Fluticasone Furoate

Introduction

Fluticasone Furoate is a synthetic corticosteroid used to treat a variety of inflammatory and allergic conditions. It is primarily available as a nasal spray for managing allergic rhinitis and asthma and as a topical treatment for skin inflammation. It works by reducing inflammation, swelling, and mucus production in the airways or affected areas.

Uses

Fluticasone Furoate is used to treat:

Allergic rhinitis (seasonal and perennial)
Asthma (as part of long-term maintenance therapy)
Chronic obstructive pulmonary disease (COPD) (in combination with other medications)
Dermatological conditions associated with inflammation, such as eczema and psoriasis (in topical formulations)

Brand Name	Fluticasone Furoate
Type
Weight
Generic	Fluticasone Furoate
Manufacturer
Available in	English বাংলা

Mechanism of Action

Fluticasone Furoate works by binding to glucocorticoid receptors in cells, inhibiting the release of pro-inflammatory mediators, such as cytokines and histamines. This reduces inflammation in the respiratory tract (in asthma and allergic rhinitis) and in the skin (in dermatological conditions). It decreases airway hyperresponsiveness and mucus production, leading to improved breathing in asthma and COPD.

How Long Does It Take to Work?

For nasal allergies, Fluticasone Furoate typically begins to relieve symptoms within 8 to 24 hours after the first dose, with maximum effects seen after a few days of consistent use. In asthma, it may take up to one week to see significant improvement in symptoms. For skin conditions, relief may be noticeable within a few hours of topical application.

Absorption

When administered intranasally or inhaled, Fluticasone Furoate has minimal systemic absorption due to extensive first-pass metabolism in the liver. After topical application, systemic absorption is also low, but it can be increased in certain conditions (e.g., broken skin or prolonged use). Bioavailability is approximately 0.5% for the nasal spray and inhalation forms.

Route of Elimination

Fluticasone Furoate is primarily eliminated through hepatic metabolism by the cytochrome P450 enzyme CYP3A4. The drug and its metabolites are excreted mainly via the feces, with a small percentage excreted in the urine.

Dosage

Fluticasone Furoate Nasal Spray:

Adults & Children over 12 years: 2 sprays in each nostril once a day. In some cases 2 sprays into each nostril twice daily, not exceeding 4 sprays.
Children under 12 years (2-11 Years): 1 spray in each nostril once a day. Patients should use Fluticasone Furoate nasal spray at regular intervals as directed since its effectiveness depends on its regular use.
Children (under 2 years of age): There are no data to recommend use of Fluticasone Furoate Nasal Spray for the treatment of seasonal or perennial allergic rhinitis in children under 2 years of age.

Fluticasone Furoate Inhalation Capsule: should be administered as 1 inhalation once daily by the orally inhaled route. Fluticasone Furoate should be used at the same time every day. Do not use fluticasone furoate more than 1 time every 24 hours.

Adults and Adolescents Aged 12 Years and Older: The starting dosage for Fluticasone Furoate should be based upon patients' asthma severity.
The usual recommended starting dose for adults and adolescents aged 12 years and older not on an inhaled corticosteroid (ICS) is 100 mcg.
For other adults and adolescents aged 12 years and older, the starting dose should be based on previous asthma drug therapy and disease severity.
For adults and adolescents aged 12 years and older who do not respond to Fluticasone Furoate 100 mcg after 2 weeks of therapy, replacement with Fluticasone Furoate 200 mcg may provide additional asthma control.

If a dosage regimen of Fluticasone Furoate fails to provide adequate control of asthma, the therapeutic regimen should be re-evaluated and additional therapeutic options, e.g., replacing the current strength of Fluticasone Furoate with a higher strength, initiating an ICS and long- acting beta 2 -agonist (LABA) combination product, or initiating oral corticosteroids, should be considered.

The highest recommended daily dose in adults and adolescents aged 12 years and older is 200 mcg. After asthma stability has been achieved, it is desirable to titrate to the lowest effective dosage to help reduce the possibility of side effects.

Pediatric Patients Aged 5 to 11 Years: The recommended dosage for children aged 5 to 11 years is 50 mcg administered once daily

Typical dosages include:

For Allergic Rhinitis: 110 mcg once daily (1 spray per nostril) for adults and children over 12 years.
For Asthma: 100 mcg to 200 mcg inhaled once daily, adjusted based on severity and response.
For COPD: 100 mcg inhaled once daily, often in combination with a long-acting bronchodilator.
For Dermatological Conditions: Applied as a thin layer to the affected skin 1 to 2 times daily.

Administration

Fluticasone Furoate is available as a nasal spray, inhalation powder, and topical cream/ointment.

Nasal spray: Shake the bottle well before use, and spray into each nostril as prescribed.
Inhalation powder: Administer through a specific inhaler device, following the instructions for proper use.
Topical application: Apply a thin layer to the affected skin area, avoiding broken skin unless directed by a physician.

Side Effects

Common side effects include:

Headache
Nasal irritation or dryness (for nasal spray)
Throat irritation (for inhalation)
Hoarseness or voice changes
Skin irritation or dryness (for topical use)

Serious side effects may include:

Increased risk of infection (due to immune suppression)
Oropharyngeal candidiasis (thrush)
Suppression of adrenal gland function (with high doses)

Toxicity

Overuse or high doses of Fluticasone Furoate can lead to systemic corticosteroid effects, such as adrenal suppression, Cushing's syndrome, hyperglycemia, and increased risk of infections. Prolonged topical use can cause skin thinning, stretch marks, or contact dermatitis. Acute overdose is unlikely due to low systemic bioavailability.

Precautions

Precautions should be taken in patients with:

Untreated infections (especially fungal, bacterial, or viral infections)
Glaucoma or cataracts (due to increased intraocular pressure)
Severe liver disease (due to impaired metabolism)

Patients should avoid long-term use without medical supervision.

Interaction

Fluticasone Furoate interacts with other drugs that inhibit the CYP3A4 enzyme, such as:

Ritonavir and other HIV protease inhibitors
Ketoconazole and other strong CYP3A4 inhibitors

These interactions can increase systemic corticosteroid exposure, leading to potential side effects.

Disease Interaction

Caution should be used in patients with:

Active infections (may worsen due to immune suppression)
Ocular conditions like glaucoma or cataracts
Severe hepatic impairment (due to reduced drug clearance)

Drug Interaction

Fluticasone Furoate can interact with:

Strong CYP3A4 inhibitors (e.g., ritonavir, ketoconazole), which may increase systemic exposure and risk of side effects.
Other corticosteroids, which can increase the risk of systemic side effects.

Food Interactions

No significant food interactions have been reported with Fluticasone Furoate . However, grapefruit juice may increase systemic exposure by inhibiting CYP3A4 enzyme activity.

Pregnancy Use

Fluticasone Furoate is classified as pregnancy category C. While animal studies have shown adverse effects on the fetus, there are insufficient human studies. It should be used during pregnancy only if the potential benefits justify the risks to the fetus.

Lactation Use

There is limited information regarding the excretion of Fluticasone Furoate into human breast milk. Caution is advised when administering to breastfeeding mothers, and the risks and benefits should be carefully considered.

Acute Overdose

Acute overdose of Fluticasone Furoate is unlikely due to its low systemic bioavailability. However, chronic overuse can lead to systemic corticosteroid side effects such as adrenal suppression, Cushing's syndrome, and hyperglycemia. Treatment involves discontinuing the drug and providing supportive care.

Contraindication

Fluticasone Furoate is contraindicated in:

Patients with known hypersensitivity to Fluticasone or any of its components.
Patients with untreated systemic infections (e.g., fungal, bacterial, viral).

Use Direction

Fluticasone Furoate should be used exactly as prescribed:

Nasal spray: 1 to 2 sprays in each nostril once daily for allergic rhinitis.
Inhalation: Administer daily for asthma or COPD, following proper inhalation technique.
Topical: Apply thinly to the affected area once or twice daily, depending on the severity of the skin condition.

Storage Conditions

Fluticasone Furoate products should be stored at room temperature, away from light and moisture. Keep out of reach of children. Nasal spray and inhaler devices should be capped tightly when not in use.

Volume of Distribution

The volume of distribution for Fluticasone Furoate is approximately 608 liters, indicating extensive tissue distribution, including the lungs.

Half-Life

The terminal half-life of Fluticasone Furoate is approximately 24 hours when administered intranasally or via inhalation. The long half-life allows for once-daily dosing.

Clearance

The clearance of Fluticasone Furoate is primarily hepatic, with a clearance rate of around 65 liters per hour. It is metabolized by the CYP3A4 enzyme system and eliminated mainly through fecal excretion.

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