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, acute bronchospasm

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); care must be taken to avoid exposure

Hypercorticism and adrenal suppression may occur with high dosages or at regular dosage in susceptible individuals; if such changes occur, taper withdrawal gradually

May decrease growth velocity in children; monitor growth of pediatric patients

Assess for decrease in bone mineral density initially and periodically thereafter

Use with caution in immunocompromised patients

Prolonged use of corticosteroids may increase incidence of secondary infection

Risk of infections of nose and pharynx, including Candida albicans; must rinse mouth after inhalation to reduce risk

Excessive use may suppress hypothalamic-pituitary-adrenal function; monitor closely, especially postoperatively or during periods of stress

During periods of stress or severe status asthmaticus, supplementary systemic corticosteroids may be immediately required; patient should carry warning card indicating possible need for supplementary systemic steroids in such emergencies

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