KEFLIN IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KEFLIN IN PLASTIC CONTAINER (KEFLIN IN PLASTIC CONTAINER).
Cephalothin is a first-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation and autolysin activity, leading to cell lysis and death.
| Metabolism | Partially metabolized by ester hydrolysis to desacetylcephalothin; primarily renal excretion (60-90% unchanged); minor hepatic metabolism. |
| Excretion | Renal: 60-80% unchanged; biliary/fecal: minimal (<1%) |
| Half-life | 0.5-1 hour in normal renal function; prolonged to 20-30 hours in severe renal impairment (CrCl <10 mL/min) |
| Protein binding | 60-70% bound to serum albumin |
| Volume of Distribution | 0.1-0.2 L/kg; primarily extracellular fluid |
| Bioavailability | IM: 100%; Oral: not administered (parenteral only) |
| Onset of Action | IV: Immediate; IM: 5-10 minutes |
| Duration of Action | 6-8 hours for susceptible organisms; shorter in severe infections |
| Molecular Weight | 418.42 |
1 to 2 g IV or IM every 4 to 6 hours. Maximum 12 g/day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: 1-2 g every 6-8 hours; CrCl 10-29 mL/min: 1-2 g every 12 hours; CrCl <10 mL/min: 1-2 g every 24 hours. |
| Liver impairment | No adjustment required for hepatic impairment. |
| Pediatric use | Infants and children: 50-100 mg/kg/day IV or IM divided every 4-6 hours; severe infections: 100-150 mg/kg/day divided every 4-6 hours. |
| Geriatric use | Adjust dose based on renal function; consider lower initial doses due to age-related decreased renal clearance. |
| 1st trimester | Generally considered safe; cefalotin crosses placenta but no evidence of teratogenicity in animal studies. |
| 2nd trimester | Safe for use when clinically indicated; monitor for maternal adverse effects. |
| 3rd trimester | Safe for use; consider risk of neonatal sensitization or diarrhea. |
Clinical note
Comprehensive clinical and safety monograph for KEFLIN IN PLASTIC CONTAINER (KEFLIN IN PLASTIC CONTAINER).
| Placental transfer | Crosses placenta; fetal serum concentrations may reach 50-100% of maternal levels. |
| Breastfeeding | Cefalotin is excreted into breast milk in low concentrations; unlikely to cause adverse effects in term infants. Caution in premature infants or those with glucose-6-phosphate dehydrogenase deficiency. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to cephalosporinsSevere immediate hypersensitivity to penicillins (anaphylaxis)
| Precautions | Hypersensitivity reactions (including anaphylaxis) may occur, especially in patients with penicillin allergy; superinfection with prolonged use; Clostridioides difficile-associated diarrhea; renal impairment requires dose adjustment; positive direct Coombs' test; neutropenia with prolonged therapy; thrombophlebitis at injection site. |
| Food/Dietary | No significant food interactions. Avoid alcohol while on cephalosporins to reduce disulfiram-like reaction risk (rare). Take with food if GI upset occurs. |
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| Teratogenic Risk | Cephalothin is a first-generation cephalosporin. Animal studies have not revealed teratogenic effects. There are no adequate well-controlled studies in pregnant women. During organogenesis (first trimester), risk is considered low, but data are limited. In second and third trimesters, cephalothin is generally considered safe when clinically indicated. However, avoid use in pregnancy unless clearly needed. |
| Fetal Monitoring | Monitor maternal renal function (cephalothin is renally eliminated) and for signs of hypersensitivity. In prolonged treatment, monitor for superinfection and Clostridium difficile colitis. No specific fetal monitoring recommended; standard prenatal care. |
| Fertility Effects | No known adverse effects on fertility in animal studies. Human data are lacking. Cephalothin is not expected to impair fertility or reproductive performance. |
| Clinical Pearls |
| Cephalothin is a first-generation cephalosporin with activity against Gram-positive cocci (except MRSA and enterococci) and some Gram-negative rods. It is primarily used for surgical prophylaxis and skin/soft tissue infections. Administer IV or IM; avoid intra-arterial injection. Monitor renal function in elderly or renally impaired patients; adjust dose per CrCl. Cross-sensitivity with penicillins occurs in ~5-10% of patients. Do not confuse cephalothin with cephalexin; cephalothin is parenteral only. |
| Patient Advice | Take this medication exactly as prescribed; it is given by injection or infusion. · Report any signs of allergic reaction, such as rash, itching, or difficulty breathing. · Inform your doctor if you have a history of penicillin allergy. · Complete the full course of therapy even if you feel better. · Notify your healthcare provider if you experience severe diarrhea, as this may be Clostridioides difficile colitis. |