CEFOTAXIME AND DEXTROSE 3.9% IN PLASTIC CONTAINER
Clinical safety rating: safe
Probenecid may decrease cephalosporin excretion May cause diarrhea including Clostridium difficile-associated diarrhea.
Cefotaxime is a third-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), leading to cell lysis and death. It has broad-spectrum activity against gram-positive and gram-negative bacteria.
| Metabolism | Cefotaxime is metabolized primarily by deacetylation in the liver to desacetylcefotaxime, which has some antibacterial activity. It is partly metabolized by esterases and does not involve cytochrome P450 enzymes. |
| Excretion | Primarily renal (80-90% unchanged within 24 hours); biliary/fecal elimination accounts for <10% |
| Half-life | Terminal elimination half-life: 0.8-1.4 hours in adults with normal renal function; prolonged to 2.5-15 hours in renal impairment; clinical context: dosing interval adjustment required for CrCl <20 mL/min |
| Protein binding | 35-50% bound primarily to albumin |
| Volume of Distribution | 0.2-0.4 L/kg; clinical meaning: reflects moderate tissue distribution, crosses placenta and enters CSF with inflamed meninges |
| Bioavailability | IM: 90-100% absolute bioavailability; IV: 100% |
| Onset of Action | IV: Immediate; IM: 30 minutes to peak serum concentration |
| Duration of Action | 6-8 hours for susceptible organisms, requiring q6-8h dosing; clinical note: higher doses extend post-antibiotic effect for Gram-negative pathogens |
| Molecular Weight | Cefotaxime: 455.46 Da; Dextrose: 180.16 Da |
1-2 g IV every 4-6 hours; maximum 12 g/day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 20-50 mL/min: 1-2 g every 8-12 hours; CrCl 10-20 mL/min: 1-2 g every 12-24 hours; CrCl <10 mL/min: 1-2 g every 24 hours. |
| Liver impairment | No specific adjustment required for hepatic impairment. |
| Pediatric use | Neonates 0-1 week: 50 mg/kg IV every 12 hours; 1-4 weeks: 50 mg/kg IV every 8 hours; Infants and children: 50-180 mg/kg/day IV divided every 4-6 hours; maximum 12 g/day. |
| Geriatric use | Dose based on renal function; consider lower initial doses due to age-related renal decline. |
| 1st trimester | Use only if clearly needed. No well-controlled studies in humans; animal studies show no evidence of fetal harm. |
| 2nd trimester | Generally considered safe; crosses placenta but no known teratogenic effects. |
| 3rd trimester | Generally considered safe; may cause alteration of neonatal gut flora. |
Clinical note
Probenecid may decrease cephalosporin excretion May cause diarrhea including Clostridium difficile-associated diarrhea.
| FDA category | Human |
| Placental transfer | Crosses placenta; concentrations in cord blood are 30-50% of maternal serum levels. |
| Breastfeeding | Cefotaxime is excreted into breast milk in small amounts. Effects on nursing infant are unlikely; caution with history of hypersensitivity or diarrhea. |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | Diarrhea |
| Serious Effects |
Hypersensitivity to cefotaxime or other cephalosporinsSevere immediate hypersensitivity reaction to penicillins
| Precautions | Hypersensitivity reactions: Cross-allergenicity with other beta-lactams; serious and occasionally fatal reactions (anaphylaxis) can occur., Clostridium difficile-associated diarrhea: Consider in patients who develop diarrhea during or after therapy., Seizures: May occur at high doses, especially in patients with renal impairment., Hematologic effects: Prolonged use may cause neutropenia, thrombocytopenia, and bleeding disorders., Renal impairment: Dose adjustment required; monitor renal function., Superinfection: Prolonged use may result in overgrowth of non-susceptible organisms. |
| Food/Dietary |
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| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | Cefotaxime is a pregnancy category B drug. Animal studies have not demonstrated fetal risk, and there are no adequate and well-controlled studies in pregnant women. Cefotaxime crosses the placenta. In the first trimester, theoretical risk of neural tube defects is negligible due to its antibacterial mechanism not affecting DNA synthesis. No teratogenic effects have been reported in humans. In the second and third trimesters, no increased risk of malformations; monitor for potential alterations in maternal gut flora and neonatal infection risk if used close to delivery. |
| Fetal Monitoring | Monitor maternal renal function, hepatic function, and complete blood count during prolonged therapy. Monitor for signs of superinfection and Clostridioides difficile colitis. For the fetus, monitor growth if used in second/third trimester. At delivery, observe neonate for signs of infection due to possible group B streptococcal prophylaxis use. |
| Fertility Effects | No evidence of impaired fertility in animal studies. In humans, cefotaxime has no known adverse effects on fertility or reproductive function based on available data. |
| No specific food interactions. Avoid alcohol during therapy and for 48 hours after completion due to possible disulfiram-like reaction. Dextrose content may affect blood glucose; diabetic patients should monitor glucose levels. |
| Clinical Pearls | Cefotaxime is a third-generation cephalosporin with good CSF penetration. The 3.9% dextrose solution provides ~130 kcal/L; monitor blood glucose in diabetic patients. Administer over 30 minutes for intermittent infusion. Dose adjustment required in severe renal impairment (CrCl <20 mL/min). Contraindicated in patients with cephalosporin hypersensitivity and caution in penicillin allergy (cross-reactivity ~10%). |
| Patient Advice | Complete the full course of antibiotics even if you feel better. · Report any signs of allergic reaction: rash, hives, difficulty breathing, swelling. · Monitor for diarrhea, especially watery or bloody stools, which may indicate Clostridioides difficile infection. · This medication contains dextrose (sugar); inform your doctor if you have diabetes. · Do not mix with alcohol-containing solutions; alcohol may cause disulfiram-like reaction. |