fluticasone inhaled (Rx)

>10%

Oral candidiasis (<31%)

Throat irritation (3-22%)

Upper respiratory tract infection (16-18%)

Fatigue or malaise (16%)

Nasal congestion (16%)

Rhinitis (≤13%)

Musculoskeletal pain (2-12%)

Headache (5-11%)

1-10%

Nasal congestion (8%)

Sinusitis or sinus infection (4-7%)

Cough (4-6%)

Bronchitis (2-6%)

Hoarseness or dysphonia (2-6%)

Allergic rhinitis (5%)

Nasal discharge (5%)

Upper respiratory inflammation (2-5%)

Muscle injury (≤5%)

Gastrointestinal (GI) discomfort or pain (1-4%)

Frequency Not Defined

Hypersensitivity reactions (including anaphylaxis, angioedema, rash, urticaria)

Respiratory: Rhinitis, rhinorrhea or postnasal drip, nasal sinus disorders, laryngitis

GI: Diarrhea, loss of taste, viral infections, dyspeptic symptoms, discomfort, pain, hyposalivation

Muscular: Musculoskeletal pain, stiffness, tightness, rigidity, injuries, soreness

Other: Dizziness, migraine, fever, viral infection, pain, chest symptoms, viral skin infections, soft tissue injuries, urinary infections

Postmarketing Reports

Special senses: Aphonia, facial and oropharyngeal edema, throat soreness, irritation, cataracts

Endocrine: Cushingoid features, growth velocity reduction in children and adolescents, hyperglycemia, osteoporosis, weight gain

GI: Dental caries, tooth discoloration, esophageal candidiasis

Psychiatry: Agitation, aggression, anxiety, depression, restlessness; behavioral changes, including hyperactivity and irritability (rarely and primarily in children)

Immunologic: Immediate and delayed hypersensitivity reactions, including urticaria, anaphylaxis, rash, angioedema, bronchospasm

Respiratory: Asthma exacerbation, chest tightness, cough, dyspnea, immediate and delayed bronchospasm, paradoxical bronchospasm, pneumonia, wheezing

Skin: Contusions, cutaneous hypersensitivity reactions, ecchymoses, pruritus

Rare cases of systemic eosinophilic conditions (some with features of vasculitis consistent with Churg-Strauss syndrome, which is often treated with systemic corticosteroids)

Eye: Cataracts, blurred vision, and central serous chorioretinopathy

Nervous system disorders: Tremor

Contraindications

Hypersensitivity to drug, components or milk proteins, which may result in anaphylaxis, angioedema, rash, and urticaria

Primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required

Cautions

Respiratory tract tuberculosis, untreated fungal or bacterial infections, viral or parasitic infections, ocular herpes simplex; care must be taken to avoid exposure

Nasal septum perforation, epistaxis, wheezing

Glaucoma, increased intraocular pressure, and cataracts reported in patients following long-term administration of drug; monitor closely; consider referral to an ophthalmologist in patients who develop ocular symptoms or use inhaler long term

Risk of more serious or fatal course of chickenpox or measles in susceptible patients (eg, unvaccinated or immunologically unexposed individuals); if patient exposed to chickenpox, may administer prophylaxis with varicella-zoster immune globulin (VZIG); if a patient is exposed to measles, may administer prophylaxis with pooled intramuscular immunoglobulin (IG; See respective package inserts for complete VZIG and IG prescribing information); if chickenpox develops, treatment with antiviral agents may be considered; use with caution, if at all, in patients with active or quiescent tuberculosis infections of respiratory tract; systemic fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex

Use with caution in immunocompromised patients

Risk of infections of nose and pharynx, including Candida albicans; must rinse mouth after inhalation to reduce risk; treat with appropriate local or systemic (eg, oral) antifungal therapy while treatment continues; at times therapy may need to be interrupted

Paradoxical bronchospasm may occur with immediate increase in wheezing after dosing; if bronchospasm occurs following dosing treat immediately with an inhaled, short-acting bronchodilator; discontinued therapy immediately; and institute alternative therapy

Orally inhaled corticosteroids may cause a reduction in growth velocity when administered to pediatric patients; monitor growth of pediatric patients receiving ICS routinely (eg. via stadiometry); to minimize systemic effects of orally inhaled corticosteroids, titrate each patient’s dosage to lowest dosage that effectively controls his/her symptoms

Decreases in bone mineral density (BMD) reported with long-term administration of products containing ICS; clinical significance of small changes in BMD with regard to longterm consequences such as fracture is unknown; monitor and treat patients with established standards of care patients with major risk factors for decreased bone mineral content, such as prolonged immobilization, family history of osteoporosis, postmenopausal status, tobacco use, advanced age, poor nutrition, or chronic use of drugs that can reduce bone mass (eg, anticonvulsants, oral corticosteroids)

Anaphylactic reactions in patients with severe milk protein allergy after inhalation of powder products containing lactose reported; patients with severe milk protein allergy should not use product

Therapy not to be regarded as bronchodilator and not indicated for rapid relief of bronchospasm; instruct patient to contact physicians immediately when episodes of asthma that are not responsive to bronchodilators occur during course of treatment; during such episodes, patients may require therapy with oral corticosteroids

Eosinophilic conditions

• In rare cases, patients on inhaled fluticasone propionate may present with systemic eosinophilic conditions; some patients have clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition that is often treated with systemic corticosteroid therapy; these events, have been associated (not always) with reduction and/or withdrawal of oral corticosteroid therapy following introduction of fluticasone propionate
• Cases of serious eosinophilic conditions have also been reported with other ICS in this clinical setting; physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients; a causal relationship between fluticasone propionate and these underlying conditions not established

Transferring patients from systemic corticosteroid therapy

• Particular care needed for patients transferred from systemically active corticosteroids to ICS; deaths due to adrenal insufficiency during and after transfer from systemic corticosteroids to less systemically available ICS
• After withdrawal from systemic corticosteroids, a number of months are required for recovery of hypothalamic-pituitary-adrenal (HPA) function
• During periods of stress or a severe asthma attack, instruct patients who have been withdrawn from systemic corticosteroids to resume oral corticosteroids (in large doses) immediately and to contact their physicians for further instruction; patients should carry warning card indicating possible need for supplementary systemic steroids in such emergencies
• Patients requiring oral corticosteroids should be weaned slowly from systemic corticosteroid use after transferring to ICS; prednisone reduction can be accomplished by reducing the daily prednisone dose by 2.5 mg on a weekly basis during therapy with ICS
• Lung function (mean forced expiratory volume in 1 second [FEV1] or morning peak expiratory flow [AM PEF]), beta-agonist use, and asthma symptoms should be carefully monitored during withdrawal of oral corticosteroids
• Patients should be observed for signs and symptoms of adrenal insufficiency, such as fatigue, lassitude, weakness, nausea and vomiting, and hypotension
• Transfer of patients from systemic corticosteroid therapy to ICS may unmask allergic conditions previously suppressed by the systemic corticosteroid therapy (e.g., rhinitis, conjunctivitis, eczema, arthritis, eosinophilic conditions)
• Systemic corticosteroid effects such as hypercorticism and adrenal suppression (including adrenal crisis) may appear in a small number of patients who are sensitive to these effects; if effects occur, ICS dose should be reduced slowly, consistent with accepted procedures for reducing systemic corticosteroids, and other treatments for management of asthma symptoms should be considered

Pregnancy

There are no randomized clinical studies in pregnant women; in women with poorly or moderately controlled asthma, there is increased risk of several perinatal adverse outcomes (eg, pre-eclampsia in the mother, prematurity, low birth weight, and small for gestational age in the neonate;)

Pregnant women with asthma should be closely monitored and medication adjusted as necessary to maintain optimal asthma control

Lactation

Fluticasone propionate concentrations in plasma after inhaled therapeutic doses are low; concentrations in human breast milk are likely to be correspondingly low

Developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from the drug or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Anti-inflammatory corticosteroid; exact mechanism of action is unknown, but agent has been shown to exhibit anti-inflammatory effect on neutrophils, eosinophils, macrophages, mast cells, lymphocytes, and mediators (histamine, leukotrienes, cytokines, eicosanoids)

Absorption

Bioavailability: 30%

Onset: 24 hr (maximum, 1-2 wk)

Distribution

Protein bound: 99%

Vd: 4.2 L/kg

Metabolism

Metabolized in liver by CYP3A4

Metabolites: 17-Beta carboxylic acid

Elimination

Half-life: 11-12 hr

Excretion: Feces (parent drug), urine (<5% metabolites)

Orally Inhaled Administration

Aerosol

• Prime inhaler (4 actuations into air) before first use and after prolonged (>7 days) idleness
• Valve holding chamber and face mask may be used for younger patients

Powder

• Does not require priming
• Do not use with a spacer
• Keep the inhaler in a cool dry place; never wash or put any part of the inhaler in water
• Routine maintenance is not required; if the mouthpiece needs cleaning, gently wipe with a dry cloth or tissue as needed
• Hold your breath for about 10 seconds after inhaling; then breathe out fully
• After each dose, rinse your mouth with water and spit it out; do not swallow the water

• Diskus

  • Always use in a level, flat position
  • Make sure the lever firmly clicks into place