SULFOSE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SULFOSE (SULFOSE).
Sulfonamide antibiotic; inhibits bacterial dihydropteroate synthase, blocking folate synthesis and bacterial growth.
| Metabolism | Primarily hepatic via N-acetylation and glucuronidation; major enzyme NAT2. |
| Excretion | Renal: ~90% as unchanged drug via glomerular filtration; biliary/fecal: <10%. |
| Half-life | Terminal elimination half-life: 3-4 hours in patients with normal renal function; prolonged to 20-50 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 25-30% bound primarily to albumin. |
| Volume of Distribution | 0.2-0.3 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | Oral: 70-80% (first-pass metabolism minimal). |
| Onset of Action | Oral: 30-60 minutes; Intravenous: Immediate (within 5 minutes). |
| Duration of Action | Oral: 6-8 hours; Intravenous: 4-6 hours. Duration is prolonged in renal impairment. |
Meningococcal meningitis: 100 mg/kg/day intravenously in 4 divided doses (maximum 6 g/day). For other infections: 2-4 g/day IV/IM in 3-4 divided doses.
| Dosage form | SUSPENSION |
| Renal impairment | GFR 30-50 mL/min: no adjustment. GFR 15-29 mL/min: 2 g every 12 hours. GFR <15 mL/min: 2 g every 24 hours. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: 75% of normal dose. Child-Pugh C: 50% of normal dose. |
| Pediatric use | Neonates: 100 mg/kg/day IV divided every 12 hours. Infants >1 month: 100 mg/kg/day IV divided every 6 hours. Children: 100-200 mg/kg/day IV divided every 6 hours; maximum 6 g/day. |
| Geriatric use | No specific dose adjustment, but monitor renal function; reduce dose based on creatinine clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SULFOSE (SULFOSE).
| Breastfeeding | Excreted into breast milk; sulfonamides are concentrated in milk (M/P ratio ~0.5-0.9). Avoid in nursing infants with glucose-6-phosphate dehydrogenase deficiency or hyperbilirubinemia. American Academy of Pediatrics recommends use with caution. |
| Teratogenic Risk | SULFOSE contains sulfamethoxazole and sulfadiazine, both FDA Pregnancy Category D. First trimester: Risk of neural tube defects, cardiovascular malformations, and cleft palate based on animal studies and limited human data. Second/third trimester: Risk of kernicterus in neonates due to bilirubin displacement from albumin; avoid near term. |
■ FDA Black Box Warning
Fatal hypersensitivity reactions including Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias have been reported.
| Serious Effects |
Hypersensitivity to sulfonamides or any component; marked hepatic or renal impairment; porphyria; pregnancy at term and nursing mothers; infants <2 months (except for congenital toxoplasmosis).
| Precautions | Hypersensitivity reactions, severe skin reactions, hematologic toxicity, hepatic and renal impairment, photosensitivity, glucose-6-phosphate dehydrogenase deficiency, sulfonamide allergy, pregnancy (avoid near term), lactation. |
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| Fetal Monitoring | Monitor maternal CBC, renal function, liver enzymes, and bilirubin levels. Fetal assessment: serial ultrasound for growth and anatomy; consider amniotic fluid volume assessment. Neonatal monitoring for jaundice, hemolysis, and kernicterus. |
| Fertility Effects | No significant impairment in fertility reported in animal studies. Sulfonamides may cause reversible sperm abnormalities in males at high doses. No documented effect on female fertility. |