PARACORT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PARACORT (PARACORT).
Paracort is a corticosteroid that acts by binding to glucocorticoid receptors, leading to modulation of gene expression and suppression of inflammatory mediators such as cytokines and prostaglandins.
| Metabolism | Primarily hepatic via CYP3A4; also involves 11β-hydroxysteroid dehydrogenase. |
| Excretion | Renal elimination of unchanged drug accounts for approximately 70% of the dose; biliary/fecal excretion accounts for 20%; the remainder is metabolized and excreted as inactive metabolites. |
| Half-life | Terminal elimination half-life is 3.5 hours (range 2.5–4.5 hours) in adults with normal renal function; prolonged to up to 10–15 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 90–95% bound to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 1.5 L/kg (range 1.2–1.8 L/kg); indicates extensive extravascular distribution and tissue binding. |
| Bioavailability | Oral: 85–95% (well absorbed; minimal first-pass metabolism); Intramuscular: 90–100%; Rectal: 60–70%. |
| Onset of Action | Oral: 30–60 minutes (peak effect at 1–2 hours); Intravenous: <5 minutes (peak effect at 15–30 minutes); Intramuscular: 10–20 minutes. |
| Duration of Action | Clinical duration: 4–6 hours for oral and IV routes; up to 8 hours with high doses. Duration is dose-dependent and prolonged in hepatic impairment due to reduced clearance. |
| Molecular Weight | 360.44 |
Prednisone 5-60 mg orally once daily; initial dose 5-15 mg daily; for acute conditions, up to 60 mg daily tapered over 2-3 weeks.
| Dosage form | TABLET |
| Renal impairment | No adjustment required for mild to moderate renal impairment. For severe renal impairment (GFR <30 mL/min): use with caution and monitor for fluid retention. No specific dose adjustment guidelines. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50% due to impaired corticosteroid metabolism. Child-Pugh C: avoid or use with extreme caution; consider alternative glucocorticoid. |
| Pediatric use | Oral: 0.1-2 mg/kg/day in divided doses every 6-12 hours; typical starting dose 1-2 mg/kg/day for anti-inflammatory effect; maximum 60 mg/day. For asthma: 1-2 mg/kg/day for 3-5 days. |
| Geriatric use | Elderly patients: initiate at lower end of dosing range (5-10 mg/day) due to increased risk of osteoporosis, hypertension, and diabetes; taper slowly; monitor for glucose intolerance, fluid retention, and adrenal suppression. |
| 1st trimester | Use only if clearly needed; limited human data suggest low teratogenic risk, but corticosteroids associated with cleft palate in animal studies. |
| 2nd trimester | May use if benefit outweighs risk; no known major risk from short-term use. |
| 3rd trimester | Prolonged use may cause adrenal suppression in neonate; monitor for hypoglycemia. |
Clinical note
Comprehensive clinical and safety monograph for PARACORT (PARACORT).
| Placental transfer | Crosses placenta; metabolized by 11β-HSD2 to less active forms, reducing fetal exposure. |
| Breastfeeding | Enters breast milk in low concentrations; doses up to 20 mg/day unlikely to affect infant. Avoid high doses or prolonged use. |
| Lactation Rating |
■ FDA Black Box Warning
None FDA-approved. However, long-term use may suppress hypothalamic-pituitary-adrenal (HPA) axis and increase infection risk.
| Serious Effects |
Systemic fungal infectionHypersensitivity to paracort or any component
| Precautions | Immunosuppression and increased infection risk, Adrenal suppression with prolonged use, Osteoporosis with long-term therapy, Hyperglycemia and diabetes mellitus, Gastrointestinal perforation risk |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may increase drug levels. Limit high-sodium foods to reduce fluid retention. Take with a meal to minimize gastrointestinal irritation. |
| Clinical Pearls |
Loading safety data…
| L2 (Safer) |
| Teratogenic Risk | First trimester: Increased risk of orofacial clefts (odds ratio 1.3–3.4) and cardiovascular defects (odds ratio 1.5–2.0). Second/third trimesters: Risk of intrauterine growth restriction, preterm birth, and adrenal suppression in the neonate. Chronic use: Increased risk of premature rupture of membranes. |
| Fetal Monitoring | Serial fetal ultrasound for growth restriction every 4 weeks; nonstress test or biophysical profile weekly after 32 weeks. Monitor maternal blood pressure, glucose tolerance, and signs of infection. Assess neonate for adrenal suppression with ACTH stimulation test if maternal dose >20 mg/day for >3 weeks. |
| Fertility Effects | May suppress ovulation via inhibition of gonadotropin release. Reversible upon discontinuation. Does not cause permanent ovarian damage. In males, may reduce sperm count and motility, reversible. |
| Paracort is a brand name for prednisolone. Monitor for hyperglycemia, especially in diabetic patients. Taper dose to avoid adrenal crisis. Corticosteroids may mask signs of infection. Use lowest effective dose for shortest duration. |
| Patient Advice | Take with food to reduce stomach upset. · Do not stop suddenly; dose must be tapered. · Report signs of infection (fever, sore throat) immediately. · Avoid live vaccines while on this medication. · Carry a steroid warning card or ID. |