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Cefalessina [DCIT];Cefalexin;Cefalexin Sodium;Cefalexina [INN-Spanish];Cefalexine [INN-French];Cefalexinum [INN-Latin];Cephalexin 1-hydrate;Cephalexin hydrate;Cephalexin monohydrate;Cephalexine;Cephalexinum;CEX;

A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of cephaloridine or cephalothin, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms. [PubChem]

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Synthesis Reference	Not Available
General Reference	Not Available

Type	small molecule

Classes

Phenethylamines Cephalosporins

Substructures

Hydroxy Compounds Acetates Amino Ketones Carboxylic Acids and Derivatives Aliphatic and Aryl Amines Benzene and Derivatives Beta Lactams Enamines Phenethylamines Heterocyclic compounds Aromatic compounds Carboxamides and Derivatives Cephalosporins Lactams Azetidines

antibacterials 抗细菌;

Indication	For the treatment of respiratory tract infections caused by Streptococcus pneumoniae and Streptococcus pyogenes; otitis media due to Streptococcus pneumoniae, Haemophilus influenzae, Staphylococcus aureus, Streptococcus pyogenes, and Moraxella catarrhalis; skin and skin structure infections caused by Staphylococcus aureus and/or Streptococcus pyogenes; bone infections caused by Staphylococcus aureus and/or Proteus mirabilis; genitourinary tract infections, including acute prostatitis, caused by Escherichia coli, Proteus mirabilis, and Klebsiella pneumoniae.
Pharmacodynamics	Cephalexin (also called Cefalexin) is a first generation cephalosporin antibiotic. It is one of the most widely prescribed antibiotics, often used for the treatment of superficial infections that result as complications of minor wounds or lacerations. It is effective against most gram-positive bacteria.
Mechanism of action	Cephalexin, like the penicillins, is a beta-lactam antibiotic. By binding to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, it inhibits the third and last stage of bacterial cell wall synthesis. Cell lysis is then mediated by bacterial cell wall autolytic enzymes such as autolysins; it is possible that cephalexin interferes with an autolysin inhibitor.
Absorption	Well absorbed from the gastrointestinal tract
Volume of distribution	Not Available
Protein binding	14%
Metabolism	No appreciable biotransformation in the liver (90% of the drug is excreted unchanged in the urine).
Route of elimination	Cephalexin 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.
Half life	1 hour
Clearance	Not Available
Toxicity	Symptoms of overdose include blood in the urine, diarrhea, nausea, upper abdominal pain, and vomiting. The oral median lethal dose of cephalexin in rats is >5000 mg/kg.
Affected organisms	Enteric bacteria and other eubacteria
Pathways	Not Available

Properties
State	solid
Experimental Properties	Property Value Source melting point 326.8 °C Not Available water solubility 1789 mg/L Not Available logP 0.65 HANSCH,C ET AL. (1995) pKa 4.5 Not Available
Predicted Properties	Property Value Source water solubility 2.97e-01 g/l ALOGPS logP 0.55 ALOGPS logP -2.1 ChemAxon logS -3.1 ALOGPS pKa (strongest acidic) 3.45 ChemAxon pKa (strongest basic) 7.44 ChemAxon physiological charge 0 ChemAxon hydrogen acceptor count 5 ChemAxon hydrogen donor count 3 ChemAxon polar surface area 112.73 ChemAxon rotatable bond count 4 ChemAxon refractivity 88.97 ChemAxon polarizability 32.52 ChemAxon

Drug	Interaction
Probenecid	Probenecid may increase the serum level of cephalexin.

• Take on empty stomach: 1 hour before or 2 hours after meals.