beclomethasone; meclometasone (Vancenase, Beconase, Vanceril, Beclovent, Qvar)
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Introduction
Tradenames: Vanceril, Beclovent.
Indications
- treatment of asthma (inhaler)
- relief of rhinitis (nasal spray)
- prevention of recurrence of nasal polyps following surgical removal
Contraindications
- status asthmaticus
- hypersensitivity to beclomethasone, fluorocarbons or oleic acid in the formula
Dosage
- 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
- nasal spray: inhalation in affected nostril(s) BID-QID 42 ug/inhalation. 16.8 g.
Pharmacokinetics
- inhaler:
- some improvement may occur within 1 week
- general 1-4 weeks required for significant improvement
- nasal spray: onset of action
- relief of symptoms generally occurs within a few days, but may take as long as 2 weeks
- 3 major metabolites are formed via CYP3A catalyzed-biotransformation of beclomethasone-17-dipropionate
- beclomethasone-17-monopropionate (most active metabolite)
- beclomethasone-21-monopropionate
- beclomethasone[8]
- lung slices metabolize beclomethasone-17-monopropionate rapidly to beclomethasone-17-monopropionate & more slowly to beclomethasone.
- protein binding is 94-96%
- 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]
elimination via liver
Adverse effects
- Vanceril
- systemic absorption is low
- if correct technique is not used, hypothalamic-pituitary-adrenal function
- oral thrush is common especially if patients do not rinse after use
- irritation: cough, hoarseness, xerostomia
- rare (< 1%)
- skin rash, bronchospasm, difficulty swallowing
- Vancenase, Beconase
- irritation of nasal mucosa
- epistaxis
- rare (< 1%)
Laboratory
Mechanism of action
- nasal preparation
- does NOT inhibit IgE synthesis or mast cell degranulation
- inhibits cytokine production, arachidonate metabolism, inflammation & mast cell proliferation
More general terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 85
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998 - not on National VA formulary
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Medical Knowledge Self Assessment Program (MKSAP) 11, American College of Physicians, Philadelphia 1998
- ↑ Prescriber's Letter 7(11):64 2000
- ↑ 7.0 7.1 Deprecated Reference
- ↑ 8.0 8.1 8.2 Highlights of Prescribing information QVAR <TM> (beclomethasone dipropionate HFA 40& 80 mcg), Inhalation https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/020911s025lbl.pdf
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2307
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=20469
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2308
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=657383
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=217100