Cefalotin


Generic Medicine Info
Indications and Dosage
Intravenous
Prophylaxis of surgical infections
Adult: 2 g as slow inj over 3-5 min or by intermittent or continuous infusion 30-60 min prior to surgery, followed by 2 g during surgery, then 2 g 6 hrly after surgery for 24 hr; continued for up to 72 hr for patients undergoing heart valve replacement or arthroplasty.

Parenteral
Susceptible infections
Adult: 0.5-1 g 4-6 hrly by slow IV inj over 3-5 min or by intermittent or continuous infusion, deep IM inj. Max: 12 g daily.
Child: 80-160 mg/kg daily in divided doses, by deep IM inj, slow IV inj, or by intermittent or continuous IV infusion.
Renal Impairment
Max dose should be given after IV loading dose of 1-2 g according to CrCl.
CrCl (mL/min) Dosage
<2 500 mg 8 hrly.
2-10 500 mg 6 hrly.
11-25 1 g 6 hrly.
26-50 1.5 g 6 hrly.
51-80 2 g 6 hrly.
Reconstitution
IM: Dissolve cefalotin 1 g in sterile water for inj 4 mL; may add a small amount of diluents (e.g. 0.2-0.4 mL) if the soln do not dissolve completely. IV: Dissolve cefalotin 1 g in saline 10 mL or glucose soln 5%.
Incompatibility
Aminoglycosides.
Contraindications
Hypersensitivity to cephalosporins.
Special Precautions
Hypersensitivity to penicillins. History of allergy. Renal impairment. Pregnancy and lactation.
Adverse Reactions
Hypersensitivity reactions (e.g. skin rashes, urticaria, eosinophilia, fever, serum sickness-like reactions); neutropenia, thrombocytopenia, bleeding complications related to hypoprothrombinaemia and/or platelet dysfunction, nephrotoxicity, acute renal tubular necrosis, acute interstitial nephritis, transient increase in liver enzyme values, convulsions and other signs of CNS toxicity, thrombophlebitis (IV) and pain (IM) at inj site. Rarely, haemolytic anaemia, agranulocytosis, hepatitis, cholestatic jaundice, GI effects (e.g. nausea, vomiting, diarrhoea).
Potentially Fatal: Anaphylaxis, pseudomembranous colitis.
Monitoring Parameters
Monitor renal and haematological status esp during prolonged and high dose therapy.
Drug Interactions
Increased risk of nephrotoxicity w/ aminoglycosides (e.g. gentamicin, tobramycin) and loop diuretics (e.g. furosemide). Antagonistic effect w/ bacteriostatic antibacterials. Probenecid may inhibit renal excretion of cefalotin.
Lab Interference
May interfere w/ Jaffe method of measuring creatinine concentrations and may produce falsely high values. Positive response to direct Coombs' test. False-positive reactions for glucose using copper-reduction reactions.
Action
Description: Cefalotin interferes w/ bacterial cell wall peptidoglycan synthesis by binding to penicillin-binding proteins, eventually leading to cell lysis and death. It has bactericidal action.
Pharmacokinetics:
Absorption: Poorly absorbed from the GI tract. Time to peak plasma concentration: W/in 30 min (IM); 15 min (IV).
Distribution: Widely distributed in body tissues and fluids except the brain and CSF (low and unpredictable concentrations). Crosses the placenta and enters breast milk (low concentrations). Plasma protein binding: Approx 70%.
Metabolism: Hepatic via deacetylation.
Excretion: Via urine (approx 60-70%) and bile (very small amount). Plasma half-life: Approx 30-50 min.
Chemical Structure

Chemical Structure Image
Cefalotin

Source: National Center for Biotechnology Information. PubChem Database. Cephalothin, CID=6024, https://pubchem.ncbi.nlm.nih.gov/compound/Cephalothin (accessed on Jan. 21, 2020)

Storage
Store below 25°C. Protect from direct sunlight.
MIMS Class
Cephalosporins
References
Buckingham R (ed). Cefalotin Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/10/2014.

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