UCERIS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for UCERIS (UCERIS).
Uceris (budesonide) is a corticosteroid with potent glucocorticoid activity. It binds to the glucocorticoid receptor, leading to inhibition of pro-inflammatory cytokines (e.g., IL-1, IL-2, IL-4, IL-5, TNF-alpha), suppression of arachidonic acid metabolism via phospholipase A2 inhibition, and reduction of inflammatory cell infiltration. It has high topical anti-inflammatory activity and undergoes extensive first-pass hepatic metabolism, minimizing systemic bioavailability.
| Metabolism | Hepatic metabolism primarily via cytochrome P450 3A4 (CYP3A4) to inactive metabolites (e.g., 6β-hydroxybudesonide, 16α-hydroxyprednisolone). Extensive first-pass effect; approximately 90% of absorbed dose is metabolized before reaching systemic circulation. |
| Excretion | Renal: <1%. Fecal: approximately 63% as budesonide and metabolites. Biliary: minor. |
| Half-life | 2.8-4.5 hours (terminal). Clinical context: short half-life supports once-daily extended-release formulation for colonic delivery. |
| Protein binding | 85-90% bound primarily to albumin. |
| Volume of Distribution | 2.2-4.3 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral extended-release: approximately 9% (systemic) due to high first-pass metabolism. Rectal foam: approximately 15% (systemic). |
| Onset of Action | Oral extended-release: 1-2 weeks for clinical improvement in active ulcerative colitis. Rectal foam/enema: 2-4 weeks. |
| Duration of Action | Oral: approximately 24 hours for once-daily dosing. Rectal: 12-24 hours after administration. |
For induction of remission in mild to moderate active ulcerative colitis: one 9 mg extended-release tablet orally once daily for up to 8 weeks.
| Dosage form | AEROSOL, FOAM |
| Renal impairment | No dose adjustment required for mild-to-moderate renal impairment. Not studied in severe renal impairment (CrCl <30 mL/min); use with caution. |
| Liver impairment | Contraindicated in patients with severe hepatic impairment (Child-Pugh Class C). For moderate hepatic impairment (Child-Pugh Class B), use with caution; no specific dose adjustment recommended. For mild impairment (Child-Pugh Class A), no adjustment needed. |
| Pediatric use | Not approved for use in pediatric patients. Safety and efficacy not established in children under 18 years. |
| Geriatric use | No specific dose adjustment recommended. Elderly patients may be more susceptible to adverse effects such as hypercorticism and adrenal suppression; monitor closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for UCERIS (UCERIS).
| Breastfeeding | Budesonide is excreted into human milk in low amounts; the milk-to-plasma ratio is approximately 0.4. Estimated infant daily dose is less than 1% of maternal weight-adjusted dose. No adverse effects reported. Caution advised with higher maternal doses or prolonged use. Consider using the lowest effective dose. |
| Teratogenic Risk | Uceris (budesonide) is a corticosteroid. In pregnant women, first-trimester exposure may be associated with a small increased risk of oral clefts (absolute risk about 1 in 1000). Second and third trimester exposure may increase risk of fetal growth restriction and adrenal suppression in the newborn. Animal studies show fetal harm at clinically relevant doses. Use only if benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to budesonide or any component of the formulation; patients with active or latent tuberculosis; untreated systemic fungal, bacterial, viral, or parasitic infections; patients receiving live or live-attenuated vaccines (due to immunosuppression); patients with severe hepatic impairment (Child-Pugh Class C) because of decreased metabolism and increased systemic exposure.
| Precautions | Hypercorticism and adrenal suppression (especially at higher doses, prolonged use, or co-administration with CYP3A4 inhibitors); increased risk of infections (including reactivation of tuberculosis, fungal, bacterial, viral, or parasitic infections); corticosteroid withdrawal symptoms upon abrupt discontinuation; gastrointestinal perforation risk in patients with active ulcers, diverticulitis, or recent intestinal anastomosis; osteoporosis and bone density loss with long-term use; glaucoma, cataracts, and increased intraocular pressure; inhibition of growth in pediatric patients; exacerbation of diabetes mellitus and hypertension. |
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| Fetal Monitoring | Monitor maternal blood pressure, blood glucose (especially in diabetes), and signs of infection. Assess fetal growth by ultrasound if prolonged use. Newborns exposed in utero should be monitored for adrenal insufficiency and hypoglycemia after birth. |
| Fertility Effects | Budesonide did not impair fertility in animal studies at relevant doses. In humans, corticosteroids may affect menstrual cycle regularity; no specific data on fertility impairment with Uceris. Consider underlying disease impact on fertility. |