Universal reference book for medicines
Product name: FORMOTEROL-NATIV (FORMOTEROL-NATIV)

Active substance: formoterol

Type: Bronchodilator-beta- 2- adrenomimetic

Composition, form of production and packaging
Capsules with powder for inhalation solid transparent, size 3, light brown; the contents of the capsules are white or almost white powder.
1 caps.

formoterol fumarate dihydrate 12 μg

Excipients: sodium benzoate - 0.02 mg, lactose monohydrate - up to 12 mg.

The composition of the capsule shell: dye caramel (E150c) - 1.4388%, hypromellose - up to 100%.

10 pieces.
- Packing contour mesh (3) in a set. with the device d / inhal. or without it - packs cardboard.
10 pieces.
- Packing contour mesh (6) in a set. with the device d / inhal. or without it - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2016.

PHARMACHOLOGIC EFFECT

Formoterol is a selective agonist?
2- adrenoreceptors (beta 2- adrenomimetic). It has a bronchodilator effect in patients with reversible airway obstruction. The action of the drug occurs quickly (within 1-3 min) and persists for 12 hours after inhalation. With the use of therapeutic doses, the effect on the cardiovascular system is minimal and is noted only in rare cases.
Formoterol inhibits the release of histamine and leukotrienes from mast cells.
In animal experiments, some of the anti-inflammatory properties of formoterol have been shown, such as the ability to inhibit the development of edema and the accumulation of inflammatory cells.
In experimental animal studies in vitro, it was shown that racemic formoterol and its (R, R) and (S, S) enantiomers are highly selective agonists?
2 receptors. (S, S) enantiomer was 800-1000 times less active than the (R, R) enantiomer and did not adversely affect the activity of the (R, R) enantiomer with respect to the effect on the smooth muscle of the trachea. No pharmacological evidence has been obtained for the advantage of using one of these two enantiomers, as compared to the racemic mixture.
In studies conducted in humans, it has been shown that formoterol effectively prevents bronchospasm caused by inhaled allergens, physical exertion, cold air, histamine or methacholine.
As the bronchodilator effect of formoterol remains pronounced within 12 hours after inhalation, the administration of the drug 2 times / day for prolonged maintenance therapy allows in most cases to provide the necessary control of bronchospasm in chronic lung diseases, both during the day and at night.
In patients with COPD stable course, formoterol, used in the form of inhalations in doses of 12 or 24 μg 2 times / day is accompanied by an improvement in the quality of life parameters.

PHARMACOKINETICS

The therapeutic dosage range of formoterol is from 12 μg to 24 μg 2 times / day.
Data on pharmacokinetics of formoterol were obtained in healthy volunteers after inhalation of formoterol in doses above the recommended range and in COPD patients after inhalation of formoterol in therapeutic doses.
Suction

After a single inhalation of formoterol at a dose of 120 μg to healthy volunteers, formoterol is rapidly absorbed into the blood plasma, C max formoterol in the blood plasma is 266 pmol / l and is reached within 5 minutes after inhalation.
In patients with COPD who received formoterol 12 or 24 μg twice daily for 12 weeks, blood plasma concentrations of formoterol measured 10 min, 2 h and 6 h after inhalation were in the ranges 11.5-25.7 lmol / L and 23.3-50.3 pmol / l, respectively.
In studies in which the total excretion of formoterol and its (R, R) and (S, S) enantiomers in the urine was studied, it was shown that the amount of formoterol in the systemic blood flow increases in proportion to the amount of inhaled dose (12-96 μg).

After inhalation of formoterol 12 or 24 μg twice a day for 12 weeks, excretion of unchanged formoterol in urine in patients with bronchial asthma (DB) increased by 63-73%, and in COPD patients - by 19-38%.
This indicates a certain cumulation of formoterol in the blood plasma after multiple inhalations. At the same time, there was no greater cumulation of one of the enantiomers of formoterol compared to another after repeated inhalations.
Most of the formoterol used with the inhaler is swallowed and then absorbed from the digestive tract.
When 80 μg of 3 H-labeled formoterol was administered, at least 65% of formoterol was absorbed into two healthy volunteers.
Distribution

The binding of formoterol to plasma proteins is 61-64%, binding to serum albumin is 34%.
In the range of concentrations noted after the application of therapeutic doses of the preparation, saturation of binding sites is not achieved.
Metabolism

The main way of metabolism of formoterol is direct conjugation with glucuronic acid.
Another way of metabolism is O-demethylation followed by conjugation with glucuronic acid (glucuronidation).
Low-value metabolic pathways include conjugation of formoterol with sulfate, followed by deforming.
The set of isoenzymes participate in the glucuronidation processes (UGT1A1, 1AZ, 1A6, 1A7, 1A8, 1A9, 1A10, 2B7 and 2B15) and 0-demethylation of formoterol (CYP2D6, 2C19, 2C9 and 2A6), which implies a low probability of drug interaction by inhibiting any one, or isoenzyme, taking part in the metabolism of formoterol. In therapeutic concentrations, formoterol does not inhibit the isoenzymes of the cytochrome P450 system.
Excretion

When taking formoterol in a dose of 12 or 24 mcg 2 times / day for 12 weeks, unchanged in the urine is released 10% and 15-18% of the total dose in patients with asthma;
7% and 6-9% of the total dose, respectively, in patients with COPD.
The calculated fractions of (R, R) and (S, S) enantiomers of unchanged formoterol in urine are 40% and 60%, respectively, after a single dose of formoterol (12-120 μg) in healthy volunteers and after single and repeated doses of formoterol in BA patients .

The active substance and its metabolites are completely eliminated from the body;
about 2/3 of the applied dose is excreted in the urine, 1/3 - with feces. The renal clearance of formoterol is 150 ml / min.
In healthy volunteers, the final T 1/2 of formoterol from the plasma after a single inhalation of the formoterol preparation at a dose of 120 μg is 10 hours;
the final T 1/2(R, R) and (S, S) enantiomers calculated from excretion in the urine are 13.9 and 12.3 hours, respectively.
Pharmacokinetics in selected patient groups

Floor

After adjusting for body weight, the pharmacokinetic parameters of formoterol in men and women do not differ significantly.

Elderly patients (over 65 years of age)

Data in favor of the need to change the dosage of formoterol in patients older than 65 years compared with younger patients was not received.

Patients with impaired hepatic and / or renal function

The pharmacokinetics of formoterol in patients with impaired hepatic and / or renal function have not been studied.

INDICATIONS

- prevention and treatment of bronchial obstruction in patients with bronchial asthma (BA) as a supplement to inhaled glucocorticosteroids;

- prevention of bronchospasm caused by inhalation of allergens, cold air or physical exertion as a supplement to inhaled glucocorticosteroids;

- prevention and treatment of bronchial obstruction in patients with COPD, with both reversible and irreversible bronchial obstruction, chronic bronchitis and emphysema.

DOSING MODE

Formoterol-native is intended for inhalation in patients over 18 years of age.
The drug is not intended for oral administration.
The dose of Formoterol-native is selected individually depending on the needs of the patient.
Use the smallest dose that provides a therapeutic effect. When the symptoms of bronchial asthma are controlled against the background of Formoterol-native therapy, it is necessary to consider the possibility of a gradual decrease in the dose of the drug. Reduction in the dose of Formoterol-native is carried out under regular medical supervision of the patient's condition.
The drug is a capsule with powder for inhalation, which should be used only with a special device - inhaler "Inhaler CDM ® ", which is included in the package.

Bronchial asthma

The dose of Formoterol-native for regular maintenance therapy (12-24 μg (contents 1-2 caps.) 2 times / day.

Formoterol-native should be used only as an adjunct to inhaled glucocorticosteroids.
Do not exceed the maximum recommended dose of the drug 48 μg / day (the contents of 4 caps.).
Given that the maximum daily dose of Formoterol-native is 48 μg, if necessary, 12-24 μg / day can be used to relieve the symptoms of bronchial asthma.

If the need for additional doses of Formoterol-native drug ceases to be episodic (for example, it becomes more frequent than 2 days a week), this may indicate a worsening of the course of bronchial asthma, you should consult a doctor.
Against the background of exacerbation of bronchial asthma should not begin treatment with Formoterol-native drug or change the dosage of the drug.
Formoterol-native should not be used to stop acute attacks of bronchial asthma.

Prevention of bronchospasm caused by physical exertion or the inevitable effects of a known allergen

Formoterol-native should be administered at a dose of 12 μg (1 capsule) 15 minutes before supposed contact with the allergen or before the load.
Additional inhalations of the drug should not be carried out within the next 12 hours.
Prevention of severe bronchospasm

Patients with severe bronchospasm in the anamnesis may require a single inhalation in a dose of 24 mcg (the contents of 2 caps.).

COPD

The dose of Formotrol-native for regular maintenance therapy of COPD is 12-24 μg (1-2 capsules content) 2 times / day.

Instructions for inhalation

In order to ensure the correct use of the drug, a doctor or other health care provider should:

1. caution the patient that the capsules are for inhalation use only and are not intended for ingestion;

2. Explain to the patient that capsules with powder for inhalation should only be taken with Inhaler CDM ® ;

3. show the patient how to use the inhaler.

Remove the capsule from the cell pack immediately before use.

Instructions for the use of the inhaler "Inhaler CDM ® "

Inhaler powder "Inhaler CDM ® " - a plastic device with a movable top and with a retractable compartment for the capsule, about 6 cm high.

"Inhaler CDM ® " is a single-dose inhaler that allows to dose and inhale the drug in very small doses.
The formoterol-native drug enters the patient's airway along with the air streams when performing an active inspiration through the mouthpiece of the device.
"Inhaler CDM ® " is very simple to use.
Follow the step-by-step instructions below.
Step 1. Remove the transparent cap from the Inhaler CDM ® device.

Step 2. Hold the device firmly with one hand, with the index finger and the thumb of the other hand, open the capsule compartment.
To do this, press the index finger on PUSH in the moving part of the Inhaler CDM ® , sliding the compartment in the opposite direction.
Step 3. While holding the device with one hand, insert the capsule with the drug into the compartment of the compartment.

Step 4. Make sure that the capsule is correctly inserted into the socket.

Step 5. While holding the "Inhaler CDM®" in the vertical position, close the compartment by pressing the thumb in the opposite direction until it stops, until a click is heard.

Step 6. Hold the device "Inhaler CDM ® " strictly vertically.

Step 7. Put it in working order.
To do this, press firmly onto the mouthpiece so that the arrow on the body disappears from the bottom of the device to the top line.Then release the mouthpiece to return it to its original position. Thus, you will pierce the capsule, opening access to the drug in the lumen of the mouthpiece.
Attention: due to the destruction of the gelatin capsule, small pieces of gelatin can be inhaled into the mouth or throat.
In order to reduce this phenomenon to a minimum, do not pierce the capsule more than 1 time.
Step 8. Attention: exhale before inhalation.
Do not exhale through the mouthpiece!
Step 9. Gently squeeze the mouthpiece "Inhaler CDM ® " with your teeth, tightly grasp it with your lips and take a deep and strong breath through your mouth.
You will hear a vibrating sound inside the capsule compartment, emitted by the capsule while rotating and dispersing the drug. Attention: the mouthpiece can not be chewed and hard to hear with your teeth! Do not press on the mouthpiece when inhaled. This can block the movement of the capsule. Hold your breath for about 10 seconds or longer, as far as possible.
Remove the inhaler from the mouth.
Make a slow exhalation. Then breathe normally.
Repeat steps 8-9 again, to ensure that the dose of the drug is inhaled.

Step 10. After the inhalation, open the capsule compartment (step 2) the capsule and then close it.

Attention

When carrying out inhalation, try not to cover the holes located on the sides of the mouthpiece.
This can interfere with the free movement of air within the inhaler, thereby reducing the dispersion of the contents of the capsule.
Always after use, close the Inhaler CDM ® cap, this will keep the mouthpiece clean.

Regularly (once a week), you should clean the mouthpiece from the outside with a dry cloth.

There are separate reports of accidental ingestion of whole capsules by the patients, without using an inhalation device.
Most of these cases are not associated with the development of adverse events. The health worker should explain to the patient how to correctly apply the medication, especially if after inhalation the patient does not have an improvement in breathing.
SIDE EFFECT

Undesired reactions are distributed according to the frequency of occurrence.
The following criteria were used to estimate the frequency: 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).
Infectious and parasitic diseases: often - pharyngitis, acute respiratory viral infection.

From the side of the immune system: very rarely - anaphylactic reactions, urticaria, angioedema (Quincke's edema), itching, rash.

From the side of metabolism and nutrition: very rarely - metabolic acidosis.

Disorders of the psyche: infrequently - agitation, anxiety, increased excitability, insomnia;
very rarely - increased fatigue.
From the nervous system: often - headache, tremor;
infrequently - dizziness; very rarely - a change in taste.
From the heart: often - a feeling of palpitations, pain in the chest;
infrequently - tachycardia; very rarely - peripheral edema; stenocardia, disturbance of the heart rhythm (including atrial fibrillation, ventricular extrasystoles, tachyarrhythmia).
From the side of the vessels: very rarely - lowering blood pressure (hypotension), increasing blood pressure (hypertension).

On the part of the respiratory system, chest and mediastinal organs: often -xinusitis, increased production of sputum;
infrequently - bronchospasm, including paradoxical, dysphonia; very rarely - cough.
From the gastrointestinal tract: infrequent - dryness of the mucous membrane of the stripes of the mouth;
very rarely - nausea.
From the musculoskeletal and connective tissue: often - pain in the back, leg cramps;
infrequently - muscle spasm, myalgia.
General disorders and disorders at the injection site: often - fever;
infrequent - irritation of the mucous membrane of the pharynx and larynx.
Laboratory and instrumental data: infrequent - flattening or inversion of the T wave, depression of the ST segment, prolongation of the QT interval on the electrocardiogram;
very rarely - hypokalemia, hyperglycemia.
If any of the side effects indicated in the manual are aggravated, or if you notice any other adverse reactions not listed in the instructions, tell your doctor.

CONTRAINDICATIONS

- hypersensitivity and / or intolerance to any of the components of the drug;

- age up to 18 years;

- lactation;

- rare hereditary diseases, such as lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

Carefully

If you have one of these diseases, always consult a doctor before using the drug.

Observance of extreme caution in the use of Formoterol-native preparation (especially in terms of dose reduction) and careful monitoring of patients is required in the presence of the following concomitant diseases: IHD;
heart rhythm disturbances and conduction, especially AV blockade III degree; severe heart failure; idiomatic hypertrophic subaortic stenosis; severe degree of arterial hypertension; aneurysm of any localization; pheochromocytoma; ketoacidosis; hypertrophic obstructive cardiomyopathy; thyrotoxicosis; known or suspected prolongation of the QTc interval (QT corrected> 0.44 sec).
Given the hyperglycemic effect characteristic of beta 2 -adrenomimetics, in patients with diabetes mellitus taking formoterol-native, an additional regular monitoring of the concentration of glucose in the blood is recommended.

PREGNANCY AND LACTATION

The safety of the use of formoterol in pregnancy and during breastfeeding has not been established to date.

Use during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.
Formoterol, as well as other beta 2 -adrenomimetiki can slow down the process of childbirth as a result of tocolytic action (relaxing effect on the smooth muscles of the uterus).
It is not known whether formoterol passes into breast milk. Therefore, if necessary, the use of formoterol, breast-feeding should be discontinued.
Data on the effect of the drug on fertility is not. Studies in experimental animals showed no effect on fertility when administered orally formoterol.
APPLICATION FOR CHILDREN

Contraindicated use of the drug for children and adolescents under the age of 18 years.

SPECIAL INSTRUCTIONS

Anti-inflammatory therapy
in patients with bronchial asthma Formoterol-native should only be used as an additional treatment for the symptoms of lack of control on monotherapy with inhaled corticosteroids or severe form of the disease that requires the use of a combination of inhaled corticosteroids and agonist? 2 -adrenoceptor prolonged action. Formoterol should not be used with other native-agonists? 2 -adrenoceptor prolonged action.
In appointing the drug Formoterol-native is necessary to assess the condition of patients with respect to the adequacy of the anti-inflammatory therapy they receive.After beginning treatment Formoterol-native drug in patients should be encouraged to continue anti-inflammatory therapy unchanged, even if the improvement is marked.
For relief of an acute attack of asthma should be used agonists?
2- adrenoreceptors. With the sudden deterioration of the patients should seek immediate medical attention.
Hypokalemia
consequence of therapy Beta 2 -adrenomimetikami including Formoterol-native, may be the development of a potentially serious hypokalemia. Hypokalemia may increase the risk of arrhythmias.
Because this action Formoterol-native product can be enhanced by hypoxia and concomitant treatment, special caution should be exercised in patients with bronchial asthma, severe. In these cases, we recommend regular monitoring of the concentration of potassium in the blood serum.
Paradoxical bronchospasm
As with other inhaled medications, Formoterol-native may cause paradoxical bronchospasm. In this case, you should immediately remove the drug and prescribe alternative treatments.
Use of formoterol in a dose exceeding 54 mg / day (over 4 inhalations) may result in positive test results for doping.
Effects on ability to drive vehicles and other vehicles, to work with moving machinery
Data on the effect of the drug Formoterol-native on the ability to drive vehicles and management mechanisms are absent. In the case of adverse reactions such as dizziness, tremor, convulsions or muscle spasm should refrain from driving motor vehicles and control mechanisms, as well as other classes of potentially hazardous activities that require high concentration and psychomotor speed reactions.
OVERDOSE

Symptoms: an overdose of formoterol may possibly lead to the development of phenomena characteristic of an overdose of the beta 2 -adrsnomimetikami or enhancement of side effects: chest pain, palpitations, tachycardia up to 200 beats / min, ventricular arrhythmias, increased blood pressure lowering fire, dryness. mouth, nausea, vomiting, headache, dizziness, tremors, nervousness, weakness, anxiety, drowsiness, metabolic acidosis, hypokalemia, hyperglycemia, seizures. As with all inhaled beta 2 -adrenomimetikov, with an overdose of formoterol, possible cardiac arrest and death.
Treatment: shown holding a supportive and symptomatic therapy. In severe cases, hospitalization is necessary.
It can be considered the use of cardioselective beta 2 adrenoblokatorov, but only under close medical supervision, subject to extreme caution since the use of such funds can cause bronchospasm. Recommended monitoring indicators of cardiac activity.
DRUG INTERACTION

Formoterol drug-native, as well as other beta 2 -adrenomimetiki should be used with caution in patients taking drugs such as quinidine, disopyramide, procainamide, phenothiazines, macrolides, MAO inhibitors, tricyclic antidepressants, antihistamines and other drugs, which are known to prolong the QT interval, as in these cases, the effect of agonists on the cardiovascular system can be enhanced and an increased risk of ventricular arrhythmias.
The simultaneous use of other sympathomimetic agents can lead to aggravation of adverse drug reactions Formoterol-native.
The simultaneous use of xanthine derivatives, corticosteroids or diuretics may enhance the potential effect gipokaliemicheskoe Formoterol-native drug.
In patients receiving anesthesia with the use of halogenated hydrocarbons, increases the risk of arrhythmias.
The preparations belonging to the beta 2 adrenoblokatorov may weaken the action of Formoterol-native preparation and result in severe bronchospasm in patients with asthma. In this regard, the preparation should not be used in conjunction Formoterol-native beta 2 adrenoblokatorami (including eye drops), unless the use of such combination preparations do not force any emergency reasons.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored protected from light and the reach at a temperature not higher than 25 ° C.
Shelf life - 2 years.
Do not use after the expiry date printed on the package.

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