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prednisone (Deltasone, Orasone, Liquid Pred, Meticortin, Rayos)

Systemic agent: Tradenames: Deltasone, Orasone, Liquid Pred. Indications: - adrenal insufficiency - *inflammation associated with many disease states - graft rejection - cardiac transplantation - lung transplantation - acute alcoholic hepatitis associated with encephalopathy - *congenital anomalies - bronchopulmonary dysplasia - adrenogenital syndrome - Diamond Blackfan syndrome - congenital adrenal hyperplasia - infantile spasm - cluster headache - *edema - cerebral edema - laryngeal edema - angioneurotic edema - pulmonary edema - *lung disease - asthma - COPD - bronchitis - bronchiolitis - beryliosis - eosinophilic pneumonia - allergic bronchopulmonary aspergillosis - pulmonary fibrosis - otitis externa - allergic otitis externa - *inflammatory infections - trichinosis - Loeffler's syndrome - pneumocystis pneumonia - Bell's palsy - pulmonary tuberculosis - *musculoskeletal inflammation - bursitis - dermatitis - seborrhea - urticaria - contact dermatitis - atopic dermatitis - dermatitis herpetiformis - pemphigus - pemphigoid - 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 - follicular lymphoma - multiple myeloma - acute lymphoblastic leukemia - chronic lymphocytic - cutaneous T-cell lymphoma - mycosis fungoides-Sezary syndrome - diffuse large B-cell lymphoma - prostate cancer [10] Dosage: 1) 0.5-2 mg/kg or 5-60 mg PO QD - 1 mg/kg may work as well as higher doses in children [8] 2) physiologic replacement: 4-5 mg/m2/day 3) prednisone taper - not necessary to taper if oral dose < 60 mg/day for 10 days [7] - taper is unnecessary when glucocorticoid therapy is < 3-4 weeks, regardless of dose [13] - failure to taper below 5 mg/day suggests adrenal insufficiency [12] - primary or secondary - see prednisone taper Tabs: 1, 2.5, 5, 10, 20, 50 mg. Delayed Release tabs: (Rayos) 1 mg, 2 mg, & 5 mg [9] Elixir: 5 mg/5 mL (120 mL, 240 mL). Pharmacokinetics: 1) oral bioavailability is 80 +/- 10% 2) protein binding: 75% 3) metabolized in liver by cyt P450 3A4 to prednisolone - prednisolone is inactivated by the placenta 4) 3% excreted in the urine 5) elimination 1/2life is 3.6 +/- 0.4 hours 6) biologic 1/2life 18-36 hours [6] Adverse effects: 1) common (> 10%) - increased appetite, insomnia [11] indigestion, nervousness, leukocytosis 2) less common (1-10%) - cataracts, glucose intolerance (hyperglycemia, diabetes mellitus), hirsutism, joint pain, epistaxis 3) uncommon (< 1%) - seizures, mood swings, headache, skin atrophy, bruising, hyperpigmentation, acne, amenorrhea, sodium & water retention, edema, Cushing's syndrome, hyperglycemia, suppression of bone growth, osteopenia, abdominal distension, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity reaction, delirium, hallucinations, euphoria 4) other a) osteoporosis - fractures secondary to osteoporosis are the greatest cause of morbidity in patients on long-term, low dose prednisone (50%) b) aseptic necrosis c) glaucoma d) hypertension e) weight gain f) depression g) steroid psychosis i) gastrointestinal (GI) intolerance j) accelerated atherogenesis k) opportunistic infections l) poor wound healing m) erythroderma following use of systemic glucocorticoids [6] n) too rapid a withdrawal may produce adrenal insufficiency, especially at total doses > 40 mg/day for 2 weeks [7] 5) NOT teratogenic - does NOT cause fetal pituitary-adrenal axis suppression Monitor: 1) blood glucose 2) blood pressure 3) ophthalmologic exam for long-term steroid use Mechanism of action: 1) intermediate-potency glucocorticoid 2) some mineralocorticoid activity - mineralocorticoid/glucocorticoid activity (1/156) [6]

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

General

glucocorticoid

Properties

MISC-INFO: elimination route LIVER pregnancy-category C safety in lactation - 1/2life 3.6 HOURS protein-binding 75%

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Saunders Manual of Medical Practice, Rakel (ed), WB Saunders, Philadelphia, 1996, pg 792
  3. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  4. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  5. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  6. Medical Knowledge Self Assessment Program (MKSAP) 11, 17, 18. American College of Physicians, Philadelphia 1998, 2015, 2018.
  7. Prescriber's Letter 10(12):68 2003
  8. Prescriber's Letter 11(2):9 2004
  9. Prescriber's Letter 19(12): 2012 Rayos (Prednisone) Delayed-Release Tablets Detail-Document#: 281207 (subscription needed) http://www.prescribersletter.com
  10. Deprecated Reference
  11. NEJM Knowledge+ Psychiatry
  12. NEJM Knowledge+ Complex Medical Care
  13. Beuschlein F, Else T, Bancos I et a; European Society of Endocrinology and Endocrine Society Joint Clinical Guideline: Diagnosis and Therapy of Glucocorticoid-induced Adrenal Insufficiency. J Clin Endocrinol Metab. 2024 Jun 17;109(7):1657-1683. PMID: 38724043 PMCID: PMC11180513 Free PMC article.

Component-of

cyclophosphamide/doxorubicin/vincristine (Oncocin)/prednisone (CHOP) cyclophosphamide/vincristine (Oncocin)/prednisone (CVP, COP) cyclophosphamide/vincristine (Oncovin)/prednisone/procarbazine (C-MOPP) melphalan/prednisone/thalidomide (ThaMP) nitrogen mustard/vincristine (Oncovin)/prednisone/ procarbazine (MOPP) recombinant parathyroid hormone (1-84) (Natpara) rituximab/cyclophosphamide/doxorubicin/vincristine (Oncocin)/prednisone (R-CHOP) rituximab/cyclophosphamide/vincristine (Oncocin)/prednisone (R-CVP)