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beclomethasone; meclometasone (Vancenase, Beconase, Vanceril, Beclovent, Qvar)

Tradenames: Vanceril, Beclovent. Indications: 1) treatment of asthma (inhaler) - chronic obstructive pulmonary disease [7] 2) relief of rhinitis (nasal spray) 3) prevention of recurrence of nasal polyps following surgical removal Contraindications: 1) status asthmaticus 2) hypersensitivity to beclomethasone, fluorocarbons or oleic acid in the formula Dosage: 1) inhaler: 2 puffs TID/QID., 42 ug/inhalation. 16.8 g - Qvar: 40 & 80 ug/inhalation; uses non-ozone-depleting hydrofluorohydrocarbons; smaller particle size; no spacer needed 2) nasal spray: inhalation in affected nostril(s) BID-QID 42 ug/inhalation. 16.8 g. Pharmacokinetics: 1) inhaler: a) some improvement may occur within 1 week b) general 1-4 weeks required for significant improvement 2) nasal spray: onset of action - relief of symptoms generally occurs within a few days, but may take as long as 2 weeks 3) 3 major metabolites are formed via CYP3A catalyzed-biotransformation of beclomethasone-17-dipropionate - beclomethasone-17-monopropionate (most active metabolite) - beclomethasone-21-monopropionate - beclomethasone [8] 4) lung slices metabolize beclomethasone-17-monopropionate rapidly to beclomethasone-17-monopropionate & more slowly to beclomethasone. 5) protein binding is 94-96% 6) the major route of elimination of inhaled beclomethasone-17-dipropionate appears to be via hydrolysis - mean elimination 1/2 life is 2.8 hours - metabolites of beclomethasone-17-dipropionate are eliminated in feces [8] Adverse effects: 1) Vanceril a) systemic absorption is low b) if correct technique is not used, hypothalamic-pituitary-adrenal function c) oral thrush is common especially if patients do not rinse after use d) irritation: cough, hoarseness, xerostomia e) rare (< 1%) - skin rash, bronchospasm, difficulty swallowing 2) Vancenase, Beconase a) irritation of nasal mucosa b) epistaxis c) rare (< 1%) - headache, rhinorrhea, nasal stuffiness, sneezing, nasal ulceration & septal perforation Laboratory: - beclomethasone dipropionate in serum/plasma - beclomethasone dipropionate in urine Mechanism of action: - nasal preparation a) does NOT inhibit IgE synthesis or mast cell degranulation b) inhibits cytokine production, arachidonate metabolism, inflammation & mast cell proliferation

Interactions

drug interactions drug adverse effects (more general classes) monitor with drug (more general classes)

General

antiasthmatic agent glucocorticoid

Properties

MISC-INFO: elimination route LIVER pregnancy-category C safety in lactation - ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 85
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
  6. Prescriber's Letter 7(11):64 2000
  7. Deprecated Reference
  8. Highlights of Prescribing information QVAR (beclomethasone dipropionate HFA 40& 80 mcg), Inhalation https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020911s025lbl.pdf

Component-of

beclomethasone/calcipotriene (Taclonex)