METICORTELONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for METICORTELONE (METICORTELONE).
Corticosteroid with glucocorticoid and mineralocorticoid activity; binds to glucocorticoid receptors, modulating gene expression to suppress inflammation and immune response.
| Metabolism | Hepatic via CYP3A4; primarily metabolized to inactive metabolites. |
| Excretion | Renal: <5% unchanged; hepatic metabolism to inactive metabolites, primarily conjugated and excreted in urine; <2% fecal |
| Half-life | Terminal elimination half-life: 3.0-3.5 hours; clinical context: requires multiple daily doses for sustained effect; biological half-life (duration of HPA suppression) longer (~24-36 hours) due to intracellular activity |
| Protein binding | 75-80% bound, primarily to corticosteroid-binding globulin (CBG, transcortin) and albumin |
| Volume of Distribution | 0.5-1.0 L/kg; clinical meaning: moderate tissue distribution, indicating extensive extravascular distribution and high tissue penetration |
| Bioavailability | Oral: approximately 80-90% (well absorbed); IM: 100% |
| Onset of Action | Oral: 1-2 hours (peak effect at 2-4 hours); IM: 2-3 hours; IV: immediate (within minutes) after bolus |
| Duration of Action | Oral: 12-36 hours (dosing interval 4-6 hours for anti-inflammatory effect, but once daily possible for replacement); IM: 4-6 days; duration of adrenal suppression longer than anti-inflammatory effect |
| Molecular Weight | 360.44 |
Prednisolone: 5-60 mg orally once daily or divided twice daily; methylprednisolone: 4-48 mg orally once daily or divided twice daily. Dose and duration vary by indication.
| Dosage form | INJECTABLE |
| Renal impairment | No specific GFR-based adjustment required; caution in severe renal impairment due to fluid retention. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Reduce dose by 75% or consider alternative. |
| Pediatric use | 0.14-2 mg/kg/day orally divided every 6-12 hours; maximum 60 mg/day. Use lowest effective dose. |
| Geriatric use | Start at lowest effective dose; monitor for osteoporosis, hypertension, hyperglycemia, and immunosuppression. Use minimum duration. |
| 1st trimester | Contraindicated due to risk of cleft palate and other malformations; use only for life-threatening conditions. |
| 2nd trimester | Use if clearly needed; associated with adrenal suppression in fetus and possible growth retardation. |
| 3rd trimester | Use if clearly needed; risk of neonatal adrenal suppression and hypoglycemia if used near term. |
Clinical note
Comprehensive clinical and safety monograph for METICORTELONE (METICORTELONE).
| Placental transfer | Crosses placenta; metabolized to prednisolone which is active. |
| Breastfeeding | Excreted in breast milk; potential for growth suppression, adrenal suppression, and other adverse effects in infant. Use caution, especially with high doses. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Systemic fungal infectionsHypersensitivity to any component
| Precautions | Adrenal suppression with prolonged use; increased susceptibility to infections; masking of infection signs; osteoporosis; glaucoma; cataracts; Cushing's syndrome; growth suppression in children; psychiatric disturbances; cardiovascular effects (hypertension, fluid retention); gastrointestinal perforation risk. |
| Food/Dietary | Avoid excessive salt intake due to potential sodium retention. Grapefruit and grapefruit juice may increase drug levels; use caution. Concurrent use with potassium-depleting diuretics may worsen hypokalemia; consider potassium-rich foods if needed. |
Loading safety data…
| L3 - Moderately Safe |
| Teratogenic Risk | Prednisolone (active metabolite of Meticortelone) crosses placenta but is largely inactivated by 11β-hydroxysteroid dehydrogenase type 2. First trimester: increased risk of cleft palate (odds ratio ~3.4) with high doses (>10-20 mg/day). Second/third trimesters: associated with fetal growth restriction, adrenal suppression, and preterm birth. Risk is dose- and duration-dependent. |
| Fetal Monitoring | Maternal: blood pressure, blood glucose (especially in gestational diabetes), signs of infection, adrenal function if prolonged therapy. Fetal: serial ultrasound for growth (every 4-6 weeks) if chronic use; monitor for adrenal insufficiency in neonates after late-term exposure. |
| Fertility Effects | No direct impairment of fertility in humans. High doses may disrupt menstrual cycles via HPA axis suppression, but effects are reversible upon dose reduction or discontinuation. No evidence of permanent ovarian toxicity. |
| Clinical Pearls |
| Meticortelone (prednisolone) is a glucocorticoid with 4-5 times the anti-inflammatory potency of hydrocortisone and minimal mineralocorticoid activity. Use with caution in patients with diabetes, hypertension, or osteoporosis. Taper dose to avoid adrenal insufficiency. Monitor for signs of infection, as immunosuppression may mask symptoms. Long-term use requires calcium and vitamin D supplementation. |
| Patient Advice | Take with food or milk to reduce gastrointestinal upset. · Do not stop abruptly; follow the doctor's tapering schedule to avoid withdrawal symptoms. · Inform all healthcare providers that you are taking this medication. · Avoid exposure to infections; report any fever, sore throat, or unusual bruising. · Monitor blood sugar if diabetic, as prednisolone may increase glucose levels. · Use caution with nonsteroidal anti-inflammatory drugs (NSAIDs) to reduce risk of gastrointestinal bleeding. |