Cephalosporins: List of Cephalosporins, Generations, Uses, Mechanism of Action, and Side Effects (With Examples) | Veterinary Updates

Cephalosporins: List of Cephalosporins, Generations, Uses, Mechanism of Action, and Side Effects (With Examples)

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Cephalosporins (discovered in 1945) are a large group of broad-spectrum bactericidal (kill bacteria) antibiotics used for killing Gram Positive and Negative Bacteria. The word Cephalosporins is derived from the “mold Acremonium” (Cephalosporium). The Scientists improved the cephalosporins structurally to make a wide range effective antibiotic against different bacterias. 

  • Class: Bacteriocidal 
  • Mechanism: Cell wall Inhibition
  • Antagonists: Gentamycin
  • Precautions: Liver Affected animals should be treated with low dose as compared to other animals.
  • Prefixes: Most cephalosporins start with cef, ceph, or kef.
Cephalosporins: List of Cephalosporins, Generations, Uses, Mechanism of Action, and Side Effects (With Examples)
Cephalosporins: List of Cephalosporins, Generations, Uses, Mechanism of Action, and Side Effects (With Examples)

What are cephalosporins used for?

Cephalosporins are highly used in treatment of

  1. Bone infections
  2. Ear infections (eg: otitis media)
  3. Skin infections
  4. Respiratory infections
  5. Urinary tract infections(UTI)

What are cephalosporins antibiotics?

Cephalosporins antibiotics are highly effective drugs specially used in treatment of respiratory, skin, UTI Infections, soft tissues Infections, bones infections and most of the bacteria including diseases that may have beta lactamase producing strains. It is poorly absorbed from GIT (Gastro Intestinal Tract).

Mechanism of Actions: 

The working way of Cephalosporins is similar to penicillins. They kill bacteria in such a way that they bind to penicillin-binding proteins of peptidoglycan called beta-lactamase Protein and promote cell wall inhibition. They stop bacteria from building strong cell walls. Which results in breaking down of the bacterial cell wall from internal pressure which results in bacterial die.

Generations of Cephalosporins

        Cephalosporins are divided into five generations based on their origin and bacteria they target. Their route of administrations includes Oral, Intravenous, intramuscular and subcutaneously.

1st Generation of Cephalosporins

First Generation Cephalosporins are more highly active antibiotics against Gram Positive Bacteria like Cocci, Proteus, E.Coli, Klebsiella than other generations. While third generation cephalosporins are good responsive against Gram Negative Bacteria (Bacilli)

     Like penicillins, first generation cephalosporins are beta-lactam antibiotics. They are bactericidal means they actively kill bacteria instead of stopping their growth.

How does it work?

They bind and inhibit specialized enzymes called beta lactamase (penicillin-binding proteins) which are essential for bacteria to build their peptidoglycan cell walls. Without a stable and complete cell wall, the internal pressure of the bacterial cell is high as that of external pressure which causes it to rupture and die.

Beta-Lactamase Resistance: 

These are structurally modified enzymes or proteins which are found to be more resistant to certain defensive enzymes like penicillinases, that bacteria use in  destruction of standard penicillins.

List of 1st Generation Cephalosporins:

  1. Cefapirin 
  2. Cefadroxil
  3. Cephalothin (e.g Keflin inj)
  4. Cephalexin (e.g: Ceporex Injection)
  5. Cephradine (e.g: Velosef Tablets)
  6. Cefazolin (Used for skin, surgical, blood and soft tissues infections)

2nd Generation of Cephalosporins

Antibiotics of this generation are broad spectrum antibiotics and highly performive to Gram Positive and Gram Negative Bacterias. They are also used for the treatment of some anaerobes. 

Classification:

  • Cefuroxime
  • Cefprozil (Used for sinus, ear, and lung infections)

3rd Generation of Cephalosporins

These are Broad spectrum antibiotics used for resistant gram-negative bacteria. These antibiotics are reported as very highly active to bacteria infections like Mastitis, Metritis etc. 

Classification:

  • Ceftriaxone (e.g: Zeftrox, Oxidil Inj etc)
  • Ceftiofur Hydrochloride (e.g: Cefur RTU): It can cause minor allergic reactions and rare bleeding disorders being reported from Cephalosporins.
  • Cefotaxime Sodium (e.g: Excef, Ceforin etc): It is antagonists of Gentamicin. Allergy, vomiting and diarrhea may occur in some animals. 
  • Cefixime (e.g: Cefim Syrup): Used for severe infections like meningitis and gonorrhea)

4th Generation of Cephalosporins

These are wide spectrum antibiotics used against tough gram-negative bacteria, including Pseudomonas. 

Classification:

  • Cefepime
  • Cefquinome (e.g: Cefanil, Cefanome inj)

5th Generation of Cephalosporins

Fifth generation antibiotics are very effective against resistant strains like MRSA. 

Classification:

  • Ceftaroline. 

Common Uses of Cephalosporins

 Fifth generation antibiotics are very effective against infections like skin infections, urinary tract infections (UTIs), pneumonia, otitis media infections (ear infections), and strep throat.

Side Effects & Precautions

Generally first-generation cephalosporins carry certain risks

  1. Gastrointestinal Upset: The complaints that have been reported for Cephalosporins include nausea, vomiting, stomach pain, and mild diarrhea.
  2. Penicillin Cross-Allergy: If you have a known allergy to penicillin, there is a 3% to 8% chance you might also react to a first-generation cephalosporin because they share a similar chemical “ring” structure.

Mild diarrhea, nausea, and pain at the injection site. They are not as highly allergic as that of penicillins. If a patient is reactive to penicillins then you can use cephalosporins as antibiotics. It will be the right choice to choose instead of penicillins during an allergic condition. similar chemical structure with penicillin. But people with severe penicillin allergies may also react to cephalosporins.