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methylprednisolone (Medrol, Solu-Medrol, Depo-Medrol)
Systemic agent: Tradenames: Medrol, Solu-Medrol, Depo-Medrol. (6-alpha-methylprednisolone)
Indications:
1) anti-inflammatory agent
2) immunosuppressive agent
Dosage:
1) 10-125 mg IV/IM* every 6 hours
2) 4-48 mg PO QD
3) spinal cord injury:
-> 30 mg/kg IV bolus followed by 5.4 mg/kg/h infusion
4) intra-articular:
a) large joints: 20-80 mg
b) small joints: 4-10 mg
5) 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:
1) does not require hepatic activation for activity
2) oral:
a) peak effect in 1-2 hours
b) duration of action: 30-36 hours
3) intramuscular (IM):
a) peak effect in 4-8 days
b) duration of action: 1-4 weeks
4) intra-articular
a) peak effect in 1 week
b) duration of action: 1-5 weeks
5) volume of distribution is 0.7-1.5 L/kg
6) metabolized in the liver by cyt P450 3A4
7) elimination 1/2life is 3-3.5 hours, with slower clearance in the elderly
Adverse effects:
1) common (> 10%)
- increased appetite, insomnia, indigestion, nervousness
2) less common (1-10%)
- cataracts, diabetes mellitus, hirsuitism, joint pain, epistaxis
3) uncommon (< 1%)
- seizures, mood swings, headache, skin atrophy, bruising, hyperpigmentation, acne, amenorrhea, Na+ & H2O retention, Cushing's syndrome, hyperglycemia, suppression of bone growth, abdominal distension, ulcerative esophagitis, pancreatitis, muscle wasting, hypersensitivity, delirium, hallucinations, euphoria
4) short-term effects
- fluid & electrolyte disturbances
- hyperglycemia
- poor wound healing
- GI disturbances
- spread of infection
5) long-term use
- osteoporosis
- bone fractures
- pituitary & adrenal insufficiency
- Cushing's syndrome
- too rapid withdrawal can result in acute adrenal insufficiency
Drug interactions:
1) aminoglutethimide
2) anticholinesterases
3) barbiturates
4) carbamazepine
5) phenytoin
6) rifampin
7) live virus vaccines
8) any drug that inhibits cyt P450 3A4 may increase levels of methylprednisolone
9) any drug that induces cyt P450 3A4 may diminish levels of methylprednisolone
Mechanism of action:
1) immediately-acting glucocorticoid
2) does not require hepatic activation for activity
3) minimal mineralocorticoid activity [7]
Notes:
- outbreak of fungal meningitis associated with epidural, paraspinal, or joint injections with contaminated methylprednisolone in 2012 [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)
General
glucocorticoid
neurologic agent
Properties
MISC-INFO: elimination route LIVER
1/2life 3-3.5 HOURS
pregnancy-category C
safety in lactation -
Database Correlations
PUBCHEM correlations
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#: 220233
(subscription needed) http://www.prescribersletter.com
- Geriatric Dosage Handbook, 6th edition, Selma et al eds,
Lexi-Comp, Cleveland, 2001
- Chiller TM et al.
Clinical findings for fungal infections caused by
methylprednisolone injections.
N Engl J Med 2013 Oct 24; 369:1610
PMID: 24152260
http://www.nejm.org/doi/full/10.1056/NEJMoa1304879
- Medical Knowledge Self Assessment Program (MKSAP) 17,
American College of Physicians, Philadelphia 2015
Component-of
bupivacaine/h2o/isopropanol/lidocaine/methylprednisolone/povidone iodine/sodium chloride
bupivacaine/isopropanol/lidocaine/methylprednisolone/povidone iodine
isopropanol/lidocaine/methylprednisolone/povidone iodine