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Budesonide volume of distribution
Tablet and capsule, healthy subjects and patients = 2.2 – 3.9 L/kg; Powder, metered = 3 L/kg
Discount Cards 16,000+
Clients Benefit 29%
Total savings $4,735,080
What is Budesonide
Budesonide is a glucocorticoid used in the management of asthma, the treatment of various skin disorders, and allergic rhinitis. The extended release oral tablet, marketed as Uceris, was FDA approved on January 14, 2013 for the management of ulcerative colitis. Budesonide is provided as a mixture of two epimers (22R and 22S). Interestingly, the 22R form is two times more active than the 22S epimer. The two forms do not interconvert.
Budesonide mechanism of action
Budesonide is an anti-inflammatory corticosteroid that exhibits potent glucocorticoid activity and weak mineralocorticoid activity. The precise mechanism of corticosteroid actions on inflammation in asthma, Crohn’s disease, or ulcerative colitis is not known. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of inhibitory activities against multiple cell types (eg, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (eg, histamine, eicosanoids, leukotrienes, and cytokines) involved in allergic and non-allergic-mediated inflammation. These anti-inflammatory actions of corticosteroids may contribute to their efficacy in the aforementioned diseases. Because budesonide undergoes significant first-pass elimination, the both oral preparations are formulated as an extended release tablet. As a result, budesonide release is delyaed until exposure to a pH . 7 in the small intestine.
Dosage forms of Budesonide
|Budesonide||100mcg||165doses Nasal Spray Solution||$36.00|
|Budesonide||3mg||100 Controlled Release Capsule||$82.00|
|Budesonide||200mcg||200ds Dry Powder Inhaler||$45.00|
|Pulmicort Nebules||1mg/2mL||20 Neb Ampules||$66.10|
|Rhinocort Turbuhaler||100mcg||200doses Aerosol (Breath activated)||$57.00|
|Rhinocort Aqua Nasal Spray||32mcg||120doses Nasal Spray Solution||$158.00|
|Entocort EC||3mg||100 Controlled Release Capsule||$206.00|
|Entocort Enema||0.02mg/mL||28 Tablet||$370.00|
|Pulmicort Turbuhale||400mcg||100doses Dry Powder Inhaler||$62.00|
|Uceris||9mg||30 Extended Release Tablet||$750.00|
|Symbicort Turbuhaler||160/4.5mcg||360doses Dry Powder Inhaler||$120.9|
|Symbicort Inhaler||200/6mcg||120doses Aerosol Inhaler||$76.90|
Par Pharmaceutical Inc.
Humans and other mammals
Indication of Budesonide
The oral capsule is used for the treatment of mild to moderate active Crohn’s disease. The oral tablet is used for induction of remission in patients with active, mild to moderate ulcerative colitis. The oral inhalation formulation is used for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis.
Toxicity of Budesonide
Single oral doses of 200 and 400 mg/kg were lethal in female and male mice, respectively. The signs of acute toxicity were decreased motor activity, piloerection and generalized edema.
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