methylprednisolone

CLINICAL USE

Corticosteroid:Suppression of inflammatory and allergic disorderImmunosuppressant Rheumatic disease Cerebral oedema

DOSE IN NORMAL RENAL FUNCTION

Oral: 2–40 mg dailyIM/IV: 10–500 mgGraft rejection: up to 1 g daily for up to 3 days. See ‘Other Information’

PHARMACOKINETICS

Molecular weight :375

%Protein binding :40–60

%Excreted unchanged in urine :

<10 :

Volume of distribution (L/kg) :1.2–1.5

half-life – normal/ESRD (hrs) :2.4–3.5/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 : Dose as in normal renal function

10 to 20 : Dose as in normal renal function

<10 : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Dialysed. Dose as in normal renal function

HD :Dialysed. Dose as in normal renal function

HDF/high flux :Dialysed. Dose as in normal renal function

CAV/VVHD :Dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Antibacterials: metabolism accelerated by rifampicin; metabolism possibly inhibited by erythromycin and clarithromycin

Anticoagulants: efficacy of coumarins may be altered

Anti-epileptics: metabolism accelerated by carbamazepine, barbiturates, phenytoin and primidone

Antifungals: increased risk of hypokalaemia with amphotericin – avoid concomitant use; metabolism possibly inhibited by itraconazole and ketoconazole

Antivirals: concentration possibly increased by ritonavir

Ciclosporin: rare reports of convulsions in patients on ciclosporin and high-dose corticosteroids; levels of ciclosporin increased with high dose methylprednisoloneCytotoxics: increased risk of haematological toxicity with methotrexate

Diuretics: enhanced hypokalaemic effects of acetazolamide, loop diuretics and thiazide diureticsVaccines: high dose corticosteroids can impair immune response to vaccines; avoid concomitant use with live vaccines

ADMINISTRATION

Reconstition

Use solvent supplied (Solu-medrone) or see manufacturer’s recommendations

Route

Oral, IM, IV peripherally or centrally

Rate of Administration

30 minutes

Comments

NB: Rapid bolus injection may be associated with arrhythmias or cardiovascular collapse

OTHER INFORMATION

A single dose of 500 mg –1 g is often given at transplantationThree 500 mg – 1 g doses at 24 hour intervals are often used as first line for reversal of acute rejection episodes. (Some units use 300–500 mg daily for 3 days.)

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