UCERIS- budesonide tablet, extended release
1 INDICATIONS AND USAGE
UCERISŪ (budesonide) extended release tablets are indicated for the induction of remission in patients with active, mild to moderate ulcerative colitis.
2 DOSAGE AND ADMINISTRATION
2.1 Mild to Moderate Ulcerative Colitis
The recommended dosage for the induction of remission in adult patients with active, mild to moderate ulcerative colitis is 9 mg taken orally once daily in the morning with or without food for up to 8 weeks. UCERIS should be swallowed whole and not chewed, crushed or broken.
2.2 CYP3A4 Inhibitors
If concomitant administration with ketoconazole, or any other CYP3A4 inhibitor, is indicated, patients should be closely monitored for increased signs and/or symptoms of hypercorticism. Avoid grapefruit juice, which is known to inhibit CYP3A4, when taking UCERIS. In these cases, discontinuation of UCERIS or the CYP3A4 inhibitor should be considered [See Drug Interactions (7) and Clinical Pharmacology (12.3)].
3 DOSAGE FORMS AND STRENGTHS
White, round, biconvex extended release tablets debossed with "MX9". Each extended release tablet contains 9 mg budesonide.
UCERIS is contraindicated in patients with hypersensitivity to budesonide or any of the ingredients of UCERIS. Anaphylactic reactions have occurred with other budesonide formulations [See Adverse Reactions (6.2)].
Reports of acute toxicity and/or death following overdosage of glucocorticosteroids are rare. Treatment consists of immediate gastric lavage or emesis followed by supportive and symptomatic therapy.
If glucocorticosteroids are used at excessive doses for prolonged periods, systemic glucocorticosteroid effects such as hypercorticism and adrenal suppression may occur. For chronic overdosage in the face of severe disease requiring continuous steroid therapy, the dosage may be reduced temporarily.
Single oral budesonide 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.
UCERISŪ (budesonide) extended release tablets, for oral administration, contain budesonide, a synthetic corticosteroid, as the active ingredient. Budesonide is designated chemically as (RS)-11β, 16α, 17,21 tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with butyraldehyde.
Budesonide is provided as a mixture of two epimers (22R and 22S). The empirical formula of budesonide is C25 H34 O6 and its molecular weight is 430.5
Budesonide is a white to off-white, tasteless, odorless powder that is practically insoluble in water, sparingly soluble in alcohol, and freely soluble in chloroform.
UCERIS, a delayed and extended-release tablet, is coated with a polymer film, which breaks down at or above pH 7.0. The tablet core contains budesonide with polymers that provide for extended release of budesonide.
Each tablet contains the following inactive ingredients: stearic acid, lecithin, microcrystalline cellulose, hydroxypropylcellulose, lactose, silicon dioxide, magnesium stearate, methacrylic acid copolymer types A and B, talc, triethylcitrate, and titanium dioxide.
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
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.