Beclometasone is a synthetic corticosteroid with potent glucocorticoid activity and minimal mineralocorticoid effects. While it is widely available in inhaled, intranasal, and topical forms for asthma, allergic rhinitis, and dermatological conditions, its oral (tablet) formulation is rarely available and used only in specific clinical settings. When given orally, beclometasone exerts systemic anti-inflammatory effects, especially in diseases involving gastrointestinal inflammation.
Available Form and Brand Names (Tablet Form)
Oral beclometasone dipropionate is available in enteric-coated tablets, designed to release the active substance in the distal small intestine and colon, where inflammatory bowel diseases commonly manifest.
Brands:
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Clenil® tablets
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Beclo Tablets
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Colifoam (rectal foam; not a tablet but used similarly for colitis)
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Enterocort® (though this name is more commonly associated with budesonide, not beclometasone)
The oral form is available in a 5 mg dose, and its enteric coating ensures that the steroid is not absorbed in the stomach but released in the terminal ileum and colon, maximizing local effect and minimizing systemic exposure.
Mechanism of Action
Beclometasone binds to cytoplasmic glucocorticoid receptors, then translocates to the nucleus to modulate gene expression, resulting in:
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Inhibition of pro-inflammatory cytokines (IL-1, IL-6, TNF-α)
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Suppression of COX-2 and prostaglandin synthesis
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Downregulation of adhesion molecules and immune cell trafficking
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Reduction of capillary permeability and fibroblast proliferation
Unlike systemic corticosteroids such as prednisolone, enteric-coated beclometasone exerts topical anti-inflammatory effects at the intestinal mucosa level with reduced systemic side effects due to low oral bioavailability.
Therapeutic Uses
Oral beclometasone is not widely available in many markets, but where it is approved, its primary indications include:
Gastrointestinal Indications:
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Ulcerative colitis (mild to moderate): Especially in left-sided colitis or pancolitis.
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Crohn’s disease: Primarily ileocolonic involvement or distal small bowel disease.
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Microscopic colitis (off-label): In lymphocytic or collagenous colitis.
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Eosinophilic colitis (off-label use)
Other Potential/Investigational Uses:
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Radiation-induced enteritis
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Graft-vs-host disease (GVHD) involving the gastrointestinal tract (as part of immunosuppressive regimens)
Note: Systemic beclometasone is not approved for asthma or dermatologic disorders due to better alternatives.
Dose and Administration
The usual oral dosage of beclometasone dipropionate tablets in inflammatory bowel disease is:
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5 mg once daily in the morning (single tablet)
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Duration: Typically 4–8 weeks, followed by a gradual taper depending on clinical response.
The tablet is:
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Enteric-coated (do not chew or crush)
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Taken on an empty stomach with water
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Designed to release in the terminal ileum and colon
If no clinical response is observed after 2–4 weeks, therapy may be discontinued or changed to systemic corticosteroids.
Pharmacokinetics
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Absorption: Limited in the upper GI tract due to enteric coating
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Onset: Effects begin within 3–5 days, maximum by 2 weeks
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Metabolism: Rapidly metabolized in the liver to inactive metabolites
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Bioavailability: Very low (<20%) due to first-pass hepatic metabolism
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Excretion: Fecal (major), renal (minor)
This favorable pharmacokinetic profile minimizes systemic corticosteroid side effects, while allowing high topical activity in the gut mucosa.
Contraindications
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Systemic fungal infections
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Known hypersensitivity to beclometasone or any formulation excipients
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Severe infections (e.g., tuberculosis, untreated systemic bacterial infections)
Precautions
Infectious risk:
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May mask signs of infection
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Use with caution in patients with latent tuberculosis, herpetic eye infections, or fungal GI infections
Adrenal suppression:
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Though minimal, prolonged use may suppress hypothalamic-pituitary-adrenal (HPA) axis
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Gradual withdrawal is necessary if used beyond 8–12 weeks
Immunosuppression:
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Increased risk of opportunistic infections
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Avoid live vaccines during therapy
Gastrointestinal effects:
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Caution in patients with gastric ulcer, diverticulitis, or intestinal perforation risk
Pediatric and elderly use:
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Not commonly used in children
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Elderly patients may be more prone to glucose intolerance, hypertension, or osteopenia
Side Effects
The incidence of systemic side effects is significantly lower compared to conventional corticosteroids like prednisolone. However, they may occur, especially with long-term or high-dose therapy.
Common (less than 10%):
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Headache
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Nausea
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Abdominal discomfort
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Bloating or flatulence
Less common:
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Oral candidiasis
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Mood disturbances
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Sleep disruption
Rare but serious:
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Adrenal suppression
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Osteopenia or osteoporosis
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Hypertension
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Hyperglycemia
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Psychiatric effects (depression, euphoria, psychosis)
The safety profile is overall favorable when used within the recommended dosage and duration.
Drug Interactions
Due to its low systemic bioavailability, significant pharmacokinetic interactions are rare. However, consider the following:
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CYP3A4 inhibitors (e.g., ketoconazole, ritonavir): May increase systemic corticosteroid exposure, though this is minimal due to beclometasone’s low absorption
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Rifampicin and phenytoin: May reduce activity via enzyme induction
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Live vaccines: Should be avoided due to immunosuppressive risk
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NSAIDs: Co-use may increase GI ulcer risk
No need to adjust doses of commonly used IBD agents (e.g., mesalamine, azathioprine) when combined with beclometasone.
Comparative Summary with Other Corticosteroids (Narrative)
Compared to prednisolone, beclometasone has less systemic exposure and a better safety profile, particularly in mild to moderate ulcerative colitis. It lacks the mineralocorticoid activity of prednisolone, making fluid retention and hypertension less likely.
Compared to budesonide, which is also an enteric steroid, beclometasone has similar efficacy in distal bowel disease. However, budesonide (Entocort, Budenofalk) is preferred for Crohn’s disease involving the terminal ileum due to targeted release and extensive study backing.
Beclometasone is not as effective for systemic inflammatory conditions (e.g., lupus, asthma) where higher systemic steroid levels are required.
Patient Counseling Points
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Swallow tablet whole with water, do not chew or crush
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Take in the morning before food, preferably on an empty stomach
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Treatment is typically limited to 8 weeks or less unless advised
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Report any symptoms of infection, visual changes, or persistent abdominal pain
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Do not stop abruptly after prolonged use; follow your doctor’s tapering instructions
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Notify your physician if taking other immunosuppressants, antifungals, or HIV medications
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Avoid live vaccines during treatment
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Advise women to notify physician if pregnant or breastfeeding
Storage and Handling
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Store at room temperature (15–25°C)
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Protect from moisture and light
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Keep out of reach of children
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Use within the expiry date on packaging
Regulatory and Clinical Notes
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Approved in several European countries (e.g., UK, Italy) for ulcerative colitis
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Not available or not widely marketed in the United States or Canada
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Often prescribed as a step-down therapy after prednisolone to reduce steroid burden
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Some guidelines (e.g., British Society of Gastroenterology) mention beclometasone as an option for induction of remission in mild to moderate UC, particularly if mesalamine fails
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