Budesonide 9mg; extended-release tabs.
Induction of remission in patients with active, mild-to-moderate ulcerative colitis.
Uceris 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. Budesonide has a high topical glucocorticosteroid (GCS) activity and a substantial first-pass elimination. Treatment with a topical, locally-acting GCS may minimize side effects which are commonly observed with systemically active GCS (ie, suppression of endogenous cortisol concentrations, impairment of HPA axis function).
Two similarly-designed, randomized, double-blind, placebo-controlled studies were conducted in a total of 970 adult patients with active, mild-to-moderate ulcerative colitis (UC) which was defined as an Ulcerative Colitis Disease Activity Index (UCDAI of ≥4 and ≤10). UCDAI is a four-component scale (total score of 0–12) that encompasses the clinical assessments of stool frequency, rectal bleeding, mucosal appearance and physician’s rating of disease activity (score of 0–3 for each of the components). The baseline median UCDAI score in both of these studies was seven. Both studies compared Uceris 9mg and 6mg with placebo and included an active reference arm (a mesalamine 2.4g in Study 1; and a controlled ileal release budesonide 9mg not approved for the treatment of UC in Study 2). The primary endpoint was induction of remission after 8 weeks of treatment. Remission was defined as a UCDAI score of ≤1, with subscores of 0 for rectal bleeding, stool frequency, and mucosal appearance and with a ≥1 point reduction in an endoscopy-only score. For the primary endpoint, results in Study 1 showed that 17.9% in the Uceris 9mg group and 13.2% in the 6mg group compared with 7.4% in the placebo group achieved combined clinical and endoscopic remission. In Study 2, results showed that 17.4% in the Uceris 9mg group and 8.3% in the 6mg group compared with 4.5% in the placebo group achieved remission. In both studies, Uceris 9mg demonstrated superiority to placebo in inducing clinical and endoscopic remission.
Swallow whole. 9mg once daily in the AM for up to 8 weeks.
Active or quiescent tuberculosis, untreated fungal, bacterial, systemic viral or parasitic infections. Supplement with systemic glucocorticosteroid in surgery or other stress situations. Caution when transferring from steroids with high systemic availability (monitor). May unmask allergies previously controlled by systemic corticosteroids. If exposed to chickenpox or measles, consider immune globulin or antiviral prophylactic therapies. Hypertension. Diabetes. Osteoporosis. Peptic ulcer. Glaucoma. Cataracts. Moderate-to-severe liver disease: monitor for hypercorticism; consider discontinuing. Elderly. Pregnancy (Cat. C). Nursing mothers: not recommended.
May be potentiated by CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin); consider discontinuing. Avoid grapefruit or grapefruit juice. May be affected by gastric acid reducing agents (eg, PPIs, H2-blockers, antacids).
Headache, nausea, decreased blood cortisol, upper abdominal pain, fatigue, flatulence, abdominal distension, acne, urinary tract infection, arthralgia, constipation; hypercorticism, adrenal suppression, immunosuppression.