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

Ophthalmic: (Pred Forte, AK-Pred) Indications: - adrenal insufficiency - graft rejection - acute alcoholic hepatitis associated with encephalopathy - congenital anomalies - bronchopulmonary dysplasia - adrenogenital syndrome - Diamond Blackfan syndrome - edema - cerebral edema - laryngeal edema - angioneuroatic edema - pulmonary edema - lung disease - asthma - status asthmaticus - respiratory distress syndrome - COPD - bronchitis - bronchiolitis - beryliosis - eosinophilic pneumonia - allergic bronchopulmonary aspergillosis - pulmonary fibrosis - otitis externa - allergic otitis externa - eye inflammation - corneal ulcer - corneal abrasion - Herpes zoster ophthalmitis - inflammatory infections - trichinosis - Loeffler's syndrome - pneumosystis pneumonia - Bell's palsy - musculoskeletal inflammation - bursitis - dermatitis - seborrhea - urticaria - contact dermatitis - atopic dermatitis - dermatitis herpetiformis - pemphigus - pemphigoid - Steven-Johnson syndrome - erythroderma - psoriasis - erythema multiforme - autoimmune disease - sarcoidosis - autoimmune hemolytic leukemia - immune thrombocytopenic purpura - myasthenia gravis - rheumatic fever - rheumatic heart disease - celiac sprue - systemic lupus erythematosus - Sjogren's syndrome - nephrotic syndrome - hypersensitivity - serum sickness - nasal polyp - allergic rhinitis - malignant neoplasms - Hodgkin's disease - non-Hodgkin's lymphoma - multiple myeloma - acute lymphoblastic leukemia - mycoses fungoides-Sezary syndrome - prostate cancer [5] Dosage: 1) 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 2) 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). Storage: - prednisolone acetate oral suspension - do not transfer to other containers to prevent loss of viscous formulation [6] Pharmacokinetics: 1) unlike prednisone, prednisolone does not require activation by hepatic enzymes for activity. 2) protein binding 65-91% 3) metabolized in the liver by cyt P450 3A4 & in other tissues to inactive compounds 4) metabolites eliminated in the urine as conjugates (sulfate, glucuronate) 5) elimination 1/2life 3.6 hours -> biological 1/2life is 18-36 hours 6) prednisolone is inactivated by the placenta Adverse effects: (ophthalmic) 1) common (> 10%) - increased appetite, insomnia, indigestion, nervousness 2) less common (1-10%) - cataracts, diabetes mellitus, hirsutism, joint pain, epistaxis 3) uncommon (< 1%) - seizures, mood swings, headache, skin atrophy, hyperpigmentation, acne, amenorrhea, sodium & water retention, Cushing's syndrome, hyperglycemia, bone growth suppression, abdominal distension, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity 4) ophthalmic agent - blurred vision - stinging - increased intraocular pressure - cataracts - open-angle glaucoma - systemic effects of glucocorticoids Drug interactions: 1) any drug that inhibits cyt P450 3A4 may increase levels of prednisolone 2) any drug that induces cyt P450 3A4 may diminish levels of prednisolone Laboratory: - prednisolone in serum/plasma - prednisolone in urine Mechanism of action: 1) intermediate-potency glucocorticoid 2) some mineralocorticoid activity - mineralocorticoid/glucocorticoid activity (1/156) [7]

Interactions

drug interactions drug adverse effects (more general classes) monitor with drug (more general classes)

Related

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

General

glucocorticoid

Properties

MISC-INFO: elimination route LIVER 1/2life 3.6 HOURS protein-binding 65-91% pregnancy-category C safety in lactation - ?

Database Correlations

PUBCHEM correlations

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#: 250106 (subscription needed) http://www.prescribersletter.com
  5. Deprecated Reference
  6. Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: 300622 (subscription needed) http://www.prescribersletter.com
  7. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015

Component-of

desmoplakin/prednisolone gentamicin/prednisolone miconazole/nitrate/polymixin b/prednisolone neomycin/polymixin b/prednisolone prednisolone/sodium phosphate/sulfacetamide prednisolone/sulfacetamide (Blephamide, Cetapred, Metimyd) prednisolone/trimeprazine