Entocort (budesonide) is a locally acting glucocorticosteroid specifically designed for the treatment of mild to moderate active Crohn’s disease affecting the ileum and/or ascending colon, and for the maintenance of clinical remission. Its advanced delivery system ensures the active ingredient is primarily released in the terminal ileum and right colon, maximizing topical efficacy at the site of inflammation while minimizing systemic exposure. This results in a highly favorable risk-benefit profile, offering patients effective symptom control with a reduced incidence of steroid-related side effects compared to conventional systemic corticosteroids.

Features

• Active ingredient: Budesonide (3 mg per capsule)
• Formulation: pH-dependent, extended-release capsules
• Mechanism: Locally acting glucocorticoid with high topical anti-inflammatory activity
• Delivery System: Designed for targeted release in the terminal ileum and ascending colon (pH > 6.4)
• Extensive first-pass metabolism: Approximately 90% metabolized in the liver, limiting systemic bioavailability to about 9%
• Half-life: 2-3 hours

Benefits

• Provides potent, targeted anti-inflammatory action directly at the site of bowel inflammation.
• Achieves high rates of clinical remission and symptom control in active Crohn’s disease.
• Significantly reduces the risk of systemic corticosteroid side effects, such as moon face, buffalo hump, and adrenal suppression, compared to prednisone.
• Supports mucosal healing, a key treatment goal in inflammatory bowel disease management.
• Offers a favorable safety profile for medium to long-term maintenance therapy in appropriate patients.
• Improves quality of life by effectively controlling debilitating symptoms like abdominal pain and diarrhea.

Common use

Entocort is primarily indicated for the treatment of mild to moderate active Crohn’s disease involving the ileum and/or the ascending colon. Its targeted release mechanism makes it particularly suitable for this specific disease localization. It is also used for the maintenance of clinical remission for up to 3 months in adult patients. While its primary use is in gastroenterology for Crohn’s, the active ingredient, budesonide, is also formulated for use in other conditions such as asthma (via inhalation) and allergic rhinitis (nasal spray), though these are distinct pharmaceutical products.

Dosage and direction

For the induction of remission in active Crohn’s disease, the recommended adult dosage is 9 mg once daily in the morning for up to 8 weeks. Re-evaluation of the patient’s condition is necessary if symptoms persist after 8 weeks of treatment. For the maintenance of clinical remission, the dosage is 6 mg once daily for up to 3 months. A gradual dose reduction is not typically required when discontinuing treatment due to its low systemic bioavailability. The capsules must be swallowed whole with water and must not be chewed or crushed. They can be taken with or without food.

Precautions

Patients should be monitored for signs of hypercorticism and adrenal suppression, especially when transferring from systemic steroids or if used for prolonged periods. Caution is advised in patients with liver impairment, as budesonide metabolism may be reduced, potentially increasing systemic exposure. The use of Entocort may mask symptoms of infection; new infections may appear, and existing infections may worsen. Live or live-attenuated vaccines should be avoided during therapy. Patients should inform their physician of any recent exposure to infections such as chickenpox or measles. Long-term use may be associated with a reduction in bone mineral density; appropriate monitoring should be considered. Ophthalmic examinations should be considered for patients with a history of increased intraocular pressure, glaucoma, or cataracts.

Contraindications

Entocort is contraindicated in patients with known hypersensitivity to budesonide or any of the excipients in the formulation. Its use is contraindicated in patients with severe liver impairment (Child-Pugh Class C), as this can significantly impair the metabolism of budesonide, leading to markedly increased systemic steroid exposure and associated adverse effects.

Possible side effect

The majority of side effects are related to the local glucocorticoid action and are generally mild. Common side effects (≥1/100 to <1/10) include:

• Headache
• Nausea
• Dyspepsia
• Abdominal pain
• Flatulence
• Fatigue Less common side effects may include:
• Acne
• Anxiety, mood changes
• Sleep disorder
• Muscle cramps
• Peripheral edema
• Increased blood pressure Although rare due to low systemic exposure, side effects typical of systemic corticosteroids (e.g., adrenal suppression, cushinoid features, glaucoma) can occur, particularly with prolonged use or in patients with liver disease.

Drug interaction

The efficacy of Entocort can be significantly altered by drugs that affect the cytochrome P450 3A4 (CYP3A4) enzyme system.

• Potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin): Concomitant use is not recommended, as these drugs can inhibit the metabolism of budesonide, leading to a several-fold increase in its systemic exposure and plasma concentration.
• Inducers of CYP3A4 (e.g., rifampicin, carbamazepine, phenytoin, St. John’s Wort): Coadministration may lead to a reduced therapeutic effect of budesonide due to increased metabolism and clearance.
• Estrogens: Oral contraceptives and hormone replacement therapy containing estrogens may moderately increase budesonide plasma levels.

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. If a full day has passed, the patient should skip the missed dose and take the next dose at the usual time. Patients should not take a double dose to make up for a forgotten one. Maintaining a consistent daily routine is important for optimal efficacy.

Overdose

Single acute overdosage is unlikely due to the formulation and low systemic bioavailability. However, acute massive overdose could potentially lead to systemic glucocorticoid effects such as hypercorticism and adrenal suppression. There is no specific antidote. Treatment should be symptomatic and supportive. In cases of chronic overdose, the dose should be reduced gradually under medical supervision.

Storage

Store below 25°C (77°F). Keep the bottle tightly closed in order to protect from moisture. Store in the original container. Keep out of the sight and reach of children. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

• “As a gastroenterologist, Entocort has become a first-line tool for managing ileal and right-sided Crohn’s flares. Its targeted action allows me to achieve remission with a side effect profile my patients tolerate far better than traditional prednisone.” – Dr. A. Sharma, MD, Gastroenterologist
• “The difference in my quality of life since switching to Entocort is night and day. My symptoms are under control, and I haven’t experienced the weight gain and mood swings I had with previous medications.” – Patient M.T., diagnosed 2018
• “From a clinical trial perspective, the data consistently shows Entocort’s superiority over mesalamine and near-equivalent efficacy to prednisone for its indicated use, but with a safety profile that allows for longer-term management strategies.” – Clinical Research Scientist
• “Finding a medication that worked for my proximal disease was a struggle. Entocort provided significant relief from abdominal pain and diarrhea within a few weeks, and I’ve been able to maintain remission on the maintenance dose.” – Patient J.K., diagnosed 2020