1. Clinical Overview
Prednisolone is a synthetic glucocorticoid, a potent anti-inflammatory and immunosuppressant agent. It is the active metabolite of prednisone, converted in the liver. It is a mainstay in managing a wide spectrum of inflammatory, allergic, autoimmune, and neoplastic conditions in the Indian healthcare setting. Its effects are mediated through genomic and non-genomic pathways.
| Onset | Duration | Bioavailability |
|---|---|---|
| Rapid. Pharmacological effects begin within 1-2 hours of oral administration. | Intermediate-acting. Biological half-life is 18-36 hours, allowing for once-daily or alternate-day dosing in many regimens. | High, approximately 80-90% following oral administration. |
2. Mechanism of Action
Prednisolone exerts its effects by diffusing across cell membranes and binding with high affinity to cytoplasmic glucocorticoid receptors (GR). The activated receptor-ligand complex translocates to the nucleus, where it modulates gene transcription (genomic effects). It binds to glucocorticoid response elements (GREs), leading to increased transcription of anti-inflammatory proteins (e.g., lipocortin-1, IκBα) and decreased transcription of pro-inflammatory proteins (e.g., cytokines, chemokines, adhesion molecules, inflammatory enzymes like COX-2). It also has rapid non-genomic effects influencing signaling pathways.
3. Indications & Uses
- Rheumatoid Arthritis (severe, active)
- Systemic Lupus Erythematosus (SLE)
- Severe Asthma and COPD exacerbations
- Acute Gout (when NSAIDs contraindicated)
- Dermatological conditions (Pemphigus vulgaris, Severe psoriasis, Exfoliative dermatitis)
- Inflammatory Bowel Disease (Ulcerative Colitis, Crohn's disease exacerbations)
- Nephrotic Syndrome (idiopathic, minimal change disease)
- Allergic conditions refractory to conventional treatment (Severe allergic rhinitis, Contact dermatitis)
- Ophthalmic inflammatory diseases (via systemic route for posterior segment involvement)
- Cerebral edema (associated with primary or metastatic brain tumors, TBI)
4. Dosage & Administration
Adult Dosage: Highly variable. Initial: 5mg to 60mg per day, often as a single morning dose or divided. E.g., Rheumatoid Arthritis: 5-10mg/day; SLE flare: 20-60mg/day; Asthma exacerbation: 30-50mg/day for 5-10 days; Nephrotic syndrome: 1mg/kg/day (up to 80mg) for 6 weeks followed by taper.
Administration: Take with food or milk to minimize gastric irritation. For once-daily dosing, take in the morning (around 8 AM) to coincide with the body's natural cortisol peak and reduce HPA axis suppression. Do not crush or chew enteric-coated tablets. Do not stop abruptly after prolonged use (>2-3 weeks). Always taper the dose under medical supervision.
5. Side Effects
Common side effects may include:
- Increased appetite, weight gain (central obesity)
- Insomnia, mood swings, nervousness
- Indigestion, dyspepsia, nausea
- Fluid retention, edema, facial rounding (moon face)
- Acne, thin fragile skin, easy bruising
- Hirsutism
- Delayed wound healing
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of gastrointestinal ulceration and bleeding. | Major |
| Anticoagulants (Warfarin) | Prednisolone may alter warfarin response (increase or decrease INR); monitor closely. | Moderate |
| Antidiabetics (Insulin, Metformin, Sulfonylureas) | Prednisolone causes hyperglycemia; may require increased antidiabetic dose. | Major |
| Diuretics (Furosemide, Hydrochlorothiazide) | Enhanced potassium loss; increased risk of hypokalemia. | Moderate |
| CYP3A4 Inducers (Rifampicin, Phenytoin, Carbamazepine) | Increased metabolism of prednisolone, reducing its efficacy. Dose increase may be needed. | Major |
| CYP3A4 Inhibitors (Ketoconazole, Itraconazole, Clarithromycin) | Decreased metabolism of prednisolone, increasing toxicity risk. Dose reduction may be needed. | Major |
| Live Vaccines (MMR, Varicella, OPV) | Diminished immune response; risk of disseminated infection. Contraindicated. | Major |
| Cardiac Glycosides (Digoxin) | Hypokalemia induced by prednisolone increases risk of digoxin toxicity. | Moderate |
7. Patient Counselling
- DO take the medicine exactly as prescribed, with food or milk.
- DO NOT stop taking the medicine suddenly if you have been on it for more than 2-3 weeks. Always taper as directed.
- DO inform all your doctors and dentists that you are taking prednisolone, especially before any surgery.
- DO carry a steroid alert card or wear medical identification jewelry.
- DO NOT take any live vaccines (e.g., MMR, chickenpox) without consulting your doctor.
- DO NOT take over-the-counter NSAIDs (like ibuprofen) without asking your doctor.
8. Toxicology & Storage
Overdose: Acute single overdose is unlikely to cause life-threatening toxicity. Symptoms would be an exaggeration of pharmacological effects: severe hypertension, hyperglycemia, fluid retention, psychosis, electrolyte imbalances (hypokalemia). Chronic overdose leads to iatrogenic Cushing's syndrome.
Storage: Store below 30°C, in a cool, dry place. Protect from light and moisture. Keep the container tightly closed. Keep out of reach of children. Do not use after the expiry date printed on the pack.