Introduction
Prednisolone is a synthetic glucocorticoid medication belonging to the corticosteroid class. It is a potent anti-inflammatory and immunosuppressive agent widely used in clinical practice for managing various inflammatory, allergic, and autoimmune conditions. As an intermediate-acting corticosteroid, prednisolone provides effective therapeutic benefits while maintaining a favorable balance between potency and side effect profile.
Mechanism of Action
Prednisolone exerts its effects through multiple mechanisms. It diffuses across cell membranes and binds to cytoplasmic glucocorticoid receptors, forming a complex that translocates to the nucleus. This complex binds to glucocorticoid response elements on DNA, modulating gene transcription. Prednisolone:
- Inhibits phospholipase A2, reducing prostaglandin and leukotriene synthesis
- Suppresses inflammatory cytokine production (IL-1, IL-2, IL-6, TNF-α)
- Impairs neutrophil and macrophage migration to inflammation sites
- Reduces capillary permeability and edema
- Decreases lymphocyte proliferation and antibody production
- Alters lymphocyte circulation patterns
Indications
FDA-Approved Indications:- Inflammatory disorders (rheumatoid arthritis, polymyalgia rheumatica)
- Allergic conditions (severe asthma, allergic rhinitis)
- Dermatological diseases (psoriasis, severe eczema)
- Ophthalmic inflammation
- Hematologic disorders (autoimmune hemolytic anemia, ITP)
- Neoplastic diseases (leukemias, lymphomas)
- Endocrine disorders (adrenal insufficiency)
- Gastrointestinal diseases (ulcerative colitis, Crohn's disease)
- Nephrotic syndrome
- Organ transplantation rejection prophylaxis
- COVID-19 pneumonia (in specific clinical scenarios)
- Acute gout attacks
- Sarcoidosis
- Thyroid eye disease
Dosage and Administration
General Dosing Principles:- Individualize dosage based on condition severity and patient response
- Use lowest effective dose for shortest duration possible
- Administer with food to minimize GI upset
- Anti-inflammatory: 5-60 mg daily in divided doses
- Rheumatoid arthritis: 5-7.5 mg daily
- Asthma: 40-60 mg daily initially, tapered to lowest effective dose
- Adrenal insufficiency: 4-5 mg/m² daily
- Geriatric: Start at lower end of dosing range due to increased susceptibility to side effects
- Hepatic impairment: May require dose adjustment due to altered metabolism
- Renal impairment: No significant adjustment needed
- Pediatric: 0.1-2 mg/kg/day in divided doses (based on condition)
- Oral tablets (most common)
- Ophthalmic solutions
- Topical preparations
- Intra-articular injections (as prednisolone acetate)
Pharmacokinetics
Absorption: Well absorbed from GI tract (bioavailability 80-90%) Distribution: Volume of distribution: 0.5-0.8 L/kg; Crosses placenta and enters breast milk Protein Binding: 90-95% bound to transcortin and albumin Metabolism: Hepatic via CYP3A4 to inactive metabolites Elimination: Half-life: 2-4 hours; Duration of action: 18-36 hours; Excretion: Primarily renal (metabolites)Contraindications
- Systemic fungal infections
- Known hypersensitivity to prednisolone or components
- Live virus vaccinations during immunosuppressive therapy
- Active untreated infections (relative contraindication)
- Idiopathic thrombocytopenic purpura (for IM administration)
Warnings and Precautions
Boxed Warning:- Corticosteroids may cause serious and fatal infections
- May exacerbate hypertension and diabetes
- Can cause psychiatric reactions including steroid psychosis
- Adrenal suppression with long-term use
- Increased infection risk (bacterial, fungal, viral, parasitic)
- Gastrointestinal perforation risk in patients with GI disorders
- Ophthalmic effects (cataracts, glaucoma)
- Osteoporosis and avascular necrosis
- Growth suppression in children
- Hyperglycemia and diabetes mellitus
- Fluid and electrolyte disturbances
- Myopathy and muscle weakness
Drug Interactions
Significant Interactions:- Anticoagulants: Altered anticoagulant effect
- Antidiabetic agents: Reduced hypoglycemic efficacy
- CYP3A4 inducers (phenytoin, rifampin): Reduced prednisolone efficacy
- CYP3A4 inhibitors (ketoconazole): Increased prednisolone levels
- NSAIDs: Increased GI ulcer risk
- Diuretics: Enhanced potassium wasting
- Live vaccines: Reduced vaccine efficacy, increased adverse reactions
- Cardiac glycosides: Increased digitalis toxicity risk
Adverse Effects
Common (≥1%):- Insomnia
- Weight gain
- Fluid retention
- Mood changes
- Increased appetite
- Dyspepsia
- Hyperglycemia
- Cushingoid appearance
- Adrenal insufficiency
- Severe infections
- Osteoporosis fractures
- Avascular necrosis
- Peptic ulcer disease
- Pancreatitis
- Psychiatric disorders
- Ophthalmic complications
- Anaphylaxis
Monitoring Parameters
Baseline Assessment:- Complete medical history and physical examination
- Blood pressure
- Blood glucose
- Electrolytes (especially potassium)
- Bone density (if long-term therapy anticipated)
- Ophthalmologic examination
- Clinical response assessment
- Blood pressure regularly
- Blood glucose (especially in diabetics)
- Weight changes
- Signs of infection
- Mood and psychological status
- Growth parameters in children
- Bone density annually for long-term therapy
- Assess for adrenal insufficiency after discontinuation
- Monitor for disease flare-ups
Patient Education
Key Points to Discuss:- Take exactly as prescribed; do not stop abruptly
- Report any signs of infection (fever, sore throat)
- Monitor for weight gain and swelling
- Be aware of potential mood changes
- Regular follow-up appointments are essential
- Carry medical alert identification
- Avoid live vaccines during therapy
- Report any vision changes
- Maintain adequate calcium and vitamin D intake
- Inform all healthcare providers about prednisolone use
- Take with food to reduce stomach upset
- Do not crush or chew delayed-release tablets
- If missed dose, take as soon as remembered unless close to next dose
- Never double dose
References
1. Liu D, et al. A practical guide to the monitoring and management of the complications of systemic corticosteroid therapy. Allergy, Asthma & Clinical Immunology. 2013;9(1):30. 2. Fardet L, et al. Corticosteroid-induced clinical adverse events: incidence, risk factors and management. Drug Safety. 2007;30(10):897-909. 3. Prednisolone [package insert]. U.S. Food and Drug Administration. 4. Barnes PJ. Anti-inflammatory actions of glucocorticoids: molecular mechanisms. Clinical Science. 1998;94(6):557-572. 5. Coutinho AE, Chapman KE. The anti-inflammatory and immunosuppressive effects of glucocorticoids, recent developments and mechanistic insights. Molecular and Cellular Endocrinology. 2011;335(1):2-13. 6. American College of Rheumatology. Guidelines for glucocorticoid-induced osteoporosis prevention. Arthritis Care & Research. 2017;69(8):1095-1110. 7. Strehl C, et al. Defining conditions where long-term glucocorticoid treatment has an acceptably low level of harm to facilitate implementation of existing recommendations: viewpoints from an EULAR task force. Annals of the Rheumatic Diseases. 2016;75(6):952-957.