|Trade names||Pulmicort, Rhinocort, Entocort, others|
|By mouth, nasal, tracheal, rectal, inhalation|
|Bioavailability||10-20% (first pass effect)|
|Elimination half-life||2.0-3.6 hours|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||430.541 g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Budesonide (BUD), sold under the brand name Pulmicort among others, is a medication of the corticosteroid type. It is available as an inhaler, pill, nasal spray, and rectal forms. The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease(COPD). The nasal spray is used for allergic rhinitis and nasal polyps. The pills in a delayed release form and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis and microscopic colitis.
Common side effects with the inhaled form include respiratory infections, cough, and headaches. Common side effects with the pills include feeling tired, vomiting, and joint pains. Serious side effects include an increased risk of infection, loss of bone strength, and cataracts. Long-term use of the pill form may cause adrenal insufficiency. Stopping the pills suddenly following long-term use may therefore be dangerous. The inhaled form is generally safe in pregnancy. Budesonide is mainly acting as a glucocorticoid.
Budesonide was initially patented in 1973. Commercial use as an asthma medication began in 1981. It is on the World Health Organization's List of Essential Medicines. Some forms are available as a generic medication. In 2019, generic budesonide was listed as involved in Teva's price fixing scheme in the United States. In 2017, it was the 190th most commonly prescribed medication in the United States, with more than three million prescriptions.
Budesonide is given by metered-dose inhaler or nebulizer for maintenance and prophylactic treatment of asthma including patients who require oral corticosteroids and those who may benefit from a systemic dose reduction.
Inflammatory bowel disease
Formulations of delayed-release budesonide are an effective treatment for mild-to-moderately active Crohn's disease involving the ileum and/or ascending colon. A Cochrane review found evidence for up to three months (but not longer) of maintenance of remission in Crohn's disease.
Budesonide is highly effective and recommended as the drug of choice in microscopic colitis, for induction and maintenance of remission, and for both the lymphocytic colitis and collagenous colitis forms.
Budesonide may cause:
- Nose irritation or burning
- Bleeding or sores in the nose
- Upset stomach
- Dry mouth
- Sore throat
- Bad taste in mouth
- Change in mucus
- Blurred vision 
In addition, the following symptoms should be reported immediately:
- Difficulty breathing or swelling of the face
- White patches in the throat, mouth, or nose
- Irregular menstrual periods
- Severe acne
- On rare occasions, behavioral changes (mostly affecting children)
Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required. It is also contraindicated for patients who have hypersensitivity to budesonide.
- Grapefruit juice may double bioavailability of oral budesonide.[medical citation needed]
- Echinacea diminishes bioavailability.[medical citation needed]
Also, high-fat meals delay absorption but do not impede absorption.[medical citation needed]
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Budesonide is an agonist of glucocorticoid receptors. Among its effects are:
- Controls the rate of protein synthesis.
- Depresses the migration of polymorphonuclear leukocytes and fibroblasts.
- Reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation.
- Has a potent glucocorticoid activity and weak mineralocorticoid activity.[medical citation needed]
- Onset of action: Nebulization: 2–8 days; Inhalation: 24 hours; Nasal: 10 hours
- Peak effect: Nebulization: 4–6 weeks; Inhalation: 1–2 weeks
- Distribution: 2.2-3.9 L/kg
- Protein binding: 85% to 90%
- Metabolism: Hepatic via CYP3A4 to two metabolites: 16 alpha-hydroxyprednisolone and 6 beta-hydroxybudesonide; minor activity
- Bioavailability: Limited by high first-pass effect; Capsule: 9% to 21%; Nebulization: 6%; Inhalation: 6% to 13%
- Half-life elimination: 2–3.6 hours
- Time to peak: Capsule: 0.5–10 hours (variable in Crohn's disease); Nebulization: 10–30 minutes; Inhalation: 1–2 hours; Tablet: 7.4-19.2 hours
- Excretion: urine (60%) and feces as metabolites.[medical citation needed]
Budesonide, also known as 11β,21-dihydroxy-16α,17α-(butylidenebis(oxy))pregna-1,4-diene-3,20-dione, is a synthetic pregnane steroid and non-halogenated cyclic ketal corticosteroid. It is the C16α hydroxyl, C16α,17α cyclic ketal with butyraldehyde derivative of prednisolone (11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione).
Society and culture
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Aeronide (TH); Aquacort (DE); B Cort (CO); Bronex (PH); Budair (MY); Budecort DP (MY); Budenofalk (DE, GB, HK, KP, PH, SG); Budeson (AR); Budeson Aqua (AR); BudeSpray (TH); Budiair (KP); Budicort Respules (IL); Budinide (KSA); Bunase (TH); Clebudan (CN); Cortiment (GB); Cycortide (HK); Denecort (PH); Duasma (TW); Eltair (MY); Entocort (AR, AT, BE, BR, CH, CZ, DK, FI, FR, GB, HK, IE, IL, IT, KP, NL, NO, PL, PT, SE, TR); Giona Easyhaler (MY, SG, TH); Inflammide (PE); Miflonid (CZ); Miflonide (BE, DE, IL, IT, NZ, PT); Neumocort (PY); Novopulmon (DE, FR); Pulmicon Susp for Nebulizer (KP); Pulmicort (AT, BE, BG, BR, CH, CL, CN, CO, CR, CZ, DE, DK, DO, EE, FI, FR, GB, GR, GT, HN, ID, IN, NI, NL, NO, PA, PK, PL, PT, RU, SE, SV, TR, TW, UY, VE, ZA); Pulmicort Nasal Turbohaler (CL, KE, MU, NG); Pulmicort Turbuhaler (KE, MU, NG); Rafton (FR); Rhinocort (AU); Rhinocort Aqua (HK); Rhinoside (GR); Symbicort (FR, US, ZA) Uceris (US)
During the 2020 pandemic, doctors and researchers observed that patients already prescribed inhaled corticosteroids appeared to develop less serious illness when diagnosed with COVID-19, despite often having conditions such as asthma that might be thought to lead to more serious illness. Subsequently, the drug was explored as a possible treatment for the disease. In June 2020, UK and Australian researchers began a UK-based trial of budesonide as an early-intervention treatment for COVID-19, with results expected in September of that year.
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