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45 Cards in this Set
- Front
- Back
Affect bacterial cell wall
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1. penicillins
2. cephalosporins |
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General principles that allows penicillins and cephalosporins to work?
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- active cells constantly produce new peptidoglycan and transport to cell envelope
- PCN and cephalosporins react w/ enzymes (PBP) required to complete process - active when cell is growing - weaken cell wall --> lysis |
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PCN and cephalosporins are categorized as what kind of antibiotics?
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Bactericidal antibiotics
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What 3 parts make up penicillin and its relatives?
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1. thiazolidine ring
2. beta-lactam ring 3. R group |
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Of the 3 parts that make up PCN, which interacts with bacterial transpepsidases (PBP)?
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Beta-lactam ring
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Of the 3 parts that make up PCN, which affects biological activity?
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R- group attached to ring affects bio activity
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What is penicillinase/beta-lactamase?
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Bacteria produce enzymes to break down PCN by splitting the beta-lactam ring of PCNs
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Which antibiotics are resistance to penicillinases?
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Methicillin
Nafcillin |
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What is the primary problem in therapy w/ PCNs?
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Allergic rxn and resistance in strains of bacteria
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What are beta-lactamase inhibitors?
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- suicide inhibitors of beta-lactamase
- beta-lactams that bind to and inactive beta-lactamase enzymes - expand spectrum of beta-lactam antibiotics |
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Examples of beta-lactamase inhibitors?
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clavulanic acid
sulbactam clavulanate + amoxicillin = augmentin clavulanate + ticarcillin = timentin |
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How are cephalosporin drugs similar to PCNs?
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- similar structure
- same mechanism of action |
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Do PCNs or cephalosporins account for the majority of all antibiotics administered?
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Cephalosporins
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What are the advantages of using cephalosporins?
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- resistant to most PCNases
- cause fewer allergic rxns - administered parenterally |
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What is the 1st generation of cephalosporins?
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1st - cefazolin & cephlathin
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What is the 2nd generation of cephalosporins?
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2nd - cefaclor & cefonacid
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What is the 3d generation of cephalosporins?
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3rd - cephalexin & cefotaxime
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What is the 4th generation of cephalosporins?
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4th - cefpirone & cefepime
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What other drugs target cell walls?
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cavitracin
isoniazid (mycobacterium tuberculosis) canvomycin |
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What antimicrobial drugs disrupt cell membrane fnxn?
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Polymyxin
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What is polymoxin and why is its use limited?
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antimicrobial drug that disrupts cel membrane and because of toxicity to kidneys
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What are the 3 classes of drugs that target DNA or RNA?
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1. quinolones
2. rifmycin 3. metronidazole |
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What is the mechanism of action of quinolones?
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Inhibits DNA topoisomerases (gyrases)
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How are fluoroquinolones better?
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- higher potency
- broad spectrum - inhibit wide variety of gram +/- bacterial species w/ minimal conc. |
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What class of drugs and which particular drugs are used for UTI, STDs, gastrointestinal infxns, osteomyelitis, resp. infxns, soft tissue infxns?
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Quinolones
ciprofloxacin and norfloxacin |
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What is the mechanism of action of rifamycin (rifampin)?
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Inhibits DNA dependent RNA polymerase, preventing RNA syn
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What is rifamycin MAINLY used for?
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infxn by several gram + rods and cocci and few gram - bacteria
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What others uses have rifamycin commonly had in the past?
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Tx of mycobacterial infxs such as tuberculosis and leprosy
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Of the drugs presented, which class/drug has a narrow spectrum?
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Cell membrane fnxn disrupting drugs/ polymyxin
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- What is the mechanism of action of metronidazole?
- What reduces the compound? |
- Reduced form acts as free radical that damages bacterial DNA
- some anaerobic bacteria produce nitroreductase that reduces compound |
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How do antibacterial drugs that block protein synthesis work?
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Most react w/ the ribosome-mRNA complex
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What are the 7 classes of drugs that block protein synthesis?
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1. aminoglycosides
2. tetracyclines 3. macrolides 4. chloramphenicols 5. clindamycin 6. streptogramin 7. oxazolidones |
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What are aminoglycosides used for?
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Tx serious infxns caused by many gram -'s and some gram +'s
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What are classified as aminoglycosides?
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Streptomycin
neomycin kanamycin gentamicin tobramycin amikacin spectinomycin |
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Aminoglycosides are described as being __________ (their effect on bacteria)
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bactericidal
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Tetracyclines are described as being _________ (their effect on bacteria)
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bacteriostatic
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What are classified as tetracyclins?
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1. tetracycline
2. doxycycline 3. minocycline |
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Macrolides are described as being ________ (effect of bacteria)
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bacteriostatic
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What are classified as macrolides?
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1. erythromycin
2. azithromycin 3. clarithromycin |
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What are the physiological advantages of macrolides?
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- broad spectrum
- low toxicity - used for wide variety of gram -/+'s |
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- Which drug is restricted due to its high human toxicity?
- what type of drug is it (general mechanism of action) |
- Chloramphenicol (tx typhoid fever)
- protein synthesis blocking drug |
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- Which drug has a broad spectrum, but has limited application due to its adverse affect on the GI tract?
- what type of drug is it (general mechanism of action) |
- clindamycin
- protein synthesis blocking drugs |
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Which drug is effective against Staph and Enterococus, and against resistant strains of Strep?
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Streptogramin (synercid)
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What is special about oxazolidones in terms of clinical pathogenic use?
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Used to tx 2 of the most difficult clinical pathogens - MRSA and VRE
-- not found in nature |
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What is the mechanism of action of sulfonamides and trimethoprim?
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Inhibit folic acid synthesis
- sulfa inhibits PABA to DHF - trimethoprim inhibits DHF to THF |