Methylprednisolone


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Cách dùng
Should be taken with food.
Hướng dẫn pha thuốc
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.
Tương kỵ
Intravenous:
Y-site: Allopurinol, amsacrine, caspofungin, ciprofloxacin, docetaxel, etoposide phosphate, fenoldopam, filgrastim, gemcitabine, ondansetron, paclitaxel, palonosetron, propofol, sargramostim, tigecycline, vinorelbine.
Chống chỉ định
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).
Thận trọng
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.
Phản ứng phụ
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.
Tương tác
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.
Tác dụng
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.
Đặc tính

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)

Bảo quản
Store between 20-25°C.
Phân loại ATC
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.

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