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