methylprednisolone (Medrol, Solu-Medrol, Depo-Medrol)
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Introduction
Systemic agent: Tradenames: Medrol, Solu-Medrol, Depo-Medrol. (6-alpha-methylprednisolone)
Indications
Dosage
- 10-125 mg IV/IM* every 6 hours
- 4-48 mg PO QD
- spinal cord injury:
- intra-articular:
- intra-lesional: 20-60 mg
Tabs: 2, 4, 8, 16, 24, 32 mg. Medrol Dosepack: tapers 24 to 0 mg over 7 days. Injection (as acetate): 40 mg/mL (1 mL); 80 mg/mL (1 mL) Injection (as succinate): 40 mg, 125 mg, 500 mg, 1000 mg
* Depo-Medrol: low solubility, sustained action IM (8 days).
Equivalent dose: -methylprednisolone 4 mg = hydrocortisone 20 mg
Pharmacokinetics
- does not require hepatic activation for activity
- oral:
- peak effect in 1-2 hours
- duration of action: 30-36 hours
- intramuscular (IM):
- peak effect in 4-8 days
- duration of action: 1-4 weeks
- intra-articular
- peak effect in 1 week
- duration of action: 1-5 weeks
- volume of distribution is 0.7-1.5 L/kg
- metabolized in the liver by cyt P450 3A4
- elimination 1/2life is 3-3.5 hours, with slower clearance in the elderly
elimination via liver
1/2life = 3-3.5 hours
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- seizures, mood swings, headache, skin atrophy, bruising, hyperpigmentation, acne, amenorrhea, Na+ & H2O retention, Cushing's syndrome, hyperglycemia, suppression of bone growth, abdominal distention, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity, delirium, hallucinations, euphoria
- short-term effects
- fluid & electrolyte disturbances
- hyperglycemia
- poor wound healing
- GI disturbances
- spread of infection
- long-term use
- osteoporosis
- bone fractures
- pituitary & adrenal insufficiency
- Cushing's syndrome
- too rapid withdrawal can result in acute adrenal insufficiency
Drug interactions
- aminoglutethimide
- anticholinesterases
- barbiturates
- carbamazepine
- phenytoin
- rifampin
- live virus vaccines
- any drug that inhibits cyt P450 3A4 may increase levels of methylprednisolone
- any drug that induces cyt P450 3A4 may diminish levels of methylprednisolone
- 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
- immediately-acting glucocorticoid
- does not require hepatic activation for activity
- minimal mineralocorticoid activity[7]
Notes
- outbreak of fungal meningitis associated with epidural, paraspinal, or joint injections with contaminated methylprednisolone in 2012[6]
More general terms
Additional terms
- 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)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
- ↑ 6.0 6.1 Chiller TM et al. Clinical findings for fungal infections caused by methylprednisolone injections. N Engl J Med 2013 Oct 24; 369:1610 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24152260 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1304879
- ↑ 7.0 7.1 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=6741
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5877
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=16922
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=584547
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4159
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=657303
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=1875