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 Effects: Decreased frequency
and severity of asthma attacks. Improves asthma
symptoms.
Pharmacokinetics
Absorption: Beclomethasone—20%; budesonide—
6–13% (Flexhaler), 6% (Respules); flunisolide—
40%; 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; Budenoside, flunisolide,
fluticasone, mometasone—metabolized by
the liver (primarily by CYP3A4) after absorption from
lungs; Budenoside—60% excreted in urine, 40% in
feces; flunisolide—50% excreted in urine, 50% 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; flunisolide—1.8 hr; fluticasone—7.8 hr
(propionate); 24 hr (furoate); mometasone—5 hr.
TIME/ACTION PROFILE (improvement in
symptoms)
ROUTE ONSET PEAK DURATION
Inhalation within 24 hr‡ 1–4 wk† unknown
†Improvement in pulmonary function;pairway responsiveness
may take longer.
‡2–8 days for budesonide respule.
Contraindications/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 dysfunction
(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 (qdose, long-term therapy only),
pgrowth (children),pbone mineral density. MS:
back pain. Misc: hypersensitivity reactions including
ANAPHYLAXIS, LARYNGEAL EDEMA, URTICARIA, and BRONCHOSPASM,
CHURG-STRAUSS SYNDROME.
Interactions
Drug-Drug: Strong CYP3A4 inhibitors, including
ritonavir, atazanavir, clarithromycin, conivaptan,
indinavir, itraconazole, ketoconazole, lopinavir,
nefazodone, nelfinavir, saquinavir, and voriconazolepmetabolism
andqlevels 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).
Flunisolide
Inhaln (Adults and Children 12 yr): 160 mcg (2
inhalations) twice daily (not to exceed 4 inhalations
twice daily).
Inhaln (Children 6–11 yr): 80 mcg (1 inhalation)
twice daily (not to exceed 2 inhalations twice daily).
Fluticasone (Aerosol Inhaler)
Inhaln (Adults and Children 12 yr): Previously
on bronchodilators alone—88 mcg twice daily initially,
may bequp to 440 mcg twice daily; Previously
on other inhaled corticosteroids—88–220 mcg
twice daily initially, may bequp to 440 mcg twice daily;
Previously on oral corticosteroids—440 mcg twice
daily initially, may bequp 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 bequp to 500 mcg twice daily;
Furoate: 100 mcg once daily, may bequp to 200 mcg
once daily after 2 wk; Previously on other inhaled
corticosteroids—Propionate: 100–250 mcg twice
daily initially, may bequp 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
bequp to 100 mcg twice daily; Previously on other
inhaled corticosteroids—50 mcg twice daily, may be
qup 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 highdose
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 (generic available)
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 singledose
ampules (5 ampules/envelope), 1 mg/2 mL in single-
dose ampules (5 ampules/envelope). In combination
with: formoterol (Symbicort). See
Appendix B.
Flunisolide
Inhalation aerosol: 80 mcg/metered inhalation in
5.1-g canisters (delivers 60 metered inhalations) or
8.9-g canisters (delivers 120 metered inhalations).
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 Appendix B.
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.
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