Mometasone (Oral Inhalation)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Aerosol, Inhalation, as furoate:

Asmanex HFA: 50 mcg/actuation (13 g); 100 mcg/actuation (13 g); 200 mcg/actuation (13 g)

Aerosol Powder Breath Activated, Inhalation, as furoate:

Asmanex (120 Metered Doses): 220 mcg/INH (1 ea) [contains milk protein]

Asmanex (14 Metered Doses): 220 mcg/INH (1 ea) [contains milk protein]

Asmanex (30 Metered Doses): 110 mcg/INH (1 ea); 220 mcg/INH (1 ea) [contains milk protein]

Asmanex (60 Metered Doses): 220 mcg/INH (1 ea) [contains milk protein]

Asmanex (7 Metered Doses): 110 mcg/INH (1 ea) [contains milk protein]

Pharmacology

Mechanism of Action

May depress the formation, release, and activity of endogenous chemical mediators of inflammation (kinins, histamine, liposomal enzymes, prostaglandins). Leukocytes and macrophages may have to be present for the initiation of responses mediated by the above substances. Inhibits the margination and subsequent cell migration to the area of injury, and also reverses the dilatation and increased vessel permeability in the area resulting in decreased access of cells to the sites of injury.

Pharmacokinetics/Pharmacodynamics

Absorption

<1%; clinical effects are due to direct local effect, rather than systemic absorption

Distribution

V_d: 152 L

Metabolism

Extensive in the liver to multiple metabolites; no major metabolites are detectable in the plasma; in vitro incubation studies identified one minor metabolite, 6 Beta-hydroxymometasone furoate, formed via cytochrome P450 CYP3A4 pathway

Excretion

Feces (~74%), urine (~8%)

Onset of Action

Maximum effects may not be evident for ≥1 to 2 weeks

Time to Peak

Plasma: 0.5 to 2.5 hours

Duration of Action

Duration after discontinuation: Several days or more

Half-Life Elimination

Mean: 5 hours

Protein Binding

98% to 99%

Use: Labeled Indications

Asthma: Maintenance treatment of asthma as prophylactic therapy in patients ≥4 years of age (Asmanex Twisthaler) and ≥5 years of age (Asmanex HFA).

Limitations of use: Not indicated for the relief of acute bronchospasm.

Guideline recommendations: A low-dose inhaled corticosteroid (in addition to an as-needed short-acting beta-2 agonist) is the initial preferred long-term control medication for children, adolescents, and adult patients with persistent asthma who are candidates for treatment according to a step-wise treatment approach (GINA 2018; NAEPP 2007).

Contraindications

Hypersensitivity to mometasone or any component of the formulation; hypersensitivity to milk proteins (Asmanex Twisthaler only); primary treatment of status asthmaticus or other acute episodes of asthma for which intensive measures are required

Documentation of allergenic cross-reactivity for corticosteroids is limited. However, because of similarities in chemical structure and/or pharmacologic actions, the possibility of cross-sensitivity cannot be ruled out with certainty.

Canadian labeling: Additional contraindications (not in US labeling): Untreated systemic fungal, bacterial, viral, or parasitic infections; active or quiet tuberculosis infection of the respiratory tract; ocular herpes simplex

Dosage and Administration

Dosing: Adult

Note: The recommended starting dose is based on previous asthma therapy and disease severity; may increase dose after 2 weeks of therapy in patients who are not adequately controlled. Titrate to the lowest effective dose once asthma is controlled.

Asthma: Oral inhalation: Note: To decrease the severity or duration of an asthma exacerbation, may consider temporarily quadrupling the dose (early in the course of illness) in patients with mild to moderate asthma with a mild flare in symptoms. Reserve this approach for patients with no prior history of life-threatening asthma exacerbations, and in those with good self-management skills; return to baseline dose after normalization of symptoms or at a maximum of 14 days of the quadrupled dose (Fanta 2019; GINA 2018; McKeever 2018).

Asmanex HFA: Metered-dose inhaler:

Patients with no prior treatment with inhaled corticosteroid: Mometasone 100 mcg: Initial: 200 mcg twice daily; maximum dose: 400 mcg twice daily (800 mcg/day).

Patients who previously received oral corticosteroids: Mometasone 200 mcg: Initial: 400 mcg twice daily; maximum dose: 400 mcg twice daily (800 mcg/day).

Asmanex Twisthaler: Dry powder inhaler: Note: The 440 mcg daily dose may be administered in divided doses or as once daily.

Patients who previously received bronchodilators alone: Initial: 220 mcg once daily in the evening; maximum dose: 440 mcg/day.

Patients who previously received inhaled corticosteroids: Initial: 220 mcg once daily in the evening; maximum dose: 440 mcg/day.

Patients who previously received oral corticosteroids: Initial: 440 mcg twice daily; maximum dose: 880 mcg/day. Note: Prednisone should be reduced slowly (ie, no faster than 2.5 mg daily on a weekly basis), beginning after at least 1 week of mometasone therapy.

Asthma Guidelines:

Global Initiative for Asthma guidelines (GINA 2018): Dry powder inhaler:

Low-dose therapy: 110 to 220 mcg/day.

Medium-dose therapy: >220 to 440 mcg/day.

High-dose therapy: >440 mcg/day.

National Asthma Education and Prevention Program guidelines (NAEPP 2007): Dry powder inhaler: Note: 220 mcg inhaler delivers 200 mcg mometasone furoate per actuation; NAEPP uses doses based on delivery, while manufacturer recommended doses are based on inhaler amount.

Low-dose therapy: 200 mcg/day.

Medium-dose therapy: 400 mcg/day.

High-dose therapy: >400 mcg/day.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Asthma: Note: Asmanex Twisthaler (110 mcg and 220 mcg Twisthaler) deliver 100 and 200 mcg mometasone furoate per actuation respectively; NAEPP uses doses based on delivery dose, while manufacturer recommended doses are based on inhaler amount. Maximum effects may not be evident for 1 to 2 weeks or longer; higher doses may provide additional asthma control in patients who do not respond adequately after 2 weeks of therapy. Doses should be titrated to the lowest effective dose once asthma is controlled.

Maintenance therapy:

Asmanex Twisthaler (dry powder inhaler):

Children 4 to 11 years (regardless of prior therapy): Note: Use 110 mcg inhaler: Oral inhalation (110 mcg/inhalation): Initial: 110 mcg once daily, administered in the evening. Maximum daily dose: 110 mcg/day.

Children ≥12 years and Adolescents: Dosing based on previous asthma therapy:

Patients previously treated with bronchodilators alone or with inhaled corticosteroids: Oral inhalation (220 mcg/inhalation): Initial: 220 mcg once daily, administered in the evening; may increase dose after 2 weeks if adequate response not obtained. Maximum daily dose: 440 mcg/day; may be administered as 1 inhalation twice daily or 2 inhalations once daily in the evening.

Patients previously treated with oral corticosteroids: Oral inhalation (220 mcg/inhalation): Initial: 440 mcg twice daily. Maximum daily dose: 880 mcg/day.

Asmanex HFA:

Children 5 to <12 years: Oral inhalation (50 mcg/inhalation): 100 mcg twice daily; maximum daily dose: 200 mcg/day.

Children ≥12 years and Adolescents: Note: Dosing based on previous asthma therapy:

Patients previously treated with inhaled medium dose corticosteroid: Oral inhalation (100 mcg/inhalation): 200 mcg twice daily; maximum daily dose: 800 mcg/day.

Patients previously treated with high-dose inhaled corticosteroids or oral corticosteroids: Oral inhalation (200 mcg/inhalation): 400 mcg twice daily; maximum daily dose: 800 mcg/day.

Asthma guidelines:

Global Initiative for Asthma Guidelines (GINA 2017): Dry powder inhaler (refers to Asmanex Twisthaler 110 mcg and 220 mcg strengths):

Children 6 to 11 years: Oral inhalation:

“Low” dose: 110 mcg/day.

“Medium” dose: ≥220 to <440 mcg/day.

“High” dose: ≥440 mcg/day.

Children ≥12 years and Adolescents: Oral inhalation:

“Low” dose: 110 to 220 mcg/day.

“Medium” dose: >220 to 440 mcg/day.

“High” dose: >440 mcg/day.

National Asthma Education and Prevention Program (NAEPP 2007): Dry powder inhaler (refers to Asmanex Twisthaler 220 mcg strength): Children ≥12 years and Adolescents: Oral inhalation:

"Low" dose: 200 mcg/day.

"Medium" dose: 400 mcg/day.

"High" dose: >400 mcg/day.

Mild flare, exacerbation: Limited data available:

Children ≥12 years and Adolescents with mild to moderate asthma, no prior history of life-threatening asthma exacerbations, and with good self-management skills:

It is recommended to temporarily quadruple the inhaled corticosteroid dose early in the course of a mild flare to decrease the severity of an asthma exacerbation. After symptoms stabilize or after a maximum of 14 days of quadrupled dose, whichever occurs first, patients should be returned to their baseline dose (GINA 2019). Quadrupling the inhaled corticosteroid dose has been shown to decrease the severity of an asthma exacerbation in select patients. In a randomized trial of adolescents ≥16 years and adults (n=1,871), temporarily quadrupling the inhaled corticosteroid dose when asthma control began to deteriorate resulted in fewer severe asthma exacerbations (ie, less treatment with systemic glucocorticoids or unscheduled appointments for asthma) compared to patients who maintained their inhaled corticosteroid dose (McKeever 2018). No data for quadrupling the dose in patients <16 years of age has been published. Quintupling the dose of inhaled corticosteroids (fluticasone) in children 5 to 11 years of age was not shown to reduce the rate of severe exacerbations and may have been associated with adverse effects (decreased linear growth, particularly in patients <8 years of age) (GINA 2019; Jackson 2018).

Conversion from oral systemic corticosteroids to orally-inhaled corticosteroids: When using mometasone oral inhalation to help reduce or discontinue oral corticosteroid therapy, begin prednisone taper after at least 1 week of mometasone inhalation therapy; prednisone should be tapered slowly (ie, no faster than 2.5 mg/day on a weekly basis); monitor patients for signs of asthma instability and adrenal insufficiency; decrease mometasone to lowest effective dose after prednisone reduction is complete.

Administration

Asmanex HFA: Metered-dose inhaler: Shake well prior to each inhalation. Administer as 2 inhalations twice daily (morning and evening). Prime before first use and when the inhaler has not been used for >5 days by releasing 4 test sprays into the air, away from the face, shaking well before each spray. Rinse mouth with water (without swallowing) and spit after each use. Clean mouthpiece with a dry wipe after every 7 days of use.

Asmanex Twisthaler: Dry-powder inhaler: When administered once daily, administer only in the evening. Exhale fully, then place mouthpiece in mouth holding it in a horizontal position and inhale quickly and deeply. Remove inhaler and hold breath for 10 seconds if possible. Do not breathe out through the inhaler. Rinse mouth after use.

Dietary Considerations

Asmanex Twisthaler may contain lactose.

Storage

Asmanex HFA: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Do not puncture. Do not use or store near heat or open flame; never throw container into fire or incinerator. Exposure to temperatures above 120°F may cause bursting. Discard when dose counter reads “0".

Asmanex Twisthaler: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Discard when dose counter reads "00" or 45 days after opening the foil pouch, whichever comes first.

Drug Interactions

Aldesleukin: Corticosteroids may diminish the antineoplastic effect of Aldesleukin. Avoid combination

Amphotericin B: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Amphotericin B. Monitor therapy

Corticorelin: Corticosteroids may diminish the therapeutic effect of Corticorelin. Specifically, the plasma ACTH response to corticorelin may be blunted by recent or current corticosteroid therapy. Monitor therapy

Cosyntropin: Corticosteroids (Orally Inhaled) may diminish the diagnostic effect of Cosyntropin. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Corticosteroids (Orally Inhaled). Management: Orally inhaled fluticasone propionate with a strong CYP3A4 inhibitor is not recommended. Monitor therapy

Deferasirox: Corticosteroids may enhance the adverse/toxic effect of Deferasirox. Specifically, the risk for GI ulceration/irritation or GI bleeding may be increased. Monitor therapy

Desmopressin: Corticosteroids (Orally Inhaled) may enhance the hyponatremic effect of Desmopressin. Avoid combination

Hyaluronidase: Corticosteroids may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving corticosteroids (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification

Loop Diuretics: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Loop Diuretics. Monitor therapy

Loxapine: Agents to Treat Airway Disease may enhance the adverse/toxic effect of Loxapine. More specifically, the use of Agents to Treat Airway Disease is likely a marker of patients who are likely at a greater risk for experiencing significant bronchospasm from use of inhaled loxapine. Management: This is specific to the Adasuve brand of loxapine, which is an inhaled formulation. This does not apply to non-inhaled formulations of loxapine. Avoid combination

Ritodrine: Corticosteroids may enhance the adverse/toxic effect of Ritodrine. Monitor therapy

Thiazide and Thiazide-Like Diuretics: Corticosteroids (Orally Inhaled) may enhance the hypokalemic effect of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tobacco (Smoked): May diminish the therapeutic effect of Corticosteroids (Orally Inhaled). Monitor therapy

Adverse Reactions

>10%:

Central nervous system: Headache (3% to 22%), fatigue (1% to 13%), depression (11%)

Gastrointestinal: Oral candidiasis (≤22%)

Neuromuscular & skeletal: Musculoskeletal pain (8% to 22%), arthralgia (13%)

Respiratory: Sinusitis (3% to 22%), allergic rhinitis (adolescents & adults 14% to 20%; children 4%), upper respiratory tract infection (8% to 15%), pharyngitis (8% to 13%)

1% to 10%:

Central nervous system: Pain (1% to <3%)

Gastrointestinal: Abdominal pain (3% to 6%), dyspepsia (5%), nausea (3%), vomiting (1% to ≤3%), anorexia (1% to <3%), gastroenteritis (1% to <3%)

Genitourinary: Dysmenorrhea (9%), urinary tract infection (children 2%)

Hematologic & oncologic: Bruise (children 2%)

Infection: Influenza (4%), infection (1% to <3%)

Neuromuscular & skeletal: Back pain (6%), myalgia (3%)

Ophthalmic: Increased intraocular pressure (3%)

Otic: Otalgia (1% to <3%)

Respiratory: Paranasal sinus congestion (9%), nasopharyngitis (5% to 8%), bronchitis (3%), dry throat (1% to <3%), epistaxis (1% to <3%), flu-like symptoms (1% to <3%), nasal discomfort (1% to <3%), voice disorder (1% to <3%)

Miscellaneous: Fever (children 7%)

Postmarketing and/or case reports: Anaphylaxis, angioedema, blurred vision, bronchospasm, cataract, cough, dyspnea, exacerbation of asthma, glaucoma, growth retardation, hypersensitivity reaction, pruritus, skin rash, wheezing

Warnings/Precautions

Concerns related to adverse effects:

• Adrenal suppression: May cause hypercortisolism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods. HPA axis suppression may lead to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. Particular care is required when patients are transferred from systemic corticosteroids to inhaled products due to possible adrenal insufficiency or withdrawal from steroids, including an increase in allergic symptoms. Adult patients receiving ≥20 mg per day of prednisone (or equivalent) may be most susceptible. Fatalities have occurred due to adrenal insufficiency in asthmatic patients during and after transfer from systemic corticosteroids to aerosol steroids; aerosol steroids do not provide the systemic steroid needed to treat patients having trauma, surgery, or infections (particularly gastroenteritis), or other conditions with severe electrolyte loss. Select surgical patients on long-term, high-dose, inhaled corticosteroids should be given stress doses of hydrocortisone intravenously during the surgical period and the dose reduced rapidly within 24 hours after surgery (NAEPP 2007).
• Bronchospasm: Paradoxical bronchospasm that may be life-threatening may occur with use of inhaled bronchodilating agents; reaction should be distinguished from inadequate response. If paradoxical bronchospasm occurs, discontinue mometasone and institute alternative therapy.
• Hypersensitivity: Hypersensitivity reactions (eg, allergic dermatitis, anaphylaxis, angioedema, bronchospasm, flushing, pruritus, rash, urticaria) may occur; discontinue use if reaction occurs.
• Immunosuppression: Prolonged use of corticosteroids may increase the incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to vaccines. Avoid use if possible in patients with ocular herpes; active or quiescent respiratory tuberculosis; or untreated viral, fungal, or bacterial or parasitic systemic infections. Exposure to chickenpox or measles should be avoided; if the patient is exposed, prophylaxis with varicella zoster immune globulin or pooled intravenous immunoglobulin, respectively, may be indicated. If chickenpox develops, treatment with antiviral agents may be considered.
• Oral candidiasis: Local oropharyngeal Candida infections have been reported; if this occurs, treat appropriately while continuing therapy. Patients should be instructed to rinse mouth with water (without swallowing) and spit after each use.

Disease-related concerns:

• Asthma: Supplemental steroids (oral or parenteral) may be needed during stress or severe asthma attacks. Short-acting beta₂-agonist (eg, albuterol) should be used for acute symptoms and symptoms occurring between treatments. Use is contraindicated in status asthmaticus or during other acute asthma episodes requiring intensive measures.
• Bone mineral density: Use with caution in patients with major risk factors for decreased bone mineral count such as prolonged immobilization, family history of osteoporosis, or chronic use of drugs that can reduce bone mass (eg, anticonvulsants, oral corticosteroids); long-term use of inhaled corticosteroids have been associated with decreases in bone mineral density.
• Ocular disease: Use with caution in patients with cataracts and/or glaucoma; blurred vision, increased intraocular pressure, glaucoma, and cataracts have occurred with prolonged use. Consider routine eye exams in long-term users.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Pediatrics: Orally inhaled corticosteroids may cause a reduction in growth velocity in pediatric patients (~1 cm per year [range: 0.3 to 1.8 cm per year] and related to dose and duration of exposure). To minimize the systemic effects of orally inhaled corticosteroids, each patient should be titrated to the lowest effective dose. Growth should be routinely monitored in pediatric patients.

Dosage form specific issues:

• Lactose: Asmanex Twisthaler: May contain lactose; very rare anaphylactic reactions have been reported in patients with milk protein allergy.

Other warnings/precautions:

• Discontinuation of systemic corticosteroid therapy: A gradual tapering of dose may be required prior to discontinuing therapy; there have been reports of systemic corticosteroid withdrawal symptoms (eg, joint/muscle pain, lassitude, depression) when withdrawing oral inhalation therapy.
• Transfer to oral inhaler: When transferring to oral inhalation therapy from systemic corticosteroid therapy, previously suppressed allergic conditions (rhinitis, conjunctivitis, eczema, arthritis, and eosinophilic conditions) may be unmasked. Withdraw systemic corticosteroid therapy by gradually tapering the dose. Monitor lung function, beta-agonist use, asthma symptoms, and for signs and symptoms of adrenal insufficiency (eg, fatigue, lassitude, weakness, nausea/vomiting, hypotension) during withdrawal.

Monitoring Parameters

FEV₁, peak flow, and/or other pulmonary function tests; bone mineral density; growth (adolescents and children via stadiometry); signs/symptoms of HPA axis suppression/adrenal insufficiency; possible eosinophilic conditions (including eosinophilic granulomatosis with polyangiitis [formerly known as Churg-Strauss]); signs/symptoms of oral candidiasis; asthma symptoms; glaucoma/cataracts

Pregnancy

Pregnancy Considerations

Uncontrolled asthma is associated with adverse events on pregnancy (increased risk of perinatal mortality, preeclampsia, preterm birth, low birth weight infants). Poorly controlled asthma or asthma exacerbations may have a greater fetal/maternal risk than what is associated with appropriately used asthma medications (ACOG 2008; GINA 2018).

Inhaled corticosteroids are recommended for the treatment of asthma during pregnancy (ACOG 2008; GINA 2018; Namazy 2016). Pregnant females adequately controlled on mometasone for asthma may continue therapy; if initiating treatment during pregnancy, use of an agent with more data in pregnant females may be preferred (Namazy 2016).

Patient Education

What is this drug used for?

• It is used to treat asthma. Talk with your doctor.

Frequently reported side effects of this drug

• Headache
• Stuffy nose
• Nausea
• Sore throat
• Abdominal pain
• Muscle pain
• Back pain

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

• Infection
• Adrenal gland problems like severe nausea, vomiting, severe dizziness, passing out, muscle weakness, severe fatigue, mood changes, lack of appetite, or weight loss
• Severe fatigue
• Irritability
• Tremors
• Fast heartbeat
• Confusion
• Dizziness
• Sweating
• Thrush
• Menstrual pain
• Severe loss of strength and energy
• Bone pain
• Joint pain
• Flu-like signs
• Flushing
• Vision changes
• Difficulty breathing
• Wheezing
• Cough
• Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.