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dexamethasone (Decadron, Maxidex, AK-Dex, Ozurdex)

Tradenames: Decadron, Maxidex, AK-Dex. Indications: - inflammation - musculoskeletal inflammation - bursitis - infections - Herpes zoster, tuberculosis, trichinosis, Loeffler's syndrome - dermatoses - contact dermatitis, atopic dermatitis - seborrheic dermatitis - dermatitis herpetiformis - erythema multiforme - erythroderma - urticaria - berylliosis - respiratory distress syndrome - autoimmune disease - serum sickness - allergic disorders - adrenal disorders - adrenal insufficiency - adrenogenital syndrome - nephrotic syndrome - hematologic disorders - anemia, thrombocytopenia due to autoimmune disease - neoplastic disorders a) antiemetic b) bone metastasis: reduces bone pain - neuropathic pain - cerebral edema, laryngeal edema, angioneurotic edema - septic shock - organ transplantation, organ transplantation rejection - diagnostic agent for Cushing's disease - ophthalmic inflammation (eye disease) - macular edema (Ozurdex), corneal ulcer, corneal abrasion, - otic: otitis externa - keloid - Blackfan-Diamond syndrome - infantile spasms [7] - adjunctive treatment for chemotherapy - intraoperative prophylaxis for post-operative nausea & vomiting [6,9] - does not predispose to surgical site infections [9] Dosage: Systemic agent: 1) anti-inflammatory: - 0.75-9 mg/day PO/IM/IV divided every 6 hours 2) cerebral edema: -> Load 10-20 mg IV, maintenance 4 mg every 6 hours 3) pediatric meningitis: 0.15 mg/kg IV. 4) tuberculous meningitis (4-6 weeks duration) - 2 weeks IV (0.3 mg/kg per day for week 1, 0.2 mg/kg per day for week 2) - 4 weeks oral (0.1 mg/kg per day for week 3, then 3 mg per day, decreasing by 1 mg each week) 5) croup: 0.6 mg/kg IM. 6) antiemetic: 10 mg IV prior to chemotherapy 7) metastatic bone pain: 4 mg IV every 6 hours 8) physiologic replacement therapy: a) 0.03-0.15 mg/kg/day b) 0.6-0.75 mg/m2/day c) divide every 6-12 hours 9) low-dose dexamethasone suppression test: a) 1 mg at 11 PM b) serum cortisol at 8 AM Tabs: 0.25, 0.5, 0.75, 1.0, 1.5, 2, 4, 6 mg. Elixir: 0.5 mg/5 mL. Injection: 8 & 16 mg/mL (dexamethasone acetate) (5 mL) Vitreal implant for treatment of macular edema: Ozurdex Topical agent: 0.1% cream BID. Soluble in EtOH, insoluble in H2O. Nasal preparation: 2 sprays BID/TID. Ophthalmic: ointment: (0.1%) BID-QID solution: 1 drop every 1-6 hours (1%) Pharmacokinetics: 1) oral bioavailability is 78 +/- 14% 2) protein binding: 68% 3) metabolized in liver 4) 3% excreted in the urine 5) elimination 1/2life - 3.0 +/- 0.8 hours 6) biologic 1/2life: 36-54 hours Adverse effects: 1) systemic a) common (> 10%) [5] - increased appetite, insomnia, indigestion, nervousness b) less common (1-10%) [5] - cataracts, diabetes mellitus, hirsutism, joint pain, epistaxis c) uncommon (< 1%) [5] - seizures, mood swings, headache, skin atrophy,bruising, hyperpigmentation, acne, amenorrhea, Na+ & H20 retention, Cushing's syndrome, hyperglycemia, suppression of bone growth, abdominal distension, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity reactions, delirium, hallucinations, euphoria d) short term use [4] - fluid & electrolyte disturbances - hyperglycemia - poor wound healing - GI disturbances - immune suppression e) long term use [4] - osteoporosis - bone fractures - pituitary & adrenal insufficiency - Cushing's syndrome - adrenal insufficiency may manifest with rapid withdrawal 2) ophthalmic agent [4] - irritation - increased intraocular pressure - cataracts 3) topical agent - uncommon (< 1%) [5] - burning, itching, irritation, dryness, folliculitis, hypertrichosis, acne, hypopigmentation, perioral dermatitis, allergic contact dermatitis, skin maceration, secondary infection, skin atrophy, striae, miliaria Drug interactions: 1) aminoglutethimide 2) anticholinesterases 3) barbiturates 4) carbamazepine 5) phenytoin 6) rifampin 7) live vaccines 8) dexamethasone induces cyt P450 3A4 - may diminish levels of drugs metabolized by cyt P450 3A4 ;;;********|**********|**********|**********|**********|*********|**********|********* Mechanism of action: 1) long-acting synthetic glucocorticoid 2) potent anti-inflammatory activity 3) minimal mineralocorticoid activity [8] 4) reduces bone pain & neuropathic pain 5) reduces vasogenic edema 6) inhibits production of prostaglandins 7) inhibits formation of vascular endothelial growth factor

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) dexamethasone suppression test

General

11 hydroxycorticosteroid 17 hydroxycorticosteroid antipruritic agent glucocorticoid neurologic agent pregnenedione

Properties

SIZE: MW = 392.47 G/M MISC-INFO: elimination route LIVER MP 262-264 C C22 H29 O5 F 1/2life 3.0 HOURS protein-binding 68% pregnancy-category C safety in lactation - ?

Database Correlations

PUBCHEM correlations

References

  1. Merck Index 11th ed #8116
  2. Research Biochemicals International 1993-94 catalog
  3. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  4. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  5. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  6. Journal Watch 24(14):113, 2004 Apfel CC, Korttila K, Abdalla M, Kerger H, Turan A, Vedder I, Zernak C, Danner K, Jokela R, Pocock SJ, Trenkler S, Kredel M, Biedler A, Sessler DI, Roewer N; IMPACT Investigators. A factorial trial of six interventions for the prevention of postoperative nausea and vomiting. N Engl J Med. 2004 Jun 10;350(24):2441-51. PMID: 15190136
  7. Deprecated Reference
  8. Medical Knowledge Self Assessment Program (MKSAP) 17, 18 American College of Physicians, Philadelphia 2015, 2018
  9. Corcoran TB et al. Dexamethasone and surgical-site infection. N Engl J Med 2021 May 6; 384:1731 PMID: 33951362 https://www.nejm.org/doi/10.1056/NEJMoa2028982

Component-of

bupivacaine/dexamethasone/isopropanol/povidone iodine ciprofloxacin/dexamethasone cyclophosphamide/dexamethasone/doxorubicin/vincristine; cyclophosphamide/vincristine/adriamycin/dexamethasone (CVAD) dexamethasone/isopropanol/lidocaine/povidone iodine dexamethasone/isopropanol/povidone iodine dexamethasone/lidocaine dexamethasone/neomycin (NeoDecadron) dexamethasone/neomycin/polymixin-B (Maxitrol, Dexasporin) dexamethasone/neomycin/thiabendazole dexamethasone/thalidomide (ThaD) dexamethasone/tobramycin (Tobradex) intravenous anti-emetic combination rituximab/cyclophosphamide/doxorubicin/vincristine (Oncocin)/dexamethasone (R-CVAD) suppository anti-emetic combination (BRD) thalidomide, dexamethasone & pegylated liposomal doxorubicin (ThADD)