Asmanex

Generic Name: Mometasone Furoate
Class: Adrenals
VA Class: RE101
Chemical Name: (11β,16α) - 9,21 - Dichloro - 17 - [(2 - furanylcarbonyl)oxy] - 11 - hydroxy - 16 - methyl - pregna - 1,4 - diene - 3,20 - dione
Molecular Formula: C27H30Cl2O6
CAS Number: 83919-23-7

Introduction

Synthetic nonfluorinated glucocorticoid.1 2 4

Uses for Asmanex

Asthma

Long-term prevention of bronchospasm in patients with asthma.1 2

Slideshow: View Frightful (But Dead Serious) Drug Side Effects

In corticosteroid-dependent patients, may permit a substantial reduction in the daily maintenance dosage or discontinuance of the systemic corticosteroid.1 6

Do not use for rapid relief of bronchospasm.1 2 8

Asmanex Dosage and Administration

General

  • Adjust dosage carefully according to individual requirements and response.1

  • After a satisfactory response is obtained, decrease dosage gradually to the lowest dosage that maintains an adequate clinical response.1 Achieve the lowest effective dosage, particularly in children, since inhaled corticosteroids have the potential to affect growth. (See Pediatric Use under Cautions.)1

  • Base initial and maximum dosages in adults and children ≥12 years of age on previous asthma therapy.1

Conversion to Orally Inhaled Therapy in Patients Receiving Systemic Corticosteroids

  • When switching from systemic corticosteroids to orally inhaled mometasone furoate, asthma should be reasonably stable before initiating treatment with oral inhalation.13 14

  • Initially, administer oral inhalation concurrently with the maintenance dosage of the systemic corticosteroid.1 After at least 1 week, gradually withdraw the systemic corticosteroid.1

  • Decrements usually should not exceed 2.5 mg daily of prednisone (or its equivalent) each week in patients receiving the oral inhalation.1 Once oral corticosteroids are discontinued and symptoms of asthma have been controlled, titrate the dosage to the lowest effective level.1

  • Death has occurred in some individuals in whom systemic corticosteroids were withdrawn too rapidly.1 (See Withdrawal of Systemic Corticosteroid Therapy under Cautions.)

Administration

Oral Inhalation

Administer by oral inhalation using the Twisthaler breath-actuated dry powder inhalation device.1 2 8

When administered once daily, use at the same time each day, preferably in the evening for optimal efficacy.1 2 5

Removal of the cap of the device (by twisting in a counterclockwise direction) releases a single 220-mcg dose of drug from the drug storage unit into the inhalation channel, making the dose available for administration via inhalation through the mouthpiece.1 8 A dose counter will decrement by 1 each time the cap is removed.8

Remove the cap with the inhaler in an upright position.1 Before inhaling the dose, exhale as completely as possible, but not into the Twisthaler device.1 8 Place the mouthpiece of the inhaler between the lips and inhale quickly and deeply through the inhaler.8 Do not cover the ventilation holes on either side of the inhaler while inhaling the dose.8 Remove the inhaler from the mouth, hold breath for about 10 seconds, then exhale slowly.8 Do not take extra doses despite not being able to taste, smell, or feel the released powder, unless otherwise instructed by a clinician.8

After inhalation, rinse mouth to minimize potential systemic or local adverse effects.1 8 Wipe the mouthpiece dry with a dry cloth or tissue.1 8 Close and reload the Twisthaler device for the next dose by twisting the cap in a clockwise direction until a click is heard.1 8

Do not wash the inhaler; store in a dry place.8 Discard the inhaler when every inhalation has been used (when the dose indicator reads “00”) or 45 days after removal from its foil overwrap pouch, whichever comes first.1 8

Dosage

Available as mometasone furoate; dosage expressed in terms of the salt.1

Dose of mometasone furoate administered as an oral inhalation powder is expressed as the nominal (labeled) dose contained in the Twisthaler device.1 The amount of drug delivered to the lungs depends on factors such as the patient’s inspiratory flow.1

Each actuation of the Twisthaler inhaler contains 110 or 220 mcg of mometasone furoate inhalation powder and delivers approximately 100 or 200 mcg of mometasone furoate, respectively, per activation from the mouthpiece.1

Pediatric Patients

Asthma
Oral Inhalation

Children 4–11 years of age: Initial and maximum dosage is 110 mcg once daily in the evening, regardless of prior therapy.1

Children ≥12 years of age previously receiving bronchodilators alone or inhaled corticosteroids: Initially, 220 mcg once daily in the evening.1 If control of asthma is inadequate after 2 weeks of therapy at the initial dosage, a higher dosage may provide additional asthma control.1 If required, dosage may be increased to a maximum 440 mcg daily, given once daily or in 2 divided doses.1

Children ≥12 years of age previously receiving oral corticosteroids: Initial and maximum dosage is 880 mcg daily, given in 2 divided doses.1

Adults

Asthma
Oral Inhalation

Previously receiving bronchodilators alone or inhaled corticosteroids: Initially, 220 mcg once daily in the evening.1 If control of asthma is inadequate after 2 weeks of therapy at the initial dosage, a higher dosage may provide additional asthma control.1 If required, dosage may be increased to a maximum 440 mcg daily, given once daily or in 2 divided doses.1

Previously receiving oral corticosteroids: Initial and maximum dosage is 880 mcg daily, given in 2 divided doses.1

Prescribing Limits

Pediatric Patients

Asthma
Oral Inhalation

Children 4–11 years of age: Maximum 110 mcg daily.1

Children ≥12 years of age previously receiving bronchodilators alone or inhaled corticosteroids: Maximum 440 mcg daily.1

Children ≥12 years of age previously receiving oral corticosteroids: Maximum 880 mcg daily.1

Adults

Asthma
Oral Inhalation

Previously receiving bronchodilators alone or inhaled corticosteroids: Maximum 440 mcg daily.1

Previously receiving oral corticosteroids: Maximum 880 mcg daily.1

Special Populations

No special population dosage recommendations at this time.1

Cautions for Asmanex

Contraindications

  • Primary treatment of severe acute asthmatic attacks or status asthmaticus when intensive measures (e.g., oxygen, parenteral bronchodilators, IV corticosteroids12 15 ) are required.1

  • Known hypersensitivity to mometasone furoate or any ingredient (e.g., lactose) in the formulation.1

Warnings/Precautions

Warnings

Withdrawal of Systemic Corticosteroid Therapy

Possible life-threatening adrenal insufficiency in patients being switched from systemic corticosteroids to orally inhaled mometasone furoate.1

Withdraw systemic corticosteroid therapy gradually 1 and monitor for objective signs of adrenal insufficiency (e.g., fatigue, lassitude, weakness, nausea, vomiting, hypotension) during withdrawal of systemic therapy.1 Lung function (FEV1 or PEFR), adjunctive β2-adrenergic agonist use, and asthma symptoms also should be carefully monitored.1 In most patients, several months are required for total recovery of HPA function following withdrawal of systemic corticosteroid therapy.1 Patients who have been maintained on ≥20 mg of prednisone (or its equivalent) daily may be most susceptible to such adverse events, particularly during the later part of the transfer.1

Monitor for corticosteroid withdrawal symptoms (e.g., joint pain, muscular pain, lassitude, depression).1

Monitor for acute adrenal insufficiency during exposure to trauma, surgery, or infection (particularly gastroenteritis) or other conditions associated with acute electrolyte loss.1

Possible unmasking of conditions previously controlled by systemic corticosteroid therapy (e.g., rhinitis, conjunctivitis, eczema, arthritis, eosinophilic conditions).1

Immunosuppressed Patients

Increased susceptibility to infections in patients who are taking immunosuppressant drugs compared with healthy individuals.1 Certain infections (e.g., varicella [chickenpox], measles) can have a more serious or even fatal outcome in such patients.1

Take particular care to avoid exposure in susceptible patients.1 If exposure to varicella or measles occurs in susceptible patients, consider administering varicella zoster immune globulin (VZIG) or pooled IM immunoglobulin (IG), respectively.1 Consider treatment with an antiviral agent if varicella develops.1

Respiratory Effects

Bronchospasm and/or wheezing may occur.1

If bronchospasm occurs, treat immediately with a short-acting bronchodilator, discontinue treatment with mometasone furoate, and institute alternative therapy.1 8

Acute Exacerbations of Asthma

Treat acute asthma symptoms with a short-acting β2-agonist bronchodilator.1 8 12 If symptoms persist, promptly reevaluate and consider initiation of systemic corticosteroids.1 12

Galactose Intolerance

Oral inhalation powder contains lactose and should not be used in those with galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption.1 2

Sensitivity Reactions

Allergic reaction, facial edema, urticaria, hypersensitivity, and throat tightness reported.1

General Precautions

Ocular Effects

Glaucoma, increased intraocular pressure, and cataracts reported rarely.1 Carefully monitor patients who have a change in vision or those with a history of increased IOP, glaucoma and/or cataracts.1

Systemic Corticosteroid Effects

Administration of higher than recommended dosages of inhaled mometasone furoate over prolonged periods of time, or in particularly sensitive individuals, may result in manifestations of hypercorticism and suppression of HPA function.1 If such changes occur, reduce the dosage of mometasone furoate slowly, consistent with accepted procedures for reducing systemic corticosteroid dosage and management of asthma symptoms.1

Take particular care in monitoring patients postoperatively or during periods of stress for evidence of inadequate adrenal response.1

Musculoskeletal Effects

Long-term use may affect normal bone metabolism, resulting in a loss of bone mineral density (BMD).1

Monitor patients with major risk factors for decreased BMD (e.g., family history of osteoporosis, prolonged immobilization, chronic use of drugs that can reduce bone mass [e.g., anticonvulsants, corticosteroids]) and treat with established standards of care.1

Infections

Localized candidal infections of the mouth and pharynx reported.1 If infection occurs, appropriate local or systemic treatment and/or discontinuance of therapy may be required.1

Use with extreme caution, if at all, in patients with clinical or asymptomatic Mycobacterium tuberculosis infections of the respiratory tract; untreated systemic fungal, bacterial, parasitic, or viral infections; or ocular herpes simplex.1

Specific Populations

Pregnancy

Category C.1

Lactation

Not known whether mometasone is distributed into milk;1 however, other corticosteroids are distributed into milk.1 Caution advised if used in nursing women.1

Pediatric Use

Safety and efficacy of mometasone oral inhalation powder not established in children <4 years of age.1

With prolonged use, may slow growth rate in children and adolescents.1 Monitor routinely (e.g., via stadiometry) the growth and development of pediatric patients receiving corticosteroid therapy.1 Weigh benefits of corticosteroid therapy versus possibility of growth suppression and the risks associated with alternative therapies.1 Use the lowest possible dosage that effectively controls asthma.1

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.1

Common Adverse Effects

Adults and children ≥12 years of age previously receiving bronchodilators and/or inhaled corticosteroids: Headache,1 3 4 7 8 allergic rhinitis,1 8 pharyngitis,1 3 4 5 7 upper respiratory tract infection,1 8 sinusitis,1 oral candidiasis,1 3 4 5 7 dysmenorrhea,1 8 musculoskeletal pain,1 8 back pain,1 8 dyspepsia.1 7

Adults and children ≥12 years of age previously receiving oral corticosteroids: Musculoskeletal pain, oral candidiasis, sinusitis, allergic rhinitis, upper respiratory infection, arthralgia, fatigue, depression, sinus congestion.1

Children 4–11 years of age previously receiving bronchodilators and/or inhaled corticosteroids: Fever,1 headache,11 allergic rhinitis,1 pharyngitis,11 upper respiratory tract infection,11 abdominal pain.1 11

Interactions for Asmanex

Metabolized by CYP3A4 isoenzyme.1

Drugs Affecting Hepatic Microsomal Enzymes

Potent inhibitors of CYP3A4: potential pharmacokinetic interaction (increased plasma mometasone furoate concentrations).1

Specific Drugs

Drug

Interaction

Comments

Ketoconazole

Increased plasma mometasone furoate concentrations1

Asmanex Pharmacokinetics

Absorption

Bioavailability

<1% following oral inhalation of a single 440-mcg dose.1 2

Onset

≥1–2 weeks of continuous therapy required to achieve optimum symptomatic relief.1

Duration

When corticosteroids are discontinued, asthma control remains stable for several days or longer.1

Distribution

Extent

Not known whether mometasone is distributed into milk;1 however, other corticosteroids are distributed into milk.1

Does not accumulate in red blood cells.1

Plasma Protein Binding

98–99%.1

Elimination

Metabolism

Extensively metabolized in the liver principally by CYP3A4 isoenzyme.1 2

Elimination Route

Excreted principally in feces and to a lesser extent in urine.1 2

Half-life

Following IV administration, approximately 5 hours.1

Special Populations

In patients with hepatic impairment, plasma concentrations of the drug may be increased.1

Stability

Storage

Oral Inhalation

Powder

25°C (may be exposed to 15–30°C) in a dry place.1 Discard the inhaler 45 days after opening the foil pouch or when dose counter reads ‘00’, whichever comes first.1

Actions

  • Reduces the inflammatory asthmatic response by inhibiting multiple cell types (e.g., mast cells, eosinophils, lymphocytes, neutrophils, macrophages).1

  • Inhibits mediator production or secretion (e.g., eicosanoids, leukotrienes, cytokines, histamine) involved in the asthmatic response.1

  • Improves lung function (e.g., forced expiratory volume in 1 second [FEV1], morning and evening peak expiratory flow rate).1 3 4

Advice to Patients

  • Importance of providing the patient a copy of the manufacturer's patient information.1

  • Importance of adequate understanding of proper storage, preparation, and inhalation techniques, including use of the Twisthaler device.1 8

  • Importance of pediatric patients receiving oral inhalation therapy under adult supervision.8

  • Importance of rinsing the mouth after oral inhalation.1 2 8

  • Importance of advising patients that mometasone furoate oral inhalation must be used at regular intervals to be therapeutically effective.1 8

  • Importance of adherence to prescribed dosage regimen; do not increase the frequency of administration without consulting a clinician.8

  • Importance of advising patients that at least 1–2 weeks of continuous therapy may be required for optimum effects to be achieved.1 8 Importance of contacting a clinician if asthma symptoms do not improve in such a time frame.1 8

  • Importance of advising patients that orally inhaled mometasone should not be used as a bronchodilator and that the drug is not indicated for emergency use (e.g., relief of acute bronchospasm).1 8

  • Importance of availability and use of a short-acting β2-adrenergic agonist for relief of acute asthma symptoms.1 8 12

  • Importance of contacting a clinician immediately if asthmatic attacks that are not controlled by bronchodilator therapy occur.1

  • Importance of gradual withdrawal from systemic corticosteroids during transfer to orally inhaled mometasone and of monitoring by a clinician during such transfer of therapy.8 (See Conversion to Orally Inhaled Therapy in Patients Receiving Systemic Corticosteroids under Dosage and Administration.)

  • Importance of advising patients being transferred from systemic corticosteroid to mometasone oral inhalation therapy to carry special identification (e.g., card, bracelet) indicating the need for supplementary systemic corticosteroids during periods of stress or severe exacerbation of asthma.1 Importance of advising patients to immediately resume therapy with large doses1 of systemic corticosteroids and contact their clinician for further instructions during stressful periods (e.g., stress, severe asthmatic attack, surgery, trauma, infection).1 8

  • Importance of informing patients that corticosteroids may decrease bone mineral density.1 8 (See Musculoskeletal Effects under Cautions.)

  • Risk of localized candidal infections of mouth and pharynx.1 8 (See Infections under Cautions.)

  • Risk of systemic corticosteroid effects (e.g., hypercorticism, potentially life-threatening adrenal suppression).1 Importance of informing a clinician of fatigue, weakness, nausea, vomiting, dizziness, or fainting.1 8 (See Systemic Corticosteroid Effects under Cautions.)

  • Risk of reduction in growth velocity with orally inhaled corticosteroids.1 (See Pediatric Use under Cautions.)

  • Importance of informing patients that long-term use of inhaled corticosteroids may increase the risk for development of some eye problems (e.g., cataracts, glaucoma).1 (See Ocular Effects under Cautions.)

  • Importance of immunosuppressed patients avoiding exposure to chickenpox or measles, and, if exposed, of immediately consulting a clinician.1 8 (See Immunosuppressed Patients under Cautions.)

  • Importance of advising immunosuppressed patients of potential worsening of existing tuberculosis, fungal, bacterial, parasitic, or viral infections, or ocular herpes simplex.1 Importance of immunosuppressed patients informing clinician of a history of infections.8

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., infections).1 8

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Mometasone Furoate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral Inhalation

Powder for inhalation

110 mcg/inhalation (delivers 100 mcg/inhalation)

Asmanex Twisthaler

Schering

220 mcg/inhalation (delivers 200 mcg/inhalation)

Asmanex Twisthaler

Schering

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Asmanex 120 Metered Doses 220MCG/INH Aerosol (SCHERING): 0/$233.99 or 1/$650.96

Asmanex 30 Metered Doses 110MCG/INH Aerosol (SCHERING): 0/$130.99 or 0/$362.96

Asmanex 30 Metered Doses 220MCG/INH Aerosol (SCHERING): 0/$139.99 or 1/$399.97

Asmanex 60 Metered Doses 220MCG/INH Aerosol (SCHERING): 0/$167.99 or 1/$462.97

Dulera 100-5MCG/ACT Aerosol (SCHERING): 13/$222.98 or 39/$648.96

Dulera 200-5MCG/ACT Aerosol (SCHERING): 13/$229.99 or 39/$659.98

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions February 15, 2013. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Schering Corporation. Asmanex Twisthaler (mometasone furoate) inhalation powder prescribing information. Kenilworth, NJ; 2008 Jan.

2. Sharpe M, Jarvis B. Inhaled mometasone furoate: a review of its uses in adults and adolescents with persistent asthma. Drugs. 2001; 61:1325-50. [PubMed 11511026]

3. Nayak AS, Banov C, Corren J et al. Once-daily mometasone furoate dry powder inhaler in the treatment of patients with persistent asthma. Ann Allergy Asthma Immunol. 2000; 84:417-24. [IDIS 445793] [PubMed 10795650]

4. Kemp JP, Berkowitz RB, Miller SD et al. Mometasone furoate administered once daily is as effective as twice-daily administration for treatment of mild-to-moderate persistent asthma. J Allergy Clin Immunol. 2000; 106:485-92. [IDIS 453105] [PubMed 10984368]

5. Noonan M, Karpel JP, Bensch GW et al. Comparison of once-daily to twice-daily treatment with mometasone furoate dry powder inhaler. Ann Allergy Asthma Immunol. 2001; 86:36-43. [IDIS 458309] [PubMed 11206236]

6. Fish JE, Karpel JP, Craig TJ et al. Inhaled mometasone furoate reduces oral prednisone requirements while improving respiratory function and health-related quality of life in patients with severe persistent asthma. J Allergy Clin Immunol. 2000; 106:852-60. [IDIS 456665] [PubMed 11080706]

7. Bernstein DI, Berkowitz RB, Chervinsky P et al. Dose-ranging study of new steroid for asthma: mometasone furoate dry powder inhaler. Respir Med. 1999; 93:603-12. [PubMed 10542973]

8. Schering Corporation. Asmanex Twisthaler (mometasone furoate) inhalation powder patient instructions for use. Kenilworth, NJ; 2008 Jan.

10. National Institutes of Health, National Heart, Lung, and Blood Institute. Global initiative for asthma: global strategy for asthma management and prevention NHLBI/WHO Workshop Report. Bethesda, MD: National Institutes of Health. 2005 Oct. NIH/NHLBI Publication No. 02-3659. Available from website. Accessed Jan. 5, 2006.

11. Berger WE, Milgrom H, Chervinsky P et al. Effects of treatment with mometasone furoate dry powder in children with persistent asthma. Ann Allergy Asthma Immunol. 2006; 97:672-80. [PubMed 17165278]

12. National Asthma Education and Prevention Program. Expert panel report 3: guidelines for the diagnosis and management of asthma. Bethesda, MD: National Institutes of Health, National Heart, Lung and Blood Institute. Aug 28. 2007. Available from website.

13. IVAX Laboratories. Qvar (beclomethasone dipropronate) HFA inhalation aerosol prescribing information. Miami, FL; 2005 Nov.

14. Schering Plough, Kenilworth, NJ: Personal communication.

15. National Institutes of Health, National Heart, Lung, and Blood Institute. Global initiative for asthma: global strategy for asthma management and prevention. Bethesda, MD: National Institutes of Health. 2009 Dec. Available from: NIH website. Accessed 2010 Sep 23.

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