Budesonide (Uceris)

1. Health Canada Product Monograph — Budesonide

• Used to induce remission in adults with active mild to moderate distal ulcerative colitis extending up to 40 cm from the anal opening.

• No studies have been done with this rectal foam in pregnant women; animal studies with injected budesonide showed skeletal abnormalities, fetal loss, and reduced fetal weight at doses relevant to human exposure.
• Should be used during pregnancy only if the potential benefit clearly justifies the risk to the fetus, and newborns exposed in-utero should be watched for signs of low adrenal function.

• Budesonide is likely to pass into breast milk in low concentrations, so it should be used with caution while breastfeeding, weighing the benefits of breastfeeding and the mother's clinical need for treatment against any potential effects on the nursing infant.

• Clinical studies did not include enough patients aged 65 and over to know whether they respond differently than younger patients.
• Dose selection should be cautious in older adults, generally starting at the low end of the dosing range, given the greater likelihood of reduced organ function or other medical conditions.

• Not authorized for use in patients under 18, as no data are available in this age group; glucocorticosteroids including budesonide can reduce growth velocity in children.

• The usual regimen is one metered dose given rectally twice daily for the first two weeks, then once daily in the evening for the following four weeks.
• The bowel should be emptied before use, the canister warmed and shaken vigorously for 10 to 15 seconds before each application, and the applicator discarded after a single use.
• Evening doses should be given just before bedtime, and the patient should try not to have a bowel movement again until the following morning.
• If a dose is missed, it should be given as soon as possible unless it is almost time for the next dose, in which case the missed dose should be skipped rather than doubling up.

• Headache may occur.
• Skin rash may occur.
• Acne may occur.
• Mild sleep disturbances such as insomnia may occur.
• Mood changes, including low mood, may occur.

Serious side effects require immediate discussion with the prescriber or emergency care.

• Reduced blood cortisol levels and adrenal insufficiency may occur, since even rectally administered budesonide is absorbed systemically; symptoms include fatigue, weakness, and low blood pressure.
• Signs of excess corticosteroid activity (Cushingoid features) may develop with prolonged use.
• Severe allergic reactions, including anaphylaxis, have been reported.
• Increased susceptibility to infection may occur, and viral illnesses such as chickenpox or measles can be more severe in patients on corticosteroids.
• Vision changes, including those related to cataracts, glaucoma, or rare fluid buildup behind the retina, have been reported with corticosteroid use.
• High blood pressure has been reported.
• Inflammation of the pancreas (pancreatitis) has been reported.
• Increased pressure in the skull (benign intracranial hypertension) may occur, particularly when switching from a more systemically active steroid.
• Severe generalized skin eruption (acute generalized exanthematous pustulosis) has been reported rarely, in association with infection.

• Use with caution in patients with infections, high blood pressure, diabetes, osteoporosis, peptic ulcer disease, glaucoma, cataracts, or a family history of diabetes or glaucoma.
• Use with caution, or avoid, in patients with severe liver impairment such as cirrhosis, since this increases systemic exposure to budesonide.
• Use with caution in patients with severe kidney impairment.
• The canister contains a flammable propellant, so avoid fire, flame, and smoking during and immediately after use.
• Patients transitioning from a more systemic corticosteroid should be monitored for withdrawal symptoms, including adrenal suppression.

• Contraindicated in patients with known hypersensitivity to budesonide or any ingredient in the formulation.
• Contraindicated in patients with active or dormant tuberculosis infection.
• Contraindicated in patients with untreated fungal, bacterial, systemic viral, or parasitic infections.
• Contraindicated in patients with ocular herpes simplex infection.

• Strong CYP3A4 inhibitors such as ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, and cyclosporine can significantly raise systemic budesonide levels and should be avoided.
• Cardiac glycosides such as digoxin may have their effects intensified if budesonide causes low potassium levels.
• Diuretics that cause potassium loss (saluretics) may worsen low potassium levels when combined with budesonide.

• Grapefruit and grapefruit juice should be avoided, as they inhibit the same enzyme that breaks down budesonide and can increase drug exposure.

• Applied twice daily (morning and evening) for the first two weeks, then once daily in the evening for the remaining four weeks of treatment, ideally right before bedtime.

• Store at 15-30 degrees C; do not refrigerate, do not expose to heat above 49 degrees C, and do not puncture or incinerate the pressurized canister.

• Uceris rectal foam is a locally-acting corticosteroid used to bring active mild to moderate ulcerative colitis into remission.
• Use it twice daily for two weeks, then once daily in the evening for four more weeks, applying it rectally after emptying the bowel.
• Common effects include headache, rash, acne, and mild mood or sleep changes.
• Contact the doctor's office promptly for unusual fatigue or weakness, vision changes, signs of infection, or severe abdominal pain, since the medication is absorbed into the body and can affect adrenal function.
• The canister contains a flammable propellant, so avoid fire, flame, or smoking during and right after use, and each applicator should be used only once.
• Store at room temperature, do not refrigerate, and keep away from heat sources.