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WEEK 18:
Pharmacology of antibiotics:
| Question | Answer |
|---|---|
| gram positive | highly charged and has a cell wall but no outer membrane. Made of peptidoglycan and acid polymer |
| gram negative | complex lipopolysaccharide outer membrane (more resistant to antibiotics) and thinner cell wall |
| anaerobic bacteria examples (2) | clostridium botulinum and clostridium difficile |
| classes of bacteria (4) | gram positive, gram negative, aerobic, and anaerobic |
| B-lactam antibiotics examples (4) | penicillins, cephalosporins (4 generations), carbapenams, and monobactams |
| bacterial cell walls are made of | alternating amino sugar units of N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAMA) |
| how does the polymeric lattice of NAMA form | transpeptidase cross links short peptide side chains of NAMA |
| structure of NAMA | polymeric lattice |
| examples of penicillins | amoxicillin, benzylpenicillin (penicillin G), flucolaxacillin, phenoxymethylpenicillin (penicillin V) |
| penicillin is a type of what | B-lactam antibiotic |
| how does penicillin work | target bacterial cell wall synthesis by binding irreversibly to transpeptidase |
| what does transpeptidase do | cross link peptidoglycans in bacterial cell wall |
| what is penicillin effective against | only dividing organisms |
| penicillins are bactericidal meaning | they cause lysis of bacteria |
| penicillin allergy | |
| resistance to penicillins by B-lactamases | |
| some penicillins are inactivated by | B-lactamases secreted by resistant bacteria |
| how do you inhibit B-lactamases | |
| cephalosporins | |
| glycopeptides inhibit what | peptidoglycan biosynthesis |
| how do glycopeptides inhibit peptidoglycan biosynthesis | bind to D-Ala-D-Ala at terminal end of growing peptide chain during cell wall synthesis leading to the inhibition of transpeptidase which further prevents elongation and cross linking (transpeptidation) |
| examples of glycopeptides | |
| vancomycin | |
| side effects of glycopeptides | |
| fosfomycin | |
| bacitracin (polyfax) | |
| examples of drugs against mycobacteria | |
| tetracycline mechanism of action | |
| macrolides | |
| aminoglycosides | |
| examples of macrolides | |
| examples of aminoglycosides | |
| half life of aminoglycosides | 2-3 hours |
| side effects of aminoglycosides | |
| describe therapeutic range of aminoglycosides | |
| what do tetracyclines, macrolides, and aminoglycosides do | |
| what do quinolones, sulphonamides, and trimethoprim do | |
| quinolones function | |
| examples of quinolones | |
| quinolones inhibit | P450 enzymes |
| metronidazole | prodrug (inactive) needed to be activated to do antibacterial/ antiprotozoal function |
| how does metronidazole work/ how is it activated | |
| clinical use of metronidazole | used against anaerobic bacteria + protozoa, for surgical prophylaxis (high risk procedures), and alcohol interaction |
| sulfonamides | bacteriostatic, analoguges of p-aminobenzoid acid (PABA) |
| sulfonamides function*** | inhibit growth of bacteria by competitively inhibiting enzyme dihydropteroate synthetase used in synthesis of folate from PABA |
| examples of sulfonamides | sulfasalazine (sulfapyridine-aminosalicylate) |
| side effects of sulfonamides (4) | skin rash, nausea, headache, and very rarely Stevens-Johnson syndrome |
| what is used to treat infected burns from sulfonamides | silver sulfadiazine |
| trimethoprim | |
| how does trimethoprim work | |
| clinical use of trimethoprim | treat simple UTIs eg cystitis |
| when should trimethoprim NOT be taken | first 3 months of pregnancy |
| trimethoprim side effects are | limited |
| resistance in trimethoprim | high degree of resistance |
| co-trimoxazole is made of | trimethoprim + sulfamethoxazole |
| clinical use of co-trimoxazole | limited but used in treatment of pneumonia caused by yeast in immunocompromised patients |
| selection of antibiotics | |
| clinical uses of sulfonamides | IBD and rheumatoid arthiritis and sulfamethoxazole |
| resistance in sulfonamides | high degree of bacterial resistance so limited use |