Budesonide

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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, the most effective and safe medicines needed in a health system. Some forms are available as a generic medication. The wholesale price in the developing world for an inhaler containing 200 doses is about US$5 to US$7 as of 2014. As of 2015 the cost for a typical month of the inhaler medication in the United States is US$100 to US$200.

Video Budesonide

Medical uses

Asthma

Budesonide is nebulized 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 3 months (but not longer) of maintenance of remission Crohn's disease.

Budesonide assists in the induction of remission in people with active ulcerative colitis.

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.

Allergic rhinitis

Nasal spray budesonide is a treatment for allergic rhinitis.

Maps Budesonide

Side effects

Budesonide may cause:

• Nose irritation or burning
• Bleeding or sores in the nose
• Lightheadedness
• Upset stomach
• Cough
• Hoarseness
• Dry mouth
• Rash
• 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)

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Contraindications

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.

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Interactions

Those taking tablets or capsules orally should avoid grapefruit juice and echinacea.

• Grapefruit juice may double bioavailability of oral budesonide.
• Echinacea diminishes bioavailability.

Also, high fat meals delay absorption but do not impede absorption.

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Pharmacology

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.

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Pharmacokinetics

• Onset of action: Nebulization: 2-8 days; Inhalation: 24 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.

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Chemistry

Budesonide, also known as 11?,21-dihydroxy-16?,17?-(butylidenebis(oxy))pregna-1,4-diene-3,20-dione, is a synthetic pregnane steroid and non-halogenated cyclic ketal corticosteroid. It is the C16? hydroxyl, C16?,17? cyclic ketal with butyraldehyde derivative of prednisolone (11?,17?,21-trihydroxypregna-1,4-diene-3,20-dione).

Stereoisomerism

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Society and culture

Brand names

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); 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)

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See also

• Azelastine
• Fluticasone propionate

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References

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External links

• Entocort EC Prescribing information Prometheus Laboratories (PDF)
• Budesonide Oral (Entocort EC) MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine
• Budesonide Nasal Spray (Rhinocort) MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine
• Budesonide Oral Inhalation (Symbicort) MedlinePlus, National Institutes of Health (NIH), U.S. National Library of Medicine

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