Methylprednisolone is a potent cortisone used in severe inflammation: asthma attacks, severe allergies, rheumatic and bowel diseases, and to prevent transplant rejection. It comes in tablets and injections.
Also known as: Medrol, Solumedrol, Depo-Medrol
DailyMed/FDA approved label — Methylprednisolone (see also Depo-Medrol and Solumedrol; combined label Physicians EZ Use M-PRED validates the pathway): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=76b15f6a-51d6-45ec-b6cb-8b10a08ed32a — with additional reference: Prontuário Terapêutico do INFARMED, INFARMED (11th ed., 2012)
Methylprednisolone raises blood glucose and antagonises metformin, with risk of diabetic decompensation.
Glucocorticoids reduce glucose tolerance and insulin sensitivity; antidiabetics antagonise the hyperglycaemic effect (Prontuário 8.2.2).
Capillary/daily glucose during the corticosteroid course.
Glucose > 250 mg/dl, ketoacidosis, polydipsia/polyuria.
Intensify glucose monitoring during corticosteroid use; temporarily adjust the antidiabetic; short courses usually resolve spontaneously.
INFARMED Prontuário Terapêutico (11th ed., 2012), Corticosteroids 8.2.2 — "In diabetics... reduced glucose tolerance and insulin sensitivity" and "Antidiabetics antagonise hyperglycaemic effects"; DailyMed — Metformin HCl Tablet label [Glenmark Pharma]: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0ef9de1a-b786-4b6c-a250-3f5ac532b16a
Methylprednisolone raises blood glucose and may require a temporary increase in the gliclazide dose.
The hyperglycaemic effect of glucocorticoids (glycogenolysis, gluconeogenesis, insulin resistance) antagonises the sulfonylurea (Prontuário 8.2.2).
Capillary glucose during the corticosteroid course and 1 week after stopping.
Persistently raised glucose, hyperglycaemic decompensation.
Monitor capillary glucose; increase the sulfonylurea dose during the corticosteroid course if needed; in unstable diabetics consider transient insulin.
INFARMED Prontuário Terapêutico (11th ed., 2012), Corticosteroids 8.2.2 — antidiabetics antagonised; DailyMed — Glipizide Tablet label (sulfonylurea class, Apotex): https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=dcf426b8-bcdc-8214-a1b6-6388bd3399a0
Rifampicin accelerates methylprednisolone metabolism, reducing its therapeutic effect (risk of addisonian crisis in corticodependent patients).
Rifampicin is a potent enzyme inducer; Prontuário 8.2.2 and Annex 7: "rifampicin accelerates corticosteroid metabolism with consequent reduction of therapeutic effect".
Corticodependence signs (fatigue, hypotension), glucose, blood pressure.
Hypotension, weakness, nausea, hyperpigmentation (addisonian crisis).
Increase the corticosteroid dose when co-administered with rifampicin; readjust when stopping the antituberculous drug; never stop the corticosteroid abruptly.
INFARMED Prontuário Terapêutico (11th ed., 2012), Corticosteroids 8.2.2 (p. 353) and Annex 7 — Rifampicin: "Corticosteroids: increased hepatic metabolism"; DailyMed — Rifampin Capsule label [RLD Rifadin]: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=50f706f9-5003-4e15-bece-85b6213b1f5c
Carbamazepine accelerates methylprednisolone metabolism via CYP3A4 induction, reducing the corticosteroid effect.
Enzyme-inducing antiepileptics (carbamazepine, phenytoin, barbiturates) increase hepatic metabolism of corticosteroids (Prontuário 8.2.2; Annex 7).
Hypocortisolism signs, blood pressure, glucose.
Fatigue, hypotension, nausea, worsening of the underlying disease.
Adjust the corticosteroid dose during co-administration; watch for adrenal insufficiency signs; readapt after stopping the antiepileptic.
INFARMED Prontuário Terapêutico (11th ed., 2012), Corticosteroids 8.2.2 — "the same occurs with antiepileptics (carbamazepine, barbiturates and phenytoin)"; DailyMed — Carbamazepine Tablet label [RLD Tegretol]: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d0121be3-b904-41d3-a81a-292aa4176491
Alcohol adds gastritis/ulcer and GI irritation risk to corticosteroids, which already impair the mucosal barrier.
Avoid or strongly moderate alcohol during treatment.
Prontuário 8.2.2 (corticosteroids — peptic ulcer); site monograph.
Taking in the morning with food reduces gastric irritation and mimics the physiological cortisol peak.
Take in the morning, with food, and never skip doses (site monograph).
Site monograph (methylprednisolone — take in the morning, with food).
Corticosteroids suppress immunity — they can disseminate active infections (varicella/zoster, latent TB, amoebiasis).
Exclude latent TB before long courses; do not use in uncontrolled infection without antimicrobial cover.
Prontuário 8.2.2 (corticosteroids — active infections, varicella/zoster); BD vocabulary (infeccao_ativa).
Corticosteroids raise blood glucose — diabetes decompensation; reinforce monitoring and adjust antidiabetics.
Monitor glucose and adjust medication during the course (site monograph).
Site monograph (methylprednisolone — monitor glucose, BP, potassium and weight).
Corticosteroids cause glucocorticoid-induced osteoporosis (vertebral and hip fractures) — caution/prevention in prolonged treatments.
Supplement calcium/vitamin D and consider bisphosphonate for courses > 3 months.
Prontuário 8.2.2 (corticosteroids — glucocorticoid-induced osteoporosis); BD vocabulary (osteoporosis).
Sodium and water retention may decompensate HF and hypertension.
Monitor weight and BP; low-sodium diet in prolonged treatments.
Prontuário 8.2.2 (corticosteroids — sodium retention).
Annex 1 refers to "Corticosteroids (systemic)": in animals they cause cleft palate and skeletal anomalies without proven relevance in humans; risk of gestational diabetes and hypertension; risk of intra-uterine growth restriction with prolonged/repeated use (factor D, 1st trimester for long courses). Antenatal corticosteroids (betamethasone/dexamethasone) for fetal maturation are established benefit.
Use only if clinically necessary, at the lowest effective dose for the shortest period; prophylaxis/treatment of exacerbations (asthma, lupus) in pregnancy should not be withheld out of drug fear.
Compatible: corticosteroids pass little into milk (prednisolone <10% of the maternal dose); with doses >20 mg/day, wait 4 hours after the dose before breastfeeding (to minimise exposure).
Prontuário Terapêutico INFARMED — Annex 1: "Corticosteroids (systemic)" (l. 39867-81); Annex 2: "Methylprednisolone — See Corticosteroids" (l. 42891).
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Potent anti-inflammatory action (5× hydrocortisone); suppression of cellular immune response and cytokine production.
Binds the intracellular glucocorticoid receptor → nuclear translocation → alters transcription: ↓ IL-1, IL-6, TNF-α, ↑ lipocortin-1 (inhibits PLA2 → ↓ prostaglandins/leukotrienes), ↑ IκB (inhibits NF-κB).
Oral: good absorption (peak 1–2 h); IV (succinate): immediate action; acetate (Depo-Medrol): intra-articular depot 1–3 weeks.
Hepatic metabolism (CYP3A4) to inactive metabolites; renal excretion; little placental inactivation compared with prednisolone.
~ 2–3 h (plasma); biological effect 12–36 h.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
