CEFOTETAN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CEFOTETAN (CEFOTETAN).
Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidase activity, and disrupting peptidoglycan cross-linking.
| Metabolism | Not significantly metabolized; primarily excreted unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Renal (80-90% unchanged), biliary (small amount, up to 20% in bile), fecal (<5%). |
| Half-life | 3-4.5 hours (6-8 hours in renal impairment). |
| Protein binding | 88-90% (primarily albumin). |
| Volume of Distribution | 8-10 L (0.13-0.16 L/kg; distributes well into tissues, including bile and peritoneal fluid). |
| Bioavailability | IM: ~100%. |
| Onset of Action | IV: Immediate (~30 minutes for therapeutic levels); IM: 30-60 minutes. |
| Duration of Action | Approximately 12 hours (dosing every 12 hours is typical; prolonged in renal impairment). |
1 to 2 g intravenously or intramuscularly every 12 hours. For severe infections, up to 2 g every 12 hours for 5-10 days.
| 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 25% of usual dose every 48 hours, given after dialysis. |
| Liver impairment | No specific adjustment for Child-Pugh A or B. For Child-Pugh C, use with caution and monitor for adverse effects; no established dose reduction. |
| Pediatric use | Children 1 month to 16 years: 40-80 mg/kg/day intravenously or intramuscularly divided every 12 hours. For severe infections, up to 100 mg/kg/day. Maximum daily dose: 6 g. |
| Geriatric use | Use lower end of dosing range based on renal function; adjust per creatinine clearance. Monitor renal function closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CEFOTETAN (CEFOTETAN).
| Breastfeeding | Cefotetan is excreted into human milk in low concentrations. The milk-to-plasma ratio (M/P) is not well established; one study reported a concentration of 0.5 mcg/mL at 2 hours after a 1 g dose. Because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. |
| Teratogenic Risk | Cefotetan did not cause fetal harm in animal studies at doses up to 1-2 times the human dose. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, cefotetan should be used during pregnancy only if clearly needed. The risk is considered low, but no trimester-specific data are available. It crosses the placenta and achieves therapeutic concentrations in fetal serum, amniotic fluid, and cord blood. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to cefotetan or other cephalosporins.","History of immediate hypersensitivity reactions (e.g., anaphylaxis) to penicillins or other beta-lactams (relative contraindication)."]
| Precautions | ["Hypersensitivity reactions: Cross-allergenicity with other beta-lactams; caution in penicillin-allergic patients.","Hemolytic anemia: Reports of immune-mediated hemolytic anemia; monitor for signs of hemolysis.","Clostridioides difficile-associated diarrhea (CDAD): May cause antibiotic-associated colitis; evaluate if diarrhea occurs.","Coagulation abnormalities: May prolong prothrombin time; monitor in patients at risk for bleeding or on anticoagulants.","Renal impairment: Dose adjustment required in moderate to severe renal dysfunction.","Superinfection: Prolonged use may lead to overgrowth of nonsusceptible organisms."] |
| Food/Dietary | Avoid alcohol and any products containing alcohol (e.g., beer, wine, liquor, certain mouthwashes, cough syrups, and elixirs) during cefotetan therapy and for at least 48 hours after the last dose due to risk of disulfiram-like reaction. No other significant food interactions. |
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| Fetal Monitoring | No specific maternal-fetal monitoring is routinely required beyond standard prenatal care. However, monitoring for adverse effects such as renal function, coagulation status (cefotetan may cause hypoprothrombinemia), and signs of superinfection should be considered during prolonged therapy. |
| Fertility Effects | No data are available on the effects of cefotetan on human fertility. Animal studies have not shown impaired fertility at doses up to 2 times the human dose. |
| Clinical Pearls | Cefotetan is a second-generation cephalosporin with activity against Bacteroides fragilis, making it useful for mixed aerobic-anaerobic infections. It has a disulfiram-like reaction with alcohol; advise patients to avoid alcohol during therapy and for 48 hours after. Cefotetan may cause hypoprothrombinemia; monitor prothrombin time in at-risk patients and consider vitamin K prophylaxis. Dose adjustment required in renal impairment (CrCl < 30 mL/min). Administer by slow IV injection over 3-5 minutes or IV infusion over 30 minutes. Do not use in patients with immediate hypersensitivity to cephalosporins or severe penicillin allergy. |
| Patient Advice | Take cefotetan exactly as prescribed; complete the full course even if you feel better. · Avoid alcohol and products containing alcohol during treatment and for 48 hours after the last dose to prevent severe nausea, vomiting, flushing, and headache. · Inform your doctor if you have a history of bleeding problems or are on blood thinners; cefotetan may increase bleeding risk. · Report any signs of allergic reaction: rash, itching, swelling, difficulty breathing. · If you experience diarrhea that is severe or contains blood/mucus, contact your doctor immediately; this may signal a Clostridium difficile infection. · Cefotetan may cause dizziness; avoid driving or operating machinery until you know how it affects you. · Store at room temperature; do not refrigerate reconstituted solution. Discard any unused solution after 24 hours. |