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. In the Indian context, it is a cornerstone therapy for a wide range of inflammatory, allergic, autoimmune, and neoplastic conditions due to its efficacy, wide availability, and cost-effectiveness. It mimics the action of cortisol but with greater potency and longer duration.
| Onset | Duration | Bioavailability |
|---|---|---|
| Rapid, with pharmacodynamic effects beginning within 1-2 hours of oral administration. | Intermediate-acting glucocorticoid with a biological half-life of 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).
3. Indications & Uses
- Rheumatoid Arthritis (as a bridge therapy or low-dose maintenance)
- Systemic Lupus Erythematosus (SLE)
- Acute Severe Asthma & COPD Exacerbations
- Allergic Conditions (Severe allergic rhinitis, contact dermatitis, drug reactions)
- Dermatological Conditions (Pemphigus vulgaris, severe psoriasis, exfoliative dermatitis)
- Nephrotic Syndrome (idiopathic, minimal change disease)
- Inflammatory Bowel Disease (Ulcerative Colitis, Crohn's disease flare-ups)
- Cerebral Edema (associated with primary or metastatic brain tumors)
4. Dosage & Administration
Adult Dosage: Highly variable. Initial: 5-60mg/day in single or divided doses based on disease severity. Maintenance: Lowest effective dose, often 5-10mg/day. For acute severe asthma: 40-60mg/day for 5-7 days, then taper.
Administration: Administer with or immediately after food to reduce gastric irritation. For once-daily dosing, take in the morning (around 8 AM) to coincide with the body's natural cortisol peak and minimize HPA axis suppression. Do not crush or chew enteric-coated tablets. Do not stop abruptly.
5. Side Effects
Common side effects may include:
- Increased appetite, weight gain
- Insomnia, mood swings, nervousness
- Fluid retention, edema, facial mooning
- Dyspepsia, heartburn
- Acne, hirsutism
- Easy bruising, thin fragile skin
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Warfarin/Acenoocoumarol | Prednisolone may alter anticoagulant response (increase or decrease INR); monitor closely. | Major |
| Phenytoin, Phenobarbital, Rifampicin | Induce CYP3A4, increasing prednisolone metabolism, reducing its efficacy. Dose increase may be needed. | Major |
| Ketoconazole, Itraconazole, Clarithromycin | Inhibit CYP3A4, decreasing prednisolone metabolism, increasing toxicity risk. 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. | Moderate |
| Antidiabetics (Insulin, Metformin) | Prednisolone causes hyperglycemia, antagonizing effect. Increased antidiabetic dose required. | Major |
| Vaccines (Live-attenuated: BCG, MMR, Varicella) | Diminished antibody response, risk of disseminated infection. Avoid. | Major |
| Digoxin | Risk of digitalis toxicity due to hypokalemia. | Moderate |
7. Patient Counselling
- DO take exactly as prescribed. DO NOT stop taking suddenly.
- DO take with food or milk to avoid stomach upset.
- DO inform all your doctors and dentists you are taking this medicine.
- DO carry a steroid alert card/bracelet.
- DO NOT receive any live vaccines 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, acute adrenal insufficiency (if stopped abruptly after overdose). Chronic overdose leads to Cushing's syndrome.
Storage: Store below 30°C in a cool, dry place, protected 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.