Dosing and uses of Entocort EC, Uceris (budesonide)
Adult dosage forms and strengths
capsule, enteric-coated and extended-release (Entocort EC)
- 3mg
tablet, enteric-coated and extended-release (Uceris)
- 9mg
Ulcerative Colitis
Induction of remission of active mild-to-moderate ulcerative colitis
Uceris: 9 mg PO qAM for up to 8 weeks
Crohn Disease
Treatment of active mild-to-moderate Crohn disease involving ileum or ascending colon; maintenance of clinical remission of mild-to-moderate Crohn disease for up to 3 months
Entocort EC: 9 mg PO qAM for up to 8 weeks; for recurring episodes of active disease, 8-week courses may be repeated
Once symptoms are controlled, may be tapered to 6 mg PO qAM for maintenance
Crohn disease maintenance
- Entocort EC: 6 mg PO qAM for up to 3 months
- If symptom control is maintained at 3 months, tapering to complete cessation may be attempted (recommended)
Immunoglobulin A Nephropathy (Orphan)
Slowing of progression of immunoglobulin A nephropathy; delaying of onset of kidney failure in patients affected by this disease
Orphan indication sponsor
- Pharmalink AB; Engelbrekts kyrkogata 7b; Stockholm, Sweden
Pediatric dosage forms and strengths
Ulcerative Colitis (Orphan)
Orphan designation (budesonide [Uceris]) for treatment ulcerative colitis in pediatric patients aged 0 through 16 years
Orphan sponsor
- Santarus, Inc.; 3611 Valley Centre Drive, Suite 400; San Diego, CA 92130
Entocort EC, Uceris (budesonide) adverse (side) effects
>10%
Headache (21%)
Acne (<5-15%)
Nausea (11%)
Respiratory infection (11%)
1-10%
Back pain (7%)
Dizziness (7%)
Abdominal pain (6%)
Dyspepsia (6%)
Vomiting (6%)
Fatigue (5%)
Frequency not defined
Adrenal suppression
Amnesia
Anaphylactic reactions
Benign intracranial hypertension
Diarrhea
Facial edema
Fever
Flu syndrome
GI irritation
Hypokalemia
Increased appetite
Insomnia
Migraine
Nervousness
Pharyngitis
Rash
Xerostomia
Weight gain
Warnings
Contraindications
Documented hypersensitivity
Cautions
High-fat meal delays absorption
May increase risk of serious or fatal infection in individuals exposed to viral illnesses such as chickenpox or measles
Use with caution in patients with diabetes mellitus, hypertension, hypothyroidism, electrolyte abnormalities, sodium and water retention, infections, immunizations, ocular herpes simplex, myasthenia gravis, peptic ulcer disease, psychosis, or renal insufficiency
Thromboembolic disorders and myopathy may occur
Delayed wound healing is possible
Patients receiving corticosteroids should avoid chickenpox- or measles-infected persons if unvaccinated
Latent tuberculosis may be reactivated (patients with positive tuberculin test should be monitored)
Some suggestion (not fully substantiated) of slightly increased cleft palate risk if corticosteroids are used in pregnancy
Prolonged corticosteroid use may result in elevated intraocular pressure, glaucoma, or cataracts and has been associated with development of Karposi sarcoma
Myopathy has been reported
Secreted in human milk; no data from controlled trials on potential serious adverse reactions in nursing infants; use with caution
When glucocorticosteroids are used chronically, systemic effects such as hypercorticism and adrenal suppression may occur; glucocorticosteroids can reduce response of hypothalamus-pituitary-adrenal (HPA) axis to stress; in situations where patients are subject to surgery or other stress situations, supplementation with systemic glucocorticosteroid recommended
Care needed in transferred from glucocorticosteroid treatment with higher systemic effects to glucocorticosteroids with lower systemic effects; symptoms attributed to withdrawal of steroid therapy, including those of acute adrenal suppression or benign intracranial hypertension, may develop; adrenocortical function monitoring may be required in these patients and dose of glucocorticosteroid treatment with high systemic effects should be reduced cautiously
Glucocorticosteroids should be used with caution, if at all, in patients with active or quiescent tuberculosis infection, untreated fungal, bacterial, systemic viral or parasitic infections
Replacement of systemic glucocorticosteroids with budesonide tablets may unmask allergies (e.g., rhinitis and eczema), which were previously controlled by the systemic drug
Reduced liver function affects elimination of glucocorticosteroids; increased systemic availability of oral budesonide has been demonstrated in patients with liver cirrhosis
Pregnancy and lactation
Pregnancy category: C
Lactation: Use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Entocort EC, Uceris (budesonide)
Mechanism of action
Anti-inflammatory corticosteroid; potent glucocorticoid activity but weak mineralocorticoid activity; controls rate of protein synthesis; decreases inflammation by suppressing migration of polymorphonuclear leukocytes (PMNs) and reducing capillary permeability; stabilizes cell and lysosomal membranes, increases surfactant synthesis, increases serum vitamin A concentration, and inhibits prostaglandin and proinflammatory cytokines; suppresses lymphocyte proliferation through direct cytolysis, inhibits mitosis, and breaks down granulocyte aggregates
Absorption
Bioavailability: Capsule, 9-21%
Peak plasma time: Capsule, 5-10 hr
Distribution
Protein bound: 85-90%
Vd: 2.2-3.9 L/kg
Metabolism
Extensive 1st-pass metabolism by CYP3A4 in liver
Metabolites: 6-Beta-hydroxybudesonide, 16-alpha-hydroxyprednisolone (inactive)
Elimination
Half-life: 2-3.6 hr
Excretion: Urine (60%), feces (minimal)
