Generic Name
Budesonide
Brand Names (Oral Formulations)
Entocort EC
Entocir
Budenofalk
Cortiment
Uceris (US)
Jorveza (orodispersible for eosinophilic esophagitis)
Budesonide MMX
Various generics available depending on region
Drug Class
Glucocorticoid
Locally acting corticosteroid
Anti-inflammatory agent for gastrointestinal use
Mechanism of Action
Budesonide is a synthetic non-halogenated corticosteroid with potent glucocorticoid activity and low systemic bioavailability due to extensive first-pass hepatic metabolism
It binds to cytoplasmic glucocorticoid receptors and modulates gene expression, leading to suppression of pro-inflammatory cytokines and chemokines, decreased migration of inflammatory cells, and stabilization of cell membranes in the gastrointestinal tract
The drug exhibits local anti-inflammatory activity with minimal systemic exposure, which reduces systemic corticosteroid-related adverse effects
Formulations and Site-Specific Release Characteristics
Enteric-Coated Capsules (Entocort EC, Budenofalk)
Release budesonide in the distal ileum and ascending colon
Used primarily for ileocecal Crohn’s disease
Extended-Release Tablets (Cortiment, Uceris)
Multi-Matrix (MMX) formulation
Release budesonide uniformly throughout the colon
Used for ulcerative colitis
Oral Granules
Designed for pediatric or adult use in Crohn’s disease affecting the ileum and colon
Often sprinkled over food or dissolved in water depending on formulation
Example: Budesonide oral granules 2 mg/sachet
Indications
Gastroenterology
Mild to moderate Crohn’s disease (terminal ileum and/or ascending colon)
Ulcerative colitis (mild to moderate, especially left-sided disease)
Microscopic colitis (collagenous or lymphocytic)
Eosinophilic esophagitis (off-label, using orodispersible forms)
Autoimmune hepatitis (as an alternative to systemic steroids in non-cirrhotic patients)
Allergy/Immunology
Off-label for graft-versus-host disease and some food-related eosinophilic gastrointestinal disorders
Dosing and Administration
Crohn’s Disease (Adults)
9 mg once daily in the morning (capsule form)
Typically for up to 8 weeks
Tapering may follow based on response
Maintenance: 6 mg once daily or alternate-day dosing (not always recommended)
Ulcerative Colitis (MMX Tablet)
9 mg once daily for up to 8 weeks
MMX formulation designed to treat the entire colon
Maintenance use not routinely recommended
Microscopic Colitis
9 mg daily (in divided doses or once daily) for 6–8 weeks
Maintenance: 6 mg daily or lowest effective dose
Eosinophilic Esophagitis (Off-Label)
Swallowed orodispersible budesonide (1–2 mg/day)
Some use crushed tablets or oral suspension to coat the esophagus
Pediatrics
Use with specialist guidance
Weight-based dosing used in children with inflammatory bowel disease
Oral granules are preferred for age-appropriate delivery
Hepatic Impairment
In cirrhotic patients, systemic exposure increases significantly
Avoid in cirrhosis or decompensated liver disease
Renal Impairment
No specific dose adjustment but monitor for signs of corticosteroid excess
Contraindications
Systemic fungal infections
Hypersensitivity to budesonide or any excipients
Caution in patients with active untreated infections
Not suitable for patients needing high systemic corticosteroid coverage
Precautions
Prolonged use may result in adrenal suppression
Risk of systemic glucocorticoid effects increases with higher doses or liver disease
Avoid abrupt discontinuation after prolonged use
Caution in patients with infections, osteoporosis, peptic ulcers, hypertension, diabetes, or glaucoma
May reactivate latent tuberculosis or increase risk of infection
Monitor for adrenal insufficiency, particularly during stress or surgery
Live vaccines should be avoided during treatment
Adverse Effects
Common (mild due to low systemic exposure)
Headache
Abdominal pain
Nausea
Flatulence
Fatigue
Acne
Mood changes
Systemic Effects (especially at higher doses or long duration)
Cushingoid features (moon face, buffalo hump)
Weight gain
Hyperglycemia
Hypertension
Osteoporosis
Adrenal suppression
Skin thinning or bruising
Muscle weakness
Infections
Increased susceptibility to viral, bacterial, or fungal infections
Oral candidiasis (rare)
Endocrine and Metabolic
Suppression of hypothalamic-pituitary-adrenal (HPA) axis
Electrolyte imbalance in rare cases
Increased intraocular pressure or cataracts with prolonged use
Rare/Serious Effects
Allergic reactions
Glaucoma
Bone fractures
Mood disturbances (irritability, depression)
Pregnancy and Lactation
Pregnancy
Generally considered low-risk for short-term use
May be used in pregnancy if benefit outweighs risk
Avoid high-dose or long-term systemic use
Lactation
Minimal transfer into breast milk
No adverse effects expected in nursing infants at standard doses
Can be used cautiously during breastfeeding
Use in Special Populations
Pediatrics
Used with caution and under supervision
May affect growth velocity if used long term
Elderly
No specific dosage adjustment
Monitor for bone loss, hypertension, glucose intolerance
Hepatic Impairment
Use with caution or avoid in cirrhosis
Increased systemic bioavailability due to reduced first-pass metabolism
Drug Interactions
CYP3A4 Inhibitors (e.g., ketoconazole, clarithromycin, grapefruit juice)
Significantly increase systemic budesonide levels
Avoid or reduce dose if concurrent use is necessary
CYP3A4 Inducers (e.g., rifampicin, phenytoin)
May reduce efficacy of budesonide
Antacids or proton pump inhibitors
May alter pH and affect enteric coating release (capsule formulations)
Estrogens and oral contraceptives
May increase systemic exposure
Live vaccines
Avoid during immunosuppressive corticosteroid treatment
Monitoring Parameters
Signs and symptoms of adrenal suppression
HPA axis suppression (especially in long-term use or hepatic impairment)
Intraocular pressure (in patients with glaucoma risk)
Bone mineral density (long-term treatment)
Blood glucose in diabetics
Cortisol levels in suspected adrenal insufficiency
Endoscopic or clinical evaluation of gastrointestinal inflammation
Formulations and Release Characteristics
Budesonide Capsules (3 mg)
Entocort EC, Budenofalk
pH-dependent release in distal ileum and proximal colon
Budesonide MMX Tablets (9 mg)
Cortiment, Uceris
Extended release across entire colon
Budesonide Oral Granules (2 mg)
Pediatric or specialized adult use
Mixed with food or dissolved before swallowing
Orodispersible Tablets (1 mg)
Jorveza for eosinophilic esophagitis
IV and Inhaled Forms
Not discussed here, as they are for respiratory indications
Patient Counseling Points
Take capsules or tablets whole, without crushing or chewing
Swallow granules as directed; do not chew
Take in the morning to mimic natural cortisol rhythm
Inform prescriber if signs of adrenal insufficiency appear (fatigue, hypotension, weight loss)
Avoid grapefruit juice due to interaction risk
Do not abruptly stop prolonged therapy; taper gradually under medical supervision
Discuss all medications and supplements with your healthcare provider
Report signs of infection or worsening gastrointestinal symptoms
Use caution during illness or surgery if recently stopped treatment
Store medication in original packaging away from moisture and heat
No comments:
Post a Comment