beclomethasone, intranasal (Rx)

>10%

Nasopharyngeal irritation (24%)

1-10%

Headache (<5%)

Nausea (<5%)

Lightheadedness (<5%)

Sneezing attacks after administration (4%)

Nasal congestion (<3%)

Nose bleeds (<3%)

Rhinorrhea (<3%)

Increased lacrimation (<3%)

Epistaxis (<3%)

Frequency Not Defined

Nasal mucosa ulceration

Nasal septum perforation

Postmarketing Reports

Blurred vision, glaucoma, cataracts, central serous chorioretinopathy (CSC), loss of taste and smell, hypersensitivity reactions, angioedema, rash, urticaria, and bronchospasm

Contraindications

Hypersensitivity

Cautions

Larger than recommended doses should be avoided

Monitor for vision change, or with history of increased IOP, glaucoma, or cataracts; consider referral to ophthalmologist in patients who develop ocular symptoms

Potential worsening of existing tuberculosis, fungal, bacterial, viral, or parasitic infections, or ocular herpes simplex

Risk for hypercorticism and adrenal suppression with higher than normal doses

Potential reduction of growth velocity in children

Prolonged corticosteroid use may result in elevated IOP, glaucoma, and/or cataracts

Nasal septal perforation and localized Candida albicans infections of the nose and/or pharynx may occur; when such an infection develops, it may require treatment with appropriate local therapy and discontinuation of treatment

During withdrawal from oral corticosteroids, some patients may experience symptoms of withdrawal, eg, joint and/or muscular pain, lassitude, and depression

If persistent nasopharyngeal irritation occurs, it may be an indication for stopping therapy

As with any long-term treatment, patients this nasal spray therapy over several months or longer should be examined periodically for possible changes in the nasal mucosa

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

Careful attention must be given when patients previously treated for prolonged periods with systemic corticosteroids are transferred to this drug formulation; this is particularly important in those patients who have associated asthma or other clinical conditions where too rapid a decrease in systemic corticosteroids may cause severe exacerbation of their symptoms

If recommended doses of intranasal beclomethasone are exceeded or if individuals are particularly sensitive or predisposed by virtue of recent systemic steroid therapy, symptoms of hypercorticism may occur, including very rare cases of menstrual irregularities, acneiform lesions, cataracts, and cushingoid features; if such changes occur, therapy should be discontinued slowly consistent with accepted procedures for discontinuing oral steroid therapy

For therapy to be effective in treatment of nasal polyps, the spray must be able to enter nose; therefore, treatment of nasal polyps with this product should be considered adjunctive therapy to surgical removal and/or use of other medications that will permit effective penetration of the drug into the nose; nasal polyps may recur after any form of treatment

Immune suppression

• Persons who are using drugs that suppress the immune system are more susceptible to infections than healthy individuals; chickenpox and measles, for example, can have more serious or even fatal course in susceptible children or adults using corticosteroids
• In 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, prophylaxis with varicella zoster immune globulin (VZIG) 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

Pregnancy

There are no adequate and well-controlled studies in pregnant women; this drug should be used during pregnancy only if potential benefit justifies potential risk to fetus

Hypoadrenalism may occur in infants born of mothers receiving corticosteroids during pregnancy; such infants should be carefully observed

Animal data

• Like other corticosteroids, beclomethasone dipropionate was teratogenic and embryocidal in the mouse and rabbit at a subcutaneous dose of 0.1 mg/kg in mice or 0.025 mg/kg in rabbits (approximately equal to the maximum recommended daily intranasal dose in adults on a mg/m2 basis)
• No teratogenicity or embryocidal effects were seen in rats when exposed to an inhalation dose of 0.1 mg/kg plus oral doses of up to 10 mg/kg per day for a combined dose of 10.1 mg/kg (approximately 240 times the maximum recommended daily intranasal dose in adults on a mg/m2 basis)

Lactation

It is not known whether beclomethasone dipropionate is excreted in human milk; because other corticosteroids are excreted in human milk, exercise caution when this drug is administered to a nursing woman

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

Corticosteroid with potent anti-inflammatory properties; elicits effects on various cells, including mast cells and eosinophils; also elicits effects on inflammatory mediators (eg, histamine, eicosanoids, leukotrienes, cytokines)

Absorption

Bioavailability: 44% (43% from swallowing portion of intranasal dose; 1% from nasal absorption)

Peak Plasma Concentration: Undetectable (<50 pg/mL)

Distribution

Protein Bound: 87%

Vd: 20 L; 424 L for B-17-MP metabolite

Metabolism

Metabolites: B-17-MP active metabolite

Metabolized by: Esterase enzymes found in most tissues

Elimination

Half-life: 0.3 hr

Excretion: feces (60%), urine (12%); after oral administration