Cefazolin

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Cefazolin, Kefzol, Servazolin; Belgium: Cefazoline, Kefzol; Bulgaria: Cefazolin; Cyprus: Zepilen; Czech Republic: Cefazolin, Cefazoline, Vulmizolin; Estonia: Cefazolin, Zepilen; France: Cefazoline; Germany: Baktozil, Basocef, Cefazolin, Cefodinin, Cephazolin, Saarzolin; Greece: Cefalin, Cephazolin, Vifazolin; Hungary: Cefazolin; Italy: Acef, Cefamezin, Cefazil, Cefazolina, Cromezin, Nefazol, Recef; Latvia: Cefazolin, Orizolin, Reflin; Lithuania: Cefazolin, Orizolin, Reflin, Zepilen; Luxembourg: Cefacidal, Kefzol; Netherlands: Cefazoline, Kefzol, Servalozin; Poland: Biofazolin, Cefazolin, Kefzol, Tarfazolin; Portugal: Cefamezin, Cefazolina; Romania: Lyzolin; Slovakia: Vulmizolin; Spain: Areuzolin, Cefazolina, Kurgan, Tecfazolina.

North America

Canada: Cefazolin; USA: Cefazolin, Kefzol (d).

Latin America

Argentina: Cefalomicina, Cefamezín, Cefazolina; Brazil: Cefazolina, Ceftrat, Duocef, Fazolón, Kefazol.

Asia

Japan: Cefamezin, Efunikol, Ohtsuka CEZ-MC, Rasenazolin, Sefmazon, Taicezolin.

Drug combinations

Chemistry

Cefazolin Sodium: C~14~H~13~N~8~NaO~4~S~3~. Mw: 476.49. (1) 5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 3-[[(5-methyl-1,3,4-thiadiazol-2-yl)thio]methyl]-8-oxo-7-[[(1H-tetrazol-1-yl)acetyl]amino]-, monosodium salt (6R-trans)-; (2) Monosodium (6R,7R)-3-[[(5-methyl-1,3,4-thiadiazol-2-yl)thio]methyl]-8-oxo-7-[2-(1H-tetrazol-1-yl)acetamido]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate; (3) 3-[[(5-Methyl-1,3,4-thiadiazol-2-yl)thio]methyl]-7-[2-(1H-tetrazol-1-yl)acetamido]-3-cephem-4-carboxylate. CAS-27164-46-1 (1972).

Pharmacologic Category

Antibacterials; First Generation Cephalosporins. (ATC-Code: J01DB04).

Mechanism of action

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins. Usually bactericidal. According to its spectrum of activity, classified as a first generation cephalosporin. Active in vitro and in clinical infections against Gram-positive aerobic bacteria, such as penicillinase-producing and nonpenicillinase-producing Staphylococcus aureus and S. epidermidis, Streptococcus pyogenes (group A β-hemolytic streptococci), S. agalactiae (group B streptococci), and S. pneumoniae. Enterococci and oxacillin-resistant (methicillin-resistant) staphylococci are resistant. Active in vitro and in clinical infections against Gram-negative aerobic bacteria such as some strains of Haemophilus influenzae, Escherichia coli, Klebsiella, Proteus mirabilis, and Enterobacter aerogenes. Inactive against most other Gram-negative bacteria, including Citrobacter, E. cloacae, Morganella, Providencia, Pseudomonas, and Serratia. Inactive against fungi and viruses.

Therapeutic use

Respiratory tract, skin and skin structure, genital, urinary tract, biliary tract, bone and joint infections, and septicemia due to susceptible bacteria. Perioperative prophylaxis.

Pregnancy and lactiation implications

Adverse effects not observed in animal reproduction studies. Cefazolin crosses the placenta. Adverse events not reported in the fetus following administration of cefazolin prior to caesarean section. Cefazolin is recommended for group B streptococcus prophylaxis in pregnant patients with a nonanaphylactic penicillin allergy. Enters breast milk (small amounts).

Unlabeled use

Prophylaxis against infective endocarditis.

Contraindications

Hypersensitivity to cefazolin sodium, any component of the formulation, or other cephalosporins.

Warnings and precautions

May be associated with increased INR, especially in nutritionally-deficient patients, prolonged treatment, hepatic or renal disease. Partial cross-sensitivity among cephalosporins and other β-lactam antibiotics, including penicillins and cephamycins (caution in patients with history of penicillin allergy; avoid use in those who have had an immediate-type (anaphylactic) hypersensitivity reaction and administer with caution in those who have had a delayed-type). Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea, and pseudomembranous colitis. Use with caution in renal impairment. Possible increased risk of renal toxicity in patients >50 years of age. Use with caution in history of seizure disorder (high levels, particularly in the presence of renal impairment, may increase risk of seizures). May cause positive direct Coombs’, false-positive urinary glucose test using cupric sulfate, false-positive serum or urine creatinine with Jaffé reaction. Some penicillin derivatives may accelerate the degradation of aminoglycosides in vitro, leading to a potential underestimation of aminoglycoside serum concentration. May cause possible emergence and overgrowth of nonsusceptible organisms, especially Enterobacter, Pseudomonas, Enterococci, or Candida. Use with caution in history of GI disease, particularly colitis. Prolonged PT reported with some cephalosporins. Use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria. Caution in overt or known subclinical diabetes mellitus or in carbohydrate intolerance (may contain dextrose). Commercial form contains sodium.

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