|Trade names||Qvar, Beconase AQ, others|
|Other names||Beclomethasone (USAN); Beclometasone dipropionate; Beclomethasone dipropionate|
|Main uses||Asthma, allergic rhinitis, nasal polyps|
|Inhalation, nasal, topical|
|Defined daily dose||0.8 mg (Inhalation aerosol) or|
0.8 mg (Inhalation powder) or
1.5 mg (Inhalation solution)
|Bioavailability||Converted to beclometasone-17-monopropionate (17-BMP) during absorption|
|Protein binding||87% of 17-BMP to albumin and transcortin|
|Metabolism||By esterase enzymes found in most tissues|
|Elimination half-life||2.8 hours|
|Excretion||Biliary (60%), renal (12%)|
|Chemical and physical data|
|Molar mass||521.05 g·mol−1|
|3D model (JSmol)|
|Melting point||117 to 120 °C (243 to 248 °F) (dec.)|
|(what is this?)|
Beclometasone, also known as beclometasone dipropionate, and sold under the brand name Qvar among others, is a steroid medication. It is available as an inhaler, cream, pills, and nasal spray. The inhaled form is used in the long-term management of asthma. The cream may be used for dermatitis and psoriasis. The pills have been used to treat ulcerative colitis. The nasal spray is used to treat allergic rhinitis and nasal polyps.
Common side effects with the inhaled form include respiratory infections, headaches, and throat inflammation. Serious side effects include an increased risk of infection, cataracts, Cushing's syndrome, and severe allergic reactions. Long-term use of the pill form may cause adrenal insufficiency. The pills may also cause mood or personality changes. The inhaled form is generally regarded as safe in pregnancy. Beclometasone is mainly a glucocorticoid.
Beclometasone dipropionate was first patented in 1962 and used medically in 1972. It was approved for medical use in the United States in 1976. It is on the World Health Organization's List of Essential Medicines. The wholesale price in the developing world for an inhaler containing 200 doses of medication is about US$3.20 as of 2014. In the United States it costs US$50–100 for a typical month supply of the inhaled form. In 2017, it was the 153rd most commonly prescribed medication in the United States, with more than four million prescriptions.
The defined daily dose is 0.8 mg (Inhalation aerosol) or 0.8 mg (Inhalation powder) or 1.5 mg (Inhalation solution) In adults the dose may be 100 to 500 micrograms twice per day while in children 50 to 200 micrograms twice per day may be used.
Common side effects with the inhaled form include respiratory infections, headaches, and throat inflammation. Serious side effects include an increased risk of infection, cataracts, Cushing's syndrome, and severe allergic reactions. Long-term use of the pill form may cause adrenal insufficiency. The pills may also cause mood or personality changes. The inhaled form is generally regarded as safe in pregnancy.
Occasionally, it may cause a cough upon inhalation. Deposition on the tongue and throat may promote oral candidiasis, which appears as a white coating, possibly with irritation. This may usually be prevented by rinsing the mouth with water after using the inhaler. Other adverse drug reaction side effects may rarely include: a smell similar to burning plastic, unpleasant taste, hoarseness or nasal congestion, pain or headache, and visual changes. Allergic reactions may occur, but rarely.
Beclometasone is mainly a glucocorticoid. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The activated glucocorticoid receptor-glucocorticoid complex up-regulates the expression of anti-inflammatory proteins in the nucleus (a process known as transactivation) and represses the expression of proinflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus (transrepression).
Beclometasone dipropionate is the INN modified and beclomethasone dipropionate is the USAN and former BAN. It is a prodrug of the free form, beclometasone (INN). The prodrug beclometasone is marketed in Norway and Russia.
Clenil, Qvar are brandnames for the inhalers. Beconase, Alanase, Vancenase, Qnasl for the nasal spray or aerosol.
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