CEFOTAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CEFOTAN (CEFOTAN).
Cefotetan is a cephamycin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting peptidoglycan cross-linking, and activating autolytic enzymes.
| Metabolism | Cefotetan is not significantly metabolized; it is primarily excreted unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Primarily renal (unchanged); ~88% excreted in urine within 24 hours. Biliary/fecal elimination is negligible (<1% as metabolites). |
| Half-life | Terminal elimination half-life: 4.5 hours (intravenous). In patients with renal impairment (CrCl <30 mL/min), half-life extends to approximately 20–30 hours, requiring dose adjustment. |
| Protein binding | 85–90%, primarily to albumin. |
| Volume of Distribution | 0.15 L/kg (approximately 10 L in adults). Indicates distribution primarily into extracellular fluid; low Vd suggests limited tissue penetration. |
| Bioavailability | Intravenous only (complete bioavailability); not available for oral administration. Intramuscular: 100% bioavailable (comparative to IV). |
| Onset of Action | Intravenous: Rapid, within minutes after injection; peak concentrations achieved by end of infusion. |
| Duration of Action | Approximately 12 hours (twice-daily dosing) due to sustained serum levels above MIC for susceptible organisms. Used for surgical prophylaxis with a single pre-operative dose. |
1-2 g IV/IM every 12 hours for 5-10 days; up to 6 g/day for severe infections.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: 1-2 g every 24 hours; CrCl 10-29 mL/min: 1-2 g every 48 hours; CrCl <10 mL/min: 1-2 g every 48 hours. Hemodialysis: administer after dialysis. |
| Liver impairment | No specific dosing adjustment recommended for hepatic impairment; monitor liver function tests. |
| Pediatric use | Neonates and infants <1 month: not recommended; Children ≥1 month: 20-40 mg/kg IV/IM every 12 hours; maximum 6 g/day. |
| Geriatric use | CrCl <60 mL/min: adjust per renal function; no specific age-related dose adjustment otherwise. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CEFOTAN (CEFOTAN).
| Breastfeeding | Cefotetan is excreted in human milk in low concentrations; M/P ratio not established. Considered compatible with breastfeeding with monitoring for diarrhea or candidiasis in the infant. |
| Teratogenic Risk | FDA Pregnancy Category B. Animal studies have not shown fetal harm, but no adequate human studies. Risk cannot be ruled out. Use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
Cefotetan contains a methylthiotetrazole (MTT) side chain which may cause hypoprothrombinemia and bleeding, especially in elderly, debilitated, or malnourished patients. Vitamin K administration may be required.
| Serious Effects |
["Hypersensitivity to cefotetan, other cephalosporins, or any component of the formulation","Previous immediate hypersensitivity reaction to penicillins (cross-sensitivity possible)"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Increased risk of bleeding due to hypoprothrombinemia","Potential for Clostridioides difficile-associated diarrhea","Superinfection with non-susceptible organisms","Dosage adjustment required in renal impairment","Pregnancy category B"] |
| Food/Dietary | Avoid alcohol and alcohol-containing products (e.g., some mouthwashes, cough syrups) during therapy and for at least 72 hours after the last dose. No other specific food restrictions; maintain adequate hydration. Cefotetan may interfere with vitamin K synthesis, so consider dietary sources of vitamin K (e.g., green leafy vegetables) but no restriction needed. |
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| Monitor renal function, hepatic function, and blood dyscrasias (prolonged use). Observe for signs of bleeding due to hypoprothrombinemia; may require vitamin K prophylaxis. |
| Fertility Effects | No known direct effects on fertility. Standard reproductive studies in animals showed no impairment. |
| Clinical Pearls | Cefotetan (a cephamycin antibiotic) has activity against anaerobes similar to cefoxitin and is often used for surgical prophylaxis, especially in colorectal and gynecologic surgeries. It can cause a disulfiram-like reaction with alcohol, so avoid concurrent alcohol ingestion. It may also cause hypoprothrombinemia and bleeding due to interference with vitamin K metabolism; monitor prothrombin time in high-risk patients. Cross-allergenicity with penicillins exists; use caution in penicillin-allergic patients. |
| Patient Advice | Take exactly as prescribed; complete the full course even if you feel better. · Do not drink alcohol during treatment and for at least 72 hours after the last dose to avoid severe nausea, vomiting, and flushing. · Report any signs of bleeding (unusual bruising, black/tarry stools) or allergic reaction (rash, itching, difficulty breathing) to your healthcare provider immediately. · If you are on blood thinners (e.g., warfarin), inform your doctor as this medication may increase bleeding risk. · Notify your doctor if you have a history of penicillin allergy, kidney disease, or bleeding disorders. |