Introduction
Celestone (betamethasone) is a potent synthetic glucocorticoid medication belonging to the corticosteroid class. It is widely used in clinical practice for its anti-inflammatory, immunosuppressive, and metabolic effects. Betamethasone is approximately 25-30 times more potent than hydrocortisone and has minimal mineralocorticoid activity, making it particularly useful for conditions requiring strong anti-inflammatory effects without significant fluid retention.
Mechanism of Action
Betamethasone exerts its effects by diffusing across cell membranes and binding to intracellular glucocorticoid receptors. This drug-receptor complex translocates to the nucleus where it modulates gene transcription by:
- Binding to glucocorticoid response elements (GREs) to initiate anti-inflammatory protein synthesis
- Inhibiting transcription factors such as NF-κB and AP-1 that promote inflammatory gene expression
- Reducing synthesis of inflammatory mediators including prostaglandins, leukotrienes, and cytokines
- Decreasing inflammatory cell migration and function
- Stabilizing lysosomal membranes and reducing capillary permeability
Indications
FDA-approved indications:- Inflammatory and allergic conditions (rheumatoid arthritis, collagen diseases, dermatologic diseases, allergic states)
- Endocrine disorders (adrenal insufficiency, congenital adrenal hyperplasia)
- Hematologic disorders (autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura)
- Respiratory diseases (bronchial asthma, aspiration pneumonitis)
- Gastrointestinal diseases (ulcerative colitis, regional enteritis)
- Neoplastic diseases (palliative management of leukemias and lymphomas)
- Ophthalmic inflammatory conditions
- Edematous states (nephrotic syndrome)
- Antenatal administration for fetal lung maturation (betamethasone is preferred over dexamethasone)
- Management of acute spinal cord injury
- Treatment of acute exacerbations of multiple sclerosis
Dosage and Administration
Adult dosing:- Oral: 0.6-7.2 mg daily in divided doses
- IM/IV: 0.5-9 mg daily (as betamethasone sodium phosphate)
- Intra-articular/soft tissue: 0.25-2.0 mL (depending on joint size)
- Hepatic impairment: Dose reduction required
- Renal impairment: Caution advised; no specific dosage adjustment
- Elderly: Lower doses may be appropriate due to increased sensitivity
- Pediatrics: 0.0175-0.25 mg/kg/day divided every 6-8 hours
- 12 mg IM every 24 hours for 2 doses
Pharmacokinetics
Absorption: Well absorbed from GI tract; oral bioavailability approximately 70-90% Distribution: Widely distributed throughout body tissues; crosses placenta and blood-brain barrier; volume of distribution approximately 1.4 L/kg; plasma protein binding 64% Metabolism: Hepatic metabolism via CYP3A4 to inactive metabolites Elimination: Primarily renal excretion (45% within 24 hours); elimination half-life 36-54 hoursContraindications
- Systemic fungal infections
- Hypersensitivity to betamethasone or any component of the formulation
- Live virus vaccinations during immunosuppressive therapy
- Idiopathic thrombocytopenic purpura (IM administration)
Warnings and Precautions
Black Box Warnings:- Corticosteroids can cause serious and fatal infections
- Recent MI risk may be increased with corticosteroid use
- Gastrointestinal perforation risk in certain disorders
- Serious skin reactions including toxic epidermal necrolysis
- Adrenal suppression with long-term use
- Increased intraocular pressure and cataract formation
- Psychiatric effects including euphoria, insomnia, mood swings, depression
- Impaired wound healing
- Osteoporosis and avascular necrosis
- Hyperglycemia and diabetes mellitus
- Hypertension and fluid retention
- Growth suppression in children
- Myopathy with high doses
Drug Interactions
Significant interactions:- Anticoagulants: Altered response to anticoagulants
- Antidiabetic agents: Reduced hypoglycemic effect
- CYP3A4 inducers (phenytoin, rifampin): Reduced betamethasone efficacy
- CYP3A4 inhibitors (ketoconazole): Increased betamethasone levels
- Diuretics: Enhanced potassium wasting
- NSAIDs: Increased risk of GI ulceration
- Vaccines: Reduced immune response to vaccines
- Cardiac glycosides: Increased risk of arrhythmias due to hypokalemia
Adverse Effects
Common (≥1%):- Insomnia
- Increased appetite
- Weight gain
- Fluid retention
- Mood changes
- Hyperglycemia
- Hypertension
- Increased susceptibility to infections
- Adrenal insufficiency
- Severe infections
- Gastrointestinal perforation
- Osteoporosis and fractures
- Avascular necrosis
- Posterior subcapsular cataracts
- Glaucoma
- Severe psychiatric reactions
- Anaphylaxis
Monitoring Parameters
Baseline assessment:- Complete blood count
- Electrolytes (especially potassium)
- Blood glucose
- Blood pressure
- Bone density (if long-term therapy anticipated)
- Ophthalmologic examination
- Weight and height (pediatrics)
- Blood glucose regularly
- Blood pressure at each visit
- Weight changes
- Signs of infection
- Electrolytes periodically
- Bone density annually for long-term therapy
- Ophthalmologic exams annually
- Growth velocity in children
- Not routinely performed
- Clinical assessment of response and adverse effects guides therapy
Patient Education
Key points to communicate:- Take exactly as prescribed; do not stop abruptly
- Report any signs of infection (fever, sore throat)
- Monitor for weight gain, swelling, or mood changes
- Regular blood sugar checks if diabetic
- Inform all healthcare providers about corticosteroid use
- Carry medical alert identification
- Avoid live vaccines while taking this medication
- Report any vision changes or eye pain
- Take with food to reduce GI upset
- Do not take with NSAIDs unless directed by physician
- Importance of regular follow-up appointments
- Calcium and vitamin D supplementation may be recommended
- Pregnancy: Discuss risks/benefits with obstetrician
- Elderly: Increased risk of adverse effects
- Pediatrics: Monitor growth carefully
References
1. Lexicomp Online. Betamethasone. Wolters Kluwer Clinical Drug Information, Inc.; 2023. 2. Micromedex Solutions. Betamethasone. IBM Watson Health; 2023. 3. Clinical Pharmacology [database online]. Betamethasone. Elsevier; 2023. 4. National Institutes of Health. Betamethasone. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury; 2021. 5. American College of Obstetricians and Gynecologists. Antenatal Corticosteroid Therapy for Fetal Maturation. ACOG Committee Opinion No. 797. Obstet Gynecol. 2020;135(2):e73-e77. 6. Liu D, Ahmet A, Ward L, et al. A practical guide to the monitoring and management of the complications of systemic corticosteroid therapy. Allergy Asthma Clin Immunol. 2013;9(1):30. 7. Czock D, Keller F, Rasche FM, Häussler U. Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. 8. Fardet L, Petersen I, Nazareth I. Suicidal behavior and severe neuropsychiatric disorders following glucocorticoid therapy in primary care. Am J Psychiatry. 2012;169(5):491-497. 9. Williams DM. Clinical pharmacology of corticosteroids. Respir Care. 2018;63(6):655-670. 10. Yasir M, Goyal A, Sonthalia S. Corticosteroid Adverse Effects. In: StatPearls. Treasure Island (FL): StatPearls Publishing; 2023.