Relvar Ellipt
Relvar Ellipta: 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: Relvar Ellipta
ATX code: R03AK10
Active ingredient: vilanterol (Vilanterol) + fluticasone furoate (Fluticasone furoate)
Producer: Glaxo Operations UK Limited (Great Britain)
Description and photo update: 28.11.2018
Prices in pharmacies: from 1499 rubles.
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Relvar Ellipta is a combined bronchodilator with anti-inflammatory action.
Release form and composition
The drug is produced in the form of a dosed powder for inhalations of white color (22 μg + 92 μg / dose or 22 μg + 184 μg / dose; 30 doses each in a plastic inhaler with a light gray body, a pale blue mouthpiece lid and a dose counter; c the inhaler contains 2 aluminum laminated strips of 30 evenly distributed cells with powder; 1 inhaler is sealed in a multilayer container made of easy-to-open aluminum foil, a cardboard box contains 1 container and instructions for use of Relvar Ellipt).
The composition of the powder for inhalation in 1 dose / cell * 22 μg + 92 μg / 22 μg + 184 μg:
- strip with vilanterol: active ingredient - micronized vilanterol triphenatate in a dose of 40 μg (equivalent to vilanterol in an amount of 25 μg **); excipients - magnesium stearate; lactose monohydrate;
- strip with fluticasone furoate: active ingredient - micronized fluticasone furoate at a dose of 100 μg ** (22 μg + 92 μg) or 200 μg ** (22 μg + 184 μg); excipient - lactose monohydrate.
* in order to compensate for losses during filling the cells, mixtures of active and auxiliary substances during the production of the finished medicinal product can be placed in the final product with an excess of up to 8%.
** the nominal amount of the active substance added during production is indicated; the delivered amount is: vilanterol - 22 μg, fluticasone furoate - 92 and 184 μg, which corresponds to the indicated dosages.
Pharmacological properties
Pharmacodynamics
Pharmacological efficacy of Relvar Ellipt is due to the action of each of its active components:
- vilanterol: long-acting selective β 2 -adrenergic agonist (LABA); The therapeutic effect of β 2 -adrenergic receptor agonists, including vilanterol, is at least to some extent associated with the stimulation of intracellular adenylate cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) into cyclic 3 ', 5'-adenosine monophosphate (cyclic AMP). With an increase in the level of cyclic AMP, relaxation of the smooth muscles of the bronchi and suppression of the release from cells (mainly from obese) of mediators of immediate hypersensitivity reactions occurs;
- fluticasone furoate: a synthetic trifluoride glucocorticosteroid (GCS) with pronounced anti-inflammatory activity; the exact mechanism of its action, providing relief of symptoms of chronic obstructive pulmonary disease (COPD) and bronchial asthma is unclear. GCS have a wide spectrum of efficacy against various types of cells (for example, lymphocytes, macrophages, eosinophils) and mediators (for example, cytokines and chemokines involved in the inflammatory response).
Interactions occur between LABA and GCS at the molecular level, as a result of which steroid hormones excite the β2-adrenergic receptor gene, increasing the number of sensitive adrenergic receptors. LABA are bound by the GCS-receptor, which results in steroid-dependent activation of the latter and stimulation of translocation into the cell nucleus. These synergistic interactions provide an increase in anti-inflammatory activity, which was recorded during in vitro and in vivo experiments with various inflammatory cells associated with the pathophysiological processes of COPD and bronchial asthma.
Data from clinical studies using biopsy samples of the respiratory tract also indicated a synergistic effect of LABA and GCS, which occurs when these drugs are prescribed to patients with COPD in therapeutic doses.
Pharmacokinetics
The absolute bioavailability of vilanterol and fluticasone furoate after inhalation of a combination of these active substances was approximately 27.3% and 15.2%, respectively. In the case of oral use, their bioavailability was insignificant and averaged less than 2 and 1.26%, respectively. The systemic effect of Relvar Ellipt after inhalation is primarily due to the absorption of a part of the powder that has entered the lungs by inhalation (given the low oral bioavailability of both substances).
After intravenous (iv) administration, vilanterol and fluticasone furoate are widely distributed, with the mean volumes of distribution (V d) at equilibrium being 165 and 661 liters, respectively. Both active components are characterized by a low binding capacity with erythrocytes. According to in vitro studies, the connection with plasma proteins, including in patients with functional disorders of the liver and kidneys, was high and reached approximately 93.9 for vilanterol and more than 99.6% for fluticasone furoate.
Both active substances of Relvar Ellipt are substrates of P-glycoprotein (P-gp), however, with the combined administration of a combination of these components with P-gp inhibitors, a change in the systemic exposure of vilanterol or fluticasone furoate is unlikely, since both substances have a high absorption capacity.
According to the results of in vitro experiments, the main metabolic pathways of fluticasone furoate and vilanterol in humans are mediated mainly by the cytochrome CYP3A4 isoenzyme. Vilanterol is metabolized mostly by O-dealkylation with the formation of a number of metabolites, showing significantly lower β 1 - and β 2 -adrenomimetic activity. The biotransformation of fluticasone furoate proceeds mainly by hydrolysis of the S-fluoromethylcarbothioate group with the formation of metabolites with significantly lower GCS activity.
A clinical study of drug interactions between Relvar Ellipt and the CYP3A4 isoenzyme was carried out during the continuous administration of a combination of vilanterol and fluticasone furoate (22 μg + 184 μg / dose) and ketoconazole (a potent inhibitor of the CYP3A4 isoenzyme) to healthy volunteers at a dose of 400 mg. The combined use of the drugs caused an increase in the average maximum concentration (C max) and the average area under the pharmacokinetic curve (AUC 0-24) of fluticasone furoate by 33 and 36%, respectively. Increases in fluticasone furoate exposure were associated with a 27% decrease in mean serum cortisol levels measured over the 0-24 hour period. Against the background of the simultaneous administration of a combination of vilanterol and fluticasone furoate and ketoconazole, an increase in the average Cmax and AUC (0 – t) of vilanterol by 22 and 65%, respectively. Prolonged exposure of vilanterol did not enhance the systemic effects that are characteristic of β-agonists in terms of heart rate (HR), corrected QT interval (QTcF) or blood potassium levels.
After oral administration of fluticasone, furoate predominantly underwent biotransformation with the formation of metabolites, mostly excreted through the gastrointestinal tract (GIT), except for a dose of radioactive substance less than 1% excreted in the urine. The estimated half-life (T 1/2) from plasma after inhalation was approximately 24 hours.
After oral administration, Vilanterol was biotransformed in the body with the formation of metabolites excreted in feces and urine, in the ratio of approximately 30 and 70% of the dose of the radioactive substance, respectively. With inhalation of a combination of vilanterol and fluticasone furoate, T 1/2 of vilanterol from plasma was approximately 2.5 hours.
In clinical studies of patients with bronchial asthma and COPD, immigrants from Japan, East and Southeast Asia (12-14% of patients), on average, higher AUC values of 0-24, but not higher than 53%, were observed for fluticasone furoata in comparison with patients of the Caucasian race. At the same time, in these populations, no signs were found indicating a higher systemic exposure associated with an increased effect on the daily excretion of cortisol in the urine.
In patients with COPD, no effect of race on the pharmacokinetic characteristics of vilanterol was found. According to the results of studies, the C max values of vilanterol were 220-287% higher, and the AUC 0-24 were comparable in patients of Asian origin with the corresponding indicators in representatives of other racial groups. However, with a higher C max of vilanterol, no clinically significant effect on heart rate was found.
According to the results of pharmacokinetic analysis, the effect of body weight, body mass index (BMI) and gender on the pharmacokinetic profile of vilanterol and fluticasone furoate in patients with bronchial asthma or COPD was not found. Individual selection of the dose of Relvar Ellipt based on data on body weight, BMI and gender is not required.
Indications for use
- bronchial asthma (as maintenance treatment);
- COPD (as a maintenance treatment for airway obstruction in patients with COPD, including chronic bronchitis and / or pulmonary emphysema).
The use of Relvar Ellipt helps to reduce the number of exacerbations of COPD in the presence of a history of repeated exacerbations.
Contraindications
Absolute:
- age up to 12 years (for the treatment of bronchial asthma);
- age up to 18 years (for COPD therapy);
- a history of hypersensitivity to any of the components of the drug or a history of severe allergic reactions to milk protein.
Relvar Ellipta 22 mcg + 184 mcg / dose is not indicated for the treatment of COPD.
Relative contraindications (the drug must be used with caution):
- pulmonary tuberculosis; the presence of chronic or untreated infections (due to the composition of the GCS);
- severe forms of cardiovascular disease (due to the increased risk of arrhythmia, including supraventricular tachycardia and extrasystole).
Relvar Ellipta, instructions for use: method and dosage
Relvar Ellipta is used only by inhalation, once a day (in the morning or in the evening at the same time). After inhalation, it is recommended to rinse your mouth with water without swallowing it.
Patients with bronchial asthma require inhalation of the drug even with an asymptomatic course of the disease. In the case of asthma symptoms occurring between injections, short-acting β 2 -agonists in inhaled form should be used for urgent relief of their severity. The doctor needs to regularly assess the patient's condition for the timely appointment, if necessary, of the optimal dosage of Relvar Ellipt. The dosage regimen can be adjusted only after consulting the attending physician.
Adolescents over 12 years old and adults are recommended to carry out 1 inhalation per day at a dose of 22 μg + 92 μg or at a dose of 22 μg + 184 μg.
Relvar Ellipt 22 mcg + 92 mcg is prescribed as an initial dose for patients who need low or medium doses of inhaled GCS in combination with long-acting β 2 -agonists, and a dosage of 22 μg + 184 μg is prescribed for patients who need a higher dose of inhaled GCS in combined with β 2 -agonists.
If the administration of the drug at a dosage of 22 mcg + 92 mcg cannot lead to adequate control of bronchial asthma, an increase in the dose to 22 mcg + 184 mcg is possible to ensure better control over the course of the disease.
For adults with COPD, it is recommended to carry out 1 inhalation of Relvar Ellipt 22 mcg + 92 mcg per day; Do not use the drug in a dosage of 22 mcg + 184 mcg for the treatment of this disease.
Rules for using the Ellipt inhaler
If the inhaler is used for the first time, there is no need for special preparation for its use or in checking its correct operation. The following recommendations for use should be followed in stages:
- The container in which the inhaler is packed contains a desiccant silica gel sachet that is not intended for inhalation or human consumption and must be disposed of.
- After the inhaler is removed from the container, the lid in the closed position should not be opened until the drug is administered. If you open and close the lid of the inhaler without taking the medication, dose loss will occur. This lost dose will be securely closed inside the inhaler and not available for intake. It is impossible to accidentally enter a large or double dose in one inhalation.
- After each opening of the lid, one dose of the drug is ready for inhalation. The dose counter shows how many doses of Relvar Ellipt are left in the inhaler. Before the start of the first procedure, the counter shows exactly 30 doses; with each subsequent opening of the inhaler lid, the number of doses decreases by one. When there are less than 10 doses left, half of the counter will turn red. After the last dose of the drug has been administered, half of the counter will turn red, it will show the number 0, this will mean that the inhaler is empty. If you then open the cover, the counter will turn red completely.
- When ready to inject the drug, open the lid and lower it down until it clicks. The drug is ready for inhalation if the counter has reduced the number of doses by one. If the number of doses does not decrease after clicking, the inhaler is not ready to deliver the drug. In this case, you need to contact by phone or at the address specified in the section "Contact for additional information." Do not shake the inhaler!
- During the procedure, before taking the drug, it is required to exhale as deeply as possible, holding the inhaler at a certain distance near the mouth. Do not breathe out into the inhaler.
- Firmly covering the mouthpiece with your lips and without covering the ventilation hole with your fingers at the same time, you should take one even, long and deep breath. It is required to hold your breath as much as possible, but not less than 3-4 seconds. Then you need to remove the inhaler from your mouth and exhale calmly and slowly. If the procedure is carried out correctly, you may not feel the flow of the drug or not feel its taste.
- If necessary, clean the mouthpiece with a dry paper towel before closing the lid. To completely close the mouthpiece, you need to pull the lid up until it stops. After using the inhaler, it is recommended to rinse your mouth with water to reduce the risk of developing adverse reactions such as pain in the mouth and throat.
Side effects
Adverse reactions observed in the course of large-scale clinical trials among patients with bronchial asthma and COPD:
- nervous system: very often - headache;
- infectious and parasitic lesions: often - oral and pharyngeal candidiasis, influenza, upper respiratory tract infections, bronchitis, pneumonia;
- cardiovascular system: infrequently - extrasystole;
- digestive system: often - abdominal pain;
- respiratory system: very often - nasopharyngitis; often - rhinitis, pharyngitis, sinusitis, cough, dysphonia, oropharyngeal pain;
- musculoskeletal system: often - back pain, arthralgia, fractures;
- general disorders: often - fever.
The safety profiles of Relvar Ellipt in patients with COPD and bronchial asthma were similar, except for pneumonia and fractures, which were most often observed during clinical studies in patients with COPD.
Violations recorded according to post-registration observation data:
- immune system: rarely - hypersensitivity reactions, including urticaria, rash, angioedema, anaphylaxis;
- cardiovascular system: rarely - heart palpitations, tachycardia;
- respiratory system: rarely - paradoxical bronchospasm;
- musculoskeletal system: often - muscle spasm;
- nervous system: rarely - tremor;
- mental disorders: rarely - anxiety.
Overdose
There are no data on overdose with the combined use of vilanterol and fluticasone furoate. Against the background of an overdose of Relvar Ellipt, symptoms may occur, caused by the action of its individual components, and are characteristic of an overdose of inhaled corticosteroids and β 2 -agonists.
There are no specific methods of therapy for overdose. Symptomatic treatment is recommended, as well as observation of the patient, if necessary. Cardioselective β-adrenergic blockers are prescribed only when severe reactions of vilanterol overdose occur, which are refractory to maintenance therapy. In the case of a history of episodes of bronchospasm, cardioselective β-blockers should be used with caution.
special instructions
Relvar Ellipta is not indicated for relieving exacerbation of COPD or acute symptoms of bronchial asthma; in these cases, it is necessary to use short-acting bronchodilators. With an increase in the frequency of taking the latter in order to relieve symptoms, it is necessary to improve control over the disease after consulting a doctor.
Patients with bronchial asthma or COPD should not discontinue drug therapy without specialist supervision, since refusal to use the drug may cause recurrence of symptoms.
After administration of the drug, as with other types of inhalation treatment, there is a risk of paradoxical bronchospasm, accompanied by a rapid increase in wheezing. The development of this complication requires the urgent use of a short-acting inhaled bronchodilator and immediate withdrawal of Relvar Ellipt. The attending physician evaluates the patient's condition and, if necessary, can prescribe an alternative therapy.
During treatment with the drug, it is possible to develop undesirable phenomena associated with the course of bronchial asthma or an exacerbation of the disease. In these conditions, it is recommended to continue taking Relvar Ellipt. It is necessary to urgently seek the advice of a doctor if at the beginning of the course the patient's condition worsened or it is not possible to establish control over the disease.
The use of any inhaled GCS, especially for a long time in high doses, can contribute to the development of systemic side effects. Such violations occur much less frequently than during treatment with oral corticosteroids. The following reactions can be manifestations of possible adverse systemic effects: glaucoma, cataracts, a decrease in bone mineral density, inhibition of the function of the hypothalamic-pituitary-adrenal system, growth retardation in children and adolescents.
In patients with COPD during treatment with Relvar Ellipt, an increase in the incidence of pneumonia was recorded, including severe forms of this disease requiring hospitalization (in some cases with a fatal outcome). In the presence of COPD, it is necessary to take into account the threat of pneumonia, since the clinical signs of this complication may overlap with symptoms of an exacerbation of COPD. The likelihood of developing pneumonia during drug therapy in patients with COPD is exacerbated by the following risk factors: a history of pneumonia, smoking, BMI less than 25 kg / m², predicted forced expiratory volume in the first second (FEV 1) less than 50% of the proper values … These factors should be taken into account when prescribing the drug, and if pneumonia develops, treatment should be reviewed.
Episodes of pneumonia in patients with bronchial asthma were recorded infrequently. Against the background of the use of the drug Relvar Ellipt 22 mcg + 184 mcg / dose in patients with asthma, an increased risk of developing pneumonia is possible when compared with patients using the drug 22 mcg + 92 mcg / dose. Risk factors have not been identified.
Influence on the ability to drive vehicles and complex mechanisms
Considering the pharmacological data of fluticasone furoate and vilanterol, it is not assumed that Relvar Ellipt has a negative effect on the ability to drive vehicles or other complex equipment.
Application during pregnancy and lactation
There is insufficient data on the use of Relvar Ellipt during pregnancy, and therefore the use of the drug in pregnant women is possible only when the expected benefit to the mother outweighs any possible threat to the fetus.
Information on the release of fluticasone furoate or vilanterol, or their metabolites during lactation is limited. However, it has been established that other GCS and β 2 -agonists penetrate into breast milk, therefore, the risk of excretion of the drug along with milk cannot be excluded. After assessing the ratio of the benefits of natural feeding for the child and treatment for the woman, it is necessary to decide whether to stop breastfeeding or drug therapy.
There is no data on the effect of Relvar Ellipt on human fertility. In the process of preclinical studies, the effect of the active substances of the drug on fertility was not revealed.
Pediatric use
In children under 12 years of age, the pharmacokinetics of the combined use of fluticasone furoate and vilanterol have not been studied. There are currently no data confirming the efficacy and safety of the drug in this age group of patients.
According to the indication of COPD, Relvar Ellipta is not prescribed for children and adolescents under 18 years of age.
When treating bronchial asthma, the use of the drug in children under 12 years of age is contraindicated. For adolescents 12 years and older, there are no recommendations for changing the mode of use of Relvar Ellipt.
With impaired renal function
The presence of severe renal impairment with creatinine clearance below 30 ml / min according to data obtained during a clinical and pharmacological study did not cause a pronounced increase in systemic exposure of vilanterol / fluticasone furoate or the occurrence of more severe systemic effects of GCS / β2-agonists when compared with similar indicators. in healthy volunteers. The effect of hemodialysis on the drug has not been studied.
Individual dose selection for patients with impaired renal function is not required.
For violations of liver function
According to the results of a clinical and pharmacological study in patients with mild, moderate and severe liver dysfunctions (according to the classification according to the Child - Pugh scale of cirrhosis stages A, B or C), there was an increase in the degree of systemic exposure of fluticasone furoate by 3 times (with an increase in C max and AUC). As a result, patients with impaired hepatic function need to use Relvar Ellipta with caution, since in this case, the risk of systemic undesirable effects caused by taking GCS is aggravated.
In patients with moderate / severe hepatic impairment, the maximum dose of Relvar Ellipt should be 22 μg + 92 μg / dose. Patients from this group need to be under medical supervision to control systemic side effects associated with the use of GCS.
Use in the elderly
Phase III clinical trials in patients over 65 years of age with bronchial asthma did not reveal evidence of the effect of age on the pharmacokinetic profile of vilanterol and fluticasone furoate. In elderly patients with COPD, despite an increase in AUC 0-24 of vilanterol by 37%, there were no signs of a change in the pharmacokinetic profile of fluticasone furoate due to the effect of age.
Individual selection of the dose of Relvar Ellipt for patients over 65 years of age with asthma and COPD is not required.
Drug interactions
- β-blockers: there is a weakening of the effect of β 2 -adrenomimetics or an antagonistic effect against the latter; it is necessary to avoid concomitant use of selective and non-selective β-blockers, except in cases where their appointment is extremely necessary;
- strong inhibitors of the cytochrome CYP3A4 isoenzyme (including ritonavir, ketoconazole): it is possible to increase the systemic effects of fluticasone furoate and vilanterol (since both substances are subjected to primary metabolism in the liver with the participation of the isoenzyme of the cytochrome CYP3A4 system), which may increase the risk of the appearance unwanted reactions; this combination requires caution;
- verapamil (a moderate inhibitor of the cytochrome CYP3A4 isoenzyme): there was no significant effect on the pharmacokinetics of vilanterol during its combination with verapamil and a potent P-gp inhibitor.
When a bronchodilator is used in therapeutic doses, significant drug interactions between fluticasone furoate and vilanterol are considered unlikely due to the low plasma concentrations of these substances as a result of inhalation.
Analogs
The analogues of Relvar Ellipt are: Avamis, Anoro Ellipta, Ventolin, DuoResp Spiromax, Atimos, Beclomethasone-aeronaut, Budekort, Pulmicort Turbuhaler, Inspirax aerosol, etc.
Terms and conditions of storage
Keep out of the reach of children at a temperature not exceeding 25 ° C.
Shelf life is 2 years.
An opened aluminum container should be used within 6 weeks.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Relvar Ellipta
Reviews of Relvar Ellipta are mostly positive. Patients note the effectiveness of the drug in the maintenance treatment of bronchial asthma. Thanks to its action, it is possible to reduce the number of exacerbations during COPD therapy. The inhaler is designed for 1 month of therapy, is simple and convenient to use, its effect lasts for 24 hours after administration.
All patients consider its high cost a disadvantage of the drug.
The price of Relvar Ellipta in pharmacies
The price of Relvar Ellipta powder for inhalation metered can be 30 doses for 1 inhaler:
- 22 mcg + 92 mcg / dose - 1750-2300 rubles;
- 22 mcg + 184 mcg / dose - 2200-2480 rubles.
Relvar Ellipta: prices in online pharmacies
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Drug name Price Pharmacy |
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Relvar Ellipta 22 mcg + 92 mcg / dose 30 doses powder for inhalation dosed 1 pc. RUB 1499 Buy |
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Relvar Ellipta 22 mcg + 184 mcg / dose 30 doses powder for inhalation dosed 1 pc. 1729 RUB Buy |
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Pore ellipse relvar. d / inhalation 22 μg + 92 μg / dose 30 doses n1 1909 RUB Buy |
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Pore ellipse relvar. d / inhalation 22mcg + 184mcg / dose 30 doses n1 2387 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!