dexamethasone (Decadron, Maxidex, AK-Dex, Ozurdex)
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Introduction
Tradenames: Decadron, Maxidex, AK-Dex.
Indications
- inflammation
- autoimmune disease
- allergic disorders
- adrenal disorders
- nephrotic syndrome
- hematologic disorders
- anemia, thrombocytopenia due to autoimmune disease
- neoplastic disorders
- antiemetic
- 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:
- anti-inflammatory:
- cerebral edema:
- Load 10-20 mg IV, maintenance 4 mg every 6 hours
- pediatric meningitis: 0.15 mg/kg IV.
- 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)
- croup: 0.6 mg/kg IM.
- antiemetic: 10 mg IV prior to chemotherapy
- metastatic bone pain: 4 mg IV every 6 hours
- physiologic replacement therapy:
- 0.03-0.15 mg/kg/day
- 0.6-0.75 mg/m2/day
- divide every 6-12 hours
- low-dose dexamethasone suppression test:
- 1 mg at 11 PM
- serum cortisol at 8 AM
Tabs: 0.25, 0.5, 0.75, 1.0, 1.5, 2, 4, 6 mg.
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
- oral bioavailability is 78 +/- 14%
- protein binding: 68%
- metabolized in liver
- 3% excreted in the urine
- elimination 1/2life
- 3.0 +/- 0.8 hours
- biologic 1/2life: 36-54 hours
elimination via liver
1/2life = 3.0 hours
protein binding = 68 %
Adverse effects
- systemic
- common (> 10%) [5]
- less common (1-10%) [5]
- 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 distention, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity reactions, delirium, hallucinations, euphoria
- short term use [4]
- fluid & electrolyte disturbances
- hyperglycemia
- poor wound healing
- GI disturbances
- immune suppression
- long term use [4]
- osteoporosis
- bone fractures
- pituitary & adrenal insufficiency
- Cushing's syndrome
- adrenal insufficiency may manifest with rapid withdrawal
- ophthalmic agent [4]
- 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
- uncommon (< 1%) [5]
Drug interactions
- aminoglutethimide
- anticholinesterases
- barbiturates
- carbamazepine
- phenytoin
- rifampin
- live vaccines
- dexamethasone induces cyt P450 3A4
- may diminish levels of drugs metabolized by cyt P450 3A4 ;;;********|**********|**********|**********|**********|*********|**********|*********
- drug interaction(s) of methotrexate with biological response modifier
- drug interaction(s) of glucocorticoids with warfarin
- drug interaction(s) of NSAIDs with glucocorticoid
Mechanism of action
- long-acting synthetic glucocorticoid
- potent anti-inflammatory activity
- minimal mineralocorticoid activity[8]
- reduces bone pain & neuropathic pain
- reduces vasogenic edema
- inhibits production of prostaglandins
- inhibits formation of vascular endothelial growth factor
More general terms
- pregnenedione
- 11 hydroxycorticosteroid
- 17 hydroxycorticosteroid
- glucocorticoid
- neurologic agent
- antipruritic agent
Additional terms
- cytochrome P450 3A4 (cytochrome P450 C3, nifedipine oxidase, P450-PCN1, NF-25, CYP3A4)
- dexamethasone suppression test
Component of
- cyclophosphamide/dexamethasone/doxorubicin/vincristine; cyclophosphamide/vincristine/adriamycin/dexamethasone (CVAD)
- dexamethasone/neomycin/thiabendazole
- dexamethasone/lidocaine
- ciprofloxacin/dexamethasone
- thalidomide, dexamethasone & pegylated liposomal doxorubicin (ThADD)
- dexamethasone/thalidomide (ThaD)
- rituximab/cyclophosphamide/doxorubicin/vincristine (Oncocin)/dexamethasone (R-CVAD)
- dexamethasone/tobramycin (Tobradex)
- dexamethasone/neomycin/polymixin-B (Maxitrol, Dexasporin)
- dexamethasone/neomycin (NeoDecadron)
- ciprofloxacin/dexamethasone otic (Ciprodex Otic)
- suppository anti-emetic combination (BRD)
- intravenous anti-emetic combination
References
- ↑ Merck Index 11th ed #8116
- ↑ Research Biochemicals International 1993-94 catalog
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ 4.0 4.1 4.2 4.3 Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ 5.0 5.1 5.2 5.3 5.4 Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ 6.0 6.1 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: https://www.ncbi.nlm.nih.gov/pubmed/15190136
- ↑ 7.0 7.1 Deprecated Reference
- ↑ 8.0 8.1 Medical Knowledge Self Assessment Program (MKSAP) 17, 18 American College of Physicians, Philadelphia 2015, 2018
- ↑ 9.0 9.1 9.2 Corcoran TB et al. Dexamethasone and surgical-site infection. N Engl J Med 2021 May 6; 384:1731 PMID: https://www.ncbi.nlm.nih.gov/pubmed/33951362 https://www.nejm.org/doi/10.1056/NEJMoa2028982