Fluticasone Air (Aerosol) Instructions for Use

Marketing Authorization Holder

PSK Pharma, LLC (Russia)

ATC Code

R03BA05 (Fluticasone)

Active Substance

Fluticasone (Rec.INN registered by WHO)

Dosage Forms

	Fluticasone Air	Metered dose inhalation aerosol 50 mcg/1 dose: aerosol canisters of 60 doses or 120 doses
		Metered dose inhalation aerosol 125 mcg/1 dose: aerosol canisters of 60 doses or 120 doses
		Metered dose inhalation aerosol 250 mcg/1 dose: aerosol canisters of 60 doses or 120 doses

Dosage Form, Packaging, and Composition

Metered dose inhalation aerosol as a white or almost white suspension.

Excipients : propellant 1,1,1,2-tetrafluoroethane – 59950 mcg.

60 doses – aluminum aerosol canisters with a metering valve (1) – cardboard packs.
120 doses – aluminum aerosol canisters with a metering valve (1) – cardboard packs.

Metered dose inhalation aerosol as a white or almost white suspension.

Excipients : propellant 1,1,1,2-tetrafluoroethane – 59875 mcg.

60 doses – aluminum aerosol canisters with a metering valve (1) – cardboard packs.
120 doses – aluminum aerosol canisters with a metering valve (1) – cardboard packs.

Metered dose inhalation aerosol as a white or almost white suspension.

Excipients : propellant 1,1,1,2-tetrafluoroethane – 59750 mcg.

60 doses – aluminum aerosol canisters with a metering valve (1) – cardboard packs.
120 doses – aluminum aerosol canisters with a metering valve (1) – cardboard packs.

Clinical-Pharmacological Group

Topical corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid, a synthetic trifluorinated compound with high affinity for glucocorticoid receptors.

It has anti-inflammatory, anti-allergic, and antipruritic effects when used intranasally, by inhalation, or topically.

In therapeutic doses, it has practically no effect on the hypothalamic-pituitary-adrenal system.

Pharmacokinetics

With inhalation use, the systemic absorption of fluticasone occurs mainly in the lungs, with absorption initially rapid followed by slowing.

Part of the dose after inhalation may be swallowed, but its systemic effect is minimal due to the poor solubility of fluticasone in water and intensive presystemic metabolism.

When administered intranasally in doses up to 1 mg, plasma concentrations of fluticasone are very low and approach the sensitivity threshold of the method (0.05 ng/ml).

When applied topically, it is practically not subject to systemic absorption.

After oral administration, 87-100% is excreted through the intestines, with up to 75% as unabsorbed unchanged substance; at a dose of 6 mg, 64% is excreted unchanged.

After IV administration, elimination is characterized by high plasma clearance.

Plasma protein binding is 91%.

It is metabolized in the liver with the participation of the CYP3A4 isoenzyme of the cytochrome P450 system to form an inactive carboxyl metabolite.

T_1/2 is 3 hours.

Indications

For inhalation use: basic anti-inflammatory therapy for bronchial asthma, COPD (including chronic bronchitis and emphysema).

For intranasal use: prevention and treatment of allergic rhinitis.

For topical use: eczema (including atopic, infantile, discoid), prurigo nodularis, psoriasis (except for widespread plaque psoriasis), neurodermatoses, lichen planus, contact dermatitis, discoid lupus erythematosus, generalized erythroderma (as an additional agent), insect bites, prickly heat, seborrheic dermatitis.

ICD codes

Dosage Regimen

Administer by inhalation, intranasally, or topically as directed. Select the appropriate product strength and formulation based on the specific indication and patient age.

For bronchial asthma in adults and adolescents (12 years and older), the initial inhalation dose is 100-500 mcg twice daily. Adjust the dose to the lowest effective amount for maintenance therapy. The maximum daily dose is 1000 mcg.

For COPD maintenance, administer 500 mcg twice daily via inhalation.

For allergic rhinitis in adults and children (12 years and older), administer two sprays (50 mcg/spray) into each nostril once daily, or one spray into each nostril twice daily. For children aged 4-11 years, use one spray in each nostril once daily.

For topical application on the skin, apply a thin layer to the affected area once or twice daily. Use the minimum amount necessary for the shortest duration required to achieve therapeutic effect. Avoid occlusive dressings unless specifically instructed.

Shake the inhalation aerosol canister well before each use. Prime the device before first use or if not used for several days. Rinse your mouth with water after inhalation to reduce the risk of oral candidiasis.

Do not use this inhaler for acute bronchospasm or status asthmaticus. Monitor growth in children receiving long-term therapy. Gradually reduce the dosage when discontinuing treatment after prolonged use.

Adverse Reactions

Immune system disorders: hypersensitivity reactions, including skin reactions, bronchospasm, angioedema (predominantly facial and oropharyngeal edema), respiratory disorders (dyspnea and/or bronchospasm); anaphylactic reactions.

Endocrine system disorders: very rarely – weight gain or obesity, slow weight gain or growth retardation in children, Cushing’s syndrome, cushingoid symptoms, suppression of adrenal cortex function, growth retardation, decreased bone mineralization, hyperglycemia or glucosuria; decreased endogenous cortisol concentration.

Eye disorders: very rarely – cataract, glaucoma.

Cardiovascular system disorders: very rarely – arterial hypertension.

Local reactions with inhalation use, development of oral and pharyngeal candidiasis, hoarseness of voice, paradoxical bronchospasm is possible; with intranasal use, very rarely – dryness and irritation of the nasopharynx, unpleasant taste and smell, perforation of the nasal septum, especially with a history of surgical interventions in the nasal cavity; with topical use, burning, itching, swelling at the application site are possible; with prolonged use, atrophic skin changes are possible – thinning, striae, dilation of superficial blood vessels, hypertrichosis, hypopigmentation; allergic contact dermatitis and secondary infection, especially when using occlusive dressings and when applied to skin fold areas.

Contraindications

Hypersensitivity to fluticasone; pediatric age – depending on the dosage form used.

For inhalation use: acute bronchospasm, status asthmaticus (as a primary agent).

For intranasal use: recent nasal trauma or surgical intervention in the nasal cavity.

For topical use: hypersensitivity to fluticasone; rosacea, acne vulgaris, perioral dermatitis, primary viral skin infections (herpes simplex, chickenpox), perianal and genital pruritus, primary skin lesions of bacterial and fungal etiology.

Use in Pregnancy and Lactation

During pregnancy and breastfeeding, it should be used only after consultation with a doctor, in cases where the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Use in Hepatic Impairment

Metabolism and excretion of fluticasone are slowed in patients with impaired liver function, which increases the risk of systemic toxicity.

Use in Renal Impairment

Metabolism and excretion of fluticasone are slowed in patients with impaired renal function, which increases the risk of systemic toxicity.

Pediatric Use

It can be used in children according to indications, in age-recommended doses and dosage forms. It is necessary to strictly follow the instructions in the fluticasone drug leaflets regarding contraindications for the use of specific fluticasone dosage forms in children of different ages.

It is necessary to regularly monitor the growth dynamics of children receiving inhaled glucocorticosteroids for a long time.

Geriatric Use

It should be used with caution in elderly patients.

Special Precautions

Regardless of the route of administration, with long-term use, the systemic action of fluticasone may manifest. Metabolism and excretion of fluticasone are slowed in patients with impaired renal and/or liver function, which increases the risk of systemic toxicity.

Inhalation use. Fluticasone is not intended for relieving an asthma attack. Sudden and progressive deterioration of asthma control is a potential life-threatening condition for the patient and requires an increase in the dose of glucocorticosteroids. Patients at risk may be prescribed daily peak flowmetry. Use with caution in concomitant pulmonary tuberculosis, as well as simultaneously with CYP3A4 isoenzyme inhibitors. Transferring a patient from oral glucocorticosteroids to inhalation use of fluticasone should be done with caution, under the control of adrenal cortex function. Treatment with fluticasone should be discontinued gradually. Particular caution should be exercised when treating patients with active or inactive forms of pulmonary tuberculosis with inhaled glucocorticosteroids.

Intranasal use. Transferring a patient from oral glucocorticosteroids to intranasal use of fluticasone should be done with caution. Fluticasone is effective in the treatment of seasonal allergic rhinitis, however, with increased allergen concentrations in the summer, additional treatment may be required. When deciding to prescribe this agent to patients with tuberculosis, an infectious process, herpetic keratitis, as well as those who have recently undergone surgery on the oral and nasal cavity, the ratio of expected benefit and potential risk should be carefully assessed.

Topical use. The agent should be applied in the minimum amount for the shortest period of time sufficient to achieve a clinical effect. Avoid getting the product into the eyes. Caution should be exercised when prescribing topical glucocorticosteroids for the treatment of psoriasis, as there are reports of early relapses, development of tolerance, risk of generalized pustular psoriasis, and local or systemic toxicity due to impaired skin barrier function. In case of secondary infection of skin lesions, appropriate antibacterial therapy should be prescribed. If signs of infection spread appear, topical glucocorticosteroids should be discontinued and appropriate antibacterial therapy should be prescribed.

Use in pediatrics

With long-term topical use in high doses, systemic absorption of fluticasone is possible with the development of symptomatic hypercortisolism (more often in infants, as diapers can act as an occlusive dressing).

It is necessary to regularly monitor the growth dynamics of children receiving glucocorticosteroids by inhalation or intranasally for a long time.

Drug Interactions

With simultaneous use of fluticasone by inhalation and inhibitors of the CYP3A4 enzyme (including ketoconazole, ritonavir), an increase in the systemic action of fluticasone is possible.

Storage Conditions

Store at 2°C (36°F) to 30°C (86°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.