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 2.5mg strength is a low-dose formulation commonly used for maintenance therapy, tapering regimens, and in conditions requiring prolonged low-dose corticosteroid treatment. It mimics the action of cortisol but with greater potency and longer duration.
| Onset | Duration | Bioavailability |
|---|---|---|
| 1 to 2 hours (oral) | 18 to 36 hours (biological half-life) | 80-90% (oral) |
2. Mechanism of Action
Prednisolone binds to intracellular glucocorticoid receptors, forming a complex that translocates to the nucleus. This complex modulates gene transcription by binding to glucocorticoid response elements (GREs) or interacting with other transcription factors like NF-κB and AP-1. This leads to increased synthesis of anti-inflammatory proteins (e.g., lipocortin-1) and decreased synthesis of pro-inflammatory mediators (e.g., cytokines, chemokines, prostaglandins, leukotrienes).
3. Indications & Uses
- Rheumatoid Arthritis (as a low-dose adjunctive therapy)
- Systemic Lupus Erythematosus (SLE)
- Asthma (severe persistent, as maintenance therapy)
- Allergic conditions (severe, refractory)
- Dermatological conditions (Pemphigus vulgaris, Severe psoriasis)
4. Dosage & Administration
Adult Dosage: Highly individualized. For anti-inflammatory/immunosuppressive: Initial: 5-60mg/day in divided doses. Maintenance: Often tapered to lowest effective dose, frequently using 2.5mg tablets for fine-tuning (e.g., 2.5-10mg daily or on alternate days).
Administration: Take with food or milk to minimize GI upset. Administer as a single daily dose in the morning (to mimic circadian rhythm) when on maintenance therapy, unless otherwise directed. Do not crush or chew unless scored. For tapering, reduce dose gradually (e.g., by 2.5mg decrements) over weeks to months.
5. Side Effects
Common side effects may include:
- Insomnia
- Increased appetite, weight gain
- Fluid retention, edema
- Mood changes (euphoria, nervousness)
- Dyspepsia
- Acne
- Easy bruising
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Warfarin | Altered anticoagulant response (increased or decreased INR); monitor closely. | Major |
| Phenytoin, Phenobarbital, Rifampicin | Increased hepatic metabolism of prednisolone, reducing its efficacy. Dose increase may be 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, leading to severe hypokalemia. | Moderate |
| Antidiabetics (Insulin, Metformin) | Prednisolone causes hyperglycemia; may require increased antidiabetic dose. | Major |
| Live Vaccines (MMR, Varicella, OPV) | Diminished immune response and risk of vaccine-induced infection. | Contraindicated |
7. Patient Counselling
- DO take exactly as prescribed. Do not stop abruptly after long-term use.
- DO take with food or milk.
- DO carry a steroid alert card/bracelet stating you are on prednisolone.
- DONT take live vaccines without consulting your doctor.
- DONT double the dose if you miss one. Take it as soon as you remember, or skip if it's almost time for the next dose.
- DO inform all your doctors (including dentists) about your prednisolone use.
8. Toxicology & Storage
Overdose: Acute overdose is unlikely to cause acute life-threatening symptoms. Chronic overdose leads to Cushingoid state: moon face, central obesity, hypertension, hyperglycemia, osteoporosis, adrenal suppression, psychosis, severe infections.
Storage: Store below 30°C. Protect from light and moisture. Keep in the original blister pack or container. Keep out of reach of children.