From the Guidelines
Oral budesonide works as a corticosteroid medication that reduces inflammation in the body by suppressing the immune system's inflammatory response. When taken orally, budesonide is absorbed in the gastrointestinal tract and acts locally on the intestinal mucosa, with minimal systemic absorption due to its high first-pass metabolism in the liver. This medication binds to glucocorticoid receptors within cells, inhibiting the production of inflammatory mediators such as cytokines, prostaglandins, and leukotrienes. Budesonide is commonly prescribed for inflammatory bowel conditions like Crohn's disease and ulcerative colitis, typically at doses of 9 mg once daily for induction of remission, followed by maintenance doses of 6 mg daily, as shown in studies such as the CORE I and CORE II studies 1. Treatment duration varies based on the condition and response, often ranging from 8-12 weeks initially. Patients should take the medication in the morning with or without food, swallow capsules whole without chewing, and taper off gradually rather than stopping abruptly to avoid withdrawal symptoms. Side effects are generally milder than systemic corticosteroids but may include headache, nausea, respiratory infections, and with long-term use, potential adrenal suppression. Some key points to consider when prescribing oral budesonide include:
- The medication's efficacy in inducing remission in mild to moderate ulcerative colitis, as demonstrated in studies such as the CORE I and CORE II studies 1
- The importance of gradual tapering to avoid withdrawal symptoms, as recommended in guidelines such as the British Society of Gastroenterology consensus guidelines 1
- The potential for oral budesonide to be used as an alternative first-line therapy to induce complete remission in patients with mild to moderate UC, as suggested in the Toronto consensus guidelines 2
- The need for careful evaluation of patients for lack of symptomatic response to corticosteroid induction therapy within 2 weeks, as recommended in guidelines such as the Toronto consensus guidelines 3
From the FDA Drug Label
Budesonide has a high topical glucocorticosteroid (GCS) activity and substantial first-pass elimination. The formulation contains budesonide in an extended-release tablet core. The tablet core is enteric coated to protect dissolution in gastric juice which delays budesonide release until exposure to a pH ≥ 7 in the small intestine Upon disintegration of the coating, the core matrix provides extended release of budesonide in a time dependent manner.
Oral budesonide works by having a high glucocorticoid effect and a weak mineralocorticoid effect. Its affinity to GCS receptors is about 200-fold that of cortisol and 15-fold that of prednisolone. The drug is associated with a suppression of endogenous cortisol concentrations and an impairment of the hypothalamus-pituitary-adrenal (HPA) axis function. 4 5 6
From the Research
Mechanism of Action
- Oral budesonide is a glucocorticoid with high topical activity and low systemic bioavailability, resulting in reduced systemic effects compared to other glucocorticoids 7.
- It has potent local anti-inflammatory effects and limited systemic bioavailability due to high first-pass hepatic metabolism 8, 9, 10.
- The mechanism of budesonide action allows for local, selective treatment of the gastrointestinal tract and the liver, minimizing systemic exposure 10.
Therapeutic Effects
- Oral budesonide is effective in treating mild to moderate active ileocecal Crohn's disease, microscopic colitis, ulcerative colitis, and non-cirrhotic autoimmune hepatitis 10.
- It produces clinical remission in 42 to 67% of patients with active Crohn's disease of the ileum, ileocaecal region, and/or ascending colon 7.
- Budesonide has similar efficacy to prednisolone in treating inflammatory bowel disease 7.
- Maintenance treatment with oral budesonide increases the duration of remission in patients with Crohn's disease, but does not appear to affect the 1-year relapse rate 7.
Safety and Efficacy
- Oral budesonide has a low incidence of adverse glucocorticoid-related effects, making it a favorable option for the treatment of acute exacerbations of inflammatory bowel disease 7.
- It may also be a useful agent for longer-term maintenance therapy, with low-dose budesonide not appearing to have adverse safety implications other than slight reductions in cortisol levels on rare occasions 10.
- Budesonide is not effective in maintaining remission in patients with Crohn's disease 11.