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CORTICOSTEROIDS (INHALATION)

General

beclomethasone

Pronunciation:
be-kloe-meth-a-sone


Trade Name(s)

  • QVAR

budesonide

Pronunciation:
byoo-dess-oh-nide


Trade Name(s)

  • Pulmicort Respules
  • Pulmicort Flexhaler

fluticasone

Pronunciation:
floo-ti-ka-sone


Trade Name(s)

  • Arnuity Ellipta
  • Flovent Diskus
  • Flovent HFA

mometasone

Pronunciation:
mo-met-a-sone

Trade Name(s)

  • Asmanex HFA
  • Asmanex Twisthaler

Ther. Class.
antiasthmatics
anti-inflammatories (steroidal)

Pharm. Class.
corticosteroids (inhalation)

Indications

  • Maintenance treatment of asthma as prophylactic therapy.
  • May decrease the need for or eliminate use of systemic corticosteroids in patients with asthma.

Action

Potent, locally acting anti-inflammatory and immune modifier.

Therapeutic Effect(s):

  • Decreased frequency and severity of asthma attacks.
  • Improves asthma symptoms.

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 and 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 hr‡1–4 wk†unknown
†Improvement in pulmonary function; ↓ airway responsiveness may take longer.‡2–8 days for budesonide respule.

Contraindication/Precautions

Contraindicated in:

  • Some products contain alcohol or lactose and should be avoided in patients with known hypersensitivity or intolerance;
  • Acute attack of asthma/status asthmaticus.

Use Cautiously in:

  • Active untreated infections;
  • Diabetes or glaucoma;
  • 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 (fluticasone);
  • OB: Lactation: Safety not established;
  • Pedi: Prolonged or high-dose therapy may lead to complications.

Adverse 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

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

Interactions

Drug-Drug

Strong CYP3A4 inhibitors, including ritonavir, atazanavir, clarithromycin, conivaptan, indinavir, itraconazole, ketoconazole, lopinavir, nefazodone, nelfinavir, saquinavir, and voriconazole ↓ metabolism and ↑ levels of budesonide, mometasone, and fluticasone; concurrent use with fluticasone not recommended.

Route/Dosage

Beclomethasone

Inhaln: (Adults and Children ≥12 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 ≥6 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 ≥12 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 ≥12 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 ≥12 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 ≥12 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).

Availability

Beclomethasone

Inhalation aerosol: 40 mcg/metered inhalation in 8.7-g canister (delivers 120 metered inhalations), 80 mcg/metered inhalation in 8.7-g canister (delivers 120 metered inhalations)

Cost: 40 mcg/metered inhalation $130.16/inhaler, 80 mcg/metered inhalation $173.67/inhaler

Budesonide

Inhalation powder (Flexhaler): 90 mcg/metered inhalation (delivers 60 metered inhalations), 180 mcg/metered inhalation (delivers 120 metered inhalations)

Cost: 90 mcg/metered inhalation $143.87/inhaler, 180 mcg/metered inhalation $192.65/inhaler

Inhalation suspension (Respules): 0.25 mg/2 mL in single-dose ampules (5 ampules/envelope), 0.5 mg/2 mL in single-dose ampules (5 ampules/envelope), 1 mg/2 mL in single-dose ampules (5 ampules/envelope)

In Combination with: formoterol (Symbicort). See combination drugs.

Fluticasone

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

Cost: 44 mcg/inhalation $137.82/inhaler, 110 mcg/inhalation $181.43/inhaler, 220 mcg/inhalation $278.14/inhaler

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

Cost: 50 mcg $144.47/60 blisters, 250 mcg $134.71/28 blisters

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

In Combination with: salmeterol (Advair), vilanterol (Breo Ellipta). See combination drugs.

Mometasone

Inhalation aerosol (Asmanex HFA): 100 mcg/metered inhalation in 13-g canisters (120 metered inhalations), 200 mcg/metered inhalation in 13-g canisters (120 metered inhalations)

Powder for inhalation (Asmanex Twisthaler): 110 mcg (delivers 100 mcg/metered inhalation; in packages of 7 and 30 inhalation units), 220 mcg (delivers 200 mcg/metered inhalation; in packages of 14, 30, 60, and 120 inhalation units)

Cost: 110 mcg $88.75/7 inhalation units, 110 mcg $157.90/30 inhalation units, 220 mcg $88.75/14 inhalation units, 220 mcg $170.47/30 inhalation units, 220 mcg $200.32/60 inhalation units, 220 mcg $287.09/120 inhalation units

Assessment

  • Monitor respiratory status and lung sounds. Assess pulmonary function tests periodically during and for several mo 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 decreased bone mineral density during prolonged therapy. Monitor patients with increased risk (prolonged immobilization, family history of osteoporosis, postmenopausal status, tobacco use, advanced age, poor nutrition, chronic use of drugs that can reduce bone mass [anticonvulsants, oral corticosteroids]) for fractures.
  • Monitor for signs and symptoms of hypersensitivity reactions (rash, pruritis, 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.

Potential Diagnoses

Implementation

  • Do not confuse Flovent with Flonase.
  • After desired clinical effect has been obtained, attempts should be made to decrease dose to lowest amount required to control symptoms. Gradually decrease 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.

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.
  • 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 medication administration techniques).
  • 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).
  • 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.
  • 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 medication administration techniques). 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).
  • 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.

Evaluation/Desired Outcomes

  • Management of the symptoms of chronic asthma.
  • Improvement in symptoms of asthma.
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Citation

Quiring, Courtney, et al. "CORTICOSTEROIDS (INHALATION)." Davis's Drug Guide, 16th ed., F.A. Davis Company, 2019. Anesthesia Central, anesth.unboundmedicine.com/anesthesia/view/Davis-Drug-Guide/110548/all/CORTICOSTEROIDS__INHALATION_.
Quiring C, Sanoski CA, Vallerand AH. CORTICOSTEROIDS (INHALATION). Davis's Drug Guide. 16th ed. F.A. Davis Company; 2019. https://anesth.unboundmedicine.com/anesthesia/view/Davis-Drug-Guide/110548/all/CORTICOSTEROIDS__INHALATION_. Accessed May 25, 2019.
Quiring, C., Sanoski, C. A., & Vallerand, A. H. (2019). CORTICOSTEROIDS (INHALATION). In Davis's Drug Guide. Available from https://anesth.unboundmedicine.com/anesthesia/view/Davis-Drug-Guide/110548/all/CORTICOSTEROIDS__INHALATION_
Quiring C, Sanoski CA, Vallerand AH. CORTICOSTEROIDS (INHALATION) [Internet]. In: Davis's Drug Guide. F.A. Davis Company; 2019. [cited 2019 May 25]. Available from: https://anesth.unboundmedicine.com/anesthesia/view/Davis-Drug-Guide/110548/all/CORTICOSTEROIDS__INHALATION_.
* Article titles in AMA citation format should be in sentence-case
TY - ELEC T1 - CORTICOSTEROIDS (INHALATION) ID - 110548 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - Davis's Drug Guide UR - https://anesth.unboundmedicine.com/anesthesia/view/Davis-Drug-Guide/110548/all/CORTICOSTEROIDS__INHALATION_ PB - F.A. Davis Company ET - 16 DB - Anesthesia Central DP - Unbound Medicine ER -