Mometasone Furoate

Pronunciation: (moe-MET-a-sone FUR-oh-ate)
Class: Corticosteroid

Trade Names

Asmanex Twisthaler
- Powder, inhalation 110 mcg/actuation
- Powder, inhalation 220 mcg/actuation

Elocon
- Cream, topical 0.1%
- Lotion, topical 0.1%
- Ointment, topical 0.1%

Mometasone Furoate
- Solution, topical 0.1%

Nasonex
- Spray, intranasal 0.05% (50 mcg/spray)

Elocom (Canada)
PMS-Mometasone (Canada)
ratio-Mometasone (Canada)
Taro-Mometasone (Canada)

Pharmacology

Medium-potency topical corticosteroid that depresses formation, release, and activity of endogenous mediators of inflammation, including prostaglandins, kinins, histamine, liposomal enzymes, and complement system; modifies the body's immune response.

Pharmacokinetics

Absorption

Following a single inhaled 400 mcg dose, plasma concentrations are frequently below the lower limit of quantitation (50 pcg/mL). Compared with IV administration, bioavailability of an inhaled dose is less than 1%. Mean C _max ranged from 94 to 114 pcg/mL and T _max ranged from approximately 1 to 2.5 h.

Distribution

Vd is 152 L. The in vitro protein binding was 98% to 99%.

Metabolism

Primarily and extensively metabolized in the liver by the CYP3A4 isozyme to multiple metabolites.

Elimination

Terminal half-life is approximately 5 h following IV dosing. Excretion up to 7 days is primarily in the feces (74%) and, to a lesser amount, in the urine (8%).

Special Populations

Renal Function Impairment

Effects on mometasone pharmacokinetics have not been adequately studied.

Hepatic Function Impairment

C _max increases with the severity of hepatic impairment; however, detectable levels are not often achieved.

Children

Pharmacokinetics have not been studied in children.

Gender

Effects on mometasone pharmacokinetics have not been adequately studied.

Race

Effects on mometasone pharmacokinetics have not been adequately studied.

Indications and Usage

Topical

Relief of inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.

Intranasal

Treatment of nasal symptoms of seasonal and perennial allergic rhinitis; prophylaxis of nasal symptoms of seasonal allergic rhinitis; relief of nasal congestion associated with seasonal allergic rhinitis; treatment of nasal polyps.

Oral inhalation

Maintenance treatment of asthma as prophylactic therapy in patients 4 y and older.

Contraindications

Primary treatment of status asthmaticus or other acute episodes of asthma in which intensive measures are required, hypersensitivity to milk proteins ( Asmanex Twisthaler ); hypersensitivity to any component of the product.

Dosage and Administration

Allergic rhinitis
Adults and Children 12 y and older

Intranasal 2 sprays in each nostril once daily.

Children 2 to 11 y of age

Intranasal 1 spray in each nostril once daily.

Asthma
Adults and Children 12 y and older

Oral inhalation Initially, 220 mcg once daily in the evening in patients who previously received bronchodilators alone or inhaled corticosteroids (max, 440 mcg/day); 440 mcg twice daily in patients who previously received oral corticosteroids (max, 880 mcg/day). In patients who do not adequately respond to the initial dose after 2 wk of therapy, higher doses may provide additional control. Titrate to lowest effective dose once asthma stability is achieved.

Children 4 to 11 y of age

Oral inhalation 110 mcg once daily in the evening (max, 110 mcg/day).

Corticosteroid-responsive dermatoses
Cream and ointment Adults and Children 2 y and older

Topical Apply a thin film to the affected areas once daily. Discontinue when control is achieved. If no improvement is seen within 2 wk, reassess diagnosis.

Lotion Adults and Children 12 y and older

Topical Apply a few drops to the affected area once daily and massage lightly until it disappears.

Nasal polyps
Adults

Intranasal 2 sprays in each nostril twice daily. A dose of 2 sprays in each nostril once daily is also effective in some patients.

General Advice

• To minimize the systemic effects of intranasal corticosteroids, including mometasone, titrate each patient to the lowest effective dose.

• Intranasal
• Prophylaxis for seasonal allergic rhinitis with mometasone is recommended 2 to 4 wk prior to the anticipated start of the pollen season.
• Prior to initial use, the pump must be primed by actuating 10 times, or until a fine spray appears. The pump may be stored unused for up to 1 wk without repriming. If unused for more than 1 wk, reprime by actuating 2 times, or until a fine spray appears. Shake well before each use.

• Oral inhalation
• For oral inhalation only. Inhale rapidly and deeply.
• Max benefit may not be achieved for 1 to 2 wk or longer after initiation of treatment.
• The 440 mcg dose may be administered in divided dosages of 220 mcg twice daily, or as 440 mcg once daily.
• When administered once daily, mometasone should only be taken in the evening.
• For patients currently receiving long-term oral corticosteroid therapy, reduce the prednisone dosage no faster than 2.5 mg/day on a weekly basis, beginning after at least 1 wk of mometasone.
• Rinse the mouth with water after inhalation.

Storage/Stability

Topical

Store between 36° and 77°F.

Intranasal

Store between 59° and 86°F. Protect from light. When removed from its cardboard container, avoid prolonged exposure of the product to direct light.

Oral inhalation

Store in a dry place between 59° and 86°F. Discard inhaler 45 days after opening the foil pouch or when the dose counter reads “00,” whichever comes first.

Drug Interactions

Strong CYP3A4 inhibitors (eg, ketoconazole)

Mometasone plasma levels may be increased. Observe the clinical response and adjust the mometasone dose as needed.

Adverse Reactions

CNS

Intranasal

Headache (26%); sinus headache (1%).

Oral inhalation

Headache (22%); fatigue (13%); depression (11%).

Dermatologic

Topical

Acneiform eruptions, burning, folliculitis, furunculosis, itching, rosacea, skin atrophy, stinging (2% to 5%).

Oral inhalation

Bruise (2%).

EENT

Cataracts, glaucoma.

Intranasal

Epistaxis (13%); pharyngitis (12%); conjunctivitis, earache, nasal irritation, otitis media, rhinitis (2% to 4%); disturbances in taste and smell, nasal burning or irritation, nasal candidiasis, nasal septal perforation, nasal ulcers (postmarketing).

Oral inhalation

Allergic rhinitis (20%); pharyngitis (13%); dry throat, earache (1% to less than 3%).

GI

Intranasal

Vomiting (5%); diarrhea, dyspepsia, nausea (2% to 4%).

Oral inhalation

Oral candidiasis (22%); abdominal pain (6%); dyspepsia (5%); nausea, vomiting (3%); anorexia, gastroenteritis (1% to less than 3%).

Genitourinary

Intranasal

Dysmenorrhea (5%).

Oral inhalation

Dysmenorrhea (9%); UTI (2%).

Musculoskeletal

Intranasal

Musculoskeletal pain (5%); arthralgia, myalgia (2% to 4%).

Oral inhalation

Musculoskeletal pain (22%); arthralgia (13%); back pain (6%); myalgia (3%).

Respiratory

Intranasal

Epistaxis (13%); coughing, upper respiratory tract infection (7%); sinusitis (5%); asthma, bronchitis, wheezing (2% to 4%); sinus headache (1%).

Oral inhalation

Sinusitis (22%); upper respiratory tract infection (15%); sinus congestion (9%); dysphonia, epistaxis, nasal irritation, respiratory disorder (1% to less than 3%); asthma aggravation, which may include cough, dyspnea, wheezing, and bronchospasm (postmarketing).

Miscellaneous

Systemic absorption may produce reversible hypothalamic-pituitary-adrenal (HPA) axis suppression, manifestations of Cushing syndrome, hyperglycemia, and glycosuria.

Intranasal

Viral infection (14%); chest pain, flu-like symptoms, skin trauma (2% to 4%); oral candidiasis; anaphylaxis, angioedema (postmarketing).

Oral inhalation

Fever (7%); flu-like symptoms, infection, pain (1% to less than 3%); immediate and delayed hypersensitivity reactions, including rash, pruritus, angioedema, and anaphylactic reaction (postmarketing).

Precautions

Monitor Oral inhalation Closely follow patients with changes in vision or a history of glaucoma, increased IOP, and/or cataracts. Monitor growth (eg, via stadiometry) of children on prolonged therapy. Monitor asthma signs and symptoms, lung function (forced expiratory volume at 1 sec or peak expiratory flow) and beta-agonist use, and observe patients for symptoms of adrenal insufficiency, such as fatigue, lassitude, weakness, nausea, vomiting, and hypotension. Monitor patients with major risk factors for decreased bone mineral content (eg, prolonged immobilization, family history of osteoporosis). Intranasal Periodically examine patients using mometasone over several months or longer for possible changes in the nasal mucosa.

Pregnancy

Category C .

Lactation

Undetermined. Because other corticosteroids are excreted in human milk, use with caution.

Children

May be more susceptible to corticosteroid-induced HPA axis suppression and Cushing syndrome.

Oral inhalation

Safety and efficacy not established in children younger than 4 y.

Intranasal

Safety and efficacy in children younger than 2 y for treatment of allergic rhinitis (children younger than 12 y for prophylaxis) and in children younger than 18 y with nasal polyps have not been established.

Lotion, oral inhalation

Safety and efficacy not established in children younger than 12 y.

Ointment, cream

Safety and efficacy not established in children younger than 2 y.

Hypersensitivity

Hypersensitivity reactions, including instances of acute wheezing, may occur after the intranasal administration, and rash, pruritus, angioedema, and anaphylactic reactions have been reported with oral inhalation use of mometasone. Discontinue if such a reaction occurs.

Special Risk Patients

Use with caution, if at all, in patients with active or quiescent tuberculosis infection of the respiratory tract, with ocular herpes simplex, or with untreated fungal, bacterial, or systemic viral infections.

Acute asthma

Oral inhalation is not indicated for rapid relief of bronchospasm or other acute asthma episodes.

Adrenal suppression

Prolonged therapy may lead to HPA suppression.

Allergic conditions

Transfer of patients from systemic corticosteroids may unmask allergic conditions previously suppressed (eg, conjunctivitis, eczema, rhinitis).

Bone mineral density

Decreases in bone mineral density (BMD) can occur with long-term administration of corticosteroids, including inhaled corticosteroids.

Bronchospasm

Bronchospasm may occur with immediate increase in wheezing following dosing, requiring immediate treatment with a fast-acting inhaled bronchodilator.

Immunosuppression

Immunosuppressed patients may be more susceptible to infections (eg, chickenpox, measles) than healthy individuals. Do not administer live virus vaccines while patients are on therapy.

Local effects

Localized infections of the nose or mouth and pharynx with Candida albicans can occur.

Nasal septum perforation

Rare instances of nasal septum perforation have been reported following intranasal use of corticosteroids.

Occlusive therapy

Do not use with mometasone treatment regimens.

Ocular effects

Nasal and inhaled corticosteroid use may result in the development of glaucoma and/or cataracts.

Transfer from systemic corticosteroids

Transfer from oral corticosteroids to inhaled corticosteroids has resulted in death caused by adrenal insufficiency related to a lower systemic bioavailability. After withdrawal from systemic corticosteroids, a number of months are needed for recovery of HPA function.

Wound healing

Because of the inhibitory effect of corticosteroids on wound healing, do not give patients experiencing recent nasal sputum ulcers, nasal surgery, or nasal trauma a nasal corticosteroid until healing has occurred.

Overdosage

Symptoms

Cushing syndrome, HPA suppression.

Patient Information

• Nasal spray
• Advise patient to read and follow the patient information leaflet.
• Advise patient that medication is used once daily (nasal polyps, twice daily) to prevent or control nasal symptoms, and is not intended to be used on an as-needed basis.
• Instruct patient that pump must be primed before using for the first time by actuating 10 times or until a fine mist appears. Remind patient that further priming is not necessary unless medication has not been used for more than 1 wk, in which case, repriming with 2 actuations or until fine mist appears is advised.
• Instruct patient to shake well before each use.
• Instruct patient on proper administration technique: blow nose gently to clear nasal passages; if congested, use a topical nasal decongestant 5 to 10 min before medication administration; use saline lavage if necessary to remove secretions; clean outer portion of nose with damp tissue; insert nozzle into nostril; while using finger to keep other nostril closed, inhale while activating the pump; repeat with other nostril.
• Caution patient not to spray directly into the eyes, mouth, or nasal septum.
• Inform patient that symptoms should begin to improve within 2 days of starting therapy, but may take up to 2 wk before max benefit is noted. Advise patient to contact health care provider if symptoms do not improve or if they worsen while using this medication, or if nasal irritation or nosebleed occurs.
• Warn patient that increasing the number of sprays or frequency of use does not increase the efficacy of the drug but may increase the incidence and severity of adverse reactions.
• Instruct patient to use with caution if sores develop or injuries occur in nasal passages. Drug may prevent or slow proper healing.
• Advise patient to discard bottle when labeled number of sprays have been used, even if bottle is not completely empty.
• If patient is being converted from oral steroids to nasal steroids, review signs and symptoms of adrenal insufficiency that may occur days or weeks after conversion is complete.
• Warn patients taking immunosuppressant doses of corticosteroids to avoid exposure to measles and chickenpox. If exposed, advise patient to seek medical advice without delay.

• Oral inhalation
• Review proper inhaler preparation and administration technique. Have patient demonstrate techniques to ensure ability to prepare and use the delivery system effectively.
• Warn patient that drug is an asthma controller and is not to be used to treat an acute asthma attack. Rescue medication (bronchodilator) must be used to obtain rapid relief of asthma symptoms.
• Instruct patient not to stop the medication once symptoms have been controlled. Continued daily use is necessary to control symptoms.
• Instruct patient to record the date of pouch opening on the cap label and to discard the inhaler 45 days after opening the foil pouch or when the dose counter reads “00,” whichever comes first.
• Advise patient to rinse mouth thoroughly with water after using the oral inhalation medication.
• Instruct patient to carry medical identification (eg, card, bracelet) if they experience acute, severe asthma attacks requiring rapid systemic treatment.
• Advise patient to report the following symptoms to health care provider: cough, sore throat or mouth, voice change, worsening asthma symptoms (increasing need for bronchodilator).
• If patient is being converted from oral steroids to nasal steroids, review signs and symptoms of adrenal insufficiency that may occur days or weeks after conversion is complete.
• Warn patients taking immunosuppressant doses of corticosteroids to avoid exposure to measles and chickenpox. If exposed, advise patient to seek medical advice without delay.
• Advise patients that localized infections with Candida albicans may occur in the mouth and pharynx in some patients and that therapy may need to be temporarily interrupted under close medical supervision.
• Advise patients who are at an increased risk for decreased BMD that the use of corticosteroids may pose an additional risk and should be monitored.
• Inform patients that orally inhaled corticosteroids may cause a reduction in growth velocity when administered to children.
• Warn patients that hypersensitivity reactions, including rash, pruritus, angioedema, and anaphylactic reaction, have been reported and to discontinue use if such reactions occur.
• Inform patients that mometasone contains small amounts of lactose, which contains trace levels of milk proteins, and that anaphylactic reactions may occur in patients with milk protein allergy.

• Ointment, cream, and lotion
• Advise patient to apply medication once daily as directed by health care provider.
• Caution patient not to apply in greater quantity or more frequently than prescribed by health care provider.
• Teach patient or caregiver proper technique for applying ointment, cream, or lotion: wash or soak the affected area before applying medication, unless it irritates the affected area(s); wash hands; apply sufficient ointment, cream, or lotion to cover affected area(s) sparingly; gently massage into skin; wash hands after applying mometasone.
• Caution caregiver of a child not to use mometasone to treat diaper dermatitis.
• Caution patient not to bandage, cover, or wrap treated skin areas, or use cosmetics or other skin products over treated areas unless advised by health care provider.
• Advise patient who has been advised to use an occlusive dressing to do the following after applying medication to affected area(s): cover the area with plastic wrap (eg, Saran Wrap , Handi-Wrap ). The plastic may be held in place with a gauze or elastic bandage or adhesive tape on the normal skin beside the treated area. Advise patient that instead of using plastic wrap, plastic gloves may be used for the hands, plastic bags for the feet, or a shower cap for the scalp; leave the plastic wrapping or covering in place as long as instructed by health care provider. Instruct patient to cleanse the skin and reapply the medication each time a new plastic wrapping is applied.
• Advise patient that if an application is missed, to apply it as soon as remembered and then continue on regular schedule. If it is almost time for the next application, instruct patient to skip the application and continue on regular schedule. Caution patient not to apply double doses.
• Caution patient not to apply to face, underarms, or groin area unless directed by health care provider.
• Caution patient to avoid contact with the eyes. Advise patient that if medication does come into contact with the eyes, to wash them with large amounts of cool water and to contact health care provider if eye irritation occurs.
• Advise patient that symptoms should begin to improve soon after starting treatment and to notify health care provider if condition does not improve or worsens, or if application-site reactions (eg, burning, itching, redness, stinging) develop.
• Advise patient that therapy is usually discontinued when control has been achieved.

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