Beclomethasone

Therapeutic Class
Corticosteroid
Indications

Oral inhalation: Maintenance and prophylactic treatment of asthma; includes those who require corticosteroids and those who may benefit from a dose reduction/elimination of systemically-administered corticosteroids. Not for relief of acute bronchospasm

Adult Doses

Nasal inhalation and oral inhalation dosage forms are not to be used interchangeably.

Asthma: 

Inhalation, oral (doses should be titrated to the lowest effective dose once asthma is controlled)

Initial dose 40-80 mcg twice daily; maximum dose 320 mcg twice day

NIH Asthma Guidelines (NIH, 2007): Administer in divided doses:

“Low” dose: 80-240 mcg/day

“Medium” dose: >240-480 mcg/day

“High” dose: >480 mcg/day

Pediatric Doses

Asthma:
Inhalation, oral (doses should be titrated to the lowest effective dose once asthma is controlled)
Children 5-11 years
Initial: 40 mcg twice daily;
maximum dose: 80 mcg twice daily

Children ≥12 years: Refer to adult dosing

Contraindications

Hypersensitivity to beclomethasone or any component of the formulation; status asthmaticus

Warnings / Precautions

Not to be used in status asthmaticus or for the relief of acute bronchospasm.
long-term use has been associated with fluid retention and hypertension; take precaution in heart failure patients, hepatic impairment, including cirrhosis, renal impairment.

Adrenal suppression: May cause hypercorticism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods.
Osteoporosis:  high doses and/or long-term use of corticosteroids have been associated with increased bone loss and osteoporotic fractures especially on oral treatment.
Myasthenia gravis: exacerbation of symptoms may occur especially during initial treatment with corticosteroids.
Myocardial infarct (MI): corticosteroids have been associated with myocardial rupture.
Immunosuppression: Prolonged use of corticosteroids may also increase the incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to vaccines.
Bronchospasm: May occur with wheezing after inhalation
Psychiatric disturbances: Corticosteroid use may cause psychiatric disturbances, including depression, euphoria, insomnia, mood swings, and personality changes.
Kaposi's sarcoma: Case reports shows that prolonged treatment with corticosteroids has been associated with the development of Kaposi's sarcoma .
Diabetes:  May alter glucose production/regulation leading to hyperglycemia.
Gastrointestinal disease: Risk of perforation in patient with GI diseases (diverticulitis, peptic ulcer, ulcerative colitis).
Seizure disorders: case reports show that adrenal crisis can lead to seizure.
Thyroid disease: metabolic clearance of corticosteroids increases in hyperthyroid patients and decreases in hypothyroid ones.
Children: Orally-inhaled corticosteroids may cause a reduction in growth velocity in pediatric patients.
Withdraw systemic therapy with gradual tapering of dose, otherwise withdrawal symptoms (eg, joint/muscle pain, lassitude, depression) may occur.

Adverse Reactions

Central nervous system: Agitation, depression, dizziness, dysphonia, headache, lightheadedness, mental disturbances

Dermatologic: Acneiform lesions, angioedema, atrophy, bruising, pruritus, purpura, striae, rash, urticaria

Endocrine & metabolic: Cushingoid features, growth velocity reduction in children and adolescents, HPA function suppression

Gastrointestinal: Dry/irritated nose, throat and mouth, hoarseness, localized Candida or Aspergillus infection, loss of smell, loss of taste, nausea, unpleasant smell, unpleasant taste, vomiting, weight gain

Ocular: Cataracts, glaucoma, intraocular pressure increased

Respiratory: Cough, paradoxical bronchospasm, pharyngitis, sinusitis, wheezing

Miscellaneous: Anaphylactic/anaphylactoid reactions, death (due to adrenal insufficiency, reported during and after transfer from systemic corticosteroids to aerosol in asthmatic patients), immediate and delayed hypersensitivity reactions

Mechanism of Actions

Controls the rate of protein synthesis; depresses the migration of polymorphonuclear leukocytes, fibroblasts; reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation.

Pharmacodynamics

Onset of action: Therapeutic effect: 1-4 weeks
Absorption: Readily; quickly hydrolyzed by pulmonary esterases to active metabolite (beclomethasone-17-monoproprionate [17-BMP]) prior to absorption
Distribution: Beclomethasone dipropionate (BDP): 20 L; 17-BMP: 424 L
Protein binding: 17-BMP: 94% to 96%
Metabolism: Pro-drug; undergoes rapid conversion to 17-BMP during absorption; followed by additional metabolism via CYP3A4 to other, less active metabolites (beclomethasone-21-monopropionate [21-BMP] and beclomethasone [BOH])
Half-life elimination: BDP: 0.5 hours; 17-BMP: 3 hours
Time to peak, plasma: Oral inhalation: BDP: 0.5 hours; 17-BMP: 0.7 hours
Excretion: Feces (60%); urine (<10% to 12%)

 

Administration

Rinse mouth and throat after use to prevent Candida infection. Do not wash or put inhaler in water; mouth piece may be cleaned with a dry tissue or cloth. Prime canister before using.

Pregnancy Category

C: Drug Pregnancy Category Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

ATC Classification
A07EA07,D07AC15,R01AD01,R03BA01
GenericPedia Classification
  • Available As
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