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 30mg strength is typically used for short-term, high-dose 'pulse therapy' or as part of a tapering regimen for severe inflammatory and autoimmune conditions. It mimics the action of cortisol but with greater potency and longer duration.
| Onset | Duration | Bioavailability |
|---|---|---|
| Rapid. Peak plasma concentrations reached within 1-2 hours after oral administration. | Intermediate-acting glucocorticoid. Biological half-life is 18-36 hours, allowing for once-daily dosing. | High, approximately 80-90% after 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 non-genomic rapid effects.
3. Indications & Uses
- Severe allergic conditions (anaphylaxis, angioedema)
- Rheumatic disorders (Severe Rheumatoid Arthritis, Polymyalgia Rheumatica, Acute Gout)
- Systemic Lupus Erythematosus (SLE) flare
- Severe asthma exacerbation or COPD exacerbation
- Autoimmune hepatitis and other severe liver diseases
- Nephrotic syndrome
- Inflammatory bowel disease (Severe Ulcerative Colitis, Crohn's disease) flare
- Dermatological conditions (Pemphigus vulgaris, Severe Erythema multiforme, Exfoliative dermatitis)
- Cerebral edema (associated with brain tumors)
- Prevention of graft rejection in organ transplantation
4. Dosage & Administration
Adult Dosage: Highly individualized. For severe diseases: Initial dose 20-60mg/day, often starting at 30-40mg/day in single or divided doses. 30mg is a common initiating dose for conditions like polymyalgia rheumatica, severe asthma, or autoimmune hepatitis. Must be tapered based on response.
Administration: Take with or immediately after food to minimize gastric irritation. Administer as a single daily dose 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. For the 30mg dose, ensure it's part of a prescribed tapering schedule. Never stop abruptly.
5. Side Effects
Common side effects may include:
- Insomnia, mood changes, nervousness
- Increased appetite, weight gain
- Fluid retention, edema, facial mooning
- Dyspepsia, heartburn
- Hyperglycemia (especially in diabetics)
- Easy bruising, thin fragile skin
- Hirsutism, acne
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Warfarin/Acenoocumarol | Prednisolone may alter anticoagulant response (increase or decrease INR). | Major |
| Phenytoin, Phenobarbital, Carbamazepine, Rifampicin | CYP3A4 inducers increase metabolism of prednisolone, reducing its efficacy. Dose increase may be needed. | Major |
| Ketoconazole, Itraconazole, Clarithromycin, Erythromycin, Ritonavir | CYP3A4 inhibitors decrease metabolism of prednisolone, increasing risk of toxicity. Dose reduction may be needed. | Major |
| NSAIDs (e.g., Ibuprofen, Diclofenac) | Increased risk of gastrointestinal ulceration and bleeding. | Major |
| Diuretics (e.g., Furosemide, Hydrochlorothiazide) | Enhanced potassium loss, leading to severe hypokalemia. | Major |
| Antidiabetics (Insulin, Metformin, Sulfonylureas) | Prednisolone causes hyperglycemia, antagonizing their effect. Increased antidiabetic dose may be needed. | Major |
| Vaccines (Live-attenuated: MMR, Varicella, OPV) | Increased risk of vaccine-induced infection. Avoid during immunosuppressive doses. | Contraindicated |
| Digoxin | Hypokalemia induced by prednisolone increases risk of digoxin toxicity. | Moderate |
7. Patient Counselling
- DO take exactly as prescribed, usually with food.
- DO take your dose in the morning (around 8 AM) if on once-daily dosing.
- DO NOT stop taking the medicine suddenly. It must be tapered under doctor's guidance.
- DO carry a steroid alert card or wear medical identification.
- DO inform all your doctors and dentists that you are taking this medicine.
- 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 overdose is unlikely to cause acute life-threatening toxicity but will exaggerate pharmacological effects: severe fluid retention, hypertension, hyperglycemia, psychosis, electrolyte imbalances (hypokalemia), and acute myopathy. Chronic overdose leads to Cushing's syndrome.
Storage: Store at room temperature (15-25°C), protected from light and moisture. Keep in the original container, tightly closed. Keep out of reach of children. Do not use after the expiry date printed on the pack.