1. Clinical Overview
Prednisolone is a synthetic glucocorticoid, a potent anti-inflammatory and immunosuppressant agent. It is the active metabolite of prednisone, formed in the liver. It is a mainstay of therapy for a wide range of inflammatory, allergic, autoimmune, and neoplastic conditions in the Indian healthcare setting. Its efficacy must be balanced against a significant risk of dose and duration-dependent adverse effects.
| Onset | Duration | Bioavailability |
|---|---|---|
| Rapid; anti-inflammatory and immunosuppressive effects begin within 1-2 hours of oral administration. | Intermediate-acting glucocorticoid; biological half-life is 18-36 hours, allowing for once-daily dosing in many regimens. | High, approximately 80-90% following oral administration. |
2. Mechanism of Action
Prednisolone binds to the cytosolic glucocorticoid receptor (GR), forming a complex that translocates to the nucleus. This complex binds to Glucocorticoid Response Elements (GREs) in DNA, modulating gene transcription. It increases transcription of anti-inflammatory proteins (e.g., lipocortin-1, IL-10) and decreases transcription of pro-inflammatory proteins (e.g., cytokines, chemokines, adhesion molecules, inflammatory enzymes like COX-2). It also has post-transcriptional effects.
3. Indications & Uses
- Rheumatoid Arthritis
- Systemic Lupus Erythematosus (SLE)
- Acute Severe Asthma & COPD Exacerbations
- Allergic Conditions (Severe allergic rhinitis, contact dermatitis)
- Dermatological Conditions (Pemphigus vulgaris, severe psoriasis)
- Nephrotic Syndrome
- Inflammatory Bowel Disease (Ulcerative colitis, Crohn's disease flare-ups)
- Organ Transplantation (Immunosuppression)
4. Dosage & Administration
Adult Dosage: Highly variable based on condition. Anti-inflammatory/Immunosuppressive: 5-60 mg/day orally in single or divided doses. Severe conditions: Initial dose up to 60 mg/day, tapered. Adrenal insufficiency replacement: 4-5 mg/m²/day.
Administration: Administer with or immediately after food to reduce GI irritation. Single daily doses should be taken in the morning (around 8 AM) to mimic the body's natural cortisol rhythm and minimize HPA axis suppression. Do not crush or chew enteric-coated tablets. For tapering, reduce dose gradually (e.g., 2.5-5 mg every 3-7 days) based on response and duration of therapy.
5. Side Effects
Common side effects may include:
- Increased appetite, weight gain (central obesity)
- Insomnia, mood changes (euphoria, irritability)
- Fluid retention, edema, hypertension
- Dyspepsia, gastritis
- Hyperglycemia (steroid-induced diabetes)
- Cushingoid appearance (moon face, buffalo hump)
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of GI ulceration and bleeding | Major |
| Warfarin | Altered INR response (may increase or decrease); monitor INR closely | Moderate |
| Antidiabetics (Insulin, Metformin) | Prednisolone causes hyperglycemia; may require dose adjustment of antidiabetics | Major |
| Diuretics (Furosemide, Hydrochlorothiazide) | Enhanced potassium loss, severe hypokalemia | Major |
| Phenytoin, Phenobarbital, Rifampicin | Increased hepatic metabolism of prednisolone, reducing its efficacy | Major |
| Ketoconazole, Itraconazole, Clarithromycin | Inhibit CYP3A4, increasing prednisolone levels and toxicity | Major |
| Live Vaccines (MMR, Varicella, OPV) | Reduced immune response, risk of vaccine-induced infection | Contraindicated |
7. Patient Counselling
- DO take the medicine exactly as prescribed. Do not stop suddenly.
- DO take with food or milk to avoid stomach upset.
- DO inform all your doctors and dentists that you are taking this medicine.
- DO carry a steroid alert card/bracelet.
- DON'T take live vaccines (like MMR, chickenpox) without consulting your doctor.
- DON'T take over-the-counter NSAIDs (like ibuprofen) without asking your doctor.
- DON'T change the brand or formulation without medical advice, as bioavailability may differ.
8. Toxicology & Storage
Overdose: Acute overdose is unlikely to cause acute life-threatening toxicity in a single instance. Symptoms would be an exaggeration of pharmacological effects: severe hypertension, hyperglycemia, fluid retention, hypokalemia, psychosis, and acute gastritis. Chronic overdose leads to Cushing's syndrome.
Storage: Store at room temperature (15-25°C), protected from light and moisture. Keep out of reach of children. Do not use after the expiry date printed on the pack. Do not flush unused medication; consult a pharmacist for safe disposal.