Brands, Medical Use, Clinical Data
- Bronchodilator Agents
- Anti-inflammatory Agents
- Capsule (sustained-release)
- Metered-dose (aerosol)
Brands / Synonyms
Bidien; Budeson; Budesonide, Pharma; Cortivent; Desonide; Desowen; Entocort; Entocort EC; Micronyl; Preferid; Pulmicort; Pulmicort Nebuamp; Pulmicort Respules; Pulmicort Turbuhaler; Rhinocort; Rhinocort Aqua; Rhinocort Turbuhaler; Spirocort; Tridesilon
For the treatment of mild to moderate active Crohn's disease.
Budesonide is a synthetic corticosteroid indicated for the treatment of mild to moderate active Crohn's disease involving the ileum and/or the ascending colon. Budesonide is 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.
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.
Side effects include headache, respiratory infection, nausea, back pain, dyspepsia, dizziness, abdominal pain, flatulence, vomiting, fatigue
Biotrnasformation / Drug Metabolism
Rapidly and extensively biotransformed, mainly by CYP3A4
ENTOCORT EC is contraindicated in patients with known hypersensitivity to budesonide.
Concomitant oral administration of ketoconazole (a known inhibitor of CYP3A4 activity in the liver and in the
intestinal mucosa) caused an eight-fold increase of the systemic exposure to oral budesonide. If treatment with
inhibitors of CYP3A4 activity (such as ketoconazole, intraconazole, ritonavir, indinavir, saquinavir, erythromycin,
etc.) is indicated, reduction of the budesonide dose should be considered. After extensive intake of grapefruit juice
(which inhibits CYP3A4 activity predominantly in the intestinal mucosa), the systemic exposure for oral budesonide
increased about two times. As with other drugs primarily being metabolized through CYP3A4, ingestion of grapefruit or
grapefruit juice should be avoided in connection with budesonide administration.