Version May 2024
Ulcerative colitis, mildly to moderately active (alternative agent):
Note: May be used as alternative monotherapy for distal disease in patients who cannot tolerate preferred topical agents, or in combination with other therapies (eg, oral agents) for refractory distal, left-sided, or extensive colitis (Ref).
Rectal foam: 2 mg (one metered dose) once or twice daily for 2 weeks, followed by 2 mg (one metered dose) once daily at bedtime for 4 weeks; may be extended an additional 2 weeks if symptoms (eg, diarrhea, bleeding) persist (Ref).
Rectal enema [Canadian product]: Initial: ~2 mg (one enema) once daily at night prior to bedtime for 4 weeks; if remission is not induced may continue for additional 4 weeks (total therapy duration: 8 weeks).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Rectal foam: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). However, dosage adjustment unlikely due to low systemic absorption.
Rectal enema [Canadian product]: There are no dosage adjustments provided in the manufacturer's labeling.
Rectal foam:
Mild impairment (Child-Pugh class A): No dosage adjustment necessary.
Moderate or severe impairment (Child-Pugh class B or C): There are no dosage adjustments provided in the manufacturer's labeling. However, dosage adjustment unlikely due to low systemic absorption. Monitor for increased signs and/or symptoms of hypercortisolism; discontinue use if signs or symptoms are observed.
Rectal enema [Canadian product]: There are no dosage adjustments provided in the manufacturer's labeling.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not always defined.
>10%: Endocrine & metabolic: Decreased plasma cortisol (17%)
1% to 10%:
Endocrine & metabolic: Adrenocortical insufficiency (4%), hpa-axis suppression, hypercortisolism
Gastrointestinal: Nausea (2%)
<1%, postmarketing, and/or case reports: Acne vulgaris, adrenal cortex hypofunction, agitation, allergic dermatitis, anaphylaxis, anxiety, depression, diarrhea, dizziness, drowsiness, dysphoria, emotional lability, exacerbation of diabetes mellitus, fever, flatulence, hyperacidity (peptic ulcer), hyperglycemia, hypertension, insomnia, maculopapular rash, pancreatitis, peripheral edema, pruritus, pseudotumor cerebri, skin rash, sleep disorder, urticaria
Hypersensitivity to budesonide or any component of the formulation
Entocort enema [Canadian product]: Hypersensitivity to budesonide or any component of the formulation; imminent bowel perforation as well as the probability of obstruction, abscess or other pyogenic infection, fresh intestinal anastomoses, extensive fistulas and sinus tracts; systemic or local bacterial, fungal, or viral infections; tuberculosis (TB) disease (active TB).
Concerns related to adverse effects:
• Adrenal suppression: May cause hypercortisolism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in patients receiving high doses for prolonged periods, or with concomitant CYP3A4 inhibitor use. HPA axis suppression may lead to adrenal crisis. Withdrawal and discontinuation of a corticosteroid should be done slowly and carefully. In situations where patients are subject to surgery or other stress situations, supplementation with systemic glucocorticoids is recommended.
• Impaired adrenal suppression in patients transferred from other glucocorticoids: Monitor patients transferred from systemic corticosteroids to corticosteroids with lower systemic effects (eg rectal foam), since steroid withdrawal, including benign intracranial hypertension or acute adrenal suppression, may occur. Replacement of systemic corticosteroids with rectal foam may unmask allergies (eg, rhinitis and eczema) previously controlled by systemic drug. Adrenocortical function monitoring may be required in these patients; reduce dose cautiously.
• Immunosuppression: Prolonged use of corticosteroids may also increase the incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to vaccines. Exposure to chickenpox should be avoided; if exposed, therapy with varicella zoster immune globulin (VZIG) or pooled intravenous immunoglobulin (IVIG) may be needed; antivirals may be needed if chickenpox develops. Exposure to measles may require pooled intramuscular immunoglobulin use. Corticosteroids should not be used to treat ocular herpes simplex. Corticosteroids should not be used for viral hepatitis. Close observation is required in patients with tuberculosis (TB) infection (latent TB) and/or TB reactivity; restrict use in TB disease (active TB) (only in conjunction with antituberculosis treatment).
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with hypertension, acute coronary disease, or limited cardiac reserve.
• Diabetes: Use with caution in patients with diabetes or a family history of diabetes; may alter glucose production/regulation leading to hyperglycemia.
• GI disease: Use with caution in patients with peptic ulcer disease.
• Hepatic impairment: Use with caution in patients with hepatic impairment, including cirrhosis; increased oral bioavailability has been reported in patients with cirrhosis.
• Myasthenia gravis: Use may cause transient worsening of myasthenia gravis (MG) (eg within first 2 weeks of treatment); monitor for worsening MG (AAN [Narayanaswami 2021]).
• Ocular disease: Use with caution in patients with cataracts and/or glaucoma or a family history of these diseases; increased intraocular pressure, open-angle glaucoma, and cataracts have occurred with prolonged glucocorticoid use.
• Osteoporosis: Use with caution in patients with osteoporosis; high doses and/or long-term use of corticosteroids have been associated with increased bone loss and osteoporotic fractures.
• Psychiatric disturbances: Systemic corticosteroid use may cause psychiatric disturbances, including depression, euphoria, insomnia, mood swings, and personality changes. Preexisting psychiatric conditions may be exacerbated by corticosteroid use.
• Thyroid disease: Metabolic clearance of corticosteroids increases in hyperthyroid patients and decreases in hypothyroid patients.
Special populations:
• Older adult: Because of the risk of adverse effects, corticosteroids should be used cautiously in older adults at the smallest possible effective dose for the shortest duration.
Dosage form specific issues:
• Flammable contents: Rectal foam contains flammable propellants. Avoid fire, flame and smoking during and immediately following administration. Temporarily discontinue use before initiation of bowel preparation for colonoscopy; consult health care provider prior to resuming therapy.
Each Uceris rectal foam canister contains 14 metered doses.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Foam, Rectal:
Uceris: 2 mg/actuation (33.4 g) [contains cetyl alcohol, edetate (edta) disodium, propylene glycol]
Generic: 2 mg (33.4 g)
Yes
Foam (Uceris Rectal)
2 mg/ACT (per gram): $14.61
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Foam, Rectal:
Uceris: 2 mg/actuation (33.4 g) [contains cetyl alcohol, edetate (edta) disodium, propylene glycol]
Kit, Rectal:
Entocort: 0.02 mg/mL
Rectal: Rectal foam: For rectal use only; not for oral use. Wash hands before and after use. Prior to use, patients should use the bathroom to empty the bowel; when administering evening dose (immediately prior to bedtime), do not empty bowels again until the next morning if possible. Attach applicator to canister nozzle. 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 to 15 seconds prior to use. Unlock the canister by twisting the domed canister top until it is aligned with the nozzle. May be used in a standing, lying or sitting position (eg, while sitting on the toilet). Turn the canister upside down and gently insert applicator tip into rectum as far as is comfortable. Push down on the pump dome with forefinger and hold for 2 seconds; release finger pressure on pump dome and hold applicator in place for 10 to 15 seconds. After administering, applicators can only be used one time and should be discarded in provided plastic trash bag. Avoid fire, flame and smoking during and immediately following administration. Temporarily discontinue use before initiation of bowel preparation for colonoscopy; consult provider prior to resuming therapy.
Rectal enema [Canadian product]: For rectal use only; not for oral use. Remove cap after preparation and screw 1 nozzle (pouch labeled ‘applicator enema’) onto the bottle prior to administration. May lubricate nozzle with petroleum jelly to improve comfort. Patient should lie down on either side with bottom slightly higher than the rest of body, shake the reconstituted enema bottle, gently ease nozzle into the rectum as far as comfortable, and then empty most of contents into rectum (bottle designed to keep some solution after use). Patient should roll over on stomach and remain in this position for 5 minutes, then lie in a comfortable position. Enema should be retained the whole night if possible or as long as possible. An optional plastic bag (supplied) may be used to hold bottle during administration and easily dispose of the bottle after administration.
Ulcerative colitis, mildly to moderately active: Remission induction in patients with active mild to moderate distal ulcerative colitis extending up to 40 cm from the anal verge
Entocort Enema [Canadian product]: Management of distal ulcerative colitis (rectum, sigmoid, and descending colon)
Substrate of CYP3A4 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Budesonide (Topical). Risk X: Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Budesonide (Topical). Risk X: Avoid combination
Nirmatrelvir and Ritonavir: May increase the serum concentration of Budesonide (Topical). Management: Consider the risks of systemic corticosteroid adverse effects versus the benefits of coadministration. Monitor patients for systemic corticosteroid adverse effects if combined. Risk D: Consider therapy modification
Grapefruit juice doubles bioavailability of oral budesonide by inhibiting gut mucosal CYP3A4; altered effects with rectal use are possible. Management: Grapefruit or grapefruit juice should be avoided during therapy.
Fertility may be decreased in females with active inflammatory bowel disease. Corticosteroids used for the management of inflammatory bowel disease are not expected to decrease female fertility (AGA [Mahadevan 2019]).
Hypoadrenalism may occur in newborns following maternal use of corticosteroids in pregnancy; monitor.
Because systemic corticosteroids may increase the risk of gestational diabetes and other adverse pregnancy outcomes, use for maintenance therapy in pregnant women with inflammatory bowel disease is not recommended. However, corticosteroids may be used to treat disease flares in pregnant patients (AGA [Mahadevan 2019]).
Budesonide can be detected in breast milk following oral inhalation; exposure to a breastfeeding child may be higher following maternal rectal use than oral inhalation.
According to the manufacturer, the decision to breastfeed following oral use should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Corticosteroids used for inflammatory bowel disease are considered compatible with breastfeeding (AGA [Mahadevan 2019]).
Avoid consumption of grapefruit or grapefruit juice during treatment
Baseline hepatic function tests; serum glucose, electrolytes; presence of infection, signs/symptoms of hypercortisolism, blood pressure as clinically indicated.
Controls the rate of protein synthesis; depresses the migration of polymorphonuclear leukocytes, fibroblasts; reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation. Has potent glucocorticoid activity and weak mineralocorticoid activity.
Absorption: Rectal foam: Minimal; Rectal enema [Canadian product]: Rapid and essentially complete within 3 hours
Distribution: Vd: 2.2 to 3.9 L/kg
Protein binding: 85% to 90%
Metabolism: Extensive hepatic metabolism, primarily by CYP3A4 to 2 major metabolites (negligible glucocorticoid activity)
Bioavailability: Rectal enema [Canadian product]: 3% to 27%
Half-life elimination: Rectal enema [Canadian product]: 2 to 3 hours
Time to peak: Rectal enema [Canadian product]: 1.5 hours
Excretion: Urine: Oral dose: ~60%; Feces: ~30%
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