Methylprednisolone


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Anti-inflammatory or immunosuppressive Initial: 2-60 mg/day, depending on the disease being treated. Allergic conditions 24 mg on day 1; 20 mg on day 2; 16 mg on day 3; 12 mg on day 4; 8 mg on day 5; 4 mg on day 6. All doses to be given as a single or in divided doses. IV As methylprednisolone Na succinate: Anti-inflammatory or immunosuppressive 10-500 mg/day. Acute allograft rejection in organ transplant recipients 0.5-1 g/day. Status asthmaticus 40 mg, repeated according to patient’s response. IM Anti-inflammatory or immunosuppressive As methyprednisolone Na succinate: 10-80 mg once daily. As methylprednisolone acetate: 10-80 mg every 1-2 wk. Intra-articular Anti-inflammatory or immunosuppressive As methylprednisolone acetate: 4-10 mg (small joints); 10-40 mg (medium joints); 20-80 mg (large joints). May be repeated every 1-5 wk. Intralesional Anti-inflammatory or immunosuppressive As methylprednisolone acetate: 20-60 mg every 1-5 wk. Corticosteroid-responsive dermatoses As methylprednisolone acetate: 20-60 mg, may repeat up to 4 inj at intervals depending on the type of lesion and patient’s response to the initial inj. Topical Corticosteroid-responsive dermatoses As 0.1% methylprednisolone aceponate oint, cream or lotion: Apply thinly to affected area once daily for up to 12 wk.
Dosage Details
Intra-articular
Anti-inflammatory or immunosuppressive
Adult: As methylprednisolone acetate: 4-10 mg (small joints); 10-40 mg (medium joints); 20-80 mg (large joints). May be repeated every 1-5 wk depending on patient’s response.

Intralesional
Corticosteroid-responsive dermatoses
Adult: As methylprednisolone acetate: 20-60 mg; 1-4 inj may be given at intervals depending on the type of lesion and the duration of improvement from the initial inj.

Intralesional
Anti-inflammatory or immunosuppressive
Adult: As methylprednisolone acetate: 20-60 mg every 1-5 wk depending on patient’s response.

Intramuscular
Anti-inflammatory or immunosuppressive
Adult: As methyprednisolone Na succinate: 10-80 mg once daily. As methylprednisolone acetate: 10-80 mg every 1-2 wk.
Child: As methylprednisolone Na succinate: 0.5-1.7 mg/kg daily or 5-25 mg/m2 daily in divided doses 6-12 hrly. "Pulse" therapy: 15-30 mg/kg/dose over ≥30 min given once daily for 3 days.

Intravenous
Anti-inflammatory or immunosuppressive
Adult: As methylprednisolone Na succinate: 10-500 mg daily. Doses ≤250 mg are given by inj over at least 5 min while doses >250 mg are given slowly over at least 30 min.
Child: As methylprednisolone Na succinate: 0.5-1.7 mg/kg daily or 5-25 mg/m2 daily in divided doses 6-12 hrly. “Pulse” therapy: 15-30 mg/kg/dose over ≥30 min given once daily for 3 days.

Intravenous
Status asthmaticus
Adult: As methylprednisolone Na succinate: 40 mg, repeated according to patient’s response.
Child: As methylprednisolone Na succinate: 1-4 mg/kg daily for 1-3 days.

Intravenous
Acute allograft rejection in organ transplant recipients
Adult: As methylprednisolone Na succinate: 0.5-1 g daily; continue until the patient has stabilised, usually not beyond 48-72 hr.
Child: As methylprednisolone Na succinate: 10-20 mg/kg daily for up to 3 days. Max: 1,000 mg daily.

Oral
Allergic conditions
Adult: 24 mg on day 1 (8 mg before breakfast, 4 mg after lunch, 4 mg after supper, and 8 mg at bedtime) or 24 mg as a single or in 2-3 divided doses upon initiation (regardless of time of day); 20 mg on day 2 (4 mg before breakfast, 4 mg after lunch, 4 mg after supper, and 8 mg at bedtime); 16 mg on day 3 (4 mg before breakfast, 4 mg after lunch, 4 mg after supper, and 4 mg at bedtime); 12 mg on day 4 (4 mg before breakfast, 4 mg after lunch, and 4 mg at bedtime); 8 mg on day 5 (4 mg before breakfast and 4 mg at bedtime); 4 mg on day 6, given before breakfast.

Oral
Anti-inflammatory or immunosuppressive
Adult: Initially, 2-60 mg daily in 1-4 divided doses, depending on the disease being treated.
Child: As methylprednisolone Na succinate: 0.5-1.7 mg/kg daily or 5-25 mg/m2 daily in divided doses 6-12 hrly. "Pulse" therapy: 15-30 mg/kg/dose over ≥30 min given once daily for 3 days.

Topical/Cutaneous
Corticosteroid-responsive dermatoses
Adult: As 0.1% methylprednisolone aceponate oint, cream or lotion: Apply thinly to affected area once daily for up to 12 wk.
Child: As 0.1% methylprednisolone aceponate oint, cream or lotion: Apply thinly to affected area once daily for up to 4 wk.
Administration
Should be taken with food.
Reconstitution
Methyprednisolone Na succinate: IM/IV inj: Add bacteriostatic water for inj containing benzyl alcohol 0.9% according to the manufacturer’s instructions. IV infusion: Dilute further w/ dextrose 5%, NaCl 0.9%, dextrose 5% in NaCl 0.9% inj or other compatible IV soln.
Incompatibility
Intravenous:
Y-site: Allopurinol, amsacrine, caspofungin, ciprofloxacin, docetaxel, etoposide phosphate, fenoldopam, filgrastim, gemcitabine, ondansetron, paclitaxel, palonosetron, propofol, sargramostim, tigecycline, vinorelbine.
Contraindications
Systemic fungal infections unless specific anti-infective therapy is employed; IM admin in idiopathic thrombocytopenic purpura. Intrathecal admin. Concurrent admin of live or live, attenuated vaccines (in patients receiving immunosuppressive doses).
Special Precautions
Patient w/ heart failure, HTN, DM, GI disease (e.g. diverticulitis, intestinal anastomoses, peptic ulcer, ulcerative colitis), multiple sclerosis, myasthenia gravis, acute MI, cataracts, glaucoma, osteoporosis, history of seizure disorder, thyroid disease. Avoid abrupt withdrawal. Renal and hepatic impairment (including cirrhosis). Childn. Pregnancy and lactation.
Adverse Reactions
Adrenal suppression, anaphylactoid reactions, immunosuppression, acute myopathy, Kaposi’s sarcoma, psychiatric disturbances (e.g. depression, euphoria, insomnia, mood swings, personality changes), increased susceptibility and severity of infections, impaired healing, HTN, Na and fluid retention, CV collapse (high dose), peptic ulcer, cataract subcapsular, skin atrophy, acne, muscular weakness, growth retardation, decreased blood K; dermal/subdermal skin depression at inj site. Topical: Itching, burning erythema, vesiculation; rarely, folliculitis, hypertrichosis, perioral dermatitis, skin discolouration, allergic skin reactions.
MonitoringParameters
Monitor BP, blood glucose, electrolytes, growth in childn.
Drug Interactions
Loss of corticosteroid-induced adrenal suppression w/ aminoglutethimide. Risk of hypokalaemia w/ K-depleting agents (e.g. amphotericin B, diuretics). Decreased clearance w/ macrolide antibiotics. May decrease serum levels of isoniazid. Increased clearance w/ cholestyramine. Risk of convulsions w/ ciclosporin. Increased risk of arrhythmias w/ digitalis glycosides. Decreased metabolism w/ oestrogens, including OCs. Enhanced metabolism w/ CYP3A4 inducers (e.g. rifampicin, barbiturates). Increased plasma concentrations w/ CYP3A4 inhibitors (e.g. ketoconazole, erythromycin). Risk of GI effects w/ aspirin or other NSAIDs. May increase the anticoagulant effect of warfarin. May reduce the therapeutic effect of antidiabetics.
Potentially Fatal: May diminish response to live or live, attenuated vaccines.
Lab Interference
May suppress reactions to skin test.
Action
Description: Methylprednisolone binds to and activates intracellular glucocorticoid receptors. Activated glucocorticoid receptors bind to promoter regions of DNA (which may activate or suppress transcription) and activate transcription factors resulting in inactivation of genes through deacetylation of histones.
Onset: Peak effect: 1-2 hr (oral); 4-8 days (IM); 1 wk (intra-articular).
Duration: 30-36 hr (oral); 1-4 wk (IM); 1-5 wk (intra-articular).
Pharmacokinetics:
Absorption: Rapidly absorbed (oral); absorbed from joints over a wk but is more slowly absorbed following deep IM inj (as acetate); rapidly absorbed after IM inj (Na succinate ester). Time to peak plasma concentration: 2 hr (Na succinate ester).
Distribution: Fairly rapidly distributed (oral). Crosses the placenta. Volume of distribution: 0.7-1.5 L/kg.
Excretion: Plasma half-life: ≥3.5 hr.
Chemical Structure

Chemical Structure Image
Methylprednisolone

Source: National Center for Biotechnology Information. PubChem Database. Methylprednisolone, CID=6741, https://pubchem.ncbi.nlm.nih.gov/compound/Methylprednisolone (accessed on Jan. 22, 2020)

Storage
Store between 20-25°C.
ATC Classification
D10AA02 - methylprednisolone ; Belongs to the class of topical corticosteroids used in the treatment of acne.
H02AB04 - methylprednisolone ; Belongs to the class of glucocorticoids. Used in systemic corticosteroid preparations.
D07AA01 - methylprednisolone ; Belongs to the class of weak (group I) corticosteroids. Used in the treatment of dermatological diseases.
References
Anon. Methylprednisolone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 28/10/2015.

Buckingham R (ed). Methylprednisolone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 28/10/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Methylprednisolone, Methylprednisolone Acetate, Methylprednisolone Sodium Succinate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 28/10/2015.

Methylprednisolone Acetate Injection, Suspension (Teva Parenteral Medicines, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/10/2015.

Methylprednisolone Tablet (BluePoint Laboratories). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 28/10/2015.

Disclaimer: This information is independently developed by MIMS based on Methylprednisolone from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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