Formisonide-Nativ 160 mcg + 4.5 mcg/dose, 60 pcs.

Formisonide®-antibody is a combination medication containing formoterol and budesonide which have different mechanisms of action and show additive effects with respect to the severity of bronchial asthma (BA) symptoms, improvement of lung function and reduction of the frequency of exacerbations of bronchial asthma and chronic obstructive pulmonary disease (COPD).

The special properties of budesonide and formoterol make it possible to use their combination in the treatment of bronchial asthma simultaneously as maintenance therapy and for the relief of attacks, or as maintenance therapy.

Budesonide is a glucocorticosteroid (GCS) that has a rapid (within hours) and dose-dependent anti-inflammatory effect on the airway, reducing the severity of symptoms and the frequency of exacerbations of bronchial asthma after inhalation in the recommended doses. When prescribing inhaled budesonide, there is a lower incidence of serious adverse effects than when using systemic GCS. Budesonide reduces the severity of bronchial mucosal edema, mucus production, sputum formation and airway hyperresponsiveness. The exact mechanism of anti-inflammatory action of GCS is unknown.

Formoterol is a selective β2-adrenomimetic (selective β2-adrenoreceptor agonist) that causes rapid and prolonged relaxation of bronchial smooth muscle in patients with reversible airway obstruction.

The bronchodilator effect is dose-dependent, occurs within 1-3 minutes after inhalation and persists for at least 12 hours after a single dose.

The effect of Formisonide®-antibody on lung function is similar to that of the combination of budesonide and formoterol monotherapy and greater than that of budesonide alone.

Indications

– Bronchial asthma, as maintenance therapy and for seizure management (insufficiently controlled using inhaled GCS and short-acting β2-adrenomimetics as on-demand therapy, or adequately controlled with inhaled GCS and long-acting β2-adrenomimetics);

– Chronic obstructive pulmonary disease (symptomatic therapy in patients with severe COPD with an ORP1 < 50% of the estimated calculated level and with a history of recurrent exacerbations, in the presence of severe disease symptoms despite therapy with long-acting bronchodilators).

Active ingredient

Composition

On one capsule:

The active ingredient: 80 µg + 4.5 µg 160 µg + 4.5 µg 320 µg + 9 µg

Budesonide 80 µg 160 µg 320 µg

p> Formoterol fumarate dihydrate 4.5 µg 4.5 µg 9 µg

Excipients:

sodium benzoate,

lactose monohydrate

How to take, the dosage

The drug is not intended to be taken orally. The dose of Formoterol-nativ is selected individually according to the needs of the patient. The lowest dose that provides therapeutic effect should be used. When achieving control of bronchial asthma symptoms during therapy with Formoterol Nativ, it is necessary to consider the possibility of gradual reduction of the drug dose. Dose reduction of Formoterol-nativ should be performed under regular medical supervision of the patient.

The drug is capsules with powder for inhalation, which should be used only with a special device – Inhaler CDM®, which is included in the package. Bronchial asthma The dose of Formoterol-nativ for regular maintenance therapy (12-24 mcg (contents 1-2 capsules) 2 times per day. Formoterol-nativ should only be used as adjunctive therapy to inhaled GCS. Do not exceed the maximum recommended dose of the drug of 48 mcg/day (contents of 4 capsules).

As the maximum daily dose of Formoterol Nativ is 48 mcg, if necessary, an additional 12-24 mcg/day may be used to relieve bronchial asthma symptoms. If the need for additional doses of Formoterol topical is no longer episodic (e.g. more than 2 days a week), this may indicate a worsening of bronchial asthma, a physician should be consulted. Against the background of bronchial asthma exacerbation should not start treatment with Formoterol-nativ or change the dosage of the drug. Formoterol-nativ should not be used to relieve acute attacks of bronchial asthma.

Prevention of bronchospasm caused by exercise or unavoidable exposure to a known allergen Formoterol-nativ should be used in a dose of 12 micrograms (1 capsule contents) 15 min before the intended exposure to the allergen or before exercise. Additional inhalations of the drug should not be carried out during the next 12 h. Prevention of severe bronchospasm Patients with a history of severe bronchospasm may require a single inhaled dose of 24 mcg (contents of 2 capsules). COPD The dose of Formotrol-Nativ for regular maintenance therapy of COPD is 12-24 mcg (contents of 1-2 capsules) 2 times daily.

Adolescents (12-17 years old):

Formisonide-nativ 80 mcg + 4.5 mcg and 160 mcg + 4.5 mcg 1-2 inhalations twice daily

Formisonide-nativ 320 mcg + 9 mcg 1 inhalation twice daily

Children over 6 years old:

Formisonide-nativ 80 mcg + 4.5 mcg 1-2 inhalations twice a day.

Interaction

In concomitant administration of ketoconazole in a dose of 200 mg once daily and budesonide in a dose of 3 mg, the concentration of budesonide in plasma is increased by an average of 6 times. When taking ketoconazole 12 hours after budesonide administration, the concentration of the latter in plasma increases on average by 3 times. There is no information about similar interaction with budesonide when administered by inhalation, but a marked increase in plasma concentrations of budesonide should be expected.

The use of Formisonide®-nativ is not recommended as maintenance therapy and for seizure control in patients receiving potent CYP3A4 inhibitors. Since there are no data for dose recommendations, the above drug combination should be avoided. If a combination of the above drugs cannot be avoided, the intervals between doses should be maximized. Decreasing the dose of budesonide should also be considered.

Formisonide®-nativ should not be administered concomitantly with β-adrenoblockers (including eye drops) because they may impair or inhibit the effects of formoterol except when necessary.

The concomitant use of Formisonide®-nativ and quinidine, disopyramide, procainamide, phenothiazines, antihistamines (terfenadine), monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants may prolong QTC interval and increase the risk of ventricular arrhythmias.

Levodopa, levothyroxine sodium, oxytocin, and ethanol may decrease cardiac muscle tolerance to β2-adrenomimetics.

The concomitant administration of Formisonide®-native monoamine oxidase inhibitors (MAOIs) as well as drugs with similar properties may increase blood pressure.

In anesthesia with preparations of halogenated hydrocarbons during administration of Formisonide®-Nativ, there is an increased risk of arrhythmias in patients.

The concomitant administration of Formisonide®-nativ and other β-adrenomimetic agonists may increase the side effect of formoterol.

The hypokalemic effect of β2-adrenomimetics may be enhanced with concomitant administration of xanthine derivatives, mineral GCS derivatives and diuretics. Hypokalemia increases the predisposition to develop arrhythmias in patients taking cardiac glycosides.

Methandienone, estrogens enhance the effects of budesonide.

No interactions of budesonide with other medications used to treat bronchial asthma have been noted.

Special Instructions

It is recommended that the dose of the drug be gradually reduced before discontinuing treatment, and abrupt withdrawal of treatment is not recommended.

The doses of 80 + 4.5 mcg/dose and 320 + 9 mcg/dose are not intended to treat patients with severe bronchial asthma.

Formisonide®-nativ is not indicated for initial therapy selection in the initial stages of treatment of bronchial asthma and COPD.

If therapy is not effective enough or the maximum recommended doses of Formisonide®-nativ are exceeded, the treatment regimen should be reconsidered.

An increase in the frequency of administration of bronchodilators as an emergency medication indicates a worsening of the course of the underlying disease and is reason to reconsider treatment tactics for bronchial asthma.

An unexpected and progressive worsening of bronchial asthma or COPD symptom control is a potentially life-threatening condition and requires urgent medical intervention. In this situation, consider increasing the dose of GCS, i.e. starting a course of oral GCS or antibiotic treatment if there is an infection.

Patients should always carry emergency medication: Formisonide®-antive (for patients with bronchial asthma using Formisonide®-antive for maintenance therapy and for attack control) or short-acting β2-adrenomimetics (for patients using Formisonide®-antive only for maintenance therapy).

The need for regular maintenance doses of Formisonide®-nativ should be explained to the patient according to the therapy chosen, even when there are no symptoms of the disease.

Inhaled Formisonide®-nativ (80 + 4.5 mcg/dose and 160 + 4.5 mcg/dose) to control attacks should only be given when symptoms occur, but it is not indicated for regular prophylactic use, i.e. before exercise. In such cases, use of a separate short-acting β2-adrenomimetic is indicated.

If the symptoms of bronchial asthma can be controlled, the dose of Formisonide®-nativ can be gradually reduced, and it is important to monitor the patients’ condition continuously. The lowest effective dose should be prescribed (see section “Dosage and administration”).

The treatment with Formisonide®-nativ should not be started during an exacerbation of bronchial asthma.

As with the use of any other inhaled drug, paradoxical bronchospasm with immediate increase in rales after a dose of Formisonide®-nativ may occur. In this case Formisonide®-nativ should be discontinued, the therapy should be reconsidered and, if necessary, alternative therapy should be prescribed.

Any inhaled GCS, especially when taking high doses over a long period of time, may have systemic effects. Systemic effects are less likely to occur with inhaled therapy than with oral GCS. Possible systemic effects include adrenal suppression, decreased bone mineral density, cataracts and glaucoma.

Because of the potential effect of inhaled GCS on bone mineral density special attention should be given to patients taking high doses over a long period of time with risk factors for osteoporosis. Studies of long-term use of inhaled budesonide in adults at a daily dose of 800 micrograms (measured dose) showed no significant effect on bone mineral density. There are no data regarding the effect of higher doses of the drug on bone mineral density.

If there is reason to believe that adrenal function has been impaired on prior systemic GCS therapy, precautions should be taken when transferring patients to Formisonide®-Native.

Inhaled therapy with budesonide generally minimizes the need for oral GCS, but patients who discontinue oral GCS therapy may have long-term adrenal insufficiency. Patients who in the past have needed urgent high-dose GCS or have received long-term high-dose inhalation GCS treatment may also be at this risk. It should be remembered about the possibility of residual adrenal dysfunction in such patients in extreme cases and any situations that may cause stress (including surgical interventions). Adequate GCS treatment should be provided in such situations. Depending on the degree of adrenal dysfunction, a specialist may need to be consulted prior to the recommended procedures.

The development of candidal infection of the oral cavity is possible. To reduce the risk, patients are advised to rinse their mouth thoroughly with water after each inhalation of the drug. If oral candidiasis infection develops, local antifungal therapy may be performed without discontinuing treatment with Formisonide®-nativ.

Particular precautions should be observed in patients with unstable bronchial asthma who use short-acting β2-adrenomimetics to relieve attacks during exacerbations of severe bronchial asthma, since the risk of hypokalemia increases with hypoxia and other conditions when there is an increased chance of developing hypokalemic symptoms. In such cases it is recommended to control potassium content in blood serum.

The blood glucose concentration in diabetic patients should be monitored during treatment.

The use of formoterol in a dose greater than 54 mcg/day (over 12 inhalations of Formisonide®-nativ in doses of 80+4.5 mcg or 160+4.5 mcg or over 6 inhalations of 320+9 mcg) may lead to positive doping tests.

Particulars of action of the drug when discontinued

Because of the risk of exacerbations, abrupt withdrawal of Formisonide®-Nativ should be avoided and the dose of the drug should be reduced gradually under medical supervision.

Contraindications

If you have any of these disorders, please consult your doctor before taking this medicine. Extra caution should be exercised with Formoterol Nativ (especially with regard to dose reduction) and patients should be closely monitored in the presence of the following comorbidities CHD; cardiac rhythm and conduction disorders, especially grade III AV blockade; severe heart failure; idiomatic hypertrophic subaortic stenosis; severe degree of arterial hypertension; any localized aneurysm; pheochromocytoma; ketoacidosis; hypertrophic obstructive cardiomyopathy; thyrotoxicosis; known or suspected QTc interval prolongation (QT corrected >0.44 sec). Given the hyperglycemic effect inherent to beta2-adrenomimetics, additional regular monitoring of blood glucose concentrations is recommended in diabetic patients taking Formoterol-Nativ.

Side effects

There has been no increase in the incidence of adverse reactions when budesonide and formoterol have been coadministered.

The undesirable reactions were distributed according to the frequency of occurrence. The following criteria were used to assess frequency: very common (>1/10), common (1/100 to 1/10), infrequent (1/1000 to 1/100), rare (1/10000 to 1/1000), very rare (<1/10000), (including individual reports).

Infectious and parasitic diseases: often – rhinopharyngitis, nasal congestion, sinusitis, upper respiratory tract infections, bronchitis, oropharyngeal candidiasis (candidiasis of the oral mucosa and larynx).

Immune system disorders: rarely – anaphylactic reactions, including angioedema (Quincke’s edema); bronchospasm, including paradoxical.

Endocrine system disorders: rare – hypokalemia; very rare – hyperglycemia, symptoms of systemic glucocorticosteroid effects (including hypocorticism, hypercorticism.

Mental disorders: infrequent – psychomotor agitation, restlessness, anxiety, dizziness, sleep disorders; very rare – depression, behavior disorders, aggressive behavior, nervousness, taste disorders.

Central nervous system disorders: often – headache.

Visual system disorders: very rarely – cataracts, glaucoma (with prolonged use of high doses), increased intraocular pressure.

Cardiac disorders: often – palpitations, infrequently – tachycardia, rarely – arrhythmias, including atrial fibrillation, supraventricular tachycardia, extrasystole; very rarely – angina pectoris, atrial and ventricular tachyarrhythmia.

Vascular disorders: very rare – changes in blood pressure (arterial hypotension, arterial hypertension).

Respiratory system, chest and mediastinum disorders: frequently – irritation in the throat, cough, hoarseness of voice; rarely – dysphonia, (disappearing after discontinuation of therapy or reduction of the drug dose).

Gastrointestinal disorders: frequent – discomfort in the stomach, rare – vomiting, very rare – nausea, dysphagia (impaired swallowing).

Skin and subcutaneous tissue disorders: infrequent – bruising, rare – urticaria, itching, dermatitis, rash, very rare – redness of the skin.

Muscular and connective tissue disorders: common – tremor, infrequent – muscle cramps, rare – osteoporosis (decreased bone mineral density), back pain.

The systemic effects of inhaled GKS may be observed when taking the drug in high doses for a long time.

The use of β2-adrenomimetics may increase blood levels of insulin, free fatty acids, glycerol, and ketone derivatives.

If any of the side effects listed in the instructions worsen, or if you notice any other manifestations not listed in the instructions, tell your doctor.

Overdose

Symptoms: no clinically significant symptoms are expected in acute overdose of budesonide, a component of Formisonide®-Nativ. If budesonide is taken chronically in excessive doses, systemic GCS effects may occur.

In case of formoterol overdose, tremor, nervousness, insomnia, headache, dizziness, palpitations, tachycardia, angina pectoris, blood pressure changes, metabolic acidosis, in some cases, hyperglycemia, hypokalemia, prolongation of QTC interval, arrhythmias, nausea, increased nervous excitability, muscle spasms may be observed.

Treatment: supportive and symptomatic treatment is indicated.

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