budesonide intranasal (Rx, OTC)

1-10%

Epistaxis (8%)

Pharyngitis (4%)

Bronchospasm (2%)

Cough (2%)

Nasal irritation (2%)

Postmarketing Reports

Immune system disorders: immediate and delayed hypersensitivity reactions (including anaphylactic reaction, urticaria, rash, dermatitis, angioedema and pruritus)

Eye disorders: glaucoma, increased intraocular pressure, cataracts

Respiratory, thoracic, and mediastinal disorders: nasal septum perforation, anosmia, pharynx disorders (throat irritation, throat pain, swollen throat, burning throat, and itchy throat), and wheezing

Cardiac disorders: palpitations

Musculoskeletal and connective tissue disorders: growth suppression

Contraindications

Hypersensitivity to drug or excipients

Cautions

Anaphylaxis, urticaria, rash, dermatitis, angioedema, and pruritus may occur

Epistaxis reported with use

Because of inhibitory effect of corticosteroids on wound healing, patients who have experienced recent nasal septal ulcers, nasal surgery, or nasal trauma should not use a nasal corticosteroid until healing has occurred

Intranasal corticosteroids may cause a reduction in growth velocity when administered to pediatric patients; monitor growth routinely of pediatric patients receiving long-term treatment; to minimize systemic effects of intranasal corticosteroids, titrate each patient’s dosage to lowest one that effectively controls his/her symptoms

Nasal septum perforation reported following intranasal application

Development of localized infections of the nose and pharynx with Candida albicans reported; when such an infection develops, may require treatment with appropriate local or systemic therapy and discontinuation of treatment with this drug; patients receiving therapy over several months or longer should be examined periodically for evidence of Candida infection or other signs of adverse effects on nasal mucosa

Glaucoma increased intraocular pressure, and cataracts reported following the intranasal application of corticosteroids, including budesonide; therefore, close monitoring is warranted in patients with a change in vision or with a history of increased intraocular pressure, glaucoma, and/or cataracts

Immunosuppression

• Patients who are on drugs that suppress the immune system are more susceptible to infections than healthy individuals; chickenpox and measles can have a more serious or even fatal course in susceptible children or adults using corticosteroids; in such children or adults who have not had these diseases or been properly immunized, particular care should be taken to avoid exposure
• How the dose, route, and duration of corticosteroid administration affect risk of developing a disseminated infection is not known; the contribution of the underlying disease and/or prior corticosteroid treatment to the risk is also not known
• If exposed to chickenpox, therapy with varicella-zoster immune globulin (VZIG) or pooled intravenous immunoglobulin (IVIG), as appropriate, may be indicated
• If exposed to measles, prophylaxis with pooled intramuscular immunoglobulin (IG) may be indicated; if chickenpox develops, treatment with antiviral agents may be considered
• Corticosteroids should be used with caution, if at all, in patients with active or quiescent tuberculosis infection, untreated fungal, bacterial, systemic viral or parasitic infections, or ocular herpes simplex

Hypercorticism and adrenal suppression

• When intranasal steroids are used at higher than recommended dosages or in susceptible individuals at recommended dosages, systemic corticosteroid effects such as hypercorticism and adrenal suppression may occur; if such changes happen, therapy should be discontinued slowly, consistent with accepted procedures for discontinuing oral corticosteroid therapy
• The replacement of a systemic corticosteroid with a topical corticosteroid can be accompanied by signs of adrenal insufficiency, and in addition, some patients may experience symptoms of corticosteroid withdrawal, eg, joint and/or muscular pain, fatigue, weakness, nausea, vomiting, hypotension, lassitude, and depression
• Patients previously treated for prolonged periods with systemic corticosteroids should be weaned off slowly when transferred to topical corticosteroids and carefully monitored for acute adrenal insufficiency in response to stress
• In patients who have asthma or other clinical conditions requiring long-term systemic corticosteroid treatment, too rapid a decrease in systemic corticosteroids may cause a severe exacerbation of their symptoms

Drug interactions overview

• Caution should be exercised when considering the coadministration of this drug with ketoconazole and other known strong CYP3A4 inhibitors (eg, ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, saquinavir, telithromycin) because adverse effects related to increased systemic exposure to budesonide may occur

Pregnancy

Adverse events (eg, hypoadrenalism) observed with systemic corticosteroids in animal reproduction studies

Increased risk of abnormalities has not been demonstrated in pregnant women using intranasal budesonide

Clinical considerations: Intranasal corticosteroids are recommended for allergic rhinitis during pregnancy

Lactation

Excreted in breast milk after oral inhalation (~0.3-1% of the maternal dose)

Plasma budesonide levels obtained from infants after breast-feeding were below the limit of quantification

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Anti-inflammatory corticosteroid that elicits potent glucocorticoid activity (week mineralocorticoid activity)

Corticosteroids have a wide range of inhibitory activities against multiple cell types (eg, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (eg, histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic and nonallergic-mediated inflammation

Absorption

Bioavailability: Low (~10% PO); 34% (nasal mucosa absorption)

Peak Plasma Time: 0.5 hr

Peak Plasma Concentration: 0.3 nmol/L

Distribution

Protein Bound: 85-90%

Vd: 2-3 L/kg

Metabolism

Metabolized by CYP3A4

Metabolites: 16-alpha-hydroxyprednisolone; 6-beta-hydroxybudesonide (negligible activity)

Elimination

Half-life, terminal: 2-3 hr

Total body clearance: 1-1.4 L/min

Excretion: as metabolites in feces (33%) and urine (66%)