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. |
| Molecular Weight | 430.53 |
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 | Use only if clearly needed; limited human data; may be associated with orofacial clefts if used in first trimester. |
| 2nd trimester | Use only if benefits outweigh risks; monitor fetal growth. |
| 3rd trimester | Use only if benefits outweigh risks; potential for adrenal suppression in neonate. |
Clinical note
Comprehensive clinical and safety monograph for ENTOCORT EC (ENTOCORT EC).
| Placental transfer | Minimal; budesonide is extensively metabolized and has low bioavailability; limited placental transfer. |
| Breastfeeding | Enters breast milk in low amounts; minimal risk to infant at therapeutic doses; monitor infant for potential effects on adrenal function. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to budesonide or any componentSevere hepatic impairmentAcute infection (e.g., herpes simplex, varicella)
| 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 |
| Food/Dietary | Avoid grapefruit and grapefruit juice during therapy as they inhibit CYP3A4, increasing budesonide serum levels and risk of systemic corticosteroid effects. No other significant food interactions. |
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| 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. |
| 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. |
| Clinical Pearls | ENTOCORT EC (budesonide) is a glucocorticosteroid with high first-pass hepatic metabolism, reducing systemic bioavailability. It is formulated as enteric-coated capsules to release drug in the ileum and ascending colon, making it effective for Crohn's disease involving the terminal ileum and/or ascending colon. Do not crush or chew capsules. Monitor for hypercorticism with prolonged use or high doses. |
| Patient Advice | Swallow the capsule whole; do not crush, chew, or open it. · Take exactly as prescribed; do not change dose or stop without consulting your doctor. · Avoid grapefruit juice as it can increase drug levels and risk of side effects. · Contact your doctor if you experience steroid-related side effects such as mood changes, weight gain, or easy bruising. · Do not take during acute infectious episodes unless specifically instructed. |