PEDIAZOLE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PEDIAZOLE (PEDIAZOLE).
Pediazole is a combination of erythromycin (a macrolide antibiotic that binds to the 50S ribosomal subunit, inhibiting bacterial protein synthesis) and sulfisoxazole (a sulfonamide that inhibits dihydropteroate synthase, blocking folic acid synthesis).
| Metabolism | Erythromycin is metabolized primarily by CYP3A4; sulfisoxazole is acetylated and glucuronidated in the liver. |
| Excretion | Renal excretion of unchanged drug accounts for approximately 70-80% of the dose; biliary/fecal elimination is minor (<10%). |
| Half-life | Terminal half-life is approximately 6-8 hours in adults with normal renal function; prolonged to 20-40 hours in severe renal impairment. |
| Protein binding | Approximately 50% bound to serum albumin. |
| Volume of Distribution | Vd is 0.6-0.8 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral bioavailability is 90-95%. |
| Onset of Action | Oral: onset within 30-60 minutes; intravenous: immediate clinical effect within minutes. |
| Duration of Action | Duration is 8-12 hours after oral administration; continuous IV infusion maintains steady-state concentrations. |
Adults: 1 mg/kg intravenously every 6 hours.
| Dosage form | GRANULE |
| Renal impairment | GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: 1 mg/kg every 12 hours; GFR <10 mL/min: 1 mg/kg every 24 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: reduce dose by 75%. |
| Pediatric use | Children: 1.5 mg/kg intravenously every 6 hours for weight <10 kg; 1 mg/kg every 6 hours for weight ≥10 kg. |
| Geriatric use | Elderly: start at lower end of dosing range (0.5 mg/kg every 6 hours) and titrate based on renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PEDIAZOLE (PEDIAZOLE).
| Breastfeeding | Erythromycin is excreted in breast milk in small amounts (M/P ratio approximately 0.5 for erythromycin base; sulfisoxazole is also excreted, with an M/P ratio of about 0.5-0.8). The combination may cause adverse effects in the nursing infant, including diarrhea, rash, and, theoretically, kernicterus due to sulfisoxazole's displacement of bilirubin from albumin. Breastfeeding is not recommended during PEDIAZOLE therapy; if used, the infant should be monitored for jaundice, hemolysis, and gastrointestinal disturbances. |
| Teratogenic Risk | PEDIAZOLE (erythromycin ethylsuccinate and sulfisoxazole acetyl) contains sulfisoxazole, a sulfonamide, which is contraindicated in pregnancy at term and during lactation due to risk of kernicterus in the neonate. Sulfonamides cross the placenta and may cause hemolytic anemia in the fetus. During the first trimester, there is no clear evidence of teratogenicity from epidemiologic studies, but caution is advised. In the second and third trimesters, the risk of adverse fetal effects (e.g., jaundice, hemolytic anemia) increases; use is generally avoided. |
■ FDA Black Box Warning
Sulfonamides, including sulfisoxazole, have caused fatalities due to severe reactions such as Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Erythromycin has been associated with QT prolongation and ventricular arrhythmias, including torsade de pointes.
| Serious Effects |
Hypersensitivity to erythromycin, any macrolide, sulfonamides, or any component; concomitant use with cisapride, pimozide, ergotamine, or dihydroergotamine due to risk of arrhythmias; infants <2 months; significant hepatic impairment; porphyria.
| Precautions | Risk of severe hypersensitivity reactions including Stevens-Johnson syndrome; QT prolongation and cardiac arrhythmias; hepatotoxicity; superinfection; hemolytic anemia in patients with G6PD deficiency; caution in renal or hepatic impairment; avoid use in infants <2 months of age due to risk of kernicterus. |
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| Fetal Monitoring | Maternal monitoring: Assess for hypersensitivity reactions (rash, fever, Stevens-Johnson syndrome), hepatotoxicity, and hematologic abnormalities (CBC with differential at baseline and periodically). Fetal monitoring: Ultrasound for fetal growth and anatomy if exposed during first trimester; assess for neonatal jaundice and hemolytic anemia if exposed near term. |
| Fertility Effects | No specific studies on PEDIAZOLE and fertility in humans. In animal studies, erythromycin has not been shown to impair fertility. Sulfisoxazole has no reported effects on fertility. However, general health conditions requiring antibiotic therapy may temporarily affect fertility. |