Fluticasone (Nasal)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Exhaler Suspension, Nasal, as propionate:

Xhance: 93 mcg/actuation (16 mL) [contains benzalkonium chloride, edetate disodium dihydrate, polysorbate 80]

Suspension, Nasal, as furoate:

Flonase Sensimist: 27.5 mcg/spray (5.9 mL, 6.6 mL, 9.1 mL) [contains benzalkonium chloride, edetate disodium, polysorbate 80]

Veramyst: 27.5 mcg/spray (10 g [DSC]) [contains benzalkonium chloride]

Suspension, Nasal, as propionate:

Flonase Allergy Relief: 50 mcg/actuation (9.9 mL, 11.1 mL, 15.8 mL, 18.2 mL) [contains benzalkonium chloride, polysorbate 80]

GoodSense Nasoflow: 50 mcg/actuation (15.8 mL [DSC]) [contains alcohol, usp, benzalkonium chloride, polysorbate 80]

Generic: 50 mcg/actuation (16 g, 9.9 mL, 15.8 mL)

Therapy Pack, Nasal, as propionate:

Ticaspray: 50 mcg/actuation (1 ea [DSC]) [contains benzalkonium chloride, polysorbate 80]

Pharmacology

Mechanism of Action

Fluticasone belongs to a group of corticosteroids which utilizes a fluorocarbothioate ester linkage at the 17 carbon position; extremely potent vasoconstrictive and anti-inflammatory activity

Pharmacokinetics/Pharmacodynamics

Distribution

Fluticasone propionate: 4.2 L/kg; Fluticasone furoate: V_d,ss: 608 L

Metabolism

Hepatic via CYP3A4 to 17 beta-carboxylic acid (negligible activity)

Excretion

Oral: Feces (as parent drug and metabolites); Urine (<5% as metabolites)

Onset of Action

Maximal benefit may take several days or several months (Xhance)

Half-Life Elimination

IV: Fluticasone propionate: ~8 hours (~7.8 hours [Xhance]); Fluticasone furoate: ~15 hours

Protein Binding

99%

Use in Specific Populations

Special Populations: Hepatic Function Impairment

Accumulation of fluticasone in plasma may occur in patients with hepatic impairment.

Use: Labeled Indications

Rx products:

Allergic rhinitis (Veramyst, Avamys [Canadian product], Flonase [Canadian product]): Management of seasonal and perennial allergic rhinitis in adults and children ≥2 years of age (Veramyst, Avamys) and in patients 4 to 17 years of age (Flonase)

Nasal polyps (Xhance): Treatment of nasal polyps in patients ≥18 years of age

Nonallergic rhinitis (Flonase): Management of the nasal symptoms of perennial nonallergic rhinitis in adults and pediatric patients ≥4 years of age

OTC products:

Upper respiratory allergies: Relief of hay fever or other upper respiratory allergies (eg, itchy and watery eyes, nasal congestion, runny nose, sneezing, itchy nose) in adults and children ≥4 years of age (Clarispray, Flonase Allergy Relief, Good Sense Nasoflow) or children ≥2 years of age (Flonase Sensimist)

Use: Off Label

Acute bacterial rhinosinusitis, adjunct to antibiotics (empiric treatment)yes

Based on the Infectious Diseases Society of America (IDSA) guidelines for acute bacterial rhinosinusitis (ABRS) in children and adults and the American Academy of Otolaryngology-Head and Neck Surgery Foundation (AAO-HNS) guidelines for adult sinusitis, fluticasone (nasal), among other intranasal corticosteroids, is effective and recommended as an adjunctive treatment to antibiotic therapy for the management of ABRS, primarily when a history of allergic rhinitis exists (according to IDSA guidelines).

Chronic rhinosinusitisyes

Based on the American Academy of Otolaryngology-Head and Neck Surgery Foundation (AAO-HNS) guidelines for adult sinusitis, fluticasone (nasal), among other intranasal corticosteroids, is effective and recommended (with or without nasal saline irrigation) for the symptomatic relief of chronic rhinosinusitis.

Viral rhinosinusitis symptomatic reliefyes

Based on the American Academy of Otolaryngology-Head and Neck Surgery Foundation (AAO-HNS) guidelines for adult sinusitis, topical intranasal steroids (including fluticasone), analgesics, and/or nasal saline irrigation may be recommended for symptomatic relief of viral rhinosinusitis Rosenfeld 2015.

Contraindications

Hypersensitivity to fluticasone or any component of the formulation

OTC labeling: When used for self-medication, do not use in children <4 years of age (Clarispray, Flonase Allergy Relief, Good Sense Nasoflow) or children <2 years of age (Flonase Sensimist), for the treatment of asthma, or with current injury or surgery to nose that is not fully healed.

Documentation of allergenic cross-reactivity for intranasal steroids is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Canadian labeling: Additional contraindications (not in US labeling): Flonase: Untreated fungal, bacterial, or tuberculosis infections of the respiratory tract

Dosage and Administration

Dosing: Adult

Allergic rhinitis (fluticasone furoate): Intranasal:

Veramyst (Rx): Initial: Two sprays (27.5 mcg/spray) per nostril once daily (110 mcg/day); once symptoms are controlled, may reduce dosage to 1 spray per nostril once daily (55 mcg/day) for maintenance therapy.

Avamys (Rx) [Canadian product]: Two sprays (27.5 mcg/spray) per nostril once daily (110 mcg/day). Total daily dosage should not exceed 2 sprays in each nostril (110 mcg/day).

Nasal polyps (fluticasone propionate): Intranasal: Xhance (Rx): One spray (93 mcg/spray) per nostril twice daily (372 mcg/day); some patients may require 2 sprays per nostril twice daily (744 mcg/day); maximum dose: 2 sprays per nostril twice daily (744 mcg/day).

Nonallergic rhinitis (fluticasone propionate): Intranasal: Flonase (Rx): Initial: Two sprays (50 mcg/spray) per nostril once daily (200 mcg/day); alternatively, the same total daily dosage may be divided and given as 1 spray per nostril twice daily (200 mcg/day). After the first few days, dosage may be reduced to 1 spray per nostril once daily for maintenance therapy (100 mcg/day) (maximum: 2 sprays in each nostril [200 mcg]/day).

Upper respiratory allergies (OTC): Intranasal:

ClariSpray, Flonase Allergy Relief, Good Sense Nasoflow (fluticasone propionate): Initial: Two sprays (50 mcg/spray) per nostril once daily (200 mcg/day); after 1 week, may adjust to 1 or 2 sprays per nostril once daily (100 to 200 mcg/day). Do not use for more than 6 months unless instructed by health care provider.

Flonase Sensimist (fluticasone furoate): Initial: Two sprays (27.5 mcg/spray) per nostril once daily (110 mcg/day); after 1 week, may adjust to 1 or 2 sprays per nostril once daily (55 to 110 mcg/day). Do not use for more than 6 months unless instructed by healthcare provider.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Note: Product formulations are not interchangeable; use extra caution to ensure proper salt form and dose.

Rhinitis, nonallergic: Flonase (fluticasone propionate, 50 mcg/spray): Children ≥4 years and Adolescents: Intranasal: Initial: 1 spray per nostril once daily (total daily dose: 100 mcg/day). If response is inadequate, increase to 2 sprays per nostril once daily (total daily dose: 200 mcg/day). Once symptoms are controlled, reduce dose to 1 spray per nostril once daily (total daily dose: 100 mcg/day). Maximum daily dose: 2 sprays per nostril once daily (total daily dose: 200 mcg/day). Note: For optimal effects, nasal spray should be used at regular intervals.

Rhinitis, allergic (seasonal and perennial):

Fluticasone furoate (27.5 mcg/spray):

Veramyst, Avamys [Canadian product]: Intranasal:

Children 2 to 11 years: Initial: 1 spray per nostril once daily (total daily dose: 55 mcg/day); if response is inadequate, increase to 2 sprays per nostril once daily (total daily dose: 110 mcg/day); once symptoms have been controlled, the dosage may be reduced to 1 spray per nostril once daily (total daily dose: 55 mcg/day). Maximum daily dose: 2 sprays per nostril once daily (total daily dose: 110 mcg/day)

Children ≥12 years and Adolescents: Initial: 2 sprays per nostril once daily (total daily dose: 110 mcg/day); once symptoms are controlled, dosage may be reduced to 1 spray per nostril once daily (total daily dose: 55 mcg/day)

Fluticasone propionate (50 mcg/spray):

Canadian labeling: Flonase (fluticasone propionate 50 mcg/spray): Intranasal:

Children 4 to 11 years: 1 to 2 sprays per nostril once daily (total daily dose: 100 to 200 mcg/day); maximum daily dose: 2 sprays per nostril once daily (total daily dose: 200 mcg/day). Once symptoms are controlled, reduce dose to 1 spray per nostril once daily (total daily dose: 100 mcg/day).

Children ≥12 years and Adolescents ≤17 years: 2 sprays per nostril once daily (total daily dose: 200 mcg/day); patients with severe rhinitis may benefit from 2 sprays in each nostril twice daily (total daily dose: 400 mcg/day); maximum daily dose: 4 sprays per nostril once daily (total daily dose: 400 mcg/day)

Upper respiratory allergies (OTC):

Fluticasone furoate (27.5 mcg/spray) (eg, Flonase Sensimist): Intranasal:

Children 2 to 11 years: 1 spray per nostril once daily (total daily dose: 55 mcg/day)

Children ≥12 years and Adolescents: 2 sprays per nostril once daily (total daily dose: 110 mcg/day) for 1 week; then may adjust to 1 or 2 sprays per nostril once daily (total daily dose range: 55 to 110 mcg/day)

Fluticasone propionate (50 mcg/spray) (eg, Flonase allergy relief, ClariSpray): Intranasal:

Children 4 to 11 years: 1 spray per nostril once daily (total daily dose: 100 mcg/day)

Children ≥12 years and Adolescents: 2 sprays per nostril once daily (total daily dose: 200 mcg/day) for 1 week; then may adjust to 1 or 2 sprays per nostril once daily (total daily dose range: 100 to 200 mcg/day)

Administration

For intranasal use only; do not spray in eyes or mouth. Administer at regular intervals. Shake bottle gently before each use. Blow nose to clear nostrils. Insert applicator into nostril, keeping bottle upright, and close off the other nostril. Breathe in through nose. While inhaling, press pump to release spray. Discard after labeled number of doses has been used, even if bottle is not completely empty.

Flonase: Prime pump (press 6 times until fine spray appears) prior to first use or if spray unused for ≥7 days. Once weekly, nasal applicator may be removed and rinsed with warm water to clean.

Veramyst, Avamys [Canadian product]: Prime pump (press 6 times until fine spray appears) prior to first use, if spray unused for ≥30 days, or if cap left off bottle for ≥5 days. After each use, nozzle should be wiped with a clean, dry tissue. Once weekly, inside of cap should be cleaned with a clean, dry tissue.

Flonase Sensimist: Shake bottle vigorously before using. Prime pump. Sniff gently after each spray. Wipe spray nozzle after each use with clean, dry tissue and replace cap.

Xhance: Avoid spraying directly on the septum. Prior to first use, prime pump by gently shaking and press bottle 7 times until fine mist appears; if not used for ≥7 days, re-prime pump again by shaking and releasing 2 sprays into the air. Insert nosepiece deep into one nostril and form a tight seal and then place the flexible mouthpiece into the mouth; blow into the mouthpiece, and while continuing to blow, push the bottle up to actuate the spray pump; continue to blow through the mouth, but do not inhale or exhale through the nose at the time of actuation; repeat in the other nostril for a full dose.

Storage

ClariSpray, Flonase, Flonase Allergy Relief, Good Sense Nasoflow: Store between 4°C to 30°C (39°F to 86°F).

Veramyst, Flonase Sensimist: Store between 15°C to 30°C (59°F to 86°F); do not refrigerate or freeze. Store Veramyst in upright position with cap on.

Xhance: Store at 15°C to 25°C (59°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Avoid exposure to extreme heat, cold, or light.

Avamys [Canadian product]: Store between 4°C to 30°C (39°F to 86°F); do not refrigerate or freeze. Store in upright position with cap on.

Drug Interactions

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Fluticasone (Nasal). Avoid combination

Desmopressin: Corticosteroids (Nasal) may enhance the hyponatremic effect of Desmopressin. Avoid combination

Esketamine: Corticosteroids (Nasal) may diminish the therapeutic effect of Esketamine. Management: Patients who require a nasal corticosteroid on an esketamine dosing day should administer the nasal corticosteroid at least 1 hour before esketamine. Consider therapy modification

Ritodrine: Corticosteroids may enhance the adverse/toxic effect of Ritodrine. Monitor therapy

Adverse Reactions

>10%: Central nervous system: Headache (4% to 16%)

1% to 10%:

Central nervous system: Body pain (1% to 3%), dizziness (1% to 3%), generalized ache (1% to 3%)

Endocrine & metabolic: Weight gain (1% to <3%)

Gastrointestinal: Nausea and vomiting (3% to 5%), abdominal pain (1% to 3%), diarrhea (1% to 3%), abdominal distress (1% to <3%), toothache (1% to <3%)

Local: Local irritation (nose: 4% to 6%)

Ophthalmic: Increased intraocular pressure (1% to <3%)

Respiratory: Epistaxis (6% to 12%), nasal mucosa ulcer (3% to 8%; includes nasal septal ulceration), pharyngitis (3% to 8%), nasopharyngitis (8%), acute asthma (7%), nasal congestion (6%), acute sinusitis (5%), cough (4%), blood in nasal mucosa (1% to 3%), bronchitis (1% to 3%), flu-like symptoms (1% to 3%), rhinorrhea (1% to 3%), dry nose (1% to <3%), oropharyngeal pain (1% to <3%), sinusitis (1% to <3%)

Miscellaneous: Fever (1% to 3%)

<1%, postmarketing, and/or case reports: Altered sense of smell, anaphylactoid reaction, anaphylaxis, angioedema, blurred vision, bronchospasm, cataract, conjunctivitis, contact dermatitis, dry eye syndrome, dry throat, dysgeusia, dyspnea, esophageal candidiasis, eye irritation, facial edema, glaucoma, growth suppression, hoarseness, hypersensitivity reaction, intestinal candidiasis, nasal candidiasis, nasal septum perforation, pharyngeal candidiasis, pruritus, skin rash, sore throat, throat irritation, tongue edema, urticaria, voice disorder, wheezing

Warnings/Precautions

Concerns related to adverse effects:

• Adrenal suppression: May cause hypercortisolism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods. HPA axis suppression may lead to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. Pediatric patients may be more susceptible to systemic toxicity. Particular care is required when patients are transferred from systemic corticosteroids to inhaled products due to possible adrenal insufficiency or withdrawal from steroids, including an increase in allergic symptoms. Adult patients receiving ≥20 mg per day of prednisone (or equivalent) may be most susceptible. Concurrent use of ritonavir (and potentially other strong inhibitors of CYP3A4) may increase fluticasone levels and effects on HPA suppression.
• Delayed wound healing: Avoid use in patients with recent nasal septal ulcers, nasal surgery, or nasal trauma until healing has occurred.
• Hypersensitivity: Hypersensitivity reactions (including anaphylaxis, angioedema, rash, contact dermatitis, hypotension, bronchospasm, and urticaria) have been reported; discontinue for severe reactions.
• Immunosuppression: Prolonged use of corticosteroids may also increase the incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to vaccines. Exposure to chickenpox and/or measles should be avoided, especially if not immunized; if the patient is exposed, prophylaxis with varicella zoster immune globulin or pooled intramuscular immunoglobulin, respectively, may be indicated; if chickenpox develops, treatment with antiviral agents may be considered.
• Local nasal effects: Nasal septal perforation, nasal ulceration, nasal erosion, epistaxis, and localized Candida albicans infections of the nose and/or pharynx may occur. Monitor patients periodically for adverse nasal effects; discontinuation of therapy may be necessary if an infection occurs; discontinue therapy if nasal septal perforation occurs.

Disease-related concerns:

• Hepatic impairment: Use with caution in patients with moderate to severe hepatic impairment (accumulation may occur); monitor patients closely.
• Infections: Use caution or avoid use in patients with active or quiescent tuberculosis infections of the respiratory tract, systemic fungal, bacterial, viral, or parasitic infections, or ocular herpes simplex. Do not use in untreated localized infection involving the nasal mucosa; concurrent antimicrobial therapy should be administered if bacterial infection of the sinuses is suspected/confirmed.
• Ocular disease: Use with caution in patients with cataracts and/or glaucoma; increased intraocular pressure, open-angle glaucoma, and cataracts have occurred with prolonged use. Consider routine eye exams in long-term users or in patients who report visual changes.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Pediatrics: Avoid using higher than recommended dosages; suppression of linear growth (ie, reduction of growth velocity), reduced bone mineral density, or hypercortisolism (Cushing syndrome) may occur; titrate to lowest effective dose. Reduction in growth velocity may occur when corticosteroids are administered to pediatric patients, even at recommended doses via intranasal route (monitor growth). Use for the shortest amount of time necessary to achieve symptom relief.

Other warnings/precautions:

• Appropriate use: Prior to use, the dose and duration of treatment should be based on the risk vs benefit for each individual patient. In general, use the smallest effective dose for the shortest duration of time to minimize adverse events. There have been reports of systemic corticosteroid withdrawal symptoms (eg, joint/muscle pain, lassitude, depression) when withdrawing inhalation therapy.
• Self-medication (OTC use): Consult a health care provider before use if you taking medicine for HIV infection (eg, ritonavir), steroid for asthma, allergies, or skin rash, or ketoconazole (for a fungal infection). Discontinue use and consult a health care provider if you have come in contact with someone who has chicken pox, measles, or tuberculosis, symptoms do not get better within 7 days or new symptoms occur (eg, severe facial pain, thick nasal discharge), constant whistling sound from nose, changes in vision, or severe or frequent nosebleeds. Stinging or sneezing may occur for a few seconds after use.
• Withdrawal: Symptoms of corticosteroid withdrawal (eg, joint pain, muscle pain, lassitude, depression) may occur when transferring from a systemic corticosteroid to a topical corticosteroid.

Monitoring Parameters

Growth (adolescents and children); signs/symptoms of HPA axis suppression/adrenal insufficiency; possible eosinophilic conditions (including eosinophilic granulomatosis with polyangiitis [formerly known as Churg-Strauss]); ocular changes; signs/symptoms of Candida infection (long-term therapy); hepatic function

Pregnancy

Pregnancy Considerations

Fluticasone can be detected in cord blood following maternal use via oral inhalation during pregnancy; one woman in the study was also using intranasal fluticasone (Battista 2016). Hypoadrenalism may occur in newborns following maternal use of corticosteroids in pregnancy; monitor.

Intranasal corticosteroids, including fluticasone, may be acceptable for the treatment of rhinitis during pregnancy when used at recommended doses (Lal 2016; Wallace 2008). Pregnant females adequately controlled on fluticasone may continue therapy; if initiating treatment during pregnancy, use of an agent with more data during pregnancy may be preferred (Namazy 2016; Wallace 2008).

Patient Education

What is this drug used for?

• It is used to ease allergy signs.

Frequently reported side effects of this drug

• Headache
• Nausea
• Vomiting
• Cough
• Stinging
• Sneezing

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

• Adrenal gland problems like severe nausea, vomiting, severe dizziness, passing out, muscle weakness, severe fatigue, mood changes, lack of appetite, or weight loss.
• Severe stuffy nose
• Nasal sores
• Severe nosebleeds
• Wheezing
• Thrush
• Abnormal nasal discharge
• Severe face pain
• Runny nose
• Nasal crusting
• Bone pain
• Chills
• Severe sore throat
• Vision changes
• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.