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Additional information about the drug Budesonide


Budesonide ( BUD ), sold under the brand name Pulmicort among others, is a medication of the corticosteroid type.
Common side effects with the inhaled form include respiratory infections, cough, and headaches.
Budesonide was initially patented in 1973.
Contents
1 Medical uses
1.1 Asthma
1.2 Inflammatory bowel disease
1.3 Allergic rhinitis
2 Side effects
3 Contraindications
4 Interactions
5 Pharmacology
6 Pharmacokinetics
7 Chemistry
7.1 Stereoisomerism
8 Society and culture
8.1 Brand names
9 See also
10 References
11 External links
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.
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.
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)
Contraindications
Budesonide is contraindicated as a primary treatment of status asthmaticus or other acute episode of asthma where intensive measures are required.
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.
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.
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.
Chemistry
See also: List of corticosteroids and List of corticosteroid cyclic ketals
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.
Stereoisomerism
Budesonide (2 stereoisomers)
(22 R )-configuration
(22 S )-configuration
Society and culture
Brand names
Inhaler for a powder based in budesonide and formoterol
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)
See also
Azelastine
Fluticasone propionate

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