CEPHALOTHIN SODIUM W/ DEXTROSE IN PLASTIC CONTAINER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CEPHALOTHIN SODIUM W/ DEXTROSE IN PLASTIC CONTAINER (CEPHALOTHIN SODIUM W/ DEXTROSE IN PLASTIC CONTAINER).
Cephalothin is a first-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), leading to cell lysis and death. It has bactericidal activity against susceptible gram-positive and some gram-negative bacteria.
| Metabolism | Cephalothin is partially metabolized to desacetylcephalothin, a less active metabolite, primarily in the liver. The parent drug and metabolite are excreted renally. |
| Excretion | Primarily renal (60-70% unchanged) via glomerular filtration and tubular secretion; minor biliary (5-10%) and fecal (<1%) elimination. |
| Half-life | 30-60 minutes in normal renal function; prolonged to 2-8 hours in severe renal impairment (CrCl <10 mL/min). |
| Protein binding | 65-80% bound, primarily to albumin. |
| Volume of Distribution | 0.2-0.3 L/kg; low Vd indicates limited distribution, mainly in extracellular fluid. |
| Bioavailability | Not applicable (IV only); IM bioavailability near 100%. |
| Onset of Action | Intravenous: immediate; intramuscular: 15-30 minutes. |
| Duration of Action | 2-4 hours for IV/IM; prolonged in renal impairment. Serum levels >10 mcg/mL maintained for 6-8 hours with high doses. |
| Molecular Weight | 396.44 |
1-2 g IV every 4-6 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 8-12 hours; CrCl <10 mL/min: 1-2 g every 12-24 hours. |
| Liver impairment | No specific adjustments for Child-Pugh class; use standard dosing with monitoring. |
| Pediatric use | Neonates: 20 mg/kg IV every 6-12 hours; Infants and children: 10-25 mg/kg IV every 4-6 hours; severe infection: up to 40 mg/kg IV every 6 hours. |
| Geriatric use | Initiate at lower end of dosing range (e.g., 1 g every 6-8 hours) based on renal function; monitor for renal impairment and adjust per renal guidelines. |
| 1st trimester | Cephalothin is a first-generation cephalosporin. Animal studies have not shown fetal harm, but adequate human studies in the first trimester are lacking. Generally considered safe if clinically indicated. |
| 2nd trimester | No evidence of teratogenicity. Use if clearly needed. |
| 3rd trimester | Considered safe during late pregnancy. No known adverse effects on the fetus. |
Clinical note
Comprehensive clinical and safety monograph for CEPHALOTHIN SODIUM W/ DEXTROSE IN PLASTIC CONTAINER (CEPHALOTHIN SODIUM W/ DEXTROSE IN PLASTIC CONTAINER).
| Placental transfer | Cephalothin crosses the placenta to a limited extent. Fetal serum concentrations are approximately 10-20% of maternal serum levels. Appears to be minimal placental transfer. |
| Breastfeeding | Cephalothin is excreted into breast milk in small amounts. It is considered compatible with breastfeeding due to low oral bioavailability in infants and minimal risk of adverse effects. However, monitor for potential gastrointestinal disturbances or allergic reactions in the nursing infant. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to cephalothin or any cephalosporinHistory of immediate-type hypersensitivity reaction (e.g., anaphylaxis) to penicillins (cross-sensitivity)
| Precautions | Hypersensitivity reactions including anaphylaxis (cross-sensitivity with other beta-lactams)., Clostridioides difficile-associated diarrhea (CDAD)., Renal impairment: Dose adjustment required., Positive direct Coombs test (may cause hemolytic anemia). |
| Food/Dietary | No significant food interactions are expected. However, cephalothin may cause gastrointestinal upset; take with food or milk if tolerated to reduce stomach discomfort. |
Loading safety data…
| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | Cephalothin is a first-generation cephalosporin. Animal studies have not shown evidence of fetal harm. There are no adequate and well-controlled studies in pregnant women. However, cephalosporins are generally considered low risk. The drug crosses the placenta. The US FDA categorizes cephalosporins as Pregnancy Category B. No known teratogenic effects in any trimester. |
| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN) and hepatic enzymes due to potential toxicity. Observe for signs of hypersensitivity reactions, diarrhea, or superinfection. No specific fetal monitoring required beyond routine prenatal care. |
| Fertility Effects | In animal studies, no adverse effects on fertility or reproductive performance were observed. There are no human data suggesting impairment of fertility. |
| Clinical Pearls |
| Cephalothin is a first-generation cephalosporin with activity against Gram-positive bacteria including Streptococcus pneumoniae, Streptococcus pyogenes, and Staphylococcus aureus (including penicillinase-producing strains). It is not active against MRSA. Administer IV only; IM injection is painful. Monitor renal function due to nephrotoxicity risk, especially with aminoglycosides or loop diuretics. False-positive urinary glucose tests may occur with Clinitest but not with glucose oxidase methods. |
| Patient Advice | This medication is given intravenously (through a vein) and must be administered by a healthcare professional. · Report any signs of allergic reaction such as rash, itching, swelling, or difficulty breathing immediately. · Inform your provider if you have a history of allergy to penicillins or other cephalosporins. · This medicine may cause diarrhea, nausea, or vomiting; contact your doctor if diarrhea becomes severe or bloody. · Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding. |