Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2021 Publisher: Milpharm Limited, Ares, Odyssey Business Park, West End Road, South Ruislip HA4 6QD, United Kingdom
Pharmacotherapeutic group: Antibacterials for systemic use, first generation cephalsporins
ATC code: J01DB01
Cefalexin is bactericidal and has antimicrobial activity similar to that of cephaloridine or cephalothin against both gram-positive and gram-negative organisms.
In vitro tests demonstrate that cephalosporins are bactericidal because of their inhibition of cell-wall synthesis.
Cefalexin is active against the following organisms in vitro:
Beta haemolytic streptococci
Staphylococci, including coagulase positive, coagulase negative and penicillinase-producing strains.
Streptococcus pneumoniae
Escherichia coli
Proteus mirabilis
Klebsiella species
Haemophilus influenzae
Branhamella catarrhalis
Most strains of enterococci (Streptococcus faecalis) and a few strains of staphylococci are resistant to cefalexin. It is not active against most strains of Enterobacter species, Morganella morganii and Pr. vulgaris. It has no activity against Pseudomonas or Herellea species or Acinetobacter calcoaeticus. Penicillin-resistant Streptococcus pneumoniae is usually cross-resistant to beta-lactam antibiotics. When tested by in vitro methods, staphylococci exhibit cross resistance between cefalexin and methicillin type antibiotics.
Human pharmacology – Cefalexin is acid stable and may be given without regard to meals.
It is rapidly absorbed after oral administration from the gastro-intestinal tract and produces peak plasma concentrations about 1 hour after administration. Following doses of 250mg, 500mg and 1g, average peak serum levels of approximately 9, 18 and 32 mg/L respectively were obtained at 1 hour. Measurable levels were present 6 hours after administration.
Cefalexin is almost completely absorbed from the gastro-intestinal tract, and 75-100% is rapidly excreted in active form in the urine. If cefalexin is taken with food there is delayed and slightly reduced absorption and there may be delayed elimination from the plasma.
The half-life is approximately 60 minutes in patients with normal renal function. Haemodialysis and peritoneal dialysis will remove cefalexin from the blood.
The biological half-life has been reported to range from 0.6 to at least 1.2 hours and this increases with reduced renal function. About 10 to 15% of a dose is bound to plasma proteins.
Peak blood levels are achieved one hour after administration, and therapeutic levels are maintained for 6-8 hours. About 80% of the active drug is excreted in the urine within 6 hours. No accumulation is seen with dosages above the therapeutic maximum of 4g/day.
The half-life may be increased in neonates due to their renal immaturity, but there is no accumulation when given at up to 50mg/kg/day.
Cefalexin is excreted in the urine by glomerular filtration and tubular secretion. Studies showed that over 90% of the drug was excreted unchanged in the urine within 8 hours. During this period peak urine concentrations following the 250mg, 500mg and 1g doses were approximately 1000, 2200 and 5000mg/L respectively.
The daily oral administration of cefalexin to rats in doses of 250 or 500mg/kg prior to and during pregnancy, or to rats and mice during the period of organogenesis only, had no adverse effect on fertility, foetal viability, foetal weight, or litter size.
Cefalexin showed no enhanced toxicity in weanling and newborn rats as compared with adult animals.
The oral LD50 of cefalexin in rats is 5,000mg/kg.
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