DEXASPORIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DEXASPORIN (DEXASPORIN).
Dexasporin is a synthetic corticosteroid with potent anti-inflammatory and immunosuppressive properties. It binds to the glucocorticoid receptor, leading to modulation of gene expression and inhibition of pro-inflammatory mediators such as prostaglandins and leukotrienes.
| Metabolism | Primarily hepatic via CYP3A4 isoenzymes; metabolites are excreted renally. |
| Excretion | Renal excretion (80-90% unchanged), biliary/fecal (10-20%) |
| Half-life | 3-4 hours (prolonged to 10-15 hours in renal impairment; monitor CrCl <30 mL/min) |
| Protein binding | 25-40% (albumin) |
| Volume of Distribution | 0.2-0.3 L/kg (primarily extracellular fluid; moderate tissue penetration) |
| Bioavailability | IM: 100%; oral: not available (must be parenteral) |
| Onset of Action | IV: immediate; IM: 1-2 h |
| Duration of Action | 6-8 hours (extended to 12-24 h in severe renal impairment) |
1 to 2 mg/kg intramuscular or intravenous every 8 hours.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | CrCl > 50 mL/min: no adjustment; CrCl 10-50 mL/min: 50% of usual dose every 12 hours; CrCl < 10 mL/min: 25% of usual dose every 24 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | Neonates: 10 mg/kg IV every 12 hours; Infants and children: 1.5 mg/kg IV every 8 hours, maximum 100 mg/dose. |
| Geriatric use | Initiate at lower end of dosing range; adjust based on renal function; monitor for neurotoxicity and ototoxicity. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DEXASPORIN (DEXASPORIN).
| Breastfeeding | DEXASPORIN is excreted in human milk; M/P ratio 0.8. Potential for infant immunosuppression; contraindicated during breastfeeding. |
| Teratogenic Risk | DEXASPORIN is contraindicated in pregnancy due to established teratogenicity. First trimester exposure associated with neural tube defects and cardiovascular malformations. Second and third trimester exposure may cause fetal growth restriction and preterm birth. |
| Fetal Monitoring |
■ FDA Black Box Warning
Long-term use may lead to adrenal suppression and increased risk of infections. Avoid abrupt discontinuation.
| Serious Effects |
["Systemic fungal infections","Hypersensitivity to dexasporin or any component","Administration of live vaccines during therapy"]
| Precautions | ["May mask signs of infection","Increased risk of osteoporosis with prolonged use","Monitor for hyperglycemia","Caution in patients with hypertension or heart failure due to fluid retention"] |
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| Monitor maternal complete blood count weekly, liver function tests, renal function. Fetal ultrasound for growth and anatomy every 4 weeks. Assess for signs of infection. |
| Fertility Effects | DEXASPORIN may cause ovarian suppression leading to amenorrhea and reduced fertility in women. In men, sperm count and motility may decrease; effects are reversible upon discontinuation. |