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 |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for KEFLIN IN PLASTIC CONTAINER (KEFLIN IN PLASTIC CONTAINER).
| Breastfeeding | Cephalothin is excreted into breast milk in small amounts (M/P ratio not established; estimated less than 1% of maternal dose). It is considered compatible with breastfeeding by the American Academy of Pediatrics. Caution in infants with G6PD deficiency or history of allergy. Monitor infant for diarrhea, rash, or candidiasis. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to cephalothin, any cephalosporin, or beta-lactam antibiotics; history of immediate-type hypersensitivity reaction to penicillins (cross-sensitivity).
| 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. |
Loading safety data…
| 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. |