Dosing and uses of Uceris Rectal Foam (budesonide rectal)
Adult dosage forms and strengths
rectal foam
- 2mg/metered dose
Ulcerative Colitis
Indicated for the induction of remission in patients with active mild-to-moderate distal ulcerative colitis extending up to 40 cm from the anal verge
1 metered dose (2 mg) PR BID for 2 weeks followed by 1 metered dose PR once daily in evening for 4 weeks
Administration
For rectal administration only; not for oral use
Before administration, use the bathroom to empty your bowels
Each applicator is coated with a lubricant; if additional lubrication is needed, petrolatum or petroleum jelly can also be used
Warm the canister in the hands while shaking it vigorously for 10-15 seconds before use
Can be used in a standing, lying, or sitting position (eg, while using the toilet)
When applied in the evening, use immediately prior to bedtime; try not to empty your bowels again until the next morning
Pediatric dosage forms and strengths
Safety and efficacy not established
Uceris Rectal Foam (budesonide rectal) adverse (side) effects
>10%
Decreased blood cortisol (17%)
1-10%
Adrenal insufficiency (4%)
Nausea (2%)
<1%
Insomnia (0.4%)
Sleep disorder (0.4%)
Acne (0.4%)
Depression (0.4%)
Hyperglycemia (0.4%)
Postmarketing Reports
Cardiac disorders: Hypertension
Gastrointestinal disorders: Pancreatitis
General disorders and administration-site conditions: Pyrexia, peripheral edema
Immune system disorders: Anaphylactic reactions
Nervous system disorders: Dizziness, benign intracranial hypertension
Psychiatric disorders: Mood swings
Skin and subcutaneous tissue disorders: Pruritus, maculopapular rash, allergic dermatitis
Warnings
Contraindications
Hypersensitivity
Cautions
Long-term use of corticosteroids may cause hypercorticism and adrenal suppression
Taper systemic corticosteroids slowly when transitioning from corticosteroids with higher systemic effects to those with lower effects (eg, budesonide rectal); symptoms attributed to withdrawal of steroid therapy, including those of acute adrenal suppression or benign intracranial hypertension, may develop
Corticosteroids (prolonged use or high doses) are known to be immunosuppressive; monitor patients with active or quiescent tuberculosis infection, ocular herpes simplex, or untreated fungal, bacterial, systemic viral, or parasitic infections
Monitor patients with hypertension, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma, or cataracts; any family history of diabetes or glaucoma; or with any other conditions in which glucocorticosteroids may have unwanted effects
Moderate-to-severe hepatic impairment; monitor for increased signs and/or symptoms of hypercorticism
Avoid use of strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, grapefruit juice) during 6-week treatment period; may increase budesonide systemic exposure
Rectal foam is flammable; store away from flame or heat sources
Pregnancy and lactation
Pregnancy category: C
Lactation: Rectal foam is likely to result in budesonide in human milk as budesonide delivered by inhalation from a dry-powder inhaler is present in human milk at low concentrations
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 Uceris Rectal Foam (budesonide rectal)
Mechanism of action
Elicits glucocorticosteroid activity, including anti-inflammatory effects
Absorption
AUC: 4.31 ng•hr/mL
Distribution
Protein bound: 85-90%
Vd: 2.2-3.9 L/kg
Metabolism
Subject to first-pass metabolism
Rapidly and extensively biotransformed in liver, mainly by CYP3A4, to its 2 major metabolites, 6-beta-hydroxy budesonide and 16-alpha-hydroxy prednisolone
Glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound
Elimination
Plasma clearance: 0.9-1.8 L/min
Excretion: Urine and feces in form of metabolites
