The serum concentration of the drug decreases stepwise, the average terminal half-life (T 1/2) is 45.5-126 hours. T1 / 2, calculated on the basis of the cumulation of indacaterol after repeated applications, varied in the range of 40-56 hours, which is consistent with the established time to reach C ss (12-15 days).
Special patient groups:
- body weight, gender and age: no changes in pharmacokinetic characteristics in patients with COPD have been identified;
- race: a change in pharmacokinetics is unlikely. The experience of using indacaterol in patients of the Negroid race is limited;
- renal function: excretion of the drug by the kidneys is insignificant, therefore, its pharmacokinetics in patients with functional impairment of renal function has not been studied;
- liver function: in mild and moderate disorders, the pharmacokinetics does not change significantly. In severe disorders, the parameters of the drug have not been studied.
Indications for use
Onbrez Breezhaler is indicated for long-term maintenance therapy of impaired bronchial obstruction in patients with chronic obstructive pulmonary disease.
Contraindications
Absolute:
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- age up to 18 years;
- period of pregnancy and lactation;
- hypersensitivity to any component of the drug.
Relative (Onbrez Breezhaler is used with caution, after assessing the benefits and risks):
- diabetes;
- thyrotoxicosis;
- seizure disorders;
- cardiovascular disorders (acute myocardial infarction, ischemic heart disease, arterial hypertension, arrhythmias);
- congenital lengthening of the QT interval;
- the use of drugs that lengthen the QT interval (class IA and III antiarrhythmic drugs, macrolides, antipsychotics, tetracyclic and tricyclic antidepressants, antifungal agents, imidazole derivatives, some antihistamines, including astemizole, ebastine, terfenadine);
- the use of drugs from the group of barbiturates for general anesthesia;
- a history of an inadequate response to the action of β 2 -adrenoreceptor agonists.
Onbrez Breezhaler, instructions for use: method and dosage
Onbrez Breezhaler is intended for inhalation use only. The powder contained in the capsules is inhaled through the mouth using a special Breezhaler device, which is included with the drug.
Remove capsules from the blister immediately before use. You can’t take them inside.
Adult patients are usually prescribed 1 capsule 150 mcg 1 time per day. In some cases, with severe COPD, the dose may be increased to 300 mcg.
The maximum daily dose is 300 mcg and cannot be exceeded.
Inhalation must be carried out at the same time of the day. If the next dose is missed, you should not double it in the next dose, you need to adhere to the usual treatment schedule.
The doctor will teach you how to use the inhalation device correctly. If there is no improvement in respiratory function, you should make sure that the patient is using Onbrez Breezhaler correctly.
Instructions for using the drug
The inhalation device (Breezhaler) contained in the package is intended for use only with Onbrez Breezhaler capsules. Do not use any other device to inhale powder capsules. It is also forbidden to use Breezhaler with any other medication.
Rules for using Breezhaler:
- Remove the cover.
- Holding the Breezhaler by the base and tilting the mouthpiece in the direction of the arrow, open the device.
- With clean, dry hands, remove the capsule from the blister and insert it into the Breezhaler, placing it in a specially designated place (do not put it in the mouthpiece).
- Close Breezhaler (you should hear a click).
- To pierce the capsule: holding the device strictly vertically, simultaneously press the buttons of the piercing device on both sides (a click should be heard, indicating a puncture of the capsule) and release them. Do not press the buttons more than once.
- Exhale completely (do not blow into the mouthpiece).
- Holding the Breezhaler in your hand, place the mouthpiece in your mouth and close your lips tightly around it. Take a quick, even and deepest breath. During inhalation, a sweetish taste of the drug may be felt in the mouth. A rattling sound will be heard (due to capsule rotation and powder spraying), if not, check the capsule. If it gets stuck in the cell, you need to carefully remove it by tapping slightly on the base of the device. Never press the side buttons repeatedly to eject the capsule.
- Hold your breath as long as possible, at this time the mouthpiece can be removed.
- Exhale.
- Open the device and check if any powder remains in the capsule. If yes, close Breezhaler and repeat the inhalation procedure. For the complete release of the capsule, usually 1-2 inhalations are sufficient.
- Opening the Breezhaler by tilting the mouthpiece, remove the empty capsule and discard it.
- Close the mouthpiece and inhaler.
- For the convenience of accounting for inhalations, make a mark in the calendar on the inner surface of the package.
In rare cases, when inhaled, some of the powder gets into the mouth. This is not a reason to stop inhaling the drug.
Cough may occur immediately after inhalation. Do not worry, this is a frequent occurrence, not fraught with serious consequences, since the patient received a full dose of Onbrez Breezhaler.
Important notes:
- never swallow capsules;
- for inhalation use only the device supplied in the kit;
- do not store capsules in Breezhaler;
- store capsules in a blister and take out just before inhalation;
- store blisters in a dry place;
- never put a capsule in the mouthpiece;
- always pierce the capsule before inhalation;
- do not get hooked on the lancing device more than once;
- never blow into the mouthpiece;
- do not disassemble Breezhaler and do not wash it;
- store Breezhaler in a dry place;
- when starting a new package of the drug, always use a new Breezhaler;
- clean the Breezhaler once a week - wipe the mouthpiece inside and out with a clean dry cloth;
- never use water to clean the Breezhaler.
Side effects
Possible side effects of Onbrez Breezhaler (criteria for assessing the frequency of their development: very often - ≥ 1/10, often - from ≥ 1/100 to <1/10, infrequently - from ≥ 1/1000 to <1/100, rarely - from ≥ 1/10 000 to <1/1000, very rarely - <1/10 000, including individual messages):
- from the respiratory system: often - a feeling of irritation in the throat, sore throat, rhinorrhea, cough *; infrequently - paradoxical bronchospasm;
- from the digestive system: often - dry mouth;
- from the immune system: infrequently - hypersensitivity reactions;
- on the part of the cardiovascular system: often - ischemic heart disease; infrequently - tachycardia, atrial fibrillation;
- from the nervous system: often - dizziness; infrequently - paresthesia;
- from the musculoskeletal system: often - bone pain, muscle spasm; infrequently - myalgia;
- on the part of metabolism: often - hyperglycemia or newly diagnosed diabetes mellitus;
- on the part of the skin and subcutaneous tissue: often - itching, rash;
- infections and invasions: very often - nasopharyngitis, upper respiratory tract infections; often - sinusitis;
- others: often - peripheral edema, noncardiogenic pain in the chest area.
* A sporadic cough lasting about 5 seconds developed within 15 seconds after inhalation in 17–20% of patients observed in clinical studies. This violation somewhat worried the patients, but did not require discontinuation of drug treatment. Cough is a symptom of COPD, therefore, only 8.2% of patients associated its development with the use of Onbrez Breezhaler. The onset of cough immediately after inhalation is not associated with exacerbation of COPD, worsening of COPD, the development of bronchospasm and a decrease in the effectiveness of treatment.
In cases of using Onbrez Breezhaler at a maximum (not recommended) dose of 600 mcg 1 time per day, there were no significant differences in the safety profile in patients receiving the drug 1 time per day, 150 or 300 mcg. Peripheral edema, nasopharyngitis, headache, and muscle spasms were more common. Tremors and anemia were additional side effects.
Overdose
In patients with COPD, after a single dose of 10 times the maximum recommended dose, there was an increase in blood pressure, lengthening of the QT s interval, and a moderate increase in heart rate.
Other possible overdose symptoms: nausea, vomiting, palpitations, tremors, ventricular arrhythmias, tachycardia, drowsiness, headache, metabolic acidosis, hyperglycemia and hypokalemia (due to increased systemic beta 2 -adrenomimetic action).
Overdose treatment is supportive and symptomatic. In severe cases, patients are hospitalized. If necessary, prescribe cardioselective beta-blockers, but they are used only under close medical supervision, since there is a risk of developing bronchospasm.
special instructions
Onbrez Breezhaler is not intended for the relief of acute bronchospasm. If, during therapy, the course of the disease worsens, you should consult a doctor to re-evaluate the condition and revise treatment tactics.
There are no data on long-term use of indacaterol in bronchial asthma. Long- acting β 2 -adrenoceptor agonists are known to increase the likelihood of serious side effects. In this regard, with bronchial asthma, Onbrez Breezhaler should not be prescribed.
There are known cases of development of immediate-type hypersensitivity reactions in patients receiving indacaterol. If symptoms of an allergic reaction develop (skin rash, hives, swelling of the tongue / lips / face, difficulty breathing or swallowing), the drug should be discontinued and an alternative therapy should be selected.
Like any inhalation agent, Onbrez Breezhaler can cause paradoxical bronchospasm, a serious life-threatening complication. In this case, treatment with the drug should be discontinued and alternative therapy should be prescribed.
Β 2 -adrenoreceptor agonists can cause side effects from the cardiovascular system (increased blood pressure and heart rate), which requires discontinuation of treatment. Some electrocardiographic changes are also possible (lengthening of the QT interval, flattening of the T wave, depression of the ST segment), but their clinical significance is not precisely known.
In high doses, Onbrez Breezhaler can increase plasma glucose levels, so patients with diabetes should monitor this indicator. In clinical studies in patients receiving therapeutic doses of indacaterol, there was an increase in the incidence of clinically significant hyperglycemia by an average of 1–2% compared with the placebo group. There are no data on the safety and efficacy of bronchodilatory therapy in patients with uncompensated diabetes mellitus.
Β 2 -adrenoceptor agonists can cause severe hypokalemia, leading to the development of unwanted cardiovascular disorders. A slight decrease in serum potassium is usually transient and does not require dose adjustment of indacaterol. In severe COPD, hypokalemia can be exacerbated by hypoxia and the concomitant use of certain drugs, which increases the risk of arrhythmias.
Influence on the ability to drive vehicles and complex mechanisms
There is no information on the effect of Onbrez Breezhaler on reaction speed and the ability to concentrate.
Application during pregnancy and lactation
In animals, the use of indacaterol in doses equivalent to therapeutic doses in humans did not cause any reproductive toxicity. However, in humans during pregnancy, the safety of the drug has not been established. Onbrez Breezhaler is contraindicated in pregnant women, unless there is an absolute need for therapy, when the expected benefit is definitely higher than the potential risks. It should be borne in mind that β 2 -adrenoreceptor agonists, due to their relaxing effect on the smooth muscles of the uterus, can slow down the process of childbirth.
In animal studies, it was found that indacaterol penetrates into milk, which gives reason to predict its adverse effects on a breastfed baby. In this regard, it is contraindicated to use Onbrez Breezhaler during lactation, or breastfeeding should be stopped.
Pediatric use
Due to the lack of data on the safety and effectiveness of the use of indacaterol in pediatrics, Onbrez Breezhaler is not prescribed for children and adolescents under 18 years of age.
With impaired renal function
With mild and moderate functional impairment of the kidneys, correction of the dosage regimen is not required. The safety of indacaterol in severe renal impairment has not been studied.
For violations of liver function
With mild and moderate functional disorders of the liver, correction of the dosage regimen is not required. The safety of using indacaterol in severe hepatic impairment has not been studied.
Use in the elderly
There is no need to adjust the dose for elderly patients.
Drug interactions
Onbrez Breezhaler is contraindicated to be used simultaneously with other long-acting β 2 -adrenoreceptor agonists and drugs containing long-acting β 2 -agonists.
Indacaterol is able to prolong the QT interval. This effect can be enhanced by other drugs. In this connection, caution should be exercised when prescribing monoamine oxidase (MAO) inhibitors, tricyclic antidepressants or other drugs that prolong the QT interval to patients. With prolongation of the QT interval, the likelihood of developing ventricular arrhythmias increases.
Sympathomimetics increase the risk of side effects.
Onbrez Breezhaler can cause hypokalemia, which is enhanced by the combined use of potassium-excreting diuretics, glucocorticosteroids, methylxanthine derivatives.
The simultaneous administration of β 2 -adrenoreceptor blockers (including in the dosage form of eye drops) is contraindicated, since they can weaken and even block the action of β 2 -adrenoceptor agonists. If it becomes necessary to use such a combination, cardioselective β 2 -adrenoreceptor blockers should be preferred and treatment should be carried out with extreme caution.
The interaction of indacaterol with specific inhibitors of the isoenzyme CYP3A4 and P-glycoprotein, such as verapamil, erythromycin, ketoconazole, ritonavir, was studied. With the combined use of verapamil, an increase in AUC (area under the concentration-time curve) by 1.4–2 times and C max by 1.5 times was noted. The simultaneous use of erythromycin led to an increase in C max by 1.2 times and AUC by 1.4–1.6 times. The combined administration of ketoconazole caused a 2-fold increase in AUC and a 1.4-fold increase in C max. This increase in exposure did not change the safety profile of the drug. The combination therapy with ritonavir led to a 1.6-1.8-fold increase in AUC, but the C max did not change.
With the joint use of indacaterol with other drugs, interactions were not observed. In vitro studies have shown that indacaterol is characterized by an insignificant potential for interaction with drugs at the level of membrane carriers and at the level of enzyme metabolism during systemic exposure, achieved with the use of therapeutic doses.
Analogs
The analogues of Onbrez Breezhaler are Astalin, Atimos, Berotek, Ventolin, Vertasort, Clenbuterol, Kombipek, Salamol Eco Light Breath, Salbutamol, Salgim, Foradil, Fenoterol-native, Cybutol Cyclocaps, etc.
Terms and conditions of storage
Store in a dry place, out of reach of children, at a temperature not exceeding 30 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Onbrez Breezhaler
Reviews about Onbrez Breezhaler are mostly positive. Its regular inhalation use reduces the severity of shortness of breath, the need for first aid medications and the frequency of exacerbations. Patients note that during therapy it becomes easier to breathe, mucus goes better, and there are no attacks during exercise. An additional advantage is the convenience of using the drug - only once a day.
Of the side effects, cough in the first 20 seconds after inhalation, headache, nasopharyngitis, upper respiratory tract infections are most often mentioned. In most cases, adverse events were mild and did not require discontinuation of therapy.
Price for Onbrez Breezhaler in pharmacies
Depending on the region of sale and the pharmacy network, the approximate price for Onbrez Breezhaler for a pack of 30 capsules may be: dosage 150 mcg - 1455-1750 rubles, dosage 300 mcg - 1100-1580 rubles.
Onbrez Breezhaler: prices in online pharmacies
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Drug name Price Pharmacy |
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Onbrez Breezhaler 300 mcg capsules with powder for inhalation complete with Breezhaler inhaler 30 pcs. 1362 RUB Buy |
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Onbrez Breezhaler capsules for inhalation. 300μg 30 pcs. 1467 RUB Buy |
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Onbrez Breezhaler 150 mcg powder capsules for inhalation complete with Breezhaler inhaler 30 pcs. 1484 RUB Buy |
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Onbrez Breezhaler capsules for inhalation. 150μg 30 pcs. 1554 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
