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Antibiotics

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2025/2026 Written for academic year
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TAMILNADU Dr.MGR MEDICAL UNIVERSITY
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1️⃣ First Generation • Drugs: Cefazolin, Cephalexin • Spectrum: Gram +++ Gram – • Uses: Skin infections, surgical prophylaxis • No BBB penetration 2️⃣ Second Generation • Drugs: Cefuroxime, Cefaclor • Spectrum: Gram + Gram – + anaerobes • Covers Bacteroides fragilis • Cefuroxime crosses BBB • Uses: Respiratory, anaerobic infections 3️⃣ Third Generation (Very Important) • Drugs: Ceftriaxone, Cefotaxime, Ceftazidime • Spectrum: Gram – Gram + • Strong against severe infections Special points: • Ceftazidime, Cefoperazone → Pseudomonas • Ceftriaxone → Typhoid, Gonorrhea, Meningitis 4️⃣ Fourth Generation • Drug: Cefepime • Broad spectrum (like 3rd gen but stronger) • Used for hospital-acquired infections 5️⃣ Fifth Generation • Drugs: Ceftaroline, Ceftobiprole • Active against MRSA • Mechanism: binds PBP-2a

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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

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April 1, 2026
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2025/2026
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  • cephalosporins
  • antibiotics
  • mechanism of action
  • uses
  • adr

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