Flutiair-FT Nasal Spray

For the use only of a Registered medical practitioner, Hospital or a laboratory

Fluticasone Furoate Nasal Spray

FLUTIAIR-FT

FOR INTRANASAL USE ONLY

Shake well before use.

Each Spray Delivers
Fluticasone Furoate                          27.5 mcg

COMPOSITION:

Fluticasone Furoate                        0.055 %w/w
Benzalkonium Chloride BP            0.015%w/w
(Added as Preservative)
Excipients                                           q.s.

CHEMISTRY: 6α,11β,16α,17α)-6,9-difluoro-17-{[(fluoromethyl)thio]carbonyl}-11-hydroxy-16-methyl-3-oxoandrosta-1,4-dien-17-yl 2-furancarboxylate

CATEGORY: Synthetic fluorinated corticosteroid

DESCRIPTION: FLUTIAIR-FT nasal spray is an aqueous suspension of micronized fluticasone furoate for topical administration to the nasal mucosa by means of a metering (50 microliters), atomizing spray pump. After initial priming, each actuation delivers 27.5 mcg of fluticasone furoate in a volume of 50 microliters of nasal spray suspension.

PHARMACOLOGY

Pharmacodynamics

Fluticasone furoate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. The precise mechanism through which fluticasone furoate affects rhinitis symptoms is not known. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation.

Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor that is approximately 29.9 times that of dexamethasone and 1.7 times that of fluticasone propionate.

Pharmacokinetics

Absorption

Following intranasal administration of fluticasone furoate, most of the dose is eventually swallowed and undergoes incomplete absorption and extensive first-pass metabolism in the liver and gut, resulting in negligible systemic exposure. The average absolute bioavailability is 0.50%. Oral bioavailability is on average 1.26%, and the majority of the circulating radioactivity is due to inactive metabolites.

Distribution

Binding of fluticasone furoate to human plasma proteins is greater than 99%.

Metabolism

Fluticasone furoate is cleared from systemic circulation principally by hepatic metabolism via CYP3A4. The principal route of metabolism is hydrolysis of the Sfluoromethyl carbothioate function to form the inactive 17β-carboxylic acid metabolite.

Elimination

Fluticasone furoate and its metabolites are eliminated primarily in the feces, accounting for approximately 101% and 90% of the orally and intravenously administered dose, respectively. Urinary excretion accounted for approximately 1% and 2% of the orally and intravenously administered dose, respectively.

INDICATION AND USAGE

FLUTIAIR-FT (fluticasone furoate) nasal spray is indicated for the treatment of the symptoms of seasonal and perennial allergic rhinitis in patients aged 2 years and older.

DOSAGE AND ADMINISTRATION

• Administer FLUTIAIR-FT nasal spray by the intranasal route only.
• Before using FLUTIAIR-FT nasal spray for the first time, shake well and release 6 sprays into the air away from the face.
• When FLUTIAIR-FT nasal spray has not been used for more than 30 days or if the cap has been left off the bottle for 5 days or longer, prime the pump again until a fine mist appears.
• Shake FLUTIAIR-FT nasal spray well before each use.
• Titrate an individual patient to the minimum effective dosage to reduce the possibility of side effects.

Adults and Adoles cents Aged 12 Years and Older

The recommended starting dosage is 110 mcg once daily administered as 2 sprays (27.5 mcg/spray) in each nostril. When the maximum benefit has been achieved and symptoms have been controlled, reducing the dosage to 55 mcg (1 spray in each nostril) once daily may be effective in maintaining control of allergic rhinitis symptoms.

Children Aged 2 to 11 Years

The recommended starting dosage in children is 55 mcg once daily administered as 1 spray (27.5 mcg/spray) in each nostril. Children not adequately responding to 55 mcg may use 110 mcg (2 sprays in each nostril) once daily. Once symptoms have been controlled, dosage reduction to 55 mcg once daily is recommended.

CONTRAINDICATION

FLUTIAIR-FT nasal spray is contraindicated in patients with hypersensitivity to any of its ingredients.

WARNINGS AND PRECAUTIONS

• Epistaxis, nasal ulceration, Candida albicans infection, nasal septal perforation, impaired wound healing. Monitor patients periodically for signs of adverse effects on the nasal mucosa. Avoid use in patients with recent nasal ulcers, nasal surgery, or nasal trauma.
• Development of glaucoma or posterior subcapsular cataracts. Monitor patients closely with a change in vision or with a history of increased intraocular pressure, glaucoma, and/or cataracts.
• Hypersensitivity reactions, including anaphylaxis, angioedema, rash, and urticaria, may occur after administration of FLUTIAIR-FT nasal spray.
• Potential worsening of existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex.
• More serious or even fatal course of chickenpox or measles in susceptible patients. Use caution in patients with the above because of the potential for worsening of these infections.
• Hypercorticism and adrenal suppression with very high dosages or at the regular dosage in susceptible individuals. If such changes occur, discontinue FLUTIAIR-FT nasal spray slowly.
• Potential reduction in growth velocity in children. Monitor growth routinely in pediatric patients receiving FLUTIAIR-FT nasal spray.
• KEEP FLUTIAIR-FT NASAL SPRAY OUT OF THE REACH OF CHILDREN.

DRUG INTERACTIONS

Potent inhibitors of cytochrome P450 3A4 (CYP3A4) may increase exposure to fluticasone furoate.

• Co-administration of ritonavir is not recommended.
• Use caution with co-administration of other potent CYP3A4 inhibitors, such as ketoconazole.

USE DURING PREGNANCY AND LACTATION

FLUTIAIR-FT nasal spray should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Since there are no data from controlled trials on the use of intranasal fluticasone furoate by nursing mothers, caution should be exercised when FLUTIAIR-FT nasal spray is administered to a nursing woman.

ADVERSE REACTIONS

Systemic and local corticosteroid use may result in the following:

• Epistaxis, headache, pharyngo-laryngeal pain, back pain, pyrexia, cough, nasal ulcerations, Candida albicans infection, impaired wound healing and nasal septal perforation
• Cataracts and glaucoma
• Immunosuppression
• Hypersensitivity reactions
• Hypothalamic-pituitary-adrenal (HPA) axis effects, including growth reduction

OVERDOSAGE

Chronic overdosage may result in signs/symptoms of hypercorticism.

There are no data on the effects of acute or chronic overdosage with FLUTIAIR-FT nasal spray because of low systemic bioavailability and an absence of acute drug-related systemic effects.

PACKING

Fluticasone Furoate Nasal Spray 27.5mcg is supplied in an amber glass vial fitted with a silver metering atomizing pump, transparent nasal adapter, and white dust cover in a box with patient’s instructions for use.

STORAGE

Store in a dry place below 300C.

Protect from light. Do not freeze.

Keep out of reach of children.

Last Update: August 2016.