Flunisolide eent

Synthetic fluorinated corticosteroid.a

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

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

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

• 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

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.
• Nose irritation.
• Bad nosebleeds.
• Nose sores.
• Whistling sound when you breathe.
• Redness or white patches in mouth or throat.
• Sneezing.
• Fever or chills.
• Sore throat.

Data not available

Data not available

Flunisolide has been assigned to pregnancy category C by the FDA. At high doses, flunisolide has been shown to be teratogenic in rabbits and rats. There are no controlled data in human pregnancy. Flunisolide is only recommended for use during pregnancy when there are no alternatives and benefit outweighs risk.

In a review of 229,101 deliveries to Michigan Medicaid patients, 141 first-trimester exposures to flunisolide and 322 exposures anytime during pregnancy were recorded. A total of 5 birth defects were reported with first-trimester exposures (5 expected). (written communication, Franz Rosa, MD, Food and Drug Administration, 1994) These data do not support an association with adverse fetal outcome.