MEDROL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MEDROL (MEDROL).
Methylprednisolone is a synthetic glucocorticoid that binds to the glucocorticoid receptor, leading to modulation of gene expression and suppression of inflammatory cytokines (e.g., IL-1, IL-2, TNF-alpha). It inhibits phospholipase A2, reducing prostaglandin and leukotriene synthesis.
| Metabolism | Primarily hepatic metabolism via CYP3A4 to inactive metabolites; also undergoes phase II conjugation. |
| Excretion | Renal (approximately 80-90% as metabolites, <5% unchanged); biliary/fecal (minor, <5%) |
| Half-life | Terminal half-life of methylprednisolone is 2.5-3.5 hours; for the active metabolite (prednisolone), half-life is 2.1-3.5 hours. Clinical context: Despite short half-life, pharmacodynamic effects persist beyond plasma presence due to receptor-mediated actions. |
| Protein binding | Methylprednisolone: 78% bound to albumin and corticosteroid-binding globulin (CBG). Prednisolone (active metabolite): 70-90% bound (concentration-dependent due to saturable CBG binding). |
| Volume of Distribution | Methylprednisolone: 0.5-1.0 L/kg (15-20 L total); indicates extensive tissue distribution, including penetration into synovial fluid and cerebrospinal fluid. |
| Bioavailability | Oral: 75-85% (peak plasma concentrations in 1-2 hours); IM: 90% (peak in 2-4 hours); IV: 100%; rectal: 30-50%</s> |
| Onset of Action | Oral: 1-2 hours; IV: within 1 hour; IM: 1-2 hours; intra-articular: 6-12 hours; topical: 1-2 days |
| Duration of Action | Duration: 1-2 days for hypothalamic-pituitary-adrenal (HPA) suppression after a single dose; anti-inflammatory effects last 12-36 hours depending on dose and condition. Clinical note: HPA suppression duration is a measure of systemic activity. |
| Action Class | Glucocorticoids |
| Brand Substitutes | Predace 4 Tablet, Coelone 4mg Tablet, Pilsone 4mg Tablet, Premisol 4mg Tablet, Doralon 4mg Tablet, Rednisol 8 Tablet, Prelid 8mg Tablet, Predace 8mg Tablet, Sterio 8 Tablet, MP 8mg Tablet, Prelid 16mg Tablet, Predace 16 Tablet, Imicort 16mg Tablet, Mepresso T 16mg Tablet, Rednisol 16mg Tablet |
4 to 48 mg orally once daily or every other day, depending on condition. Initial dose may be up to 48 mg/day.
| Dosage form | ENEMA |
| Renal impairment | No dose adjustment required for renal impairment because methylprednisolone is primarily hepatically metabolized. |
| Liver impairment | In Child-Pugh class C (severe hepatic impairment), reduce dose by 50% and monitor for toxicity. |
| Pediatric use | 0.5 to 1.5 mg/kg/day (or 5 to 60 mg/m2/day) orally in divided doses every 6 to 12 hours; adjust based on severity and response. |
| Geriatric use | Start at lowest effective dose and titrate cautiously; monitor for osteoporosis, hyperglycemia, and infection risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MEDROL (MEDROL).
| Breastfeeding | Enters breast milk; M/P ratio ~0.5. Limited data; avoid high doses. Use lowest effective dose; monitor infant for growth and adrenal suppression. |
| Teratogenic Risk | First trimester: Increased risk of cleft palate (odds ratio ~3.6). Second/third trimester: Fetal adrenal suppression, growth restriction, oligohydramnios with prolonged use. Chronic use may cause neonatal adrenal insufficiency. |
| Fetal Monitoring |
■ FDA Black Box Warning
Contraindicated in patients receiving live or live-attenuated vaccines due to risk of generalized vaccinia. Not recommended for use in systemic fungal infections unless specific therapy is administered. Avoid abrupt withdrawal after prolonged use due to risk of acute adrenal insufficiency.
| Serious Effects |
["Systemic fungal infections (except when used in life-threatening situations with appropriate antifungal therapy)","Live or live-attenuated vaccine administration","Hypersensitivity to methylprednisolone or any component of the formulation","Intrathecal route of administration (contraindicated due to risk of arachnoiditis)","Idiopathic thrombocytopenic purpura (ITP) when used intramuscularly"]
| Precautions | ["Cardiovascular: Increased risk of myocardial infarction, stroke, hypertension, and fluid retention.","Endocrine: HPA axis suppression, Cushing's syndrome, hyperglycemia, growth retardation in children.","Gastrointestinal: Peptic ulcer disease, pancreatitis, esophageal ulceration.","Hepatic: Hepatotoxicity, hepatic steatosis.","Immunologic: Increased susceptibility to infections, reactivation of latent infections (e.g., tuberculosis, hepatitis B), immunosuppression.","Musculoskeletal: Osteoporosis, avascular necrosis, myopathy, growth suppression.","Neuropsychiatric: Mood swings, psychosis, euphoria, depression, insomnia.","Ophthalmic: Cataracts, glaucoma, central serous chorioretinopathy.","Renal: Renal impairment, sodium and water retention, hypokalemia.","Skin: Impaired wound healing, skin atrophy, striae."] |
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| Maternal: Blood pressure, blood glucose, signs of infection. Fetal: Ultrasound for growth restriction and oligohydramnios with prolonged use. Neonatal: Monitor for adrenal insufficiency if exposed late in pregnancy. |
| Fertility Effects | May suppress ovulation and spermatogenesis via hypothalamic-pituitary-adrenal axis inhibition. Reversible upon discontinuation. |