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

Cautions

Reports of epistaxis, Candida albicans infections, nasal septal perforation, and impaired wound healing; avoid with recent nasal ulcers, surgery, or trauma

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

Potential worsening of infections (eg, existing tuberculosis, fungal bacterial, viral, or parasitic infections; or ocular herpes simplex); more serious or even a fatal course of chickenpox or measles can occur in susceptible patients

Hypercorticism and adrenal suppression may occur with very high dosages or at the regular dose in susceptible individuals

Because of potential for HPA-axis suppression, monitor growth of pediatric patients

May increase risk for glaucoma and cataracts

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%)