* Derivatives of **7-aminocephalosporanic acid** * With **2 sites** **of attachment** for various R1 and R2 groups * More stable to many bacterial β–lactamases, has broader spectrum of activity
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Giuseppe Brotzu
* Isolated Cephalosporin C compound in from the fungus **Acremonium**, previously known as "**Cephalosporium**” in 1945. * Found in the sea near a sewage outfall in Su Siccu, by Cagliari harbour in Sardinia, Italy
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R group at **7-position**
alters antibacterial activity
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R group at **3-position**
modifies pharmacokinetic profile
* whether they can traverse the blood-brain barrier or not * hydrophobic or hydrophilic * biliary or urinary
Cephalosporins are “**LAME**” because they are inactive against
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Cephalexin
### First Generation:
* effective against **pharyngitis** (above umbilicus infections) which (back then) were mostly gram-positive * cell wall will be **thicker for gram-positive** * gram-negative are resistant with beta lactams
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Cefazolin
### First Generation:
* parenteral route (IV) * longer duration of action, but similar spectrum
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Cefuroxime
### Second Generation:
* given parenterally * longer half life * it can cross blood brain barrier * used for **community-acquired bronchitis & pneumonia**
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Cefuroxime axetil
### **Second** Generation:
* twice daily * quite resistant even against to beta-lactamase-producing organism
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Ceftriaxone
### **Third** Generation:
* effective against **genital, anal and pharyngeal penicillin-resistant neisseria gonorrhoeae** * excreted through the **bile**
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Ceftazidine
### **Third** Generation:
* anti-pseudomonal coverage * **Pseudomonas** are hospital-acquired germ with numerous resistance
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Cefotaxime
### **Third** Generation:
* good choice for infections (bacterial encephalitis & bacterial meningitis)
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Cefepime
### **Fourth** Generation:
* anti-pseudomonal property
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**interstitial nephritis and tubular necrosis**
* if combined with **aminoglycoside** (protein synthesis inhibitor * cephalosporin don’t go along well w/ aminoglycoside