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Indications

REMS

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CNS: headache, agitation, depression, dizziness, fatigue, insomnia, restlessness.

EENT: dysphonia, hoarseness, cataracts, glaucoma, nasal congestion, pharyngitis, sinusitis.

Resp: bronchospasm, cough, wheezing.

GI: diarrhea, dry mouth, dyspepsia, esophageal candidiasis, taste disturbances, nausea.

Endo: adrenal suppression ( dose, long-term therapy only), growth (children), bone mineral density.

MS: back pain.

Misc: HYPERSENSITIVITY REACTIONS INCLUDING ANAPHYLAXIS, LARYNGEAL EDEMA, URTICARIA, AND BRONCHOSPASM, CHURG-STRAUSS SYNDROME.

Interactions

Drug-Drug:

Availability

Beclomethasone

Budesonide

(generic available)

Fluticasone

Mometasone

Route/Dosage

Beclomethasone

  • Inhaln (Adults and Children ge.gif12 yr): Previously on bronchodilators alone — 40–80 mcg twice daily (not to exceed 320 mcg twice daily); Previously on inhaled corticosteroids — 40–160 mcg twice daily (not to exceed 320 mcg twice daily).
  • Inhaln (Children 5–11 yr): Previously on bronchodilators alone — 40 mcg twice daily (not to exceed 80 mcg twice daily); Previously on inhaled corticosteroids — 40 mcg twice daily (not to exceed 80 mcg twice daily).

Budesonide (Pulmicort Flexhaler)

  • Inhaln (Adults): 180–360 mcg twice daily (not to exceed 720 mcg twice daily).
  • Inhaln (Children ge.gif6 yr): 180–360 mcg twice daily (not to exceed 360 mcg twice daily).

Budesonide (Pulmicort Respules)

  • Inhaln (Children 1–8 yr): Previously on bronchodilators alone — 0.5 mg once daily or 0.25 mg twice daily (not to exceed 0.5 mg/day); Previously on other inhaled corticosteroids — 0.5 mg once daily or 0.25 mg twice daily (not to exceed 1 mg/day); Previously on oral corticosteroids — 1 mg once daily or 0.5 mg twice daily (not to exceed 1 mg/day).

Fluticasone (Aerosol Inhaler)

  • Inhaln (Adults and Children ge.gif12 yr): Previously on bronchodilators alone — 88 mcg twice daily initially, may be up to 440 mcg twice daily; Previously on other inhaled corticosteroids — 88–220 mcg twice daily initially, may be up to 440 mcg twice daily; Previously on oral corticosteroids — 440 mcg twice daily initially, may be up to 880 mcg twice daily.
  • Inhaln (Children 4–11 yr): 88 mcg twice daily (not to exceed 88 mcg twice daily).

Fluticasone (Dry Powder Inhaler)

  • Inhaln (Adults and Children ge.gif12 yr): Previously on bronchodilators alone — Propionate: 100 mcg twice daily initially, may be up to 500 mcg twice daily; Furoate: 100 mcg once daily, may be up to 200 mcg once daily after 2 wk; Previously on other inhaled corticosteroids — Propionate: 100–250 mcg twice daily initially, may be up to 500 mcg twice daily; Previously on oral corticosteroids — Propionate: 500–1000 mcg twice daily.
  • Inhaln (Children 4–11 yr): Previously on bronchodilators alone — 50 mcg twice daily initially, may be up to 100 mcg twice daily; Previously on other inhaled corticosteroids — 50 mcg twice daily, may be up to 100 mcg twice daily.

Mometasone (Aerosol Inhaler)

  • Inhaln (Adults and Children ge.gif12 yr): Previously on medium-dose inhaled corticosteroids — Two 100–mcg inhalations twice daily; Previously on high-dose inhaled corticosteroids or oral corticosteroids — Two 200–mcg inhalations twice daily (not to exceed 800 mcg/day).

Mometasone (Dry Powder Inhaler)

  • Inhaln (Adults and Children ge.gif12 yr): Previously on bronchodilators or other inhaled corticosteroids — 220 mcg once daily in evening, up to 440 mcg/day as a single dose or 2 divided doses; Previously on oral corticosteroids — 440 mcg twice daily (not to exceed 880 mcg/day).
  • Inhaln (Children 4–11 yr): 110 mcg once daily in evening (not to exceed 110 mcg/day).

US Brand Names

beclomethasone: QVAR

budesonide: Pulmicort Respules, Pulmicort Flexhaler

fluticasone: Arnuity Ellipta, Flovent Diskus, Flovent HFA

Mometasone: Asmanex HFA, Asmanex Twisthaler

Action

  • Potent, locally acting anti-inflammatory and immune modifier.
Therapeutic Effects:
  • Decreased frequency and severity of asthma attacks.
  • Improves asthma symptoms.

Classifications

Therapeutic Classification: antiasthmatics, corticosteroids

Pharmacologic Classification: corticosteroids (inhalation)

Pharmacokinetics

Absorption: Beclomethasone — 20%; budesonide — 6–13% (Flexhaler), 6% (Respules); fluticasone — <7% (aerosol), 8–14% (powder); mometasone — <1%. Action is primarily local after inhalation.

Distribution: 10–25% is deposited in airways if a spacer device is not used. All cross the placenta and enter breast milk in small amounts.

Metabolism/Excretion: Beclomethasone — after inhalation, beclomethasone dipropionate is converted to beclomethasone monopropionate, an active metabolite that adds to its potency, primarily excreted in feces (<10% excreted in urine; Budesonide, fluticasone, mometasone — metabolized by the liver (primarily by CYP3A4) after absorption from lungs; Budesonide — 60% excreted in urine, 40% in feces; fluticasone — primarily excreted in feces (<5% excreted in urine); mometasone — 75% excreted in feces.

Half-life: Beclomethasone — 2.8 hr; budesonide — 2–3.6 hr; fluticasone — 7.8 hr (propionate); 24 hr (furoate); mometasone — 5 hr.

Time/Action Profile

(improvement in symptoms)

ROUTEONSETPEAKDURATION
Inhalationwithin 24 hr1–4 wkunknown

†Improvement in pulmonary function; airway responsiveness may take longer.

†2–8 days for budesonide respule.

Patient/Family Teaching

  • Advise patient to take medication as directed. Take missed doses 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 new information. Advise patient not to discontinue medication without consulting health care professional; gradual decrease 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.
  • Caution patient to avoid smoking, known allergens, and other respiratory irritants.
  • Advise patient to notify health care professional if sore throat or sore mouth occurs.
  • Advise patient to stop using medication and notify health care professional immediately if signs and symptoms of hypersensitivity reactions occur.
  • Advise female patients to notify health care professional if pregnancy is planned or suspected or if breast feeding.
  • 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.
  • Metered-Dose Inhaler: Instruct patient in proper use of metered-dose inhaler. Most inhalers require priming before first use. 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. Remove 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. Clean mouthpiece weekly with clean, dry tissue or cloth. Do not place in water (see Appendix F).
  • Pulmicort Flexhaler: Advise patient to follow instructions supplied. Before first-time use, prime unit by turning cover and lifting off; hold upright with mouthpiece up and twist brown grip fully to right, then fully to left until it clicks. To administer dose, hold upright, twist brown grip fully to right, then fully to left until it clicks. Turn head away from inhaler and exhale (do not blow into inhaler). Do not shake inhaler. Place mouthpiece between lips and inhale deeply and forcefully. Remove inhaler from mouth and exhale (do not exhale into mouthpiece). Repeat procedure if 2nd dose required. Replace cover; rinse mouth with water (do not swallow).
  • Pulmicort Respules: Administer with a jet nebulizer connected to adequate air flow, equipped with a mouthpiece or face mask. Adjust face mask to avoid exposing eyes to nebulized medication. Wash face after use of face mask. Ultrasonic nebulizers are not adequate for administration and not recommended. Store respules upright, away from heat and protected from light. Do not refrigerate or freeze. Respules are stable for 2 wk at room temperature after opening aluminum foil envelope. Open respules must be used promptly. Unused respules should be returned to aluminum foil envelope.
  • Flovent Diskus/Arnuity Ellipta: 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. Remove inhaler from mouth and breathe out gently. Allow 1–2 min between inhalations. After inhalation, rinse mouth with water and spit out (see Appendix F). Never wash the mouthpiece or any part of the Diskus inhaler. Discard Diskus inhaler device (Flovent Diskus) 6 wks (50-mcg strength) or 2 mo (100-mcg and 250-mcg strengths) or blister tray (Arnuity Ellipta) 6 wks after removal from protective foil overwrap pouch or after all blisters have been used (whichever comes first).
  • Asmanex Twisthaler: Advise patient to remove cap while device is in upright position. To administer dose, exhale fully, then place mouthpiece between lips and inhale deeply and forcefully. Remove device from mouth and hold breath for 10 sec before exhaling (do not exhale into mouthpiece). Wipe the mouthpiece dry, if necessary, and replace the cap on the device. Rinse mouth with water. Advise patient to discard twisthaler 45 days from opening or when dose counter reads "00", whichever comes first.

Pronunciation

beclomethasone: be-kloe-METH-a-sone

budesonide: byoo-DESS-oh-nide

fluticasone: floo-TI-ka-sone

Mometasone: mo-MET-a-sone