Prednisolone is a synthetic glucocorticoid, a potent anti-inflammatory and immunosuppressant agent. It is the active metabolite of prednisone, converted in the liver. The 1gm formulation is a high-dose preparation used for specific, severe conditions, often in hospital settings for pulse therapy or in specialized treatment protocols. It exerts its effects by modulating gene expression, leading to profound suppression of inflammation and immune responses.
Adult: 1gm dose is NOT a standard daily dose. It is used in specific PULSE THERAPY protocols: e.g., 1gm intravenous infusion over 1-4 hours, repeated daily for 3-5 days. For some oral pulse regimens, 1gm may be given as a single morning dose for 1-3 days. MUST be prescribed by a specialist. Always follow institutional or published protocol guidelines.
Note: For IV pulse: Reconstitute/dilute as per manufacturer instructions. Administer as a slow IV infusion over 1-4 hours (commonly 2-3 hours) to minimize cardiovascular effects. Monitor ECG and BP continuously during infusion. For oral pulse: Administer as a single dose in the morning with food or milk to minimize GI upset. Do not crush or chew delayed-release tablets if using that formulation.
Prednisolone is a glucocorticoid receptor (GR) agonist. It diffuses passively across cell membranes and binds with high affinity to cytosolic GRs. The activated receptor-ligand complex translocates to the nucleus, where it binds as a dimer to Glucocorticoid Response Elements (GREs) on DNA. This modulates the transcription of specific target genes, leading to increased synthesis of anti-inflammatory proteins (like lipocortin-1) and decreased synthesis of pro-inflammatory mediators (like cytokines, chemokines, adhesion molecules, and enzymes such as COX-2). It also induces apoptosis of lymphocytes.
Pregnancy: FDA Category C. May cross placenta. Use only if potential benefit justifies potential fetal risk. Chronic use associated with low birth weight, adrenal suppression in neonate. High-dose pulse therapy in pregnancy is reserved for life-threatening maternal conditions under specialist care.
Driving: May cause dizziness, vertigo, or visual disturbances. Patients should not drive or operate machinery if affected.
| Warfarin/Acenoocoumarol | Prednisolone may alter anticoagulant response (increase or decrease INR). | Major |
| Phenytoin, Phenobarbital, Rifampicin | Induce CYP3A4, increasing prednisolone metabolism, reducing its efficacy. | Major |
| Ketoconazole, Itraconazole, Clarithromycin | Inhibit CYP3A4, decreasing prednisolone metabolism, increasing toxicity risk. | 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 |
| Antidiabetics (Insulin, Metformin) | Prednisolone causes hyperglycemia, antagonizing effect. Requires dose adjustment. | Major |
| Vaccines (Live-attenuated: MMR, Varicella, OPV) | Reduced immune response, risk of disseminated vaccine infection. | Contraindicated |
| Digoxin | Hypokalemia increases risk of digoxin toxicity. | Moderate |
Same composition (Prednisolone (1gm)), different brands: