Mechanisms of action, some uses
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| penicillins | β-lactam
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| cephlosporins | β-lactam
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| Selective toxicity | Harming bacterial cells while leaving human cells alone
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| Are bacteriocidal | β-lactam
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| Vancomycin | Used to combat MRSA
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| Target of β-lactam drugs | Transpepidase enzyme
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| Penicillin V | Orally active penicillin
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| Penicillin G | Orally inactive penicillin
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| β-lactam | Resemble natural substrate for transpepidase enzyme (non-competitive inhibitor)
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| Augmentin | Includes a β-lactamase inhibitor
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| Methicillin | β-lactamase resistant
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| Amoxicillin | Broad-spectrum penicillin
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| Carbenicillin | Extended-spectrum penicillin
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| Vancomycin | Looks like substrate that binds to peptide chains and stops elongation of strand
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| Vancomycin | Minimal resistance due to very specific interaction with D-Ala-D-Ala
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| Bacitracin | Carrier is its target
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| Sulphonamides & Trimethoprim | Inhibit folate pathway in bacteria by resembling PABA bit of folic acid
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| Dihydropteroate synthetase | Target for sulphonamides
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| Dihydrofolate reductase | Target for trimethoprim
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| Example of a sequential blockade | Use of SMX-TMP
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| Bacterial Ribosome Size | 50-30s
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| Human Ribosome Size | 60-40s
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| Aminoglycosides | Ribosomal Inhibitors
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| Sulphonamides and Trimethoprim | Anti-folates
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| Streptomycin | An aminoglycoside
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| Tetracyclines | Easily orally and topically absorbed drugs that prevent attachment of tRNA to acceptor site on mRNA
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| Aminoglycosides | Very polar drugs that bind to bacterial ribosome and change their shape
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| Chloramphenicol | Binds to 50s ribosomal subunit and prevents formation of peptide bond
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| Erythromycin | A macrolide
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| Clindamycin | A lincosamde
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| Lincosamides | Binds to 50s subunit, inhibiting peptidyl-transferase and translocation
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| All bind to 50s subunit | Reason Chloramphenicol, Erythromycin, and Clindamycin are viewed as a threesome
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| Chloraphenicol | Lipid soluable so able to easily penetrate blood brain barrier
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| Tetracyclines | Good for chlamydia and rickettsial infections
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| Tetracyclines | Shouldn't be given to children because of binding to Ca++ in bone and teeth
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| Aminoglycosides | Shouldn't be given to children because of ototoxicity
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| Chloramphenicol | Can cause serious myelosuppression
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| Clindomycin | Associated with pseudomembranous colitis due to overgrowth of C. difficile
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| Fluoroquinolones | Broad spectrum drugs that Inhibit topoisomerase (gyrase) II enzyme
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| Ciprofloxacin | A Fluoroquinolone
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