Prednisolone

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Pharmacokinetics 5 Adverse-effects 6 Drug-interactions 7 More General Terms 8 Additional Terms 9 Internet Database 10 References

Introduction

• Ophthalmic: (Pred Forte, AK-Pred)

Indications

• inflammatory conditions of the eye
• corneal injury
• graft rejection
• acute alcoholic hepatitis associated with encephalopathy

Dosage

• systemic

• adults: 5-60 mg IV/ IM/ PO QD
• children: 1-2 mg/kg/day PO divided QD- BID for 3-5 days

• Tabs: 5 mg.
• Liquid: 5 mg/5 mL (120 mL), 15 mg/5 mL.
• Syrup: 15 mg/5 mL (240 mL).
• Flo-Pred: viscous, 'spill-proof', oral prednisolone liquid
• ophthalmic

• 1-2 drops every hour during the day & every 2 hours at night
• after response is obtained, 1 drop every 4 hours
• post-operative inflammation

• 1-2 drops into affected eye QID beginning 24 hours after surgery
• continue for 2 weeks

• Suspension: ( acetate): 0.12% (5 mL, 10 mL) & 1% (5 mL, 10 mL). ( phosphate): 0.125% (5 mL), 1% (5 mL).

Pharmacokinetics

• unlike prednisone, prednisolone does not require activation by hepatic enzymes for activity.
• protein binding 65-91%
• metabolized in the liver by cyt P450 3A4 & in other tissues to inactive compounds
• metabolites eliminated in the urine as conjugates ( sulfate, glucuronate)
• elimination 1/2life 3.6 hours

• biological 1/2life is 18-36 hours

• prednisolone is inactivated by the placenta
  

• elimination via liver
• 1/2life = 3.6 hours
• protein binding = 65-91 %

Adverse-effects

• ( ophthalmic)

• common (> 10%)

• increased appetite, insomnia, indigestion, nervousness

• less common (1-10%)

• cataracts, diabetes mellitus, hirsutism, joint pain, epistaxis

• uncommon (< 1%)

• seizures, mood swings, headache, skin atrophy, hyperpigmentation, acne, amenorrhea, sodium & water retention, Cushing's syndrome, hyperglycemia, bone growth suppression, abdominal distention, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity

• ophthalmic agent

• blurred vision
• stinging
• increased intraocular pressure
• cataracts
• open-angle glaucoma
• systemic effects of glucocorticoids
  
• drug adverse effects of glucocorticoids
• drug adverse effects of immunosuppressive agents

Drug-interactions

• any drug that inhibits cyt P450 3A4 may increase levels of prednisolone
• any drug that induces cyt P450 3A4 may diminish levels of prednisolone
  
• drug interaction(s) of glucocorticoids with warfarin

More General Terms

• glucocorticoid

Additional Terms

• cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
• methylprednisolone (Medrol, Solu-Medrol, Depo-Medrol)
• sulfacetamide/prednisolone (Blephamide, Cetapred, Metimyd)

Internet Database

PubChem: 4897
PubChem: 5755
PubChem: 15582
PubChem: 4894

References

1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
4. Prescriber's Letter 16(1): 2009 Comparison of Oral Prednisolone Formulations Detail-Document#: [1] (subscription needed) [2]

prednisolone; deltahydrocortisone; metacortandralone (Pred Forte, AK-Pred, Inflamase, Pediapred, Pred Mild, Prelone, Flo-Pred, Veripred 20)