Class: Adrenals
ATC Class: R03BA03
VA Class: NT200
Chemical Name: (6α,11β,16α) - 6 - fluoro - 11,21 - dihydroxy - 16,17 - [(1 - methylethylidene)bis(oxy)] - pregna - 1,4 - diene - 3,20 - dione hemihydrate
Molecular Formula: C24H31FO6½H2O
CAS Number: 77326-96-6
Brands: AeroBid
Introduction
Synthetic fluorinated glucocorticoid.a
Uses for Flunisolide
Asthma
Long-term prevention of bronchospasm in patients with asthma.102 104 105
In corticosteroid-dependent patients, may permit a substantial reduction in the daily maintenance dosage of the systemic corticosteroid or gradual discontinuance of systemic corticosteroid maintenance dosages.105
Oral inhalation should not be used for the treatment of nonasthmatic bronchitis or for rapid relief of bronchospasm.105
Flunisolide Dosage and Administration
General
Adjust dosage carefully according to individual requirements and response.105
After a satisfactory response is obtained, decrease dosage gradually to the lowest possible dosage that maintains an adequate clinical response.b Achieve the lowest effective dosage, particularly in children, since inhaled corticosteroids have the potential to affect growth.c (See Pediatric Use under Cautions.)
Conversion to Orally Inhaled Therapy in Patients Receiving Systemic Corticosteroids
When switching from systemic corticosteroids to orally inhaled flunisolide, asthma should be reasonably stable before initiating treatment with the oral inhalation.b
Initially, administer oral inhalation concurrently with the maintenance dosage of the systemic corticosteroid.b After about 1 week, gradually withdraw the systemic corticosteroid.a b
Decrements usually should not exceed 2.5 mg of prednisone (or its equivalent) every 1–2 weeks in patients receiving the oral inhalation. b c
During withdrawal of oral therapy, symptoms of systemic corticosteroid withdrawal may occur despite maintenance or even improvement in pulmonary function; continue oral inhalation therapy but monitor for objective signs of adrenal insufficiency.b If evidence of adrenal insufficiency occurs, increase systemic corticosteroid dosage temporarily and continue withdrawal more slowly.b
Death has occurred in some individuals in whom systemic corticosteroids were withdrawn too rapidly.105 (See Withdrawal of Systemic Corticosteroid Therapy under Cautions.)
If exacerbations of asthma occur after transfer to oral inhalation therapy, administer short courses of systemic corticosteroids, then taper dosage as symptoms subside.a Supplemental systemic corticosteroid therapy may also be required during periods of stress.b
Administration
Oral Inhalation
Administer by oral inhalation using an oral aerosol inhaler.a b
Administer twice daily in the morning and evening.105
Shake well immediately prior to use and hold inhaler upright prior to actuation.106 Exhale out as completely as possible and place the mouthpiece of the inhaler well into the mouth with lips closed firmly around it.106 Inhale slowly through the mouth while pressing the metal canister down with the forefinger.106 After holding the breath for as long as possible, remove the mouthpiece and exhale slowly.106 If additional inhalations are required, wait 1 minute between inhalations, shake the inhaler again, and repeat the procedure.106
Following each treatment, rinse mouth thoroughly with water or mouthwash to remove drug deposited in the oropharyngeal area.106
Clean inhaler every few days by removing canister from the inhaler and rinsing plastic cap and inhaler in warm water; allow to dry thoroughly.106
Dosage
Available as flunisolide hemihydrate; dosage expressed in terms of flunisolide.105
Oral inhalation aerosol delivers 250 mcg of flunisolide from the actuator (mouthpiece) per metered spray.105 The inhaler system delivers at least 100 metered sprays.105
Pediatric Patients
Asthma
Oral
Children 6–15 years of age: 500 mcg (2 inhalations) twice daily.105
Adults
Asthma
Oral
Initially, 500 mcg (2 inhalations) twice daily.105 If required, dosage may be increased to 1 mg (4 inhalations) twice daily.105 Higher dosages have been recommended by some clinicians for patients with severe persistent asthma.104 105
Prescribing Limits
Pediatric Patients
Oral
Dosages >500 mcg (2 inhalations) twice daily not evaluated.105
Adults
Oral
Manufacturer recommends maximum 1 mg (4 inhalations) twice daily (2 mg total daily dosage).104 105
Special Populations
No special population dosage recommendations at this time.b
Cautions for Flunisolide
Contraindications
Primary treatment of severe acute asthmatic attacks or status asthmaticus when intensive measures (e.g., oxygen, parenteral bronchodilators, IV corticosteroids) are required.102 104 105
Known hypersensitivity to flunisolide or any ingredient in the formulation.b
Warnings/Precautions
Warnings
Withdrawal of Systemic Corticosteroid Therapy
Possible corticosteroid withdrawal symptoms (e.g., joint pain, muscular pain, lassitude, depression);b c acute adrenal insufficiency;b c pulmonary infiltrates with eosinophilia;b or symptomatic exacerbation of allergic conditions if prolonged systemic corticosteroid therapy is replaced with oral inhalation corticosteroid therapy.b
Taper the dosage of the systemic corticosteroid, and carefully monitor patients during dosage reduction for objective signs of adrenal insufficiency (e.g., hypotension, weight loss).c
Immunosuppressed Patients
Increased susceptibility to infections in patients who are taking immunosuppressant drugs compared with healthy individuals.b Certain infections (e.g., varicella [chickenpox], measles) can have a more serious or even fatal outcome in such patients,b particularly in children.c
Exposure to varicella and measles should be avoided in previously unexposed patients.b If exposure to varicella (chickenpox) or measles occurs in susceptible patients, consider administering varicella zoster immune globulin (VZIG) or pooled immune globulin (IG), respectively.b Consider treatment with an antiviral agent if varicella develops.b
Concomitant Therapy
Concomitant use with prednisone in an alternate-day regimen could increase the likelihood of HPA-axis suppression compared with therapeutic dosages of either drug alone.b
Resume systemic corticosteroids during periods of stress (e.g., infection, trauma, surgery) or a severe asthma exacerbation in patients who were attempting a switch from systemic to orally inhaled corticosteroid therapy.b
Infections
Localized fungal infections (Candida albicans or Aspergillus niger) of the mouth, pharynx, and occasionally the larynx reported.b If infection occurs, appropriate local or systemic treatment and/or discontinuance of therapy may be required.b
Use with caution, if at all, in patients with Mycobacterium tuberculosis infections of the respiratory tract; untreated systemic fungal, bacterial, or parasitic infections; or ocular herpes simplex or untreated, systemic viral infections.b c
General Precautions
Systemic Corticosteroid Effects
Administration of higher than recommended dosages of orally inhaled flunisolide may result in manifestations of hypercorticism and suppression of hypothalamic-pituitary-adrenal (HPA) function.b c Periodically monitor patients receiving long-term therapy at a maximum daily dosage for effects on the HPA axis.105
Carefully monitor patients during periods of stress (e.g., infections, trauma, surgery) for manifestations of hypoadrenalism.b c
Monitor adrenal function to assess the risk of adrenal insufficiency in emergency situations.b Normal morning plasma cortisol concentrations (>10 mcg/dL) indicate basal pituitary-adrenal function is adequate.c
Ocular Effects
Glaucoma, increased intraocular pressure, and cataracts reported rarely.
Other Effects
Unknown long-term local and systemic effects of the drug in humans, particularly developmental or immunologic processes in the mouth, pharynx, trachea, and lung.b
Specific Populations
Pregnancy
Category C.b
Lactation
Not known whether flunisolide is distributed into milk; however, other corticosteroids are distributed into milk.b c Caution if used in nursing women.b
Pediatric Use
Safety and efficacy not established in children <6 years of age.b
Periodically monitor children receiving prolonged therapy for adverse effects on growth and development.105 b
Common Adverse Effects
Diarrhea,b nausea,b vomiting,b flu,b sore throat,b headache,b nasal congestion,b upper respiratory infection,b unpleasant taste,b cold symptoms,b upset stomach.b
Interactions for Flunisolide
Specific Drugs
Drug | Interaction | Comments |
|---|---|---|
Antidiabetic agents | May increase blood glucose concentrations in patients with diabetes mellitus | Adjust insulin and/or oral hypoglycemic dosages as needed |
Vaccines and toxoids | May cause a diminished response to toxoids and live or inactivated vaccinesc May potentiate replication of some organisms contained in live, attenuated vaccines c | May undertake immunization procedures in patients receiving nonimmunosuppressive doses of glucocorticoidsc |
Flunisolide Pharmacokinetics
Absorption
Bioavailability
Following oral inhalation, total systemic availability is 40%.b
Onset
1–4 weeks of continuous therapy may be required for optimum effectiveness.b
Distribution
Extent
Placental distribution in humans is unknown, but flunisolide apparently crosses the placenta in animals.d
Distribution into milk is unknown, but other corticosteroids are distributed into milk.c d
Plasma Protein Binding
At a plasma concentration of 1–20,000 ng/mL, about 50% bound to plasma albumin.d No binding to corticosteroid-binding globulin.d
Elimination
Metabolism
Rapidly and extensively metabolized in the liver.b
Elimination Route
Excretion pathway is unknown when inhaled; however when given systemically, metabolites are excreted in roughly equal portions in feces and urine.d
Half-life
Approximately, 1.8 hours. b
Stability
Storage
Oral Inhalation
Aerosol
25°C;e protect from excessive heat (>49°C).b
ActionsActions
Potent glucocorticoid and minimal mineralocorticoid activity.d
Demonstrates marked anti-inflammatory and antiallergic activity. b
Improves lung function (e.g., forced expiratory volume in 1 second [FEV1], morning peak expiratory flow).100
Principal sites of action are the bronchi and bronchioles; minimal systemic activity at recommended doses. b
May reduce the number of mediator cells (basophil leukocytes and mast cells) at the epithelial level, number of eosinophils, sensitivity of sensory nerves to mechanical stimuli, secretory response to cholinergic receptor stimulation, and fibroblast activity.d
May inhibit capillary dilation and permeability, and stabilize lysosomal membranes and subsequent prevention of release of proteolytic enzymes.d
Advice to Patients
Importance of instructing patient in the use of the oral inhaler and providing a copy of the manufacturer's information and/or medication guide.b
Importance of adequate understanding of proper storage, preparation, and administration techniques.b
Importance of rinsing mouth after oral inhalation. b
Importance of informing clinician if mouth becomes sore or develops a rash.b
Importance of advising patient that flunisolide oral inhalation must be used at regular intervals to be therapeutically effective.b
Importance of not exceeding the recommended dosage and of contacting a clinician immediately if asthma symptoms that are not responsive to bronchodilators occur.b
Importance of not using orally inhaled flunisolide as a bronchodilator and for emergency use (e.g., relief of acute bronchospasm).b c
Advise patients being transferred from systemic corticosteroids to flunisolide oral inhalation therapy to carry special identification (e.g., card, bracelet) indicating the need for supplementary systemic corticosteroids during periods of stress.b
Advise patients receiving orally inhaled flunisolide therapy who are currently being withdrawn from systemic corticosteroids to immediately resume full therapeutic dosages of systemic corticosteroids and to contact their clinician for further instructions during stressful periods (e.g., severe infection, severe asthmatic attack).
Importance of immunosuppressed patients avoiding exposure to chickenpox or measles, and if exposed, of immediately consulting their clinician.b
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.b
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.b
Importance of informing patients of other precautionary information.b (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral Inhalation | Aerosol | 250 mcg (of flunisolide) per metered spray | AeroBid Inhaler System (with chlorofluorohydrocarbon propellants and sorbitan trioleate) | Forest |
AeroBid-M Inhaler System (with chlorofluorohydrocarbon propellants, menthol, and sorbitan trioleate) | Forest |
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions September 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
References
100. National Asthma Education and Prevention Program. Expert panel report II: guidelines for the diagnosis and management of asthma. Bethesda, MD: National Institutes of Health; 1997 Feb.
101. National Asthma Education Program. Executive summary: guidelines for the diagnosis and management of asthma. NIH Publication No. 94-3042A. Washington, DC: US Governement Printing Office; 1994 Jul.
102. 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. 2002 Feb. NIH/NHLBI Publication No. 02-3659. Available at http://www.ginasthma.com. Accessed Sep. 26, 2002.
103. British Thoracic Society. Guidelines on the management of asthma. Thorax. 1993; 48(Suppl 2):S1-24.
104. National Asthma Education and Prevention Program. Expert panel report: guidelines for the diagnosis and management of asthma. Update on selected topics-2002. Bethesda, Md: National Heart, Lung, and Blood Institute, National Asthma Education and Prevention Program Coordinating Committee; 2003 Jun. Available from National Heart, Lung, and Blood Institute Information Center, NIH Publication No. 02-5074. Also available at . Accessed 2006 Jan. 5.
105. Forest Pharmaceuticals. AeroBID/AeroBID-M (flunisolide) inhaler system prescribing information. St. Louis, MO; 2002 Mar.
106. Forest Pharmaceuticals. Aerobid/Aerobid-M (flunisolide) inhaler system directions for use. St. Louis, MO; 2002 Mar.
a. AHFS drug information 2007. McEvoy GK, ed. Flunisolide. Bethesda, MD: American Society of Health-System Pharmacists; 2007:3048-9.
b. Forest Pharmaceuticals, Inc. Aerobid and Aerobid-M (flunisolide) aerosol, metered prescribing information. St. Louis, MO; 2006 Dec.
c. AHFS drug information 2007. McEvoy GK, ed. Corticosteroids General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2007: 3024-37.
d. AHFS drug information 2007. McEvoy GK, ed. Flunisolide. Bethesda, MD: American Society of Health-System Pharmacists; 2007:2821-3.
e. Sinha, N (Forest Pharmaceuticals, Inc. St. Louis, MO): Personal communication; 2007 Jun.
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