Formoterol-native
Formoterol-native: instructions for use and reviews
- 1.production 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: Formoterol-nativ
ATX code: R03AC13
Active ingredient: formoterol (Formoterol)
Manufacturer: LLC "Nativa" (Russia)
Description and photo update: 2019-08-07
Prices in pharmacies: from 353 rubles.
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Formoterol-native is a bronchodilator.
Release form and composition
Dosage form - capsules with powder for inhalation: solid, size No. 3, transparent, light brown; contents - almost white or white powder (in blister contour packs of 10 pcs., in a carton pack of 3 or 6 packs with or without an inhalation device, as well as instructions for the use of Formoterol-native).
Composition of 1 capsule:
- active substance: formoterol fumarate dihydrate - 12 μg;
- auxiliary components: lactose monohydrate, sodium benzoate;
- capsule shell: hypromellose, caramel dye (E150c).
Pharmacological properties
Pharmacodynamics
Formoterol is a selective β 2 -adrenoceptor agonist (β 2 -adrenomimetic), which has a bronchodilatory effect in reversible airway obstruction. The effect develops quickly (within 1-3 minutes) and lasts up to 12 hours after inhalation. On the cardiovascular system, the drug in therapeutic doses has a minimal effect and in rare cases.
Formoterol-native inhibits the release of leukotrienes and histamine from mast cells. In experimental studies on animals, some anti-inflammatory activity of the drug was revealed, in particular the ability to prevent the accumulation of inflammatory cells and the development of edema.
In in vitro animal studies, it has been established that racemic formoterol and its (R, R) and (S, S) enantiomers are highly selective β 2 receptor agonists. The (S, S) enantiomer exhibited 800–1000 times less activity than the (R, R) enantiomer and did not adversely affect the effectiveness of the (R, R) enantiomer on tracheal smooth muscle. No pharmacological evidence was obtained for the superiority of using one of these two enantiomers over the use of a racemic mixture.
In humans, a study of formoterol has shown its high efficacy in preventing bronchospasm associated with exposure to inhaled allergens, cold air, exercise, methacholine and histamine. After inhalation, the bronchodilatory effect persists for 12 hours, therefore, with long-term maintenance therapy, two-time administration of the drug per day in most patients allows adequate control of chronic lung diseases around the clock (both day and night).
With a stable course of chronic obstructive pulmonary disease (COPD), inhalations of Formoterol-native 12 or 24 μg twice a day significantly improve the quality of life parameters.
Pharmacokinetics
Formoterol is used 2 times a day at a therapeutic dose of 12-24 mcg. The pharmacokinetic parameters of the drug were studied in healthy volunteers who received inhalation at higher doses than recommended, and in patients with COPD who received the drug at therapeutic doses.
After a single dose of 120 μg in healthy volunteers, formoterol was rapidly absorbed into the blood plasma. The maximum plasma concentration (C max) of 266 pmol / l was reached within 5 minutes after inhalation.
When using formoterol 12 or 24 μg 2 times a day for 12 weeks in patients with COPD, the concentrations of the active substance measured after 10 minutes, 2 hours and 6 hours from the moment of inhalation were in the ranges 11.5-25.7 or 23, 3–50.3 pmol / l, respectively.
When studying the total excretion of formoterol and its enantiomers in the urine, it was found that the content of formoterol in the systemic circulation is proportional to the size of the applied dose (in the range from 12 to 96 μg).
When using formoterol 12 or 24 mcg 2 times a day for 12 weeks in patients with bronchial asthma, the excretion of unchanged formoterol in the urine increased by 63-73%, and in patients with COPD - by 19-38%. This indicates some cumulation of the drug in the body with repeated use of Formoterol-native. At the same time, a greater cumulation of one of the enantiomers compared to the other was not observed with repeated inhalations.
Most of the inhaled drug is swallowed and then absorbed from the gastrointestinal tract (GIT). After oral administration of 3H-labeled formoterol at a dose of 80 μg, at least 65% of the dose was absorbed in healthy volunteers.
Formoterol binds to plasma proteins by 61–64%, including 34% - to serum albumin. In the range of concentrations observed after the use of Formoterol-native in therapeutic doses, saturation of the binding sites is not achieved.
Formoterol is metabolized primarily by direct conjugation with glucuronic acid, as well as by O-demethylation followed by conjugation with glucuronic acid (glucuronidation). Other unimportant metabolic pathways include the conjugation of formoterol with sulfate and subsequent deformylation. Many isozymes are involved in the processes of glucuronidation (1A6, 1A9, 1A3, 1A8, 1A7, 1A10, 2B7, 2B15, UGT1A1) and O-demethylation (2C9, 2A6, 209, CYP2D6) of formoterol. This suggests a low likelihood of drug interactions through inhibition of any isoenzyme involved in the metabolism of formoterol. The drug used in therapeutic doses does not suppress isozymes of the cytochrome P 450 system.
When using formoterol 12 or 24 μg 2 times a day for 12 weeks in patients with bronchial asthma, 10 and 15-18% of the total dose are excreted unchanged in the urine, respectively, in patients with COPD - 7 and 6-9%, respectively …
The share of (R, R) and (S, S) enantiomers of unchanged formoterol in urine accounts for 40 and 60%, respectively, after a single dose of the drug in healthy volunteers and after single and multiple doses in patients with bronchial asthma.
Formoterol and its metabolites are completely excreted from the body. Approximately ⅔ of the dose taken orally is excreted in the urine, ⅓ in the feces. Renal clearance is 150 ml / min.
The terminal half-life (T ½) of formoterol from plasma in healthy volunteers after a single inhalation of a dose of 120 μg is 10 hours. The terminal T ½ (R, R) and (S, S) enantiomers, calculated from urinary excretion, are 13.9, respectively and 12.3 hours.
Pharmacokinetics in some cases:
- gender: in women and men, the pharmacokinetic characteristics of the drug do not differ significantly;
- age: in patients over 65 years of age, no significant differences in formoterol parameters were found, therefore, dose adjustment is not required;
- renal / liver function: in patients with functional impairment of the kidneys / liver, the pharmacokinetics of the drug have not been studied.
Indications for use
- prevention of bronchospasm caused by physical exertion, cold air or inhalation of allergens [as part of complex therapy with inhaled glucocorticosteroids (GCS)];
- treatment and prevention of violations of bronchial patency in COPD (with reversible and irreversible bronchial obstruction), chronic bronchitis and pulmonary emphysema;
- treatment and prevention of violations of bronchial patency in bronchial asthma (as part of complex therapy with inhaled GCS).
Contraindications
Absolute:
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- age up to 18 years;
- lactation period;
- hypersensitivity to any component of the drug.
Formoterol-native with extreme caution and under close medical supervision, after assessing the benefits and risks, should be used in patients with ischemic heart disease, cardiac arrhythmias and conduction disorders (especially with atrioventricular block of III degree), severe heart failure, severe arterial hypertension, idiomatic hypertrophic subaortic stenosis, aneurysm of any localization, hypertrophic obstructive cardiomyopathy, known or suspected prolongation of the QTc interval (QT corrected> 0.44 sec), ketoacidosis, pheochromocytoma, thyrotoxicosis, diabetes mellitus, as well as pregnant women.
Formoterol-native, instructions for use: method and dosage
Formoterol-native is used only by inhalation using the included Inhaler CDM inhaler. It is forbidden to take capsules inside!
The doctor selects the optimal dose individually, based on the characteristics of the disease of each patient. Formoterol-native is recommended to be prescribed in the smallest doses that provide a sufficient therapeutic effect. After achieving stable control of the symptoms of bronchial asthma, it is necessary to consider the possibility of a gradual dose reduction. Dosage reduction is carried out under close medical supervision.
Recommended dosage regimens:
- bronchial asthma: for regular maintenance therapy, a dose of 12-24 mcg (1-2 capsules) 2 times a day is indicated. The maximum allowable daily dose is 48 mcg (4 capsules). In this disease, Formoterol-native is prescribed in addition to inhaled GCS. Taking into account the maximum permitted daily dose, if necessary and depending on the initial dose, an additional episodic intake of 12-24 μg per day is possible to relieve the symptoms of bronchial asthma. If the need to take additional doses ceases to be episodic (for example, it becomes more often twice a week), this may indicate a worsening of the course of the disease, in which case a doctor's consultation is required. Do not start using Formoterol-native or change its dose during an exacerbation of the disease. The drug is not intended for the relief of acute attacks of bronchial asthma;
- COPD: for regular maintenance therapy, a dose of 12-24 mcg 2 times a day is indicated;
- prevention of bronchospasm during exercise or exposure to a known allergen: the recommended dose is 12 μg 15 minutes before exercise or expected contact with the allergen. Do not inhale additional doses within 12 hours. Patients with a history of severe bronchospasm may need to increase the single dose to 24 mcg.
Correct inhalation
To ensure the correct use of Formoterol-native capsules, a medical professional should:
- warn patients that the capsules should not be swallowed, they are allowed to be used only for inhalation, taking them out of the package immediately before use;
- explain to patients that capsules can only be used with the Inhaler CDM inhaler;
- educate patients on the use of the inhaler.
The Inhaler CDM is a plastic device about 6 cm high with a movable top and a retractable capsule compartment. This is a single-dose inhaler that allows you to inhale very small doses of the drug.
Step-by-step instructions for using the inhaler:
- Remove the transparent cap from the inhaler.
- Firmly holding the device with one hand, thumb and forefinger of the other hand, open the capsule compartment by pressing the index finger on PUSH in the moving part of the inhaler and sliding the compartment in the opposite direction.
- While holding the device with one hand, insert the capsule into the slot of the compartment with the other.
- Make sure the capsule is inserted correctly.
- While holding the inhaler strictly in an upright position, close the compartment by pressing PUSH with your thumb in the opposite direction until it stops until you hear a click.
- Bring the device to working condition: press the mouthpiece with effort so that the arrow on the body disappears beyond the boundaries of the lower part of the inhaler to the upper line, then release the mouthpiece to return it to its original position (this manipulation allows you to pierce the capsule and open access to the powder contained in the capsule, into the opening of the mouthpiece). The capsule should be pierced only once, this minimizes the ingestion of pieces of gelatin in the mouth and / or throat of the destroyed capsule shell during inhalation.
- Exhale deeply (not through the mouthpiece).
- Gently squeeze the mouthpiece with your teeth and wrap your lips tightly around it. Take a deep and strong breath through your mouth. At this point, a vibrating sound will be heard inside the capsule compartment due to the rotation of the capsule and dispersion of the drug. Do not squeeze and chew the mouthpiece with your teeth, do not press on it while inhaling, otherwise the capsule movement may be blocked. Do not close the holes located on the sides of the mouthpiece, otherwise the free movement of air inside the inhaler will be disturbed and, as a result, the dispersion of the powder will decrease.
- Hold your breath for at least 10 seconds (if possible, longer). Remove the inhaler from the mouth. Exhale slowly. Then you can breathe normally.
- Repeat steps 7-9 to ensure that the full dose is inhaled.
- Open the compartment, remove the empty capsule, close the compartment.
- Close the mouthpiece tightly with the cap.
At least once a week, the mouthpiece should be cleaned with a dry cloth on the outside.
Side effects
Formoterol-native can cause the following side effects (estimated frequency of their occurrence: very often -> 1/10 of appointments, 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, chest and mediastinal organs: often - increased sputum production, sinusitis; infrequently - dysphonia, bronchospasm (including paradoxical); very rarely - cough;
- from the immune system: very rarely - urticaria, itching, rash, angioedema, anaphylactic reactions;
- from the nervous system and psyche: often - tremor, headache; infrequently - dizziness, increased excitability, anxiety, agitation, insomnia; very rarely - a violation of taste, increased fatigue;
- from the side of metabolism and nutrition: very rarely - metabolic acidosis;
- from the heart and blood vessels: often - chest pain, palpitations; infrequently - tachycardia; very rarely - angina pectoris, decrease or increase in blood pressure (hypo- or hypertension), heart rhythm disturbances (including tachyarrhythmia, atrial fibrillation, ventricular extrasystoles), peripheral edema;
- from the musculoskeletal and connective tissue: often - back pain, cramps of the lower extremities; infrequently - myalgia, muscle spasm;
- from the gastrointestinal tract: infrequently - dryness of the oral mucosa; very rarely - nausea;
- infectious and parasitic diseases: often - pharyngitis, acute respiratory viral infection;
- laboratory and instrumental data: infrequently - depression of the ST segment, flattening or inversion of the T wave, lengthening of the QT interval on the electrocardiogram; very rarely - hyperglycemia, hypokalemia;
- others: often - fever; infrequently - irritation of the mucous membrane of the pharynx and larynx.
Overdose
Cases of overdose of Formoterol-native have not been recorded. Presumably, the development of phenomena inherent in an overdose of other β 2 -adrenomimetics, or an increase in the existing side reactions: dry mouth, nausea, vomiting, metabolic acidosis, hyperglycemia, hypokalemia, dizziness, headache, drowsiness, weakness, nervousness, anxiety, tremor, increase or decrease in blood pressure, palpitations, chest pain, ventricular arrhythmias, tachycardia up to 200 beats per minute, convulsions, cardiac arrest.
Requires symptomatic and supportive therapy. In serious cases, the patient is hospitalized. The indicators of cardiac activity should be monitored. If necessary, it is possible to use cardioselective β 2 -adrenergic blockers, but under strict medical supervision and subject to special care, since there is a risk of developing bronchospasm.
special instructions
In bronchial asthma, Formoterol-native is prescribed only in addition to the main therapy in case of insufficient control of symptoms during monotherapy with inhaled GCS or severe forms of the disease requiring the use of a combination of inhaled GCS and a long-acting β 2 -adreporeceptor agonist. Formoterol-native should not be administered concurrently with other long-acting β 2 -adrenoreceptor agonists. When prescribing a drug, the physician should assess the patient's condition with respect to the adequacy of the anti-inflammatory therapy they are receiving. It should be continued unchanged while using formoterol, even in the case of a significant improvement in the condition.
For the relief of an acute attack of bronchial asthma, the use of β 2 -adrenoreceptor agonists is indicated. In case of a sharp deterioration in the condition, you must urgently consult a doctor.
Formoterol-native in rare cases causes the development of hypokalemia, which increases the risk of arrhythmias, and can be potentially dangerous. This effect of the drug can increase with hypoxia and under the influence of concomitant treatment, therefore, special care should be taken in patients with severe bronchial asthma. It is recommended to regularly monitor serum potassium levels.
Like other inhaled drugs, Formoterol-native can cause the development of paradoxical bronchospasm. In this case, the drug is canceled and alternative treatment is carried out.
At a daily dose exceeding 54 mcg (more than 4 inhalations), formoterol can cause false positive drug test results.
There are isolated reports of accidental ingestion of Formoterol-native capsules. In most cases, no adverse events were observed.
The healthcare professional should explain to the patient how to use the drug correctly, especially if he does not have better breathing after inhalation.
Influence on the ability to drive vehicles and complex mechanisms
There is no information on the effect of formoterol on cognitive and psychophysical functions of humans. Patients in whom Formoterol-native causes undesirable reactions in the form of dizziness, tremors, muscle cramps, etc., should refrain from driving a car and potentially hazardous types of work that require speed of reactions and / or increased attention.
Application during pregnancy and lactation
The safety of formoterol when used during pregnancy and lactation has not been established.
For pregnant women, Formoterol-native can only be prescribed by a doctor if the expected benefit from the forthcoming therapy for the mother outweighs the possible risks to the fetus. It should be borne in mind that beta 2 -adrenomimetics (including formoterol) can slow down the process of childbirth due to a relaxing effect on the smooth muscles of the uterus.
It is not known whether the drug penetrates into the mother's milk. If treatment is required during this period, breastfeeding should be discontinued.
In experimental studies in animals with oral administration of formoterol, there was no negative effect on fertility. The effect of Formoterol-native on the human reproductive system has not been established.
Pediatric use
The use of Formoterol-native is contraindicated in children and adolescents under 18 years of age.
With impaired renal function
In patients with functional impairment of the kidneys, the pharmacokinetic parameters of the drug have not been studied.
For violations of liver function
In patients with functional disorders of the liver, the pharmacokinetics of the drug have not been studied.
Use in the elderly
There are no special instructions on the dosage regimen for elderly patients.
Drug interactions
Formoterol-native should be used with caution in combination with the following drugs: tricyclic antidepressants, monoamine oxidase (MAO) inhibitors, macrolides, antihistamines, phenothiazines, procainamide, disopyramide, quinidine and other drugs that can lengthen the QT interval. With such a combination, it is possible to increase the effect of adrenostimulants on the cardiovascular system and increase the risk of ventricular arrhythmias. The concomitant use of other sympathomimetics can aggravate the side effects of Formoterol-native.
Glucocorticosteroids, diuretics and xanthine derivatives can enhance the potential hypokalemic effect of formoterol.
In patients with bronchial asthma, the simultaneous use of β 2 -adrenergic blockers can weaken the effect of formoterol and lead to serious bronchospasm. Therefore, in bronchial asthma, Formoterol-native is contraindicated for use with β 2 -adrenergic blockers (including eye drops), except in cases of urgent need.
Anesthesia with halogenated hydrocarbons during formoterol therapy increases the risk of arrhythmias.
Analogs
Analogs of Formoterol-native are: Astalin, Atimos, Berotek, Ventolin, Vertasort, Clenbuterol, Kombipek, Oxis Turbuhaler, Salamol Steri-Neb, Salamol Eco Light Breathing, Salbutamol, Salgim, Foradil, Tsibutol and others Cyclokaps.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° С out of reach of children, protected from light.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Formoterol-native
On specialized sites and forums, there are very few reviews about Formoterol-native, they are mostly negative. Patients who have been prescribed the drug in addition to the main therapy of bronchial asthma call this agent a "dummy" due to the complete absence of bronchodilatory action. Some doctors note that the active substance formoterol itself is effective, however, they believe that it may not enter the lungs during inhalation due to poor-quality additives in the capsule composition.
Price for Formoterol-native in pharmacies
Depending on the region of sale and the pharmacy network, the price for Formoterol-native (capsules with powder for inhalation, 12 mcg each) can be: 290–396 rubles. per pack of 30 capsules, 548-630 rubles. for a pack of 60 capsules with an inhaler included.
Formoterol-native: prices in online pharmacies
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Drug name Price Pharmacy |
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Formoterol-native 12 mcg capsules with powder for inhalation 30 pcs. 353 r Buy |
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Formoterol-native 12 mcg capsules with powder for inhalation 60 pcs. 739 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!
