Mometasone Furoate / Formoterol Fumarate

Pronunciation: moe-MET-a-sone FUR-oh-ate/for-MOE-ter-ol fue-MA-rate
Class: Respiratory inhalant combination

Trade Names

Dulera 100/5
- Aerosol, inhalation mometasone 100 mcg/formoterol 5 mcg per actuation

Dulera 200/5
- Aerosol, inhalation mometasone 200 mcg/formoterol 5 mcg per actuation

Pharmacology

Mometasone is an anti-inflammatory corticosteroid that exhibits potent anti-inflammatory activity. Formoterol is a long-acting selective beta-2 adrenergic agonist (beta-2 agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator.

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Indications and Usage

Treatment of asthma in patients 12 y of age and older.

Contraindications

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

Dosage and Administration

Adults and Children 12 y of age and older

Oral inhalation Recommended starting dose is 2 inhalations of mometasone/formoterol (100/5 mcg or 200/5 mcg) twice daily (morning and evening), depending upon prior therapy. Max daily recommended dosage is mometasone/formoterol (800/20 mcg) given as 2 inhalations of 200/5 mcg twice daily approximately 12 h apart.

General Advice

  • Do not use more than twice daily or for more than 2 inhalations.
  • Rinse mouth with water without swallowing after inhalation.
  • If symptoms arise between doses, an inhaled, short-acting beta-2 agonist should be taken for immediate relief.
  • Shake well before using.
  • Before using for the first time, prime the inhaler by releasing 4 test sprays into the air away from the face, shaking well before each spray. Prime the inhaler again by shaking well before each spray and releasing 4 test sprays if inhaler is not used for more than 5 days.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Adrenergic agents

Use with caution because the sympathomimetic effects of formoterol may be potentiated.

Beta-blockers (eg, propranolol)

Beta-blockers and formoterol may inhibit the effect of each other. Beta-blockers inhibit the therapeutic effects of formoterol and may produce bronchospasm in patients with asthma or COPD. In these patients, consider a cardioselective beta-blocker, but administer with caution.

Corticosteroids (eg, prednisone)

Acute hypokalemic and hyperglycemic effects of formoterol may be increased by corticosteroids. Use with caution. Additional clinical and blood chemistry monitoring may be needed.

CYP3A4 inhibitors (eg, atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin)

Mometasone plasma concentrations may be elevated, increasing the pharmacologic effect and risk of adverse reactions. Use with caution.

Drugs that prolong the QT interval (eg, antiarrhythmic agents [eg, amiodarone, bretylium, disopyramide, dofetilide, procainamide, quinidine, sotalol], cisapride, mesoridazine, pimozide, probucol, thioridazine, ziprasidone)

Drugs that prolong the QT interval may potentiate formoterol CV effects, increasing the risk of ventricular arrhythmias. Coadminister with caution and use with caution within 2 wk of discontinuing such agents. If CV symptoms occur, it may be necessary to discontinue mometasone/formoterol therapy.

Linezolid

Coadministration of linezolid and formoterol may result in adverse CV effects characterized by hypertension. Use caution with or within 2 wk of coadministration of linezolid and formoterol. Monitor BP.

Loop diuretics (eg, furosemide), thiazide diuretics (eg, hydrochlorothiazide)

The hypokalemic effect of formoterol may be potentiated. The ECG changes and/or hypokalemia that may result from loop or thiazide diuretics can be acutely worsened by formoterol, especially if the recommended dose of formoterol is exceeded. Coadminister with caution.

MAOIs (eg, phenelzine), tricyclic antidepressants (eg, amitriptyline)

MAOIs may potentiate the CV effects of formoterol. Coadminister with caution and use with caution within 2 wk of discontinuing such agents. If CV symptoms occur, it may be necessary to discontinue mometasone/formoterol therapy.

Methylxanthines (eg, aminophylline, theophylline)

Concurrent treatment with methylxanthines may potentiate the hypokalemic effects of formoterol. Monitor serum potassium.

Adverse Reactions

CNS

Headache (5%).

EENT

Dysphonia, nasopharyngitis (5%).

Respiratory

Sinusitis (3%).

Miscellaneous

Oral candidiasis (1%).

Precautions

Warnings

Long-acting beta-2 adrenergic agonists, such as formoterol, may increase the risk of asthma-related death. Therefore, only use for patients not adequately controlled on a long-term asthma control medication, such as an inhaled corticosteroid, or for patients whose disease severity clearly warrants initiation of treatment with both an inhaled corticosteroid and a long-acting beta-2 adrenergic agonist. Once asthma control is achieved and maintained, assess the patient at regular intervals, step down therapy (if possible without loss of asthma control), and maintain the patient on a long-term asthma control medication, such as an inhaled corticosteroid. Do not use mometasone/formoterol for patients whose asthma is adequately controlled on low- or medium-dose inhaled corticosteroids.


Monitor

Monitor for increasing use of inhaled, short-acting beta-2 agonist, which may indicate deterioration of asthma.

Observe patients for evidence of systemic corticosteroid effects. Closely monitor patients with a change in vision or with a history of increased IOP, glaucoma, and/or cataracts. Monitor bone mineral density (BMD) in patients with major risk factors for decreased bone mineral content, family history of osteoporosis, or long-term use of drugs that can reduce bone mass (eg, anticonvulsants, corticosteroids).

During withdrawal of systemic corticosteroids, carefully monitor lung function, beta-agonist use, and asthma symptoms.

Monitor the growth of children receiving mometasone/formoterol routinely.


Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established in children younger than 12 y of age. May cause reduction in growth velocity when administered to children.

Elderly

Use with caution in elderly patients who have concomitant CV disease that could be adversely affected by beta-2 agonists.

Hypersensitivity

Immediate hypersensitivity reactions, such as urticaria, flushing, allergic dermatitis, and bronchospasm, may occur.

Hepatic Function

Concentrations of mometasone appear to increase with severity of hepatic impairment.

Special Risk Patients

Use with caution in patients with CV disorders, especially coronary insufficiency, cardiac arrhythmias, hypertension, convulsive disorders, or thyrotoxicosis.

Acute bronchospasm

Not indicated for the relief of acute bronchospasm.

Adrenal suppression

Adrenal suppression (including adrenal crisis) and hypercorticism may appear in a small number of patients.

Deterioration of disease

Do not initiate treatment in patients during rapidly deteriorating or potentially life-threatening episodes of asthma or COPD. Do not use as rescue treatment of acute episodes of bronchospasm.

Excessive use

CV effects and fatalities have been reported with excessive use of inhaled sympathomimetic agents.

Hyperglycemia and hypokalemia

Changes in blood glucose and/or serum potassium may occur.

Immunosuppression

Patients receiving immunosuppressive agents are more susceptible to infections than healthy individuals. If patient is exposed to measles or chickenpox, appropriate prophylaxis and treatment may be warranted.

Inhalation-induced bronchospasm

Life-threatening inhalation-induced bronchospasm with an immediate increase in wheezing may occur after dosing. Treat immediately with an inhaled, short-acting inhaled bronchodilator and discontinue use of mometasone/formoterol.

Metabolic effects

Long-term use of orally inhaled corticosteroids may affect normal bone metabolism, resulting in loss of BMD.

Ophthalmic effects

Glaucoma, increased IOP, and cataracts have been reported following the long-term use of corticosteroids, including mometasone.

Oropharyngeal candidiasis

Localized Candida albicans infections occurred in the mouth and pharynx.

Systemic corticosteroids

Transferring patients from systemic corticosteroid therapy to inhaled corticosteroids may unmask conditions previously suppressed by systemic corticosteroid therapy (eg, arthritis, eczema). Wean patients requiring systemic corticosteroids slowly from systemic corticosteroid use after transferring to mometasone/formoterol.

Overdosage

Symptoms

Mometasone

Hypercorticism.

Formoterol

Angina, arrhythmias, cardiac arrest, death, dizziness, dry mouth, fatigue, headache, hyperglycemia, hypertension, hypokalemia, hypotension, insomnia, malaise, metabolic acidosis, muscle cramps, nausea, nervousness, palpitation, seizures, tachycardia, tremor.

Patient Information

  • Inform patients that formoterol increases the risk of asthma-related death and may increase the risk of asthma-related hospitalizations in children and adolescents.
  • Advise patients that this medicine is not indicated to relieve acute asthma symptoms and not to use extra doses for that purpose.
  • Instruct patient to notify health care provider immediately if they experience decreasing effectiveness, need for more inhalations than usual, a decrease in lung function as outlined by the health care provider, or a marked change in symptoms.
  • Instruct patient to use exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
  • Advise patients not to use other long-acting beta-2 agonists when they are prescribed mometasone/formoterol.
  • Warn patient to avoid exposure to chickenpox or measles and to notify health care provider immediately if exposed. Inform patients of the potential worsening of existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex.
  • Advise patients that localized infections with C. albicans may occur in the mouth and pharynx of some patients. Instruct patients to rinse the mouth after inhalation.
  • Advise patients that medication may cause systemic corticosteroid effects of hypercorticism and adrenal suppression. Instruct patients that deaths due to adrenal insufficiency have occurred during and after transfer from systemic corticosteroids. Instruct patients to taper slowly from systemic corticosteroids if transferring to mometasone/formoterol.
  • Advise patients who are at an increased risk of decreased BMD that the use of corticosteroids may pose an additional risk and that they should be monitored and, when appropriate, be treated for this condition.
  • Inform patients that orally inhaled corticosteroids, including mometasone, may cause a reduction in growth velocity when administered to children.
  • Long-term use of inhaled corticosteroids may increase the risk of some eye problems (eg, glaucoma, cataracts); advise patients to consider regular eye examinations.
  • Inform patients that treatment with beta-2 agonists may lead to adverse events, such as palpitations, chest pain, rapid heart rate, tremor, or nervousness.

Copyright © 2009 Wolters Kluwer Health.

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