DrugindexOnline^{2nd edition}

Pronouncation: (moe-MET-a-sone FYU-roh-ate)
Class: Corticosteroid

Trade Names:
Asmanex Twisthaler
- Powder for inhalation 220 mcg/actuation

Trade Names:
Elocon
- Ointment 0.1%
- Cream 0.1%
- Lotion 0.1%

Trade Names:
Mometasone Furoate
- Topical solution 0.1%

Trade Names:
Nasonex
- Spray 50 mcg/spray (as monohydrate)

Elocom (Canada)

Mechanism of Action

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 body's immune response.

Pharmacokinetics

Absorption

Following an inhaled single 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 the time to C _max ranged from about 1 to 2.5 hr.

Distribution

Vd is 152 L.

Metabolism

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

Elimination

Terminal t _½ is about 5 hr. Excretion up to 7 days is primarily in the feces (74%) and, to a lesser amount, in the urine (8%).

Indications and Usage

Topical

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

Intranasal

Treatment of nasal symptoms of seasonal allergic and perennial allergic rhinitis; prophylaxis of nasal symptoms of seasonal allergic rhinitis; treatment of nasal polyps.

Oral inhalation

Maintenance treatment of asthma as prophylactic therapy; in asthma patients requiring oral corticosteroid therapy, adding Asmanex Twisthaler may reduce or eliminate the need for oral corticosteroids.

Contraindications

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

Dosage and Administration

Topical cream or ointment
Adults and children 2 yr of age and older

Apply a thin film to affected skin areas once daily.

Topical lotion
Adults and children 12 yr of age and older

Apply a few drops to affected skin areas once daily and massage lightly until it disappears.

Intranasal
Allergic Rhinitis Adults and children 12 yr of age and older

2 sprays in each nostril once daily (total daily dose, 200 mcg). Prophylaxis with 200 mcg/day is recommended 2 to 4 wk prior to the anticipated start of pollen season for patients with a known seasonal allergen that precipitates nasal symptoms.

Children 2 to 11 yr of age

1 spray in each nostril once daily (total daily dose, 100 mcg).

Nasal Polyps Adults

2 sprays in each nostril bid (total daily dose, 400 mcg).

Oral inhalation
Adults and children 12 yr of age and older

Recommended starting dosage when previous therapy was bronchodilators alone or inhaled corticosteroids is 220 mcg daily in the evening (max, 440 mcg/day). When previous therapy was oral corticosteroids, recommended starting dosage is 440 mcg bid (max, 880 mcg/day). When 220 mcg is administered once daily, Asmanex Twisthaler should only be taken in the evening. The 440 mcg/day dose may be administered as 440 mcg once daily or in divided dosages of 220 mcg bid.

Storage/Stability

Intranasal

Store at 77°F; excursions permitted to 59° to 86°F. Protect from light.

Oral solution

Store in dry place at 77°F; excursions permitted to 59° to 86°F. Discard inhaler 45 days after opening the foil pouch or when dose counter reads 00, whichever comes first.

Topical

Store between 36° and 77°F.

Drug Interactions

Ketoconazole

Mometasone furoate plasma levels may be increased.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Intranasal

Headache (at least 5%).

Oral Inhalation

Headache (at least 3%); insomnia (1% to 3%).

Dermatologic

Topical

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

Oral inhalation

Insect bite, skin irritation (1% to 3%).

EENT

Cataracts; glaucoma.

Intranasal

Pharyngitis (at least 5%); conjunctivitis, earache, nasal irritation, otitis media, rhinitis (2% to 5%); angioedema, nasal burning/irritation, nasal septal perforation (postmarketing).

Oral inhalation

Pharyngitis (at least 3%); dry throat, earache, nasal irritation (1% to 3%).

GI

Intranasal

Vomiting (at least 5%); diarrhea, dysphagia, nausea (2% to 5%).

Oral inhalation

Abdominal pain, dyspepsia, nausea, oral candidiasis (at least 3%); anorexia, flatulence, gastroenteritis, vomiting (1% to 3%).

Genitourinary

Intranasal

Dysmenorrhea (at least 5%).

Oral inhalation

Dysmenorrhea (at least 3%); menstrual disorder, UTI (1% to 3%).

Musculoskeletal

Intranasal

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

Oral inhalation

Back pain, musculoskeletal pain, myalgia (at least 3%).

Respiratory

Intranasal

Coughing, epistaxis, sinusitis, upper respiratory tract infection (at least 5%); asthma, bronchitis, wheezing (2% to 5%).

Oral inhalation

Sinusitis, upper respiratory tract infection (at least 3%); dysphonia, epistaxis, respiratory disorder (1% to 3%).

Miscellaneous

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

Intranasal

Viral infection (at least 5%); chest pain, flu-like symptoms (2% to 5%); anaphylaxis (postmarketing).

Oral inhalation

Allergic rhinitis (at least 3%); accidental injury, fatigue, flu-like symptoms, infection, pain, postprocedure pain (1% to 3%).

Precautions

Monitor Because nasal and inhaled corticosteroids have been associated with glaucoma and cataracts, patients with changes in vision and a history of glaucoma and/or cataracts should be followed closely.

Pregnancy

Category C .

Lactation

Undetermined.

Children

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

Intranasal

Safety and efficacy in children younger than 2 yr of age with allergic rhinitis and in children younger than 18 yr of age with nasal polyps have not been established.

Ointment, intranasal, cream

Safety and efficacy not established in children younger than 2 yr of age.

Oral inhalation, lotion

Safety and efficacy not established in children younger than 12 yr of age.

Special Risk Patients

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

Adrenal insufficiency

Deaths caused by adrenal insufficiency have occurred in patients during and after transfer from systemic corticosteroids to less systemically available inhaled corticosteroids.

Allergic conditions

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

Infections

People on drugs that suppress the immune system are more susceptible to infections (eg, chickenpox, measles).

Occlusive therapy

Do not use with mometasone treatment regimens.

Wound healing

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

Overdosage

Symptoms

Cushing syndrome, HPA suppression.

Patient Information

• Explain name, dose, action, and potential adverse reactions of drug.
• Obtain patient history, including drug history and any known allergies.
• Advise women to notify health care provider if pregnant, planning to become pregnant, or breast-feeding.
• Caution patient not to take any prescription or OTC drugs, herbal preparations, or dietary supplements without consulting health care provider.
• Advise patient that follow-up visits to monitor response to treatment may be necessary and to keep appointments.

• Nasal spray
• Advise patient to read and follow the Patient's Instructions for Use carefully.
• Advise patient that medication is used once daily (nasal polyps, twice daily use) 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 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 and, if exposed, to seek medical advice without delay.

• Oral inhalation
• Advise patient to review Patient's Instructions for Use before using the first time and with each refill.
• 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.
• Instruct patient to carry a medical identification card if he or she experiences 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, or 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.

• 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 pediatric patient 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, worsens, or if application site reactions (eg, burning, itching, redness, stinging) develop.
• Advise patient that therapy is usually discontinued when control has been achieved.