CEFOBID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CEFOBID (CEFOBID).
Cefoperazone is a third-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), thereby inhibiting peptidoglycan cross-linking and causing cell lysis.
| Metabolism | Primarily eliminated unchanged in bile; partial hepatic metabolism to inactive metabolites; not significantly metabolized by CYP450 enzymes. |
| Excretion | Primarily renal (80-90% unchanged in urine) and biliary (10-20%). |
| Half-life | 2 hours (prolonged in hepatic impairment and neonates). |
| Protein binding | 88-93% (albumin). |
| Volume of Distribution | 0.08-0.14 L/kg (highly distributed in extracellular fluid). |
| Bioavailability | IM: 100%. |
| Onset of Action | IM: 1-2 hours; IV: immediate. |
| Duration of Action | 12 hours (dosing every 12 hours). |
| Action Class | Cephalosporins: 3 generation |
| Brand Substitutes | Elpod DS 50mg Syrup, Zepodox 50mg Syrup, Cepoxim 50mg Syrup, Cepotuf 50mg Syrup, Podo 50mg Syrup |
2-4 g/day IV/IM divided q12h; severe infections: 6-12 g/day IV divided q8-12h
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 10-50 mL/min: 1.5-4 g q12h; CrCl <10 mL/min: 1-2 g q12h |
| Liver impairment | Child-Pugh B: reduce dose by 50% q12h; Child-Pugh C: 1 g q12h |
| Pediatric use | 50-100 mg/kg/day IV/IM divided q12h; max 6 g/day |
| Geriatric use | Max 4 g/day; reduce dose if CrCl <50 mL/min or Child-Pugh ≥B |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CEFOBID (CEFOBID).
| Breastfeeding | Cefoperazone is excreted in human milk in low concentrations. The milk-to-plasma (M/P) ratio is approximately 0.01-0.02. It is considered compatible with breastfeeding due to poor oral bioavailability and minimal infant exposure. Caution is advised in infants with hypersensitivity or gastrointestinal disturbances. |
| Teratogenic Risk | Cefoperazone (CEFOBID) is classified as FDA Pregnancy Category B. Animal reproduction studies have not demonstrated fetal risk, but no adequate and well-controlled studies in pregnant women. Therefore, it should be used during pregnancy only if clearly needed. No specific teratogenic effects have been reported in any trimester. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Known hypersensitivity to cefoperazone or any cephalosporin","History of severe immediate hypersensitivity reaction to penicillins or other beta-lactams"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Pseudomembranous colitis due to Clostridium difficile","Bleeding risk due to hypoprothrombinemia (cefoperazone contains N-methylthiotetrazole side chain)","Disulfiram-like reaction with alcohol","Renal impairment may require dose adjustment"] |
| Food/Dietary | Avoid alcohol and alcohol-containing foods (e.g., sauces, desserts with wine). No specific food interactions; may be taken with or without food. Monitor vitamin K intake; foods rich in vitamin K (e.g., leafy greens) are generally not contraindicated but may affect anticoagulation status. |
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| Fetal Monitoring | No specific monitoring is routinely required. Standard monitoring for maternal infection and fetal well-being as clinically indicated. Prolonged use may warrant monitoring for superinfection and bleeding risk due to vitamin K deficiency. |
| Fertility Effects | No adverse effects on fertility have been reported in animal studies. No human data available, but no known negative impact on reproductive function is expected. |
| Clinical Pearls | Cefoperazone (Cefobid) is a third-generation cephalosporin with a high risk of bleeding due to inhibition of vitamin K synthesis by gut flora; monitor PT/INR and consider vitamin K supplementation. It has a disulfiram-like reaction with alcohol; avoid ethanol during therapy and for 72 hours after discontinuation. Excreted primarily in bile; adjust dose in hepatic impairment but not in renal impairment. Use with caution in patients with a history of penicillin allergy (cross-sensitivity ~10%). |
| Patient Advice | Do not drink alcohol or consume products containing alcohol (e.g., mouthwash, cough syrup) while taking this medication and for 3 days after stopping. · Report any unusual bleeding or bruising, as this drug can affect blood clotting. · Take exactly as prescribed; complete the full course even if you feel better. · Inform your doctor if you have liver disease or a penicillin allergy. · Common side effects include diarrhea, rash, and injection site reactions. |