ENTOCORT EC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ENTOCORT EC (ENTOCORT EC).
Budesonide is a corticosteroid with potent glucocorticoid activity and weak mineralocorticoid activity. It binds to the glucocorticoid receptor, leading to anti-inflammatory effects via inhibition of inflammatory mediators such as cytokines and prostaglandins.
| Metabolism | Hepatic via CYP3A4 (major), with substantial first-pass metabolism; resulting metabolites have minimal glucocorticoid activity. |
| Excretion | Primarily fecal (60-70%) with minimal renal excretion (<10%); extensively metabolized hepatically, metabolites excreted in bile and feces. |
| Half-life | Terminal elimination half-life is approximately 2-3 hours; clinically, the extended intestinal release formulation maintains local activity despite short systemic half-life. |
| Protein binding | Approximately 80-85% bound, primarily to albumin and corticosteroid-binding globulin. |
| Volume of Distribution | Apparent volume of distribution is about 1.2 L/kg; indicates extensive tissue distribution due to lipophilicity. |
| Bioavailability | Oral bioavailability of budesonide from ENTOIRT EC is approximately 10-20% due to extensive first-pass metabolism; the targeted release formulation optimizes local delivery. |
| Onset of Action | Oral ENTOIRT EC: clinical effect typically noted within 2-4 weeks for Crohn's disease; peak plasma levels at 3-4 hours post-dose. |
| Duration of Action | Duration of action is 24 hours with daily dosing; clinical effect persists through local mucosal activity despite rapid systemic clearance. |
9 mg orally once daily in the morning for up to 8 weeks.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | Contraindicated in patients with severe hepatic impairment (Child-Pugh Class C). In moderate hepatic impairment (Child-Pugh Class B), use with caution; no specific dose adjustment recommended, but monitor for adverse effects. |
| Pediatric use | Not recommended for use in pediatric patients. |
| Geriatric use | No specific dose adjustment required; use with caution due to potential increased risk of osteoporosis and other corticosteroid-related adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ENTOCORT EC (ENTOCORT EC).
| Breastfeeding | Budesonide enters breast milk in low amounts; M/P ratio estimated at 0.13-0.33 (oral budesonide). At therapeutic doses (up to 9 mg/day), infant exposure is likely <1% of maternal weight-adjusted dose. Considered compatible with breastfeeding; observe infant for potential adrenal suppression with chronic high-dose use. |
| Teratogenic Risk | Corticosteroids like budesonide are associated with a small increased risk of orofacial clefts (odds ratio ~1.3) when used in the first trimester. Second and third trimester use may increase risk of intrauterine growth restriction (IUGR) and preterm birth. Overall absolute risk is low; no evidence of major congenital malformations at standard doses. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to budesonide or any component of the formulation","Untreated localized infections"]
| Precautions | ["Suppression of hypothalamic-pituitary-adrenal (HPA) axis, especially with higher doses or prolonged use","Increased risk of infections due to immunosuppression","Possible exacerbation of systemic fungal infections","May mask signs of infection","Use with caution in patients with tuberculosis, hypertension, diabetes, osteoporosis, peptic ulcer, glaucoma, or cataracts","Adrenal insufficiency may occur upon withdrawal"] |
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| Fetal Monitoring | Monitor maternal blood glucose (risk of hyperglycemia), blood pressure (risk of hypertension), and signs of adrenal suppression if long-term use. For fetal monitoring: ultrasound for growth assessment if prolonged use beyond first trimester; consider serial growth scans if IUGR suspected. |
| Fertility Effects | No known adverse effects on human fertility. In animal studies, no impairment of fertility observed at doses up to 1 mg/kg/day (approximately 5 times human dose). Corticosteroids may affect menstrual cycle; however, budesonide is less likely due to low systemic bioavailability. |