fluticasone (inhalation)

General

Pronunciation:
floo-ti-ka-sone


fluticasone (inhalation)

fluticasone (inhalation)

fluticasone (inhalation)

Trade Name(s)

  • Aermony Respiclick Canadian Trade name
  • Arnuity Ellipta
  • Flovent Diskus Canadian Trade name
  • Flovent HFA Canadian Trade name

Ther. Class.

anti-inflammatories (steroidal)

Pharm. Class.

corticosteroids

Indications

Maintenance treatment of asthma as prophylactic therapy.

Action

Potent, locally acting anti-inflammatory and immune modifier.

Therapeutic Effect(s):

Decreases frequency and severity of asthma attacks.

Pharmacokinetics

Absorption: <1% (aerosol), 8–14% (powder) absorbed following oral inhalation. Action is primarily local after inhalation.

Distribution: 10–25% of inhaled corticosteroids is deposited in the airways if a spacer device is not used. With the use of a spacer, a greater percentage may reach the respiratory tract.

Protein Binding: 91–99%.

Metabolism and Excretion: Metabolized by the liver primarily by the CYP3A4 isoenzyme after absorption from lungs; <5% excreted in urine; remainder excreted in feces.

Half-life: 7.8 hr (propionate); 24 hr (furoate).

TIME/ACTION PROFILE (improvement in symptoms)

ROUTEONSETPEAKDURATION
Inhalationwithin 24 hr1–4 wk†several days after discontinuation
†Improvement in pulmonary function; decreased airway responsiveness may take longer.

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity (aerosol contains propellants; powder contains lactose [avoid in patients with severe milk protein allergy]);
  • Acute attack of asthma/status asthmaticus.

Use Cautiously in:

  • Active untreated infections;
  • Diabetes;
  • Glaucoma or cataracts;
  • Underlying immunosuppression (due to disease or concurrent therapy);
  • Systemic corticosteroid therapy (should not be abruptly discontinued when inhalation therapy is started; additional corticosteroids needed in stress or trauma);
  • Hepatic impairment;
  • OB:   Safety not established in pregnancy;
  • Lactation:  Use while breastfeeding only if potential maternal benefit outweighs potential risk to infant;
  • Pedi:   Children <5 yr (furoate) or <4 yr (propionate) (safety and effectiveness not established; prolonged or high-dose therapy may lead to complications).

Adverse Reactions/Side Effects

EENT: cataracts, dysphonia, glaucoma, hoarseness, nasal stuffiness, oropharyngeal fungal infections, rhinorrhea, sinusitis

Endo: adrenal suppression (high-dose, long-term therapy only), Cushing's syndrome, ↓ bone mineral density, ↓ growth (in children)

GI: diarrhea

MS: muscle pain

Neuro: headache, dizziness

Resp: bronchospasm, cough, upper respiratory tract infection, wheezing

Misc: CHURG-STRAUSS SYNDROME, fever, HYPERSENSITIVITY REACTIONS (including anaphylaxis and laryngeal edema)

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

 Strong CYP3A4 inhibitors, including  ritonavir,  atazanavir,  clarithromycin,  conivaptan,  itraconazole,  ketoconazole,  lopinavir,  nefazodone,  nelfinavir, and  voriconazole, may ↑ levels and risk of toxicity; concurrent use not recommended.

Route/Dosage

Aerosol for Oral Inhalation

Inhaln (Adults and Children  ≥12 yr): No prior treatment with inhaled corticosteroid: 88 mcg twice daily initially; may ↑ dose in 2 wk if not adequately responding (max dose = 880 mcg twice daily).

Inhaln (Children 4–11 yr): 88 mcg twice daily (max dose = 88 mcg twice daily).

Powder for Oral Inhalation

Inhaln (Adults and Children ≥12 yr): No prior treatment with inhaled corticosteroid: Propionate (Flovent Diskus generic): 100 mcg twice daily initially; may ↑ dose in 2 wk if not adequately responding (max dose = 1,000 mcg twice daily); Furoate: 100 mcg once daily; may ↑ dose in 2 wk to 200 mcg once daily if not adequately responding (max dose = 200 mcg once daily);  Prior treatment with inhaled corticosteroid: Furoate: 100–200 mcg once daily (max dose = 200 mcg once daily).

Inhaln (Children 5–11 yr): Furoate: 50 mcg once daily.

Inhaln (Children 4–11 yr): No prior treatment with inhaled corticosteroid: Propionate (Flovent Diskus generic): 50 mcg twice daily initially; may ↑ dose in 2 wk to 100 mcg twice daily if not adequately responding (max dose = 100 mcg twice daily).

Availability (generic available)

Inhalation aerosol (propionate) (Flovent HFA [generic only]): 44 mcg/metered inhalation in 10.6-g canisters (120 metered inhalations), 110 mcg/metered inhalation in 12-g canisters (120 metered inhalations), 220 mcg/metered inhalation in 12-g canisters (120 metered inhalations)

Powder for inhalation (furoate) (Arnuity Ellipta): 50 mcg/blister, 100 mcg/blister, 200 mcg/blister

Powder for inhalation (propionate) (Flovent Diskus [generic only]): 50 mcg/blister, 100 mcg/blister, 250 mcg/blister

In Combination with: salmeterol (Advair Diskus, Advair HFA, AirDuo RespiClick, Wixhela Inhub); vilanterol (Breo Ellipta); umeclidinium and vilanterol (Trelegy Ellipta). See combination drugs.

Assessment

  • Monitor respiratory status and lung sounds. Assess pulmonary function tests periodically during and for several months after a transfer from systemic to inhalation corticosteroids.
  • Assess patients changing from systemic corticosteroids to inhalation corticosteroids for signs of adrenal insufficiency (anorexia, nausea, weakness, fatigue, hypotension, hypoglycemia) during initial therapy and periods of stress. If these signs appear, notify health care professional immediately; condition may be life-threatening.
  • Monitor for withdrawal symptoms (joint or muscular pain, lassitude, depression) during withdrawal from oral corticosteroids.
  • Monitor growth rate in children receiving chronic therapy; use lowest possible dose.
  • May cause ↓ bone mineral density during prolonged therapy. Monitor patients with ↑ risk (prolonged immobilization, family history of osteoporosis, postmenopausal status, tobacco use, advanced age, poor nutrition, chronic use of drugs that can ↓ bone mass [anticonvulsants, oral corticosteroids]) for fractures.
  • Monitor for signs and symptoms of hypersensitivity reactions (rash, pruritus, swelling of face and neck, dyspnea) periodically during therapy.

Lab Test Considerations:

Periodic adrenal function tests may be ordered to assess degree of hypothalamic-pituitary-adrenal (HPA) axis suppression in chronic therapy. Children and patients using higher than recommended doses are at highest risk for HPA suppression.

  • May cause ↑ serum and urine glucose concentrations if significant absorption occurs.

Implementation

  • Do not confuse Flovent with Flonase.
  • After the desired clinical effect has been obtained, attempts should be made to ↓ dose to lowest amount required to control symptoms. Gradually ↓ dose every 2–4 wk as long as desired effect is maintained. If symptoms return, dose may briefly return to starting dose.
  • Inhaln Allow at least 1 min between inhalations of aerosol medication.

Patient/Family Teaching

  • Advise patient to take medication as directed. If a dose is missed, take as soon as remembered unless almost time for next dose. Instruct patient to read the  Patient Information and Instructions for Use  before using and with each Rx refill, in case of changes. Advise patient not to discontinue medication without consulting health care professional; gradual ↓ is required.
  • Advise patients using inhalation corticosteroids and bronchodilator to use bronchodilator first and to allow 5 min to elapse before administering the corticosteroid, unless otherwise directed by health care professional.
  • Advise patient that inhalation corticosteroids should not be used to treat an acute asthma attack but should be continued even if other inhalation agents are used.
  • Patients using inhalation corticosteroids to control asthma may require systemic corticosteroids for acute attacks. Advise patient to use regular peak flow monitoring to determine respiratory status.
  • Advise patient to stop using medication and notify health care professional immediately if signs and symptoms of hypersensitivity reactions occur.
  • Caution patient to avoid smoking, known allergens, and other respiratory irritants.
  • Advise patient to notify health care professional if sore throat or mouth occurs.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking other Rx, OTC, or herbal products.
  • Advise patient to stop using medication and notify health care professional immediately if signs and symptoms of hypersensitivity reactions occur.
  • Rep:  Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
  • Instruct patient whose systemic corticosteroids have been recently reduced or withdrawn to carry a warning card indicating the need for supplemental systemic corticosteroids in the event of stress or severe asthma attack unresponsive to bronchodilators.
  • Aerosol for Oral Inhalation: Instruct patient in the proper use of the metered-dose inhaler. Inhaler should be primed before using for first time by releasing 4 sprays into air, away from face. When inhaler has not been used for more than 7 days, reprime unit by releasing 1 spray into air away from face. Shake inhaler well. Exhale completely and then close lips firmly around mouthpiece. While breathing in deeply and slowly, press down on canister. Hold breath for as long as possible to ensure deep instillation of medication. Remover inhaler from mouth and breathe out gently. Allow 1–2 min between inhalations. Rinse mouth with water or mouthwash after each use to minimize fungal infections, dry mouth, and hoarseness. Wash inhalation assembly at least once weekly in warm running water (see medication administration techniques).
  • Powder for Oral Inhalation: Do not use with a spacer. Exhale completely and then close lips firmly around mouthpiece. While breathing in deeply and slowly, press down on canister. Hold breath for as long as possible to ensure deep instillation of medication. Remover inhaler from mouth and breathe out gently. Allow 1–2 min between inhalations. After inhalation, rinse mouth with water and spit out (see medication administration techniques). Never wash the mouthpiece or any part of the Diskus inhaler. Discard Diskus inhaler device (Flovent Diskus) 6 wk (50-mcg strength) or 2 mo (100-mcg and 250-mcg strengths) after opening, or blister tray (Arnuity Ellipta) 6 wk after removal from protective foil overwrap pouch or after all blisters have been used (whichever comes first).

Evaluation/Desired Outcomes

Management of the symptoms of chronic asthma.