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flunisolide Nasal inhalant Nasalide, Nasarel
Oral inhalant AeroBid, AeroBid-M
Pharmacologic classification: glucocorticoid Therapeutic classification: anti-inflammatory, antasthmatic Pregnancy risk category C
Available forms Available by prescription only Nasal inhalant: 25 mcg/metered spray; 200 doses/ bottle Oral inhalant: 250 mcg/metered spray; at least 100 doses/inhaler
Indications and dosages
Corticosteroid-dependent asthma. Adults: 2 inhalations b.i.d. for a total daily dose of 1 mg. Maximum dose is 8 inhalations (2 mg) daily. Children age 6 and older: 2 inhalations b.i.d. Maximum dose is 4 inhalations daily.
Seasonal or perennial rhinitis. Adults: 2 sprays (50 mcg) in each nostril b.i.d. (total dose 200 mcg daily). If needed, increase to 2 sprays in each nostril t.i.d.
(total dose 300 mcg daily). Maximum dose is 8 sprays in each nostril daily (400 mcg daily). Children ages 6 to 14: 1 spray (25 mcg) in each nostril t.i.d. or 2 sprays (50 mcg) in each nostril b.i.d. (total dose 150 to 200 mcg daily). Maximum
dose is 4 sprays in each nostril daily (200 mcg/day).
Pharmacodynamics Anti-inflammatory action: Flunisolide stimulates synthesis of enzymes needed to decrease the inflammatory response. The anti-inflammatory and vasoconstrictor
potency of topically applied flunisolide is several hundred times greater than that of hydrocortisone and about equal to that
of an equal weight of triamcinolone; the metabolite, 6-beta-hydroxyflunisolide, has about three times the activity of hydrocortisone.
Antasthmatic action: The nasal inhalant form is used in the symptomatic treatment of seasonal or perennial rhinitis. In patients who require corticosteroids
to control symptoms, the oral inhalant form is used to treat bronchial asthma.
Pharmacokinetics Absorption: About 50% of a nasally inhaled dose is absorbed systemically. After oral inhalation, about 40% of dose is absorbed from the
lungs and GI tract; only about 20% of an orally inhaled dose reaches systemic circulation unmetabolized because of extensive
metabolism in the liver. Onset of action usually occurs in a few days but may take as long as 4 weeks. Distribution: Distribution following intranasal administration or oral inhalation hasn’t been described. No evidence exists of tissue storage
of flunisolide or its metabolites. Metabolism: When swallowed, undergoes rapid metabolism in the liver or GI tract to several metabolites, one of which has glucocorticoid
activity. Flunisolide and its 6-beta-hydroxy metabolite are eventually conjugated in the liver, by glucuronic acid or surface
sulfate, to inactive metabolites. Excretion: Excretion pathway is unknown when drug is given as inhalant; however, when it’s given systemically, metabolites are excreted
in roughly equal portions in feces and urine. Biologic half-life of drug averages about 2 hours.
| Route |
Onset |
Peak |
Duration |
| Inhalation |
Variable |
10-30 min |
Unknown |
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Contraindications and precautions Contraindicated in patients hypersensitive to drug. Nasal inhalant is contraindicated by an untreated localized infection
involving nasal mucosa. Oral inhalant shouldn’t be used by patients with status asthmaticus or respiratory infections. Use nasal inhalant cautiously in patients with tuberculosis; untreated fungal, bacterial, or systemic viral or ocular herpes
simplex infections; or septal ulcers, trauma, or surgery in the nasal region. Oral inhalant isn’t recommended for patients
with asthma controlled by bronchodilators or other noncorticosteroids alone or patients with nonasthma bronchial diseases.
Interactions None reported.
Adverse reactions CNS: headache with nasal inhalant; dizziness, irritability, and nervousness with oral inhalant, fever with oral inhalant. CV: chest pain, edema with oral inhalant. EENT: nasopharyngeal fungal infection; mild, transient nasal burning and stinging; stinging, dryness, sneezing, epistaxis, and watery eyes with nasal inhalant. GI: nausea and vomiting with nasal inhalant; dry mouth, abdominal pain, decreased appetite, nausea, vomiting, diarrhea, and upset stomach with oral inhalant. Respiratory: upper respiratory tract infection with oral inhalant. Skin: rash, pruritus with oral inhalant. Other: cold symptoms, flu.
Effects on lab test results None reported.
Overdose and treatment No information available.
Special considerations Drug isn’t effective for acute exacerbations of rhinitis. Decongestants or antihistamines may be needed.
ALERT Don’t confuse flunisolide with fluocinonide or Flumadine. Monitor patient for adverse reactions. Monitor patient for development of oral fungal infections. Pregnant patients Use drug during pregnancy only if potential benefits justify risk to fetus. Breast-feeding patients Use drug cautiously in breast-feeding patients. Pediatric patients Safety and efficacy haven’t been established in children younger than age 6 months.
Patient education Inform patient that drug doesn’t relieve emergency asthma attacks. Advise patient of proper administration method.
Reactions may be common, uncommon, life-threatening, or
COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use
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