Cefalotin

Intravenous
Prophylaxis of surgical infections

Parenteral
Susceptible infections

Max dose should be given after IV loading dose of 1-2 g according to CrCl.

CrCl (mL/min)	Dosage
<2	500 mg 8 hourly.
2-10	500 mg 6 hourly.
11-25	1 g 6 hourly.
26-50	1.5 g 6 hourly.
51-80	2 g 6 hourly.

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%.

Aminoglycosides.

Hypersensitivity to cephalosporins.

Hypersensitivity to penicillins. History of allergy. Renal impairment. Pregnancy and lactation.

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.

Monitor renal and haematological status esp during prolonged and high dose therapy.

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.

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.

Description:
Mechanism of Action: 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.

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

Store below 25°C. Protect from direct sunlight.

Cephalosporin

Buckingham R (ed). Cefalotin Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/10/2014.