Five generations of cephalosporins

Five generations of cephalosporins

By wamin Time: 2021-3-8

Cephalosporins, currently the most widely used β-lactamide antibiotics clinically, are semi-synthetic antibiotics synthesized by connecting different side chains with 7-aminocephalic acid (7-ACA).
There are more than sixty kinds of cephalosporins listed on the market, which are divided into five generations according to the differences of antibacterial spectrum, antibacterial activity, stability to β-lactamase and renal toxicity.

Five generations of cephalosporins

First-generation of cephalosporins

  • Representative Drugs: cephalosporins,cefazolin, cefalotin.
  • First-generation of cephalosporins mainly has a relatively good antibacterial effect against gram-positive bacteria, and also has certain antibacterial activity against gram-negative bacteria.
  • First-generation of cephalosporins are mainly used for upper respiratory tract infections, skin infection, and soft tissue infections clinically.
  • First-generation cephalosporins are not stable to β-lactamase and have certain renal toxicity.

Second-generation of cephalosporins

  • Representative Drugs:Cefuroxime, cefaclor.
  • Second-generation cephalosporins have more wide antibacterial spectrum based than the first-generation.
  • The activity against gram-positive bacteria is similar as the previous, while activity against gram-positive bacteria are better.
  • Second-generation of cephalosporins can be used for respiratory tract, skin and soft tissue, and urogenital infections.
  • Second-generation cephalosporins are slightly more stable to β-lactamase. The side effects on renal function are relatively small, but they still have certain renal toxicity.

Third-generation of cephalosporins

  • Representative Drugs: ceftriaxone, ceftazidime, cefoperazone, etc.
  • The third-generation cephalosporins are broad-spectrum antibiotics, with relatively good antibacterial activity against a variety of gram-positive bacteria, especially for gram-negative bacteria.
  • The third-generation of cephalosporins are widely used clinically for moderate and severe infections, the injection formulation such as ceftriaxone sodium for injection has big demand in many hospitals.
  • The third-generation of cephalosporins have very few kidney toxicity.

Fourth-generation of cephalosporins

  • Representative drugs: cefuroxime,cefoselis,cefquinone
  • Fourth-generation cephalosporins have not only antibacterial activities as the third-generation,but also have activity against staphylococci.
  • It can be used to treat bacterial infections resistant to third-generation cephalosporins.
  • The fourth-generation are highly stable to β-lactamase. Fourth-generation of cephalosporins have low kidney toxicity.

Fifth-generation of cephalosporins

  • Representative drug:ceflorine and Ceftobiprole
  • Fifth-generation of cephalosporins have certain activity on meticillin-resistant Staphylococcus aureus, Ceftobiprole is the first cephalosporin works against MRSA and vancomycin-resistant Staphylococcus aureus (VRSA).
  • Kidney toxicity are similar as the fourth-generation.

Each generation of cephalosporins has unique characteristics, different patients have different conditions, so cephalosporins must be used under the guidance of a doctor or pharmacist.