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. The 40mg strength is a high-dose formulation primarily used for acute, severe inflammatory conditions, autoimmune disorders, and as part of induction or pulse therapy regimens. It mimics the effects of cortisol but with greater potency and longer duration.
| Onset | Duration | Bioavailability |
|---|---|---|
| Oral: 1-2 hours for physiological effects; anti-inflammatory/immunosuppressive effects may take several hours to days. | Intermediate-acting glucocorticoid. Biological half-life is 18-36 hours. Duration of action exceeds plasma half-life due to genomic effects. | Approximately 80-90% after oral administration. |
2. Mechanism of Action
Prednisolone binds to intracellular glucocorticoid receptors (GR) in the cytoplasm. The receptor-ligand complex translocates to the nucleus, where it binds to glucocorticoid response elements (GREs) on DNA, modulating gene transcription. This leads to increased synthesis of anti-inflammatory proteins (e.g., lipocortin-1) and decreased synthesis of pro-inflammatory mediators (e.g., cytokines, chemokines, adhesion molecules, enzymes like COX-2). It also induces apoptosis of lymphocytes.
3. Indications & Uses
- Severe allergic conditions (anaphylaxis, angioedema)
- Rheumatic disorders (acute gout, severe rheumatoid arthritis, polymyalgia rheumatica)
- Autoimmune diseases (Systemic Lupus Erythematosus, dermatomyositis)
- Severe dermatological conditions (pemphigus, severe psoriasis, exfoliative dermatitis)
- Acute exacerbations of multiple sclerosis
- Organ transplantation (immunosuppression)
- Nephrotic syndrome
- Severe asthma/COPD exacerbation
4. Dosage & Administration
Adult Dosage: Highly variable. For severe conditions: 40-60mg/day in single or divided doses. Maintenance: Reduce to lowest effective dose (often 5-15mg/day). For pulse therapy: Up to 1g/day IV, oral equivalent used cautiously.
Administration: Take with food or milk to minimize GI upset. Usually taken as a single dose in the morning (8 AM) to coincide with the body's natural cortisol rhythm and reduce HPA axis suppression. Do not stop abruptly; taper gradually under medical supervision. Tablet can be crushed if needed.
5. Side Effects
Common side effects may include:
- Insomnia
- Increased appetite, weight gain
- Fluid retention, edema
- Mood swings, nervousness
- Dyspepsia, heartburn
- Acne
- Easy bruising
- Hirsutism
- Moon face
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Warfarin | Altered anticoagulant effect (increase or decrease); monitor INR closely. | Major |
| Phenytoin, Phenobarbital, Rifampicin | Increased hepatic metabolism of prednisolone, reducing its efficacy. Dose adjustment needed. | Major |
| Ketoconazole, Itraconazole, Clarithromycin | Inhibit CYP3A4, increasing prednisolone levels and risk of toxicity. | Major |
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of GI ulceration and bleeding. | Major |
| Diuretics (e.g., Furosemide, Hydrochlorothiazide) | Enhanced potassium loss, severe hypokalemia. | Major |
| Insulin, Oral Hypoglycemics | Prednisolone causes hyperglycemia; may require increased antidiabetic dose. | Major |
| Live Vaccines (MMR, Varicella, OPV) | Risk of disseminated infection; avoid. | Contraindicated |
| Digoxin | Hypokalemia increases risk of digoxin toxicity. | Moderate |
7. Patient Counselling
- DO take exactly as prescribed, with food.
- DO NOT stop taking suddenly. Dose must be tapered.
- DO carry a steroid alert card/bracelet.
- DO inform all doctors and dentists you are taking this medicine.
- DO get regular check-ups for BP, blood sugar, eyes, and bone density if on long-term therapy.
- DONT take live vaccines without consulting your doctor.
- DONT take OTC NSAIDs without asking your doctor.
8. Toxicology & Storage
Overdose: Acute: Severe electrolyte imbalance (hypokalemia), hypertension, hyperglycemia, psychosis, fluid overload, congestive heart failure. Chronic: Cushing's syndrome, adrenal suppression, severe infections, osteoporosis, myopathy.
Storage: Store below 30°C in a cool, dry place, protected from light and moisture. Keep out of reach of children. Do not use after the expiry date printed on the pack.