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QuickView for Budesonide (compound)

Summary
General Info

PubChem

PubChem Compound 3033890

PubChem Compound 3033890

Name:	Budesonide
PubChem Compound ID:	3033890
Description:	A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.
Molecular formula:	C₂₅H₃₄O₆
Molecular weight:	430.534 g/mol
Synonyms:	Budesonide; Preferid; Spirocort; Bidien; Entocort EC; Pregna-1,4-diene-3,20-dione, 16,17-butylidenebis(oxy)-11,21-dihydroxy-, (11beta,16alpha(R))-, and 16alpha,17-((S)-Butylidenebis(oxy))-11beta,21-dihydroxypregna-1,4-diene-3,20-dione; Budesonide (11beta,16alpha); Micronyl; Cortivent; Pulmicort. show more » Budesonide; Preferid; Spirocort; Bidien; Entocort EC; Pregna-1,4-diene-3,20-dione, 16,17-butylidenebis(oxy)-11,21-dihydroxy-, (11beta,16alpha(R))-, and 16alpha,17-((S)-Butylidenebis(oxy))-11beta,21-dihydroxypregna-1,4-diene-3,20-dione; Budesonide (11beta,16alpha); Micronyl; Cortivent; Pulmicort; Pregna-1,4-diene-3,20-dione, 16,17-(butylidenebis(oxy))-11,21-dihydroxy-, (11-beta,16-alpha)-; Rhinocort; CCRIS 5230; 16-alpha,17-alpha-Butylidenedioxy-11-beta,21-dihydroxy-1,4-pregnadiene-3,20-dione; 51333-22-3; Budesonido [INN-Spanish]; Budesonidum [INN-Latin]; Respules; (RS)-11beta,16alpha,17,21-Tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with butyraldehyde; Entocort; (11-beta,16-alpha)-16,17-(Butylidenebis(oxy))-11,21-dihydroxypregna-1,4-diene-3,20-dione; EINECS 257-139-7; Budeson; Budesonide [USAN:BAN:INN:JAN]; Rhinocort alpha; S 1320; Pregna-1,4-diene-3,20-dione,16,17-(butylidenebis(oxy))-11,21-dihydroxy-, (11beta,16alpha)- show less «

DrugBank

Identification

Name:	Budesonide
Name (isomeric):	DB01222
Drug Type:	small molecule
Description:	A glucocorticoid used in the management of ASTHMA, the treatment of various skin disorders, and allergic RHINITIS.
Brand:	Tridesilon, Pulmicort Respules, Budeson, Micronyl, Rhinocort Aqua, Spirocort, Desowen, Entocort EC, Bidien, Pulmicort Turbuhaler, Entocort, Preferid, Pulmicort, Cortivent, Pulmicort Nebuamp, Rhinocort Turbuhaler, Rhinocort
Brand name mixture:	Symbicort 100 Turbuhaler(Budesonide + Formoterol Fumarate Dihydrate), Symbicort 200 Turbuhaler(Budesonide + Formoterol Fumarate Dihydrate), Entocort Enema 0.02 Mg/Ml(Budesonide + Sodium Chloride)
Category:	Glucocorticoids, Bronchodilator Agents, Corticosteroids, Anti-inflammatory Agents
CAS number:	51333-22-3

Pharmacology

Indication:	For the treatment of mild to moderate active Crohn's disease. Also for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis.
Pharmacology:	Budesonide is a synthetic corticosteroid used in Crohn's disease to decrease the symptoms and inflammation associated with the disease, especially at times of flare up. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination. The formulation contains granules which are coated to protect dissolution ... show more » Budesonide is a synthetic corticosteroid used in Crohn's disease to decrease the symptoms and inflammation associated with the disease, especially at times of flare up. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first pass elimination. The formulation contains granules which are coated to protect dissolution in gastric juice, but which dissolve at pH >5.5, ie, normally when the granules reach the duodenum. Thereafter, a matrix of ethylcellulose with budesonide controls the release of the drug into the intestinal lumen in a time-dependent manner. show less «
Mechanism of Action:	The exact mechanism of action of budesonide in the treatment of Crohn's disease is not fully understood. However, being a glucocorticosteroid, budesonide has a high local anti-inflammatory effect.
Absorption:	Absorption is complete following oral administration.
Protein binding:	85-90%
Biotransformation:	Following absorption, budesonide is subject to high first pass metabolism (80-90%). In vitro experiments in human liver microsomes demonstrate that budesonide is rapidly and extensively biotransformed, mainly by CYP3A4, to its 2 major metabolites, 6b-hydroxy budesonide and 16a- hydroxy prednisolone. The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.
Route of elimination:	Budesonide is excreted in urine and feces in the form of metabolites.
Half Life:	2.0 and 3.6 hours
Clearance:	0.5 L/min [Athmatic children 4 to 6 years of age]
Toxicity:	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.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

A mean delay in time to peak concentration of 2.5 hours is observed with the intake of a high-fat meal, with no significant differences in AUC.

Drug interaction:

Conivaptan	CYP3A4 Inhibitors (Strong) may increase the serum concentration of Budesonide (Systemic, Oral Inhalation). onsider reducing the oral budesonide dose when used together with a strong CYP3A4 inhibitor. This interaction is likely less severe with orally inhaled budesonide. Any patient receiving both budesonide and a strong CYP3A4 inhibitor should be monitored closely for signs/symptoms of corticosteroid excess.
Telithromycin	Telithromycin may reduce clearance of Budesonide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Budesonide if Telithromycin is initiated, discontinued or dose changed.
Itraconazole	Itraconazole may increase levels/effect of budesonide.
Clotrimazole	CYP3A4 Inhibitors (Moderate) such as clotrimazole may increase the serum concentration of Budesonide (Systemic, Oral Inhalation). Consider reducing the oral budesonide dose when used together with a CYP3A4 inhibitor. This interaction is likely less severe with orally inhaled budesonide. Any patient receiving both budesonide and a moderate CYP3A4 inhibitor should be monitored closely for signs/symptoms of corticosteroid excess.
Bicalutamide	CYP3A4 Inhibitors like bicalutamide may increase the serum concentration of budesonide. The clinical significance of this interaction is greater for oral budesonide than for orally inhaled budesonide. Consider reducing the oral budesonide dose when used together with a CYP3A4 inhibitor.

Targets

Glucocorticoid receptor

Enzymes

Cytochrome P450 3A4