Budesonide rectal foam and enemas

Generic Name

Budesonide

Rectal Formulations

Budesonide rectal foam

Budesonide enema

Brand Names

Budenofalk Rectal Foam

Uceris Rectal Foam (US)

Entocir Rectal

Entocort Enema

Generic budesonide enemas and foams available depending on region

Drug Class

Glucocorticoid

Locally acting corticosteroid for rectal administration

Anti-inflammatory agent

Mechanism of Action

Budesonide is a potent glucocorticoid that exerts local anti-inflammatory effects on the rectal and distal colonic mucosa

It binds to intracellular glucocorticoid receptors, alters gene transcription, and downregulates the production of pro-inflammatory mediators such as TNF-α, IL-1, IL-6, and chemokines

It also stabilizes lysosomal membranes and reduces capillary permeability in inflamed tissues

Due to its high first-pass metabolism in the liver, budesonide administered rectally achieves a strong local effect with minimal systemic absorption and low risk of systemic side effects compared to oral steroids

Indications

Approved

Ulcerative proctitis

Ulcerative proctosigmoiditis

Distal ulcerative colitis extending up to the sigmoid or descending colon

Mild to moderate flare-ups of left-sided colitis

Rectal inflammation in inflammatory bowel disease (IBD) when oral treatment is inadequate or contraindicated

Off-label/Investigational

Radiation proctitis

Pouchitis (after ileal pouch-anal anastomosis)

Solitary rectal ulcer syndrome (in resistant cases)

Dosing and Administration

Rectal Foam

Standard dose: budesonide 2 mg/actuation

Usual regimen: 1 actuation (2 mg) once or twice daily

Initiate with twice daily dosing for 2 to 4 weeks

Once response is achieved, reduce to once daily or every other day

Duration: 6–8 weeks per flare, reassess afterward

Patient should empty bowels before administration

Shake canister well before each use

Administer with applicator in left lateral or knee-chest position

Hold in position for 30 seconds after administration

Avoid bowel movement for at least 30 minutes after use

Rectal Enema

Available concentrations: typically 2 mg per 100 mL enema

Usual regimen: one enema at bedtime daily for 4 to 8 weeks

Should be retained in the bowel overnight or for at least 8 hours

Recommended for disease reaching beyond the rectum (up to sigmoid or descending colon)

Warm to body temperature before use to reduce cramping

Shake bottle well and expel air from bottle before insertion

Enema may be more effective in reaching higher rectal and colonic segments than foam

Pediatric Use

Limited data; may be used under specialist supervision in adolescents

Not routinely recommended in younger children

Elderly Use

No special dose adjustments

Monitor for systemic glucocorticoid side effects in prolonged use

Hepatic Impairment

In severe liver disease, systemic exposure may increase

Avoid prolonged use in cirrhotic or decompensated patients

Renal Impairment

No dose adjustment required

Monitor for systemic effects if prolonged therapy is used

Contraindications

Known hypersensitivity to budesonide or formulation components

Severe systemic infections (e.g., tuberculosis, systemic fungal infections)

Bowel perforation or severe rectal bleeding

Intestinal obstruction or significant anorectal stenosis

Recent colorectal surgery with anastomosis (risk of impaired healing)

Precautions

Do not exceed prescribed dose or duration without medical advice

Prolonged use may suppress the hypothalamic-pituitary-adrenal (HPA) axis

Caution in patients with hepatic impairment due to increased systemic levels

Use cautiously in patients with diabetes, osteoporosis, glaucoma, peptic ulcer disease, or active infections

Not intended for maintenance therapy; evaluate regularly for need to continue

Should not replace systemic corticosteroids when systemic control is needed

Monitor for systemic corticosteroid effects if used long-term

Adverse Effects

Local Effects

Rectal discomfort or irritation

Flatulence

Tenesmus

Abdominal cramps

Urgency to defecate

Anal itching or burning

Rectal bleeding (rare)

Systemic Effects (less common due to low absorption)

Weight gain

Facial puffiness (moon face)

Mood swings or insomnia

Acne

Elevated blood glucose

Hypertension

Adrenal suppression (in prolonged or high-dose use)

Increased risk of infection

Rare/Serious Effects

Anaphylaxis (extremely rare)

Systemic glucocorticoid effects in hepatic impairment

Osteopenia with chronic use

Glaucoma or cataracts with long-term exposure

Pregnancy and Lactation

Pregnancy

Considered low risk for short-term rectal use

Minimally absorbed; preferred over oral corticosteroids if rectal disease is isolated

Use lowest effective dose for shortest duration

Lactation

Minimal systemic absorption results in low levels in breast milk

Compatible with breastfeeding

Use in Special Populations

Pediatrics

Not routinely used under age 18

Off-label use may occur in IBD under specialist care

Elderly

Tolerated well

Monitor for systemic steroid effects, especially if used for extended periods

Hepatic Impairment

Systemic exposure increases significantly

Avoid in cirrhosis or decompensated liver disease

Drug Interactions

CYP3A4 Inhibitors (e.g. ketoconazole, clarithromycin, grapefruit juice)

Can increase systemic levels of budesonide

Use with caution

CYP3A4 Inducers (e.g. rifampicin, carbamazepine)

May reduce local and systemic effectiveness

Live Vaccines

Avoid during and shortly after treatment if used frequently or long-term

Risk of diminished immune response

Monitoring Parameters

Symptom response (bleeding, stool frequency, urgency)

Endoscopic mucosal healing (in moderate/severe cases)

HPA axis suppression if prolonged therapy or symptoms of adrenal insufficiency

Signs of systemic corticosteroid side effects in long-term use

Glucose levels in diabetic patients

Bone mineral density if used repeatedly or for long-term flares

Liver function in those with hepatic disease

Formulations

Rectal Foam

2 mg per actuation

Single-use canister with multiple applicators (usually 14–28 doses)

Propellant-based; should be used at room temperature

Rectal Enema

2 mg/100 mL liquid enema

Prefilled bottles with attached applicator

Administered once daily at bedtime

Patient Counseling Points

Use rectal foam or enema after emptying the bowels

Shake foam canister well before each use

Use rectal enema at bedtime and retain overnight

Expect relief of symptoms within days to weeks

Do not abruptly stop therapy if used long term; taper if advised

Avoid grapefruit or grapefruit juice with long-term use

Report signs of infection, rectal bleeding, or systemic side effects

Keep medication stored as recommended (usually below 25°C)

Do not share applicators between individuals

Wash hands before and after use

Do not substitute oral for rectal forms unless advised by healthcare provider