History of Cephalosporins
Cephalosporins were first discovered in 1948 from a fungus named Cephalosporium. The first generation cephalosporin antibiotic cephalexin was launched in the market in 1964. Since then, several generations of cephalosporins have been developed with improved spectrum and effectiveness.
First Generation Cephalosporins
The first generation cephalosporins included cephalexin, cefadroxil and cephalothin. They were mainly effective against gram-positive bacteria like Staphylococcus. They had limited activity against gram-negative bacteria. Due to their narrow spectrum, first generation cephalosporins are not commonly used now.
Second Generation Cephalosporins
The second generation drugs like cefaclor, cefuroxime and cefoxitin came into the market in the 1970s. They had broader spectra and were active against both gram-positive as well as gram-negative bacteria except Pseudomonas. Second generation Cephalosporins Drugs remain an important choice for treating various bacterial infections.
Third Generation Cephalosporins
Cephalosporins like cefotaxime, ceftriaxone and ceftazidime were developed in the 1980s. They had an even wider coverage against gram-negative bacteria including Pseudomonas. Due to their excellent activity against various bacteria, third generation cephalosporins are frequently used as first-line drugs for treating serious bacterial infections.
Fourth Generation Cephalosporins
Cefepime was the first fourth generation cephalosporin introduced in the 1990s. It had the broadest spectrum of all generations, covering essentially all bacterial pathogens except methicillin-resistant Staphylococcus aureus. Other fourth generation drugs actively used include cefpirome and cefquinome.
Fifth Generation Cephalosporins
Ceftaroline launched in 2010 is currently the only available fifth generation cephalosporin. It has activity against methicillin-resistant Staphylococcus aureus (MRSA) and is used for complicated skin and skin structure infections. Research is ongoing to develop more novel fifth generation cephalosporins.
Mechanism of Action
All cephalosporins work by inhibiting the synthesis of peptidoglycan cell walls of bacteria, thereby killing them or preventing their growth. They exert their bactericidal effect by binding to penicillin binding proteins (PBPs) present in the bacterial cell membrane. PBPs are enzymes involved in the final stage of peptidoglycan synthesis during cell wall formation. By binding to various PBPs, cephalosporins interference with cell wall synthesis.
Administration and Uses
Cephalosporins are generally administered orally or via injection depending on the situation. Oral cephalosporins like cephalexin are given for mild to moderate infections. Injectable cephalosporins like ceftriaxone are popular choices for pneumonia, skin infections, urinary tract infections and other serious conditions requiring parenteral therapy. Some specific uses of different generation cephalosporins include:
- First generation - Otitis media, pharyngitis, skin infections.
- Second generation - Pneumonia, otitis media, tonsillitis.
- Third generation - Pneumonia, intra-abdominal infections, sepsis, meningitis.
- Fourth generation - Nosocomial pneumonia, complicated urinary tract infections.
- Fifth generation - Complicated skin and skin structure infections, community-acquired pneumonia.
Adverse Effects and Precautions
Common mild side effects of cephalosporins include diarrhea, nausea, vomiting and allergic reactions. More serious adverse effects are rare. Precautions include use in kidney or liver disease, history of penicillin allergy and during pregnancy and lactation. Drug interactions may occur with probenecid. As with all antibiotics, it is important to complete the full course of cephalosporin therapy as prescribed to prevent resistance. Periodic review of prescribing patterns helps optimize cephalosporin usage.
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