Classification of Cephalosporins
1st Generation
• Parenteral: Cefazolin
• Oral: Cephalexin, Cefadroxil
2nd Generation
• Parenteral: Cefuroxime, Cefoxitin
• Oral: Cefaclor, Cefuroxime axetil, Cefprozil
3rd Generation
• Parenteral: Cefotaxime, Ceftizoxime, Ceftriaxone, Ceftazidime, Cefoperazone
• Oral: Cefixime, Cefpodoxime proxetil, Cefdinir, Ceftibuten, Ceftamet pivoxil
4th Generation
• Parenteral: Cefepime, Cefpirome
5th Generation
• Parenteral: Ceftaroline fosamil, Ceftobiprole medocaril
Mechanism of Action
1. Bacteria contain NAM & NAG.
2. Peptidoglycan are linked by long strands and upsplit.
3. \beta-lactam antibiotics inhibit transpeptidase.
4. When bacteria divide, a cell wall deficit forms.
5. Bacteria becomes hyperosmotic \rightarrow Swell and burst \rightarrow Lysis of cell.
Pharmacokinetics
• Administration: Orally or parenterally.
• Excretion: Mainly unchanged through kidneys (Glomerular Filtration or tubular secretion).
• Metabolism: Some are metabolized before excretion.
• Interactions: Like penicillins, tubular secretion is blocked by Probenecid.
• Exception: Cefoperazone is excreted through bile.
Adverse Effects
• Hypersensitivity
1st Generation
• Parenteral: Cefazolin
• Oral: Cephalexin, Cefadroxil
2nd Generation
• Parenteral: Cefuroxime, Cefoxitin
• Oral: Cefaclor, Cefuroxime axetil, Cefprozil
3rd Generation
• Parenteral: Cefotaxime, Ceftizoxime, Ceftriaxone, Ceftazidime, Cefoperazone
• Oral: Cefixime, Cefpodoxime proxetil, Cefdinir, Ceftibuten, Ceftamet pivoxil
4th Generation
• Parenteral: Cefepime, Cefpirome
5th Generation
• Parenteral: Ceftaroline fosamil, Ceftobiprole medocaril
Mechanism of Action
1. Bacteria contain NAM & NAG.
2. Peptidoglycan are linked by long strands and upsplit.
3. \beta-lactam antibiotics inhibit transpeptidase.
4. When bacteria divide, a cell wall deficit forms.
5. Bacteria becomes hyperosmotic \rightarrow Swell and burst \rightarrow Lysis of cell.
Pharmacokinetics
• Administration: Orally or parenterally.
• Excretion: Mainly unchanged through kidneys (Glomerular Filtration or tubular secretion).
• Metabolism: Some are metabolized before excretion.
• Interactions: Like penicillins, tubular secretion is blocked by Probenecid.
• Exception: Cefoperazone is excreted through bile.
Adverse Effects
• Hypersensitivity
