Formoterol

Brand Nativa

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Clinical Pharmacology

Pharmacodynamics. Formoterol is a selective β2 – adrenoreceptor agonist (β2 – adrenomimetic). It has a bronchodilator effect in patients with reversible airway obstruction. The action of the drug comes quickly (within 1-3 minutes) and lasts for 12 hours after inhalation. When using 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 were shown, such as the ability to inhibit the development of edema and the accumulation of inflammatory cells.

Experimental studies in animals in vitro have shown that racemic formoterol and its (R, R) and (S, S) enantiomers are highly selective β2 receptor agonists. The (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 tracheal smooth muscle. No pharmacological evidence was obtained of the benefits of using one of these two enantiomers, as compared to the racemic mixture.

Studies in humans have shown that formoterol effectively prevents bronchospasm caused by inhaled allergens, exercise, cold air, histamine or methacholine. Since the bronchodilator effect of formoterol remains pronounced for 12 hours after inhalation, the administration of the drug 2 times a day for long-term 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 chronic obstructive pulmonary disease (COPD) of a stable course of formoterol, used in the form of inhalation in doses of 12 or 24 mg 2 times a day, accompanied by an improvement in the parameters of quality of life.

Pharmacokinetics. Therapeutic dose range of formoterol is from 12 μg to 24 μg 2 times a day. Data on the pharmacokinetics of formoterol were obtained from healthy volunteers after inhalation of formoterol in doses above the recommended range and in patients with COPD after inhalation of formoterol in therapeutic doses.

Suction. After a single inhalation of formoterol at a dose of 120 mcg to healthy volunteers, formoterol is rapidly absorbed into the blood plasma, the maximum concentration of formoterol in the blood plasma (Cmax) is 266 pmol / l and is reached within 5 minutes after inhalation. In patients with COPD who received formoterol in a dose of 12 or 24 μg 2 times a day for 12 weeks, plasma formoterol concentrations measured 10 minutes, 2 hours and 6 hours after inhalation were in the range of 11.5-25.7 pmol / l and 23.3-50.3 pmol / l, respectively.

In studies that studied the total excretion of formoterol and its (R, R) and (S, S) enantiomers with urine, it was shown that the amount of formoterol in the systemic circulation increases in proportion to the inhalation dose (12-96 μg).

After inhalation use of formoterol in a dose of 12 or 24 μg 2 times a day for 12 weeks, the excretion of unchanged formoterol in the urine increased in patients with bronchial asthma (BA) by 63–73%, and in patients with COPD by 19–38%. This indicates some cumulation of formoterol in the blood plasma after repeated inhalations. However, there was no greater cumulation of one of the enantiomers of formoterol compared to the other after repeated inhalations.

Most of the formoterol used with the inhaler is swallowed and then absorbed from the gastrointestinal tract (GIT). When prescribing 80 mcg of 3H-labeled formoterol, at least 65% of formoterol was absorbed by two healthy volunteers inside.

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

Metabolism. The main route of metabolism of formoterol is direct conjugation with glucuronic acid. Another route of metabolism is O-demethylation followed by conjugation with glucuronic acid (glucuronidation).

Unimportant metabolic pathways include conjugation of formoterol with sulfate, followed by deformation. Many isoenzymes are involved in the process of glucuronidation (UGT1A1, 1A3, 1A6, 1A7, 1A8, 1A9, 1A10, 2B7 and 2B15) and O-demethylation (CYP2D6, 2C19, 2C9 and 2A6) of formoterol, which suggests a low likelihood that there may be a member of the team. or an isoenzyme involved in the metabolism of formoterol. At therapeutic concentrations, formoterol does not inhibit cytochrome P450 isoenzymes.

Derivation. When taking formoterol in a dose of 12 or 24 mg 2 times a day for 12 weeks, 10% and 15-18% of the total dose in patients with BA is excreted unchanged in the urine; 7% and 6-9% of the total dose, respectively, in patients with COPD.

The calculated proportions 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 patients with BA .

The active substance and its metabolites are completely eliminated from the body; about 2/3 of the oral dose is excreted in the urine, 1/3 in the feces. Renal clearance of formoterol is 150 ml / min.

In healthy volunteers, the final half-life of formoterol from plasma after a single inhalation of the drug formoterol at a dose of 120 μg is 10 hours; the final elimination half-life of the (R, R) and (S, S) enantiomers, calculated by excretion with urine, is 13.9 and 12.3 hours, respectively.

Pharmacokinetics in certain groups of patients. Floor. After adjusting for body weight, the pharmacokinetic parameters of formoterol in men and women do not have significant differences.

Elderly patients (over 65). Data in favor of the need to change the dosage of formoterol in patients older than 65 years compared with younger patients is not received.

Patients with impaired liver and / or kidney function. The pharmacokinetics of formoterol in patients with impaired liver and / or kidney function has not been studied.

Indications

Prevention and treatment of bronchial obstruction in patients with bronchial asthma (BA) as an adjunct to treatment with inhaled glucocorticosteroids.

Prevention of bronchospasm caused by inhalation of allergens, cold air or exercise as an adjunct to therapy with inhaled glucocorticosteroids.

Prevention and treatment of bronchial obstruction in patients with chronic obstructive pulmonary disease (COPD), in the presence of both reversible and irreversible bronchial obstruction, chronic bronchitis and pulmonary emphysema.

Composition

Active ingredient: 12 mcg of formoterol fumarate dihydrate.

Formoterol is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Formoterol - Native	Nativa	Russia	Other
Atimos	Chiesi Pharmaceutical SpA	Italy	spray can
Foradil	Novartis	Switzerland	capsules
Oxis Turbuhaler	AstraZeneca	UK	powder

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Dosage and Administration

Formoterol-native is intended for inhalation use in patients over the age of 18 years. The drug is not intended for oral administration.

The dose of the drug Formoterol-native is selected individually depending on the needs of the patient. You should use the lowest dose that provides a therapeutic effect. When controlling the symptoms of bronchial asthma during therapy with Formoterol-native, it is necessary to consider the possibility of gradually reducing the dose of the drug. Reducing the dose of the drug Formoterol-native is carried out under regular medical supervision of the patient.

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 the drug Formoterol-Native for regular maintenance therapy is 12-24 μg (contents of 1-2 capsules) 2 times a day. Formoterol-native should be used only as an additional therapy to inhaled glucocorticosteroids (GCS). Do not exceed the maximum recommended dose of the drug 48 mg (contents of 4 capsules) per day. Given that the maximum daily dose of the drug Formoterol-native is 48 μg, if necessary, you can additionally use 12-24 μg per day to relieve symptoms of bronchial asthma.

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

Prevention of bronchospasm caused by exercise or the inevitable exposure to a known allergen. Formoterol-native should be used in a dose of 12 mcg (contents of 1 capsule) 15 minutes before the intended contact with the allergen or before the load. Additional inhalation of the drug should not be carried out within the next 12 hours.

Prevention of severe bronchospasms. Patients with a history of severe bronchospasm may require a single inhalation at a dose of 24 micrograms (contents of 2 capsules).

COPD The dose of the drug Formoterol-Native for regular maintenance treatment of COPD is 12-24 μg (contents of 1-2 capsules) 2 times a day.

Instructions for inhalation. In order to ensure the correct use of the drug, a doctor or other medical professional must:
1. warn the patient that the capsules are intended for inhalation use only and are not intended to be swallowed;
2. explain to the patient that the use of capsules with powder for inhalation should be done only with the help of “Inhaler CDM®”;
3. show the patient how to use the inhaler. Remove the capsule from the cellular packaging immediately before use.

Instructions for use of the Inhaler CDM® inhaler. Inhaler powder "Inhaler CDM®" - a plastic device with a moving upper part and with a retractable capsule compartment, about 6 cm high. "CDM® Inhaler" is a single-dose inhaler that allows you to dose and inhale the drug in very small doses. The drug Formoterol-Native enters the patient's respiratory tract along with the flow of air when performing an active breath through the mouthpiece of the device. "Inhaler CDM®" is very easy to use. Follow the step-by-step instructions below:
Step 1. Remove the transparent cap from the CDM® Inhaler device, as shown in Figure 1.
Step 2. Hold the device firmly with one hand, forefinger and thumb of the other hand, open the capsule compartment, as shown in Fig.2.To do this, press with the index finger on the PUSH in the moving part “Inhaler CDM®”, moving the compartment in the opposite direction.
Step 3. Holding the device with one hand, insert the capsule with the drug into the slot of the compartment (Fig. 3).
Step 4. Make sure that the capsule is correctly inserted into the slot (Fig.4).
Step 5. While holding the CDM® Inhaler in a vertical position, close the compartment by pressing your thumb in the opposite direction until it stops, until a click is heard (Fig. 5).
Step 6. Keep the “Inhaler CDM®” device strictly vertically (Fig.6).
Step 7. Bring it to working condition, as shown in Fig. 7. To do this, with an effort, press the mouthpiece so that the arrow on the case disappears beyond the borders of the lower part of the device to the upper line. Then release the mouthpiece to return it to its original position. Thereby you will pierce the capsule, opening the access of the medicinal product into the mouthpiece of the mouthpiece. Attention: due to the destruction of the gelatin capsule, small pieces of gelatin can be inhaled through the mouth or throat. In order to minimize this phenomenon, one should not pierce the capsule more than 1 time.
Step 8. Attention: before inhalation should be exhaled (Fig. 8). Do not exhale through the mouthpiece!
Step 9. Gently squeeze the “Inhaler CDM®” mouthpiece with your teeth, tightly clasp it with your lips and take a deep and strong breath through the mouth (Fig.9). You will hear a vibrating sound inside the capsule compartment, emitted by the capsule during the rotation and dissipation of the drug. Warning: the mouthpiece can not be chewed and strongly squeezed teeth! Do not press the mouthpiece when inhaled. This may block the movement of the capsule. Hold your breath for about 10 seconds or longer as possible. Remove the inhaler from the mouth. Exhale slowly. 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), remove the empty capsule and then close it, as shown in fig. 5. Attention: during inhalation try not to close the holes located on the sides of the mouthpiece. This can prevent the free movement of air inside the inhaler, thereby reducing the dispersion of the contents of the capsule.

Always close the “Inhaler CDM®” with a cap after use, this will keep the mouthpiece clean. Regularly (once a week) the mouthpiece should be cleaned outside with a dry cloth. There are separate reports of patients accidentally swallowing capsules of the drug as a whole, without the use of an inhalation device. Most of these cases are not associated with the development of adverse events. The health care provider should explain to the patient how to properly apply the drug, especially if after inhalation the patient does not improve breathing.

Adverse reactions

Undesirable 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 1/10000 to 1/1000 ), very rarely (

Infectious and parasitic diseases: often - pharyngitis, acute respiratory viral infection.

Immune system disorders: very rarely - anaphylactic reactions, urticaria, angioedema (angioedema, pruritus, rash).

Metabolic and nutritional disorders: very rarely metabolic acidosis.

Mental disorders: infrequently - agitation, anxiety, irritability, insomnia; very rarely - increased fatigue.

Nervous system disorders: often - headache, tremor; infrequent-vertigo; very rarely - a change in taste.

Cardiac abnormalities: often - palpitations, chest pain; infrequently - tachycardia; very rarely - peripheral edema, stenocardia, cardiac arrhythmias (includingatrial fibrillation, ventricular extrasystoles, tachyarrhythmia).

Vascular disorders: very rarely, lower blood pressure (hypotension), increased blood pressure (hypertension).

Disorders of the respiratory system, organs of the chest and mediastinum: often - sinusitis, increased production of sputum; infrequently - bronchospasm, including paradoxical, dysphonia; very rarely - cough.

Disorders of the gastrointestinal tract: infrequently - dryness of the oral mucosa; very rarely - nausea.

Disorders of the musculoskeletal and connective tissue: often - back pain, leg cramps; infrequently - muscle spasm, myalgia.

General disorders and disorders at the injection site: often - fever; infrequently - irritation of the mucous membrane of the pharynx and larynx.

Laboratory and instrumental data: infrequently - 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 adverse reactions indicated in the instruction are aggravated, or you have noticed any other adverse reactions that are not indicated in the instruction, inform your doctor.

Contraindications

Carefully. If you have one of these diseases, before using the drug, consult with your doctor. Observation of special caution when using the drug Formoterol-native (especially from the point of view of dose reduction) and careful monitoring of patients is required in the presence of the following concomitant diseases: coronary heart disease; cardiac rhythm and conduction disorders, especially atrioventricular block III; severe heart failure; idiopathic hypertrophic subaortic stenosis; severe arterial hypertension, aneurysm of any location; pheochromocytoma; ketoacidosis; hypertrophic obstructive cardiomyopathy; thyrotoxicosis; known or suspected lengthening of the QTc interval (QT corrected> 0.44 sec); Considering the hyperglycemic effect characteristic of β2-adrenomimetics, diabetic patients taking Formoterol-native, additional regular monitoring of blood glucose concentration is recommended.

Drug interactions

Formoterol-native, as well as other β2-adrenomimetics, should be used with caution in patients receiving drugs such as: quinidine, disopyramide, procainamide, phenothiazines, macrolides, monoamine oxidase inhibitors (MAO), tricyclic antidepressants, antihistamine, anti-depressants, antihistamine, antihistamine inhibitors, monoamine oxidase inhibitors (MAO), tricyclic antidepressants, antihistamine. there are also other drugs that are known to prolong the QT interval, since in these cases the effect of adrenergic stimulants on the cardiovascular system may increase and the risk of ventricular arrhythmias increases.

The simultaneous use of other sympathomimetic drugs may lead to the aggravation of adverse reactions of the drug Formoterol-native.

The simultaneous use of xanthine derivatives, glucocorticosteroids, or diuretics may enhance the potential hypokalemic effect of Formoterol-native.

In patients receiving anesthesia with halogenated hydrocarbons, the risk of arrhythmias increases.

Preparations related to β2-adrenergic blockers may weaken the effect of the drug Formoterol-native and lead to serious bronchospasm in patients with bronchial asthma. In this regard, do not use the drug Formoterol-native in conjunction with β2-adrenergic blockers (including eye drops), unless the use of such a combination of drugs is not forced by any extraordinary reasons.

Overdosage

Symptoms An overdose of formoterol can probably lead to the development of phenomena characteristic of an overdose of β2 – adrenergic mimics or increased manifestations of side effects: pain behind the sternum, palpitations, tachycardia up to 200 udmin, ventricular arrhythmias, increased or decreased arterial pressure, dry mouth, nausea, vomiting, headache, dizziness, tremor, nervousness, weakness, anxiety, drowsiness, metabolic acidosis, hypokalemia, hyperglycemia, convulsions. As with all inhaled β2 – adrenergic mimetics, overdose with formoterol may cause cardiac arrest and death.

Treatment. It is shown that the maintenance and symptomatic therapy. In serious cases, hospitalization is necessary. The use of cardioselective β2-blockers may be considered, but only under close medical supervision, subject to extreme caution, since the use of such agents may cause bronchospasm. Recommended monitoring of cardiac activity.