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Flunisolide eent

Pronunciation

Class: Corticosteroids
ATC Class: R01AD
VA Class: RE101
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: C24H31FO6•½H2O
CAS Number: 77326-96-6

Introduction

Synthetic fluorinated corticosteroid.a

Uses for Flunisolide

Seasonal and Perennial Rhinitis

Symptomatic treatment of seasonal or perennial rhinitisa b when conventional therapy with antihistamines or decongestants is ineffective or produces intolerable adverse effects.b

Generally provides symptomatic relief of watery rhinorrhea, nasal congestion, sneezing, postnasal drip, and pharyngeal itching;b generally does not relieve symptoms of conjunctivitis or those involving the lower respiratory tractb

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Appears to provide greater symptomatic relief in allergic rhinitis than in nonallergic rhinitisb

Serious Otitis Media

Has been used intranasally for the treatment of serous otitis media (eustachian tube dysfunction, middle ear effusion) in children. b

Corticosteroid-dependent Asthma

Although orally inhaled flunisolide is used for the treatment of asthma, the nasal solution is not recommended for this purpose, since the safety of polyethylene glycol in the vehicle of the nasal solution has not been established for this route of administration.b

Flunisolide Dosage and Administration

Administration

Intranasal Administration

Administer by nasal inhalation using a special nasal inhaler.

Avoid contact with the eyes.a

Poor clinical response can result from improper drug administration techniques, poor drug penetration (secondary to marked nasal congestion, presence of nasal polyps, or symptoms originating in the nasal sinuses), or localized infections of the nasal mucosa.b

Clear nasal passages prior to administration.b If nasal passages are blocked, a topical nasal decongestant can be administered 5–15 minutes before intranasal administration during the first 2–3 days of therapy to ensure adequate penetration of the drug and prevent loss from the nasal passages via excess secretions.b

Prior to initial use, the nasal inhaler must be assembled and primed.b

After assembly is complete, tilt the head slightly forward, insert the spray tip into one nostril, and point the tip toward the inflamed nasal turbinates and away from the nasal septum.b

Pump the drug into one nostril while holding the other nostril closed and concurrently inspire through the nose.b Repeat procedure for the other nostril.b

Advise patients to cleanse the nasal adapter and/or pump in warm water if the holes in the device become clogged.b If the nasal inhaler is disassembled for any reason (including the cleansing procedure) or not used for 5 days or longer, it must be primed again prior to use.b

Dosage

After priming, nasal inhaler delivers about 25 mcg of flunisolide per metered spray and about 200 metered sprays per 25-mL container.a

Adjust dosage according to individual requirements and response.a b

Therapeutic effects of intranasal corticosteroids, unlike those of decongestants, are not immediate.b This should be explained to the patient in advance to ensure compliance and continuation of the prescribed treatment regimen.b

Symptomatic relief is usually evident within 2–3 days of continuous therapy; however, occasionally, up to 2–3 weeks may be required for optimum effectiveness.b

Generally assess response to the initial dosage 4–7 days after starting therapy; about two-thirds will experience some relief within this time period.b

Once symptoms of seasonal or perennial rhinitis have been controlled, gradually reduce dosage to the lowest effective level.b

Discontinue intranasal flunisolide in patients who do not experience clinically important benefit within 3 weeks of initiating therapy.b

Pediatric Patients

Seasonal Rhinitis
Intranasal Inhalation

Children 6–14 years of age: 1 spray (25 mcg) in each nostril 3 times daily or 2 sprays (50 mcg) in each nostril twice daily (total dose: 150–200 mcg/day).a b

Perennial Rhinitis
Intranasal Inhalation

Children 6–14 years of age: 1 spray (25 mcg) in each nostril 3 times daily or 2 sprays (50 mcg) in each nostril twice daily (total dose 150–200 mcg/day).b

Adults

Seasonal Rhinitis
Intranasal Inhalation

Usual initial dose is 50 mcg (2 sprays) in each nostril twice daily.a b When necessary, increase to 50 mcg (2 sprays) in each nostril 3 times daily.a b

Maintenance: 25 mcg (1 spray) in each nostril daily (50 mcg total) may be sufficient.a b

Perennial Rhinitis
Intranasal Inhalation

Usual initial dose is 50 mcg (2 sprays) in each nostril twice daily.a b When necessary, increase to 50 mcg (2 sprays) in each nostril 3 times daily.a b

Maintenance: 25 mcg (1 spray) in each nostril daily (50 mcg total) may be sufficient.a b

Prescribing Limits

No evidence that higher than recommended dosages or increased frequency of administration is beneficial.b

Exceeding the maximum recommended daily dosage may only increase the risk of adverse systemic effects (e.g., HPA-axis suppression, Cushing’s syndrome).b

Pediatric Patients

Seasonal Rhinitis
Intranasal Inhalation

Children 6-14 years of age: daily dosage should not exceed 100 mcg (4 sprays) in each nostril (200 mcg total).a b

Perennial Rhinitis
Intranasal Inhalation

Children 6-14 years of age: daily dosage should not exceed 100 mcg (4 sprays) in each nostril (200 mcg total).a b

Adults

Seasonal Rhinitis
Intranasal Inhalation

Daily dosage should not exceed 200 mcg (8 sprays) in each nostril (400 mcg total).a b

Perennial Rhinitis
Intranasal Inhalation

Daily dosage should not exceed 200 mcg (8 sprays) in each nostril (400 mcg total).a b

Special Populations

Hepatic Impairment

No specific dosage recommendations for hepatic impairment.a

Renal Impairment

No specific dosage recommendations for renal impairment.a

Geriatric Patients

No specific geriatric dosage recommendations.a

Cautions for Flunisolide

Contraindications

  • Known hypersensitivity to flunisolide or any ingredient in the formulation.a b

  • Do not use in the presence of untreated localized nasal mucosa infections.a

Warnings/Precautions

Warnings

Withdrawal of Systemic Corticosteroid Therapy

Patients being switched from prolonged systemic corticosteroids to intranasal therapy should be monitored carefully since corticosteroid withdrawal symptoms (e.g., joint pain, muscular pain, lassitude, depression), acute adrenal insufficiency, and/or severe symptomatic exacerbation of asthma or other clinical conditions may occur.a b

Systemic corticosteroid dosage should be tapered, and patients should be carefully monitored during dosage reduction.b

Infection, Trauma, or Surgery

Use cautiously, if at all, in patients with clinical tuberculosis or asymptomatic Mycobacterium tuberculosis infections; untreated fungal, bacterial, or systemic viral or ocular herpes simplex infections; or septal ulcers, trauma, or surgery in the nasal region.a b

Hypothalamic-Pituitary-Adrenal (HPA) Axis Suppression

Avoid higher than recommended dosages since suppression of HPA function may occur.b

Immunosuppression

Although risk with intranasal use is unknown, consider the possibility that corticosteroid-induced immunosuppression could occur.a Avoid exposure to varicella and measles in previously unexposed patients.a

General Precautions

Systemic Corticosteroid Effects

Excessive intranasal dosages or use in patients who are particularly sensitive to corticosteroid effects may cause systemic corticosteroid effects (e.g., Cushing’s syndrome, adrenal suppression).a b

Nasopharyngeal Effects

Temporary or permanent loss of smell may occur.a

Rarely, localized candidal infections of the nose and/or pharynx.a b Treat suspected local infection appropriatelya b ; may require discontinuance of flunisolide therapy.a b

Rarely, nasal septal perforations.a

Avoid use until healing occurs in patients with recurrent epistaxis, recent nasal septal ulcers, nasal surgery, or nasal trauma.a

Oral Effects

Temporary or permanent loss of taste may occur.a

Specific Populations

Pregnancy

Category C.a

Lactation

Other corticosteroids known to be distributed into milk.a b Caution if used in nursing women.a b

May cause adverse effects (e.g., growth suppression) in nursing infants if distributed.b

Pediatric Use

May be a useful therapeutic alternative to oral corticosteroids in children ≥6 years of age with seasonal or perennial allergic rhinitis, since intranasal administration is associated with a decreased risk of adverse systemic effects.b

Intranasal corticosteroids may reduce growth velocity in pediatric patients.a b

Safety and efficacy haven’t been established in children < 6 months of age.a

Common Adverse Effects

Mild, transient nasal burning and stinging,a b aftertaste,a b nasal congestion,a b epistaxis,a b headache,a b watery eyes,a b nausea,a b vomiting,a b abdominal bloating,b upper respiratory tract infection,PDH cold symptoms.PDH

Interactions for Flunisolide

No reports to date of clinically important drug interactions.b

Drugs Affecting Hepatic Microsomal Enzymes

Phenobarbital and other agents that induce hepatic microsomal enzymes may enhance the metabolism of corticosteroids.b

Flunisolide Pharmacokinetics

Absorption

Bioavailability

About 50% of a nasally inhaled dose is absorbed systemically.b

Onset

Symptomatic relief usually is evident within 2–3 days of continuous therapy but may take up to 2–3 weeks.b

Distribution

Extent

Placental distribution in humans is unknown, but flunisolide apparently crosses the placenta in animals.b

Distribution into milk unknown, but other corticosteroids are distributed.a b

Plasma Protein Binding

At a plasma concentration of 1–20,000 ng/mL, about 50% bound to plasma albumin.b No binding to glucocorticosteroid binding globulin.b

Elimination

Metabolism

Metabolized via 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.PDH

Drug absorbed via nasopharyngeal mucosa bypasses extensive first-pass hepatic metabolism.b

Half-life

Plasma half-life: 1–2 hours.a

Stability

Storage

Solutions

Tight, light-resistant container at 15–30°C.a b c

Discard opened containers after 3 months.a b

Actions

  • Potent glucocorticoid and weak mineralocorticoid effects.b

  • Local anti-inflammatory and vasoconstrictor effects;b topical potency similar to triamcinolone acetonide.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.b

  • May inhibit capillary dilation and permeability.b

  • May stabilize lysosomal membranes and subsequently prevent the release of proteolytic enzymes.b

Advice to Patients

  • Proper techniques for assembly and priming of nasal spray pump and for administration of the nasal solution.a b Importance of not administering the entire dose (i.e., 4 sprays) into a single nostril.a b Give patients a copy of the manufacturer’s patient instructions.a b

  • Advise patients that opened containers of flunisolide nasal solution should be discarded after 3 months.b

  • Advise patients that effects are not immediate; full benefit requires regular use and usually can be achieved in several days.a

  • Importance of taking as directed.a

  • Importance of informing clinician if no improvement is seen within 3 weeks or if the condition worsens.a

  • Importance of not increasing dosage unless directed by a clinician.a

  • Importance of advising clinician if sneezing or nasal irritation occurs.a

  • Advise that concomitant nasal decongestants and/or oral antihistamines may be needed until effects of flunisolide are optimal.a

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.a b

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

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

Preparations

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

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Flunisolide

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Solution

25 mcg/metered spray*

Flunisolide Spray

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.

Flunisolide 0.03% Solution (BAUSCH &amp; LOMB): 25/$67.99 or 75/$189.98

Flunisolide 29MCG/ACT Solution (APOTEX): 25/$45.99 or 75/$129.97

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions April 1, 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

a. Bausch & Lomb Pharmaceuticals, Inc. Flunisolide Nasal Solution prescribing information. Tampa, FL: 2000 August.

b. AHFS Drug Information 2004. McEvoy, GK, ed. Flunisolide. Bethesda, MD: American Society of Health-System Pharmacists; 2004:2666-2669.

c. The United States pharmacopeia, 27rd rev, and The national formulary, 22th ed. Rockville, MD: The United States Pharmacopeial Convention, Inc; 2000:806.

PDH. Schilling McCann JA, Publisher. Pharmacists drug handbook. 2nd ed. Philadelphia, PA: Lippincott Williams and Wilkins and American Society of Health-System Pharmacists; 2003.

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