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CARDIOVASCULAR SYSTEM › VASOPROTECTIVES › AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE › Corticosteroids
prednisolone
C05AA04
Forms & Strengths
- Oral solution: 5 mg/5 mL, 10 mg/5 mL, 15 mg/5 mL, 20 mg/5 mL, 25 mg/5 mL
- Syrup: 15 mg/5 mL
- Tablet: 5 mg
- Ophthalmic suspension: 1%
- Ophthalmic solution: 0.125%
Adult Dosing
- Oral (anti-inflammatory/immunosuppressive): 5 mg to 60 mg daily in single or divided doses
- Oral (multiple sclerosis exacerbation): 200 mg daily for 1 week followed by 80 mg every other day for 1 month
- Ophthalmic: 1-2 drops into conjunctival sac 2-4 times daily; may increase frequency during initial 24-48 hours
Pediatric Dosing
- Oral (anti-inflammatory/immunosuppressive): 0.14 mg/kg to 2 mg/kg/day divided in 3 to 4 doses
- Oral (acute asthma exacerbation): 1 mg/kg to 2 mg/kg/day in 1-2 divided doses for 3-5 days
- Ophthalmic (children >2 years): 1-2 drops into conjunctival sac 2-4 times daily
Indications
- Endocrine disorders (primary or secondary adrenocortical insufficiency)
- Rheumatic disorders (rheumatoid arthritis, psoriatic arthritis)
- Collagen diseases (systemic lupus erythematosus, acute rheumatic carditis)
- Dermatologic diseases (pemphigus, severe erythema multiforme)
- Allergic states (bronchial asthma, severe seasonal or perennial rhinitis)
- Ophthalmic inflammatory conditions responsive to steroids
- Respiratory diseases (symptomatic sarcoidosis, fulminant or disseminated pulmonary tuberculosis)
Mechanism of Action
- Synthetic glucocorticoid that crosses cell membranes and binds to cytosolic glucocorticoid receptors
- Receptor-ligand complex translocates to the nucleus, modulating gene transcription
- Suppresses neutrophil and monocyte migration, inhibits phagocytosis and lysosomal enzyme release
- Decreases production of inflammatory mediators including prostaglandins, leukotrienes, and cytokines
Contraindications
- Systemic fungal infections
- Known hypersensitivity to prednisolone or any component of the formulation
- Administration of live or live-attenuated vaccines in patients receiving immunosuppressive doses
- Ophthalmic use in epithelial herpes simplex keratitis, fungal, or mycobacterial eye infections
Adverse Reactions
- Fluid retention, hypertension, and hypokalemia
- Hyperglycemia, increased appetite, and weight gain
- Osteoporosis, vertebral compression fractures, and myopathy
- Increased susceptibility to infections and delayed wound healing
- Psychiatric disturbances (mood swings, euphoria, psychosis)
- Adrenal suppression upon chronic use
- Cataracts and elevated intraocular pressure with prolonged ophthalmic or systemic use
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, phenobarbital, phenytoin) decrease prednisolone concentrations
- CYP3A4 inhibitors (e.g., ketoconazole, macrolides) increase prednisolone exposure
- Nonsteroidal anti-inflammatory drugs (NSAIDs) increase risk of gastrointestinal ulceration
- Diuretics (potassium-depleting) increase risk of severe hypokalemia
- Antidiabetic agents: corticosteroids antagonize hypoglycemic effects, requiring dose adjustment
- Coumarin anticoagulants: efficacy may be potentiated or diminished, requiring frequent INR monitoring
Curated Content: Needs Vetting Before Put to Clinical Use