Prednisolone is a synthetic glucocorticoid, a potent anti-inflammatory and immunosuppressant agent. It is a biologically active metabolite of prednisone, with approximately 4 times the anti-inflammatory potency of hydrocortisone. In the Indian market, it is widely used for a vast array of inflammatory, allergic, autoimmune, and neoplastic conditions. The 5mg/ml concentration is commonly available as oral liquid/solution and injectable formulations, allowing for flexible dosing, especially in pediatric and geriatric populations, and for conditions requiring rapid onset.
Adult: Highly variable based on condition. Initial: 5-60 mg/day (1-12 ml of 5mg/ml solution) as a single or divided dose. For severe conditions (e.g., pemphigus): 60-100 mg/day. Maintenance: Lowest effective dose. Pulse therapy: Up to 1 g/day IV for 3-5 days in specific protocols.
Note: Oral solution: Administer with food or milk to minimize GI upset. Use a calibrated measuring device. Do not stop abruptly; taper gradually. Injectable: For IV/IM use only. IV administration should be slow. For IM injection, use deep intramuscular route to avoid subcutaneous atrophy.
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 IL-1, IL-2, IL-6, TNF-α, COX-2). It also has post-transcriptional effects and influences leukocyte trafficking.
Pregnancy: FDA Category C. May be used if potential benefit justifies risk. Chronic use can cause fetal adrenal suppression, low birth weight, and cleft palate (first trimester). Should be used at the lowest effective dose for the shortest duration. Neonates may require monitoring for hypoadrenalism.
Driving: May cause dizziness, vertigo, or visual disturbances. Patients should not drive or operate machinery if they experience these effects.
| Warfarin | Altered anticoagulant effect (may increase or decrease INR); monitor closely. | 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. | Major |
| Antidiabetics (Insulin, Metformin) | Prednisolone increases blood glucose; may require dose adjustment of antidiabetics. | Major |
| Phenytoin, Phenobarbital, Rifampicin | Induce CYP3A4, increasing prednisolone metabolism and reducing its efficacy. | Major |
| Ketoconazole, Itraconazole, Clarithromycin | Inhibit CYP3A4, decreasing prednisolone metabolism and increasing toxicity risk. | Major |
| Live Vaccines (MMR, Varicella, OPV) | Risk of disseminated infection; avoid vaccination during therapy. | Contraindicated |
| Digoxin | Hypokalemia induced by prednisolone increases risk of digoxin toxicity. | Moderate |