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Budesonide


Budesonide
Systematic (IUPAC) name
16,17-(butylidenebis(oxy))-11,21-dihydroxy-, (11-β,16-α)-pregna-1,4-diene-3,20-dione
Identifiers
CAS number	51333-22-3
ATC code	A07EA06 D07AC09, R01AD05, R03BA02
PubChem	63006
DrugBank	APRD00442
Chemical data
Formula	C₂₅H₃₄O₆
Mol. mass	430.534 g/mol
Pharmacokinetic data
Bioavailability	100% (but large first pass effect)
Protein binding	85-90%
Metabolism	Hepatic CYP3A4
Half life	2.0-3.6 hours
Excretion	Renal, Faecal
Therapeutic considerations
Pregnancy cat.	C(US)
Legal status	POM(UK)
Routes	Oral, Nasal, tracheal, rectal

Budesonide is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis. Additionally, it is used for inflammatory bowel disease. It is marketed by AstraZeneca as a nasal inhalation with the brand name Rhinocort (in Denmark, as Rhinosol), as an oral inhalation with the brand name Pulmicort, and as an enema and a modified-release capsule with the brand name Entocort. It is also sold in combination with formoterol (Oxis) in a single inhaler, with the brand name Symbicort.

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Pharmacology

Budesonide has a high first pass metabolism. It has efficacy in the terminal ileum and the right colon. Budesonide in comparison with prednisolone has been associated with fewer bone density losses and unlike other corticosteroids has little influence on the hypothalamic-pituitary-adrenal axis which also limit the need of tapering before discontinuation. Overall, it has a lower incidence of systemic manifestations than similar medications.

Side Effects

Budesonide may cause:

nose irritation or burning
bleeding or sores in the nose
lightheadedness
upset stomach
cough
hoarseness
dry mouth

In addition the following should be reported:

Immediately if difficulty breathing or swelling of the face
white patches in the throat, mouth, or nose
irregular menstrual periods
severe acne

Recall

Pulmicort inhalers were recalled in 2002 because there was concern that they may not always have provided the full dosage.

v • d • e Antidiarrheals, intestinal anti-inflammatory/anti-infective agents (A07)
Intestinal anti-infectives	Antibiotics (Neomycin, Nystatin, Natamycin, Streptomycin, Polymyxin B, Paromomycin, Amphotericin B, Kanamycin, Vancomycin, Colistin, Rifaximin) Sulfonamides (Phthalylsulfathiazole, Sulfaguanidine, Succinylsulfathiazole) other (Miconazole, Broxyquinoline, Acetarsol, Nifuroxazide, Nifurzide)
Intestinal adsorbents	Charcoal - Bismuth - Pectin - Kaolin - Crospovidone - Attapulgite - Diosmectite
Antipropulsives	Diphenoxylate - Opium - Loperamide - Difenoxin
Intestinal anti-inflammatory agents	corticosteroids acting locally (Prednisolone, Hydrocortisone, Prednisone, Betamethasone, Tixocortol, Budesonide, Beclometasone) antiallergic agents, excluding corticosteroids (Cromoglicic acid) aminosalicylic acid and similar agents (Sulfasalazine, Mesalazine, Olsalazine, Balsalazide)
Antidiarrheal micro-organisms	Saccharomyces boulardii
Other antidiarrheals	Albumin tannate - Ceratonia - Racecadotril

v • d • e Decongestants and other nasal preparations (R01)
Topical: sympathomimetics, plain	Cyclopentamine - Ephedrine - Phenylephrine - Oxymetazoline - Tetryzoline - Xylometazoline - Naphazoline - Tramazoline - Metizoline - Tuaminoheptane - Fenoxazoline - Tymazoline - Epinephrine
Topical: antiallergic agents, excluding corticosteroids	Cromoglicic acid - Levocabastine - Azelastine - Antazoline - Spaglumic acid - Thonzylamine - Nedocromil - Olopatadine
Topical: corticosteroids	Beclometasone - Prednisolone - Dexamethasone - Flunisolide - Budesonide - Betamethasone - Tixocortol - Fluticasone - Mometasone furoate - Triamcinolone
Topical: other nasal preparations	Calcium hexamine thiocyanate - Retinol - Ipratropium bromide - Ritiometan - Mupirocin - Hexamidine - Framycetin
Systemic use: Sympathomimetics	Phenylpropanolamine - Pseudoephedrine - Phenylephrine

v • d • e Drugs for obstructive airway diseases: asthma/COPD (R03)
Adrenergics, inhalants	Short acting β₂-agonists: Salbutamol/Levosalbutamol • Fenoterol • Terbutaline Long acting β₂-agonists (LABA): Bambuterol • Clenbuterol • Formoterol • Salmeterol other: Epinephrine • Isoproterenol • Orciprenaline
Glucocorticoids	Beclometasone • Budesonide • Ciclesonide • Fluticasone • Mometasone
Anticholinergics	Ipratropium • Tiotropium
Mast cell stabilizers	Cromoglicate • Nedocromil
Xanthines	Aminophylline • Theobromine • Theophylline
Leukotriene antagonists	Montelukast • Pranlukast • Zafirlukast
Combination products	Budesonide/formoterol • Fluticasone/salmeterol • Ipratropium/salbutamol

v • d • e

Corticosteroids - glucocorticoid/receptor and mineralocorticoid/receptor
(A07EA, C05AA, D07, D10AA, H02, R01AD, R03BA, S01BA, S02B, and S03B)

Endogenous

Aldosterone, Cortisone, Hydrocortisone/cortisol, Desoxycortone

Others

Alclometasone, Amcinonide, Beclometasone, Betamethasone, Budesonide, Ciclesonide, Clobetasol, Clobetasone, Clocortolone, Cloprednol, Cortivazol, Deflazacort, Deoxycorticosterone, Desonide, Desoximetasone, Dexamethasone, Diflorasone, Diflucortolone, Difluprednate, Fluclorolone, Fludrocortisone, Fludroxycortide, Flumetasone, Flunisolide, Fluocinolone acetonide, Fluocinonide, Fluocortin, Fluocortolone, Fluorometholone, Fluperolone, Fluprednidene, Fluticasone, Formocortal, Halcinonide, Halometasone, Hydrocortisone aceponate, Hydrocortisone buteprate, Hydrocortisone butyrate, Loteprednol, Medrysone, Meprednisone, Methylprednisolone,Methylprednisolone aceponate, Mometasone furoate, Paramethasone, Prednicarbate, Prednisone, Prednisolone, Prednylidene, Rimexolone, Tixocortol, Triamcinolone, Ulobetasol

Categories: Glucocorticoids | Asthma

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Budesonide". A list of authors is available in Wikipedia.