KEFLIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KEFLIN (KEFLIN).
Cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), inhibiting transpeptidation and autolysin activation, leading to cell lysis.
| Metabolism | Not extensively metabolized; primarily excreted unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Renal: 70-80% unchanged via glomerular filtration and tubular secretion; biliary: minimal (<5%); fecal: <1%. |
| Half-life | Terminal elimination half-life: 0.5-1 hour (normal renal function); prolonged to 2-3 hours in anuria. Clinically, dosing every 6 hours is recommended. |
| Protein binding | 65-75% bound to serum albumin. |
| Volume of Distribution | 0.2-0.3 L/kg; indicates distribution primarily into extracellular fluid. |
| Bioavailability | Intramuscular: approximately 90% absorbed; oral: not available (parenteral only). |
| Onset of Action | Intravenous: immediate (within minutes); intramuscular: 15-30 minutes. |
| Duration of Action | 2-4 hours after IV/IM administration; requires frequent dosing due to short half-life. |
| Action Class | Cephalosporins: 3 generation |
| Brand Substitutes | Cefilab 200 Tablet, Cefix 200 Tablet, Mahacef 200 Tablet, Cefi 200 Tablet, Ceftas 200 Tablet |
1-2 g IV/IM every 4-6 hours; maximum 12 g/day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: 1-2 g every 6 hours; CrCl 10-29 mL/min: 1-2 g every 8-12 hours; CrCl <10 mL/min: 1-2 g every 24-48 hours. |
| Liver impairment | No adjustment required for mild to moderate hepatic impairment (Child-Pugh A and B); use with caution in severe impairment (Child-Pugh C) due to potential for increased toxicity. |
| Pediatric use | Infants and children: 50-100 mg/kg/day IV/IM divided every 6 hours; neonates: 50 mg/kg/day IV/IM divided every 12 hours. |
| Geriatric use | Start at lower end of dosing range (1 g every 6 hours) and adjust based on renal function; monitor for adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for KEFLIN (KEFLIN).
| Breastfeeding | Cephalothin is excreted in breast milk in low concentrations (M/P ratio not established). Considered compatible with breastfeeding; possible risk of diarrhea or allergic sensitization in infant. |
| Teratogenic Risk | FDA Pregnancy Category B. Animal studies have not demonstrated fetal risk, but no adequate human studies in pregnant women. Cephalothin crosses the placenta. First trimester: No known teratogenic effects. Second and third trimesters: Generally considered safe; use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Known hypersensitivity to cephalosporins or penicillins","Prior anaphylactic reaction to beta-lactam antibiotics"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Clostridioides difficile-associated diarrhea","Neurotoxicity with high doses or renal impairment","Antibiotic-associated colitis","Renal function monitoring"] |
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| Monitor for signs of hypersensitivity reactions in mother. No specific fetal monitoring required; standard obstetrical care. |
| Fertility Effects | No known adverse effects on fertility. Animal studies have not reported impaired fertility. |