Calcort (deflazacort) is a potent glucocorticoid medication engineered for the management of severe inflammatory and autoimmune conditions. As a second-generation corticosteroid, it offers a refined therapeutic profile, balancing high anti-inflammatory and immunosuppressive efficacy with a potentially improved tolerability spectrum compared to older agents. It is specifically indicated for conditions where rapid control of disease activity is critical to prevent tissue damage and long-term disability. This expert guide provides a comprehensive overview of its pharmacology, clinical application, and essential safety information for healthcare professionals.

Features

• Active Pharmaceutical Ingredient: Deflazacort
• Pharmacologic Class: Second-generation glucocorticoid
• Available Formulations: 6 mg and 30 mg tablets
• Mechanism of Action: Binds to intracellular glucocorticoid receptors, modulating gene transcription to exert potent anti-inflammatory and immunosuppressive effects.
• Prodrug Status: Administered as an inactive prodrug, hydrolyzed to the active metabolite, 21-desdeflazacort, after absorption.
• Bioavailability: High oral bioavailability.
• Half-life: The active metabolite has a plasma elimination half-life of approximately 1.1 to 1.9 hours, though biological activity persists longer due to genomic effects.

Benefits

• Potent and Rapid Anti-inflammatory Action: Provides swift and effective suppression of the inflammatory cascade, crucial for controlling acute exacerbations of autoimmune diseases.
• Immunosuppressive Efficacy: Effectively modulates the immune system’s aberrant response, reducing autoimmune attack on tissues and organs.
• Potential for a Favorable Side Effect Profile: Some clinical data suggests a potentially lower propensity for weight gain and fluid retention compared to prednisone at equipotent doses, though evidence is not conclusive for all side effects.
• Dosing Flexibility: Available in two tablet strengths (6 mg and 30 mg) to allow for precise titration and tailored tapering regimens based on individual patient response and disease severity.
• Established Clinical Utility: Has a well-documented history of use in managing a range of severe inflammatory conditions, providing a reliable option within the corticosteroid armamentarium.

Common use

Calcort is indicated for the treatment of inflammatory and autoimmune disorders where corticosteroid therapy is warranted. Its use is typically reserved for conditions that are severe, disabling, or unresponsive to first-line treatments. Common therapeutic applications include, but are not limited to:

• Rheumatic disorders (e.g., severe active rheumatoid arthritis, polymyalgia rheumatica)
• Systemic connective tissue diseases (e.g., systemic lupus erythematosus, dermatomyositis, polymyositis)
• Severe allergic states refractory to conventional treatment
• Severe dermatological conditions (e.g., pemphigus, severe psoriasis)
• Autoimmune-related ocular conditions (e.g., uveitis)
• Management of certain hematologic and oncologic conditions
• As an immunosuppressant in organ transplantation (adjunctive therapy)

The decision to initiate therapy with Calcort requires a careful risk-benefit assessment by a specialist physician due to its significant potential for serious adverse effects.

Dosage and direction

Administration: For oral administration. Tablets should be taken whole with a meal or a glass of milk to minimize potential gastrointestinal discomfort.

Dosage Principle: Dosage must be individualized based on the specific disease, its severity, and the patient’s response. The lowest effective dose should be used for the shortest possible duration.

Initial Dose: For many inflammatory conditions, the initial dose typically ranges from 0.5 to 1.5 mg deflazacort/kg/day (approximately 36 to 108 mg for a 72 kg patient), often administered as a single daily dose or in divided doses. In adult rheumatoid arthritis, a common starting dose is 6 to 90 mg daily.

Dosage Equivalence: 6 mg of deflazacort is approximately equivalent to 5 mg of prednisone/prednisolone in anti-inflammatory potency.

Tapering (Crucial): Abrupt withdrawal after prolonged therapy can lead to adrenal insufficiency. Dosage must be tapered gradually based on disease activity and duration of treatment. Tapering schedules are highly individualized but often involve reducing the daily dose by 5-10% weekly or biweekly until a minimal maintenance dose is reached or until therapy can be discontinued.

Missed Dose: See specific section.

Precautions

• Adrenal Suppression: Prolonged therapy suppresses hypothalamic-pituitary-adrenal (HPA) axis function. Patients are at risk for adrenal insufficiency during therapy and for up to a year after discontinuation. Stress (e.g., surgery, trauma, infection) requires supplemental corticosteroids.
• Infections: Suppression of the immune system increases susceptibility to all types of infections (viral, bacterial, fungal, parasitic, opportunistic). Latent infections (e.g., tuberculosis) may be reactivated. Monitor patients closely; any sign of infection must be investigated.
• Vaccinations: Avoid live or live-attenuated vaccines during therapy. Killed or inactivated vaccines may have a diminished response.
• Cardiovascular/Renal: Use with caution in patients with hypertension, congestive heart failure, or renal insufficiency due to risks of fluid and electrolyte disturbances (sodium retention, potassium loss, hypokalemic alkalosis).
• Musculoskeletal: Increased risk of osteoporosis, vertebral compression fractures, aseptic necrosis of bone (e.g., femoral head), myopathy, and tendon rupture. Prophylactic treatment for osteoporosis should be considered for long-term therapy.
• Ophthalmic: May cause posterior subcapsular cataracts, increased intraocular pressure (glaucoma), and exacerbate ocular viral or fungal infections.
• Gastrointestinal: Increased risk of peptic ulceration with potential for perforation and hemorrhage, pancreatitis, and ulcerative esophagitis. Use with caution in patients with GI disorders.
• Neuropsychiatric: May cause euphoria, insomnia, mood swings, personality changes, severe depression, or frank psychotic manifestations.
• Metabolic: Can cause hyperglycemia, worsening of pre-existing diabetes, increased appetite and weight gain, and lipodystrophy (Cushingoid state).
• Dermatologic: Impaired wound healing, thin fragile skin, petechiae, ecchymoses, facial erythema.

Contraindications

Calcort is contraindicated in patients with:

• Known hypersensitivity to deflazacort or any component of the formulation.
• Systemic fungal infections (unless being treated for a specific fungal infection with appropriate antifungals).
• Live virus vaccination during treatment (see Precautions).
• Important Note: Contraindications can be relative in life-threatening situations. The clinical context must always be considered.

Possible side effect

Adverse reactions are dose and duration-dependent. Common and serious side effects include:

• Very Common (>1/10): Sleep disturbance, increased appetite, weight gain, Cushingoid appearance, dyspepsia.
• Common (1/10 to 1/100): Fluid retention, hypertension, mood alterations (euphoria, depression), glucose intolerance, increased susceptibility to infections, skin atrophy, bruising, acne, hirsutism, menstrual irregularities, muscle weakness (steroid myopathy), osteoporosis.
• Uncommon (1/100 to 1/1000): Peptic ulcer, pancreatitis, increased intracranial pressure with papilledema (pseudotumor cerebri), glaucoma, cataracts, cardiac insufficiency in susceptible patients, aggravation of diabetes mellitus.
• Rare (<1/1000): Aseptic necrosis of the femoral head, severe psychiatric reactions, anaphylactoid reactions.

Drug interaction

Concomitant use with the following agents requires careful monitoring and potential dosage adjustment:

• Enzyme Inducers (e.g., Rifampicin, Phenytoin, Carbamazepine, Phenobarbital): May increase the clearance of corticosteroids, reducing their efficacy.
• Enzyme Inhibitors (e.g., Ketoconazole, Itraconazole): May decrease corticosteroid metabolism, increasing the risk of toxicity.
• Anticoagulants (e.g., Warfarin): Corticosteroids may alter the response to anticoagulants; monitor INR closely.
• Antidiabetics (Insulin, Oral Hypoglycemics): Corticosteroids increase blood glucose; antidiabetic therapy will likely need adjustment.
• Diuretics (especially potassium-depleting, e.g., Thiazides, Furosemide): Concomitant use amplifies the risk of severe hypokalemia.
• NSAIDs (e.g., Ibuprofen, Naproxen): Concurrent use significantly increases the risk of GI ulceration and bleeding.
• Cardiac Glycosides (e.g., Digoxin): Hypokalemia potentiates the risk of digitalis toxicity.
• Vaccines: See Precautions.

Missed dose

• If a dose is missed, it should be taken as soon as remembered on the same day.
• If it is not remembered until the next day’s dose is due, the patient should skip the missed dose and take the next dose at the regular time.
• Do not double the dose to make up for the missed one.

Overdose

• Manifestation: Acute overdose is unlikely to cause acute life-threatening toxicity in a single dose but may exacerbate the known dose-related adverse effects (severe metabolic disturbances, hypertension, psychosis, fluid overload).
• Management: There is no specific antidote. Treatment is supportive and symptomatic. Gastric lavage or activated charcoal may be considered if ingestion was very recent. Manage electrolyte imbalances and provide general supportive care. Monitor closely for adrenal insufficiency during subsequent days if the overdose occurred in the context of chronic therapy followed by abrupt cessation.

Storage

• Store below 25°C (77°F).
• Keep in the original package to protect from light and moisture.
• Keep out of sight and reach of children.

Disclaimer

This information is for educational purposes and is intended for healthcare professionals. It is a summary and does not replace the full manufacturer’s prescribing information or professional clinical judgment. The prescriber must refer to the complete local SmPC or product monograph for full details on indications, dosing, warnings, and contraindications before initiating therapy. Dosage, indications, and product availability may vary by country.

Reviews

• “As a rheumatologist, I find Calcort to be a valuable tool for managing severe flares of polymyalgia rheumatica. The tapering schedule is manageable, and some patients report a subjective difference in side effects like weight gain compared to their previous prednisone regimens, though this is not universally observed. Its role is firmly established in my practice for specific patient profiles.” – Dr. A. Vance, MD, Rheumatology
• “In our neurology department, we utilize deflazacort for certain inflammatory neuropathies and myositis. Its potency is reliable for achieving rapid control. The paramount concern, as with all corticosteroids, remains the meticulous management of the taper and vigilant monitoring for the long catalog of potential adverse events. Patient education is non-negotiable.” – Prof. L. Evans, Neurology
• “From a pharmacological standpoint, the prodrug nature of deflazacort and its metabolic pathway present an interesting profile. While the clinical significance of its purported ‘better tolerability’ is still debated in the literature and may be patient-specific, it remains a potent and effective glucocorticoid option within our formulary.” – M. Sharma, PharmD, Clinical Pharmacy