FeniVate (Ointment, Cream) Instructions for Use

ATC Code

D07AC17 (Fluticasone)

Active Substance

Fluticasone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Topical corticosteroids for external use

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Glucocorticosteroid, a synthetic trifluorinated compound with high affinity for glucocorticoid receptors. It exerts anti-inflammatory, anti-allergic, and antipruritic effects when used intranasally, by inhalation, or topically. In therapeutic doses, it has virtually no effect on the hypothalamic-pituitary-adrenal system.

Pharmacokinetics

When administered by inhalation, the systemic absorption of fluticasone occurs primarily in the lungs, with initial rapid absorption followed by a slower phase. A portion of the dose after inhalation may be swallowed, but its systemic effect is minimal due to the poor water solubility of fluticasone 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 intravenous administration, elimination is characterized by high plasma clearance.

Plasma protein binding is 91%.

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

The elimination half-life (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), nodular prurigo, psoriasis (except for widespread plaque psoriasis), neurodermatoses, lichen planus, contact dermatitis, discoid lupus erythematosus, generalized erythroderma (as an additional agent), insect bites, miliaria rubra, seborrheic dermatitis.

ICD codes

Dosage Regimen

Apply a thin layer of FeniVate ointment or cream to the affected skin areas once or twice daily.

Use the minimum amount necessary to cover the affected area and for the shortest duration required to achieve therapeutic effect.

Avoid application under occlusive dressings unless specifically directed by a physician, due to increased risk of systemic absorption and local adverse effects.

Do not use on the face, groin, or axillae unless prescribed by a doctor for these areas.

Discontinue treatment once control is achieved. If no improvement is seen within one week, re-evaluate the diagnosis.

Wash hands before and after application, unless hands are the treated area.

Avoid contact with eyes, mucous membranes, and open wounds.

For pediatric patients, limit application to the smallest area and shortest time possible; monitor for HPA axis suppression and growth retardation with prolonged use.

Do not use for the treatment of acne, rosacea, or perioral dermatitis.

Do not use on bacterial, fungal, or viral skin infections.

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 concentration of endogenous cortisol.

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 may occur – 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

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

Use in Renal Impairment

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

Pediatric Use

Can be used in children according to indications, in age-appropriate 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

Should be used with caution in elderly patients.

Special Precautions

Regardless of the route of administration, with prolonged use, the systemic action of fluticasone may manifest. The metabolism and excretion of fluticasone are slowed in patients with impaired renal and/or hepatic 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 poses a potential life-threatening risk to 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 concurrently with inhibitors of the CYP3A4 isoenzyme. Transferring a patient from oral glucocorticosteroids to inhalation 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 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, infectious process, herpetic keratitis, as well as those who have recently undergone oral and nasal surgery, the ratio of expected benefit to potential risk should be carefully assessed.

Topical use. The agent should be applied in the minimum amount for the shortest period 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, because 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 effect 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

Over-the-Counter

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.