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Prednisolone

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From Pharmacopedia
Prednisolone (and prednisolone sodium phosphate, acetate, etc.)
Prelone, Pediapred, Orapred ODT, Millipred, Veripred

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Summary
Common uses
Pediatric asthma exacerbation0, Autoimmune disease flare0, Glucocorticoid therapy in advanced hepatic disease (preferred over prednisone, which requires hepatic activation)0, Ophthalmic inflammation (topical drops/suspension)0
Pharmacy
Starting dose
Pediatric 1-2 mg/kg/d (max 60 mg) PO for asthma exacerbation; adult dosing similar to prednisone milligram-for-milligram (~1:1 potency)
Preparations
5 mg tablets; 5 mg/5 mL, 10 mg/5 mL, 15 mg/5 mL oral solutions (sweetened pediatric); 5 mg/5 mL syrup; ophthalmic 0.12%, 1% suspensions and 1% solution
US FDA Max
Indication-specific
Pharmacology
Routes
Oral, ophthalmic, IV (prednisolone sodium phosphate), IM
Onset
Hours
Duration
Biologic 12-36 hours (intermediate-acting)
Half-life
Plasma 2-3 hours; biologic ~18-36 hours[1]
Bioavailability
~70% (oral)[1]
Pregnancy
Use when benefits outweigh; small association with oral clefts debated.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Prednisolone is the active form of prednisone (no hepatic activation required); it binds the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription.0 Preferred over prednisone in advanced hepatic dysfunction where hepatic 11β-HSD1 activation is impaired. Liquid formulations are the workhorse pediatric oral corticosteroid for asthma and croup[1].

References

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  1. 1.0 1.1 1.2 FDA Prescribing Information, Orapred ODT (prednisolone sodium phosphate), Concordia, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021959s016lbl.pdf