Drugs to Memorize — Antibiotics – Flashcards

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question
Name 5 mechanisms for antibiotics.
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1) inhibit cell wall synthesis 2) inhibit protein synthesis 3) inhibit folic acid synthesis 4) inhibit DNA / RNA synthesis 5) distinct mechanisms
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Name 4 categories of cell wall inhibitors.
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1) penicillins 2) cephalosporins 3) carbapenems 4) other
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Name 9 categories of protein synthesis inhibitors
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1) aminoglycosides 2) macrolides 3) tetracyclines 4) chloramphenicol 5) lincosamides 6) ketolides 7) mupirocin 8) linezolid 9) streptogramins
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Name 2 classes of folic acid synthesis inhibitors
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1) sulfonamides 2) trimethoprim
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Name 3 classes of DNA / RNA synthesis inhibitors
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1) fluoroquinolones 2) lipopeptides 3) metronidazole
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Name 3 drugs with distinct mechanisms
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1) nitazoxanide 2) tinidazole 3) rifaximin
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Name 4 sub-classes of penicillins
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1) natural penicillins 2) penicillinase-resistant penicillin 3) aminopenicillin 4) antipseudomonal penicillin
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What two sub-classes of penicillins are effective exclusively on G+ bacteria?
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natural and penicillinase-resistant penicillins
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Which is oral and which is iv -- penicillin G and penicillin v?
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penicillin G -- "gold standard" = iv penicillin v -- oral
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Name an aminopenicillin?
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ampicillin or amoxicillin
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Name an antipseudomonal penicillin?
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ticarcillin or piperacillin
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Are the penicillins bacteriocidal or bacteriostatic?
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bacteriocidal
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How do pencillins work to kill bacteria?
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bind to transpeptidase enzyme (PBP) and blocks cross-linkage of NAM and NAG in bacterial cell wall
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What is the main resistance mechanisms for penicillins?
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Beta-lactamases
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What are two possible drug interactions to keep in mind with penicillins?
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1) lowers effectiveness of birth control 2) ineffective if combined with drugs that are bacteriostatic; bacteria must be replicating for penicillins to work
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What is often prescribed along with amoxicillin?
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B-lactamase inhibitor, clavulanic acid
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What is often prescribed along with ticarcillin?
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B-lactamase inhibitor, clavulanic acid
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What is often prescribed along with piperacillin?
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B-lactamase inhibitor, tazobactam
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What is route for antipseudomonal penicillins?
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iv
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What kind of bacteria are cephalosporins used for?
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G- bacteria especially Klebsiella
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What is the best antibiotic for Klebsiella?
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cephalosporins
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Name 2 carbapenems
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imipenem and meropenem
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What is the route for carbapenems?
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iv
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Name a specific cephalosporin
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cefazolin, ceftriaxone
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Cephalosporins are bacteriocidal or bacteriostatic?
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bacteriocidal
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Carbapenems are bacteriocidal or bacteriostatic?
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bacteriocidal
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Imipenem is often given along with what other drug?
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cilastatin, which inhibits enzyme that degrades imipenem
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What kind of drug is methicillin?
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penicillinase-resistant penicillin
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What is the mechanism for vancomycin?
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cell wall inhibition
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What bacteria is vancomycin used for?
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Gram positive bacteria
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Is vancomycin bacteriostatic or bacteriocidal?
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bacteriocidal
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How specifically does vancomycin work?
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binds to D-ala-D-ala portion of cell walls, blocking cell wall polymerization and cross-linking
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What bug is the drug cycloserine used for?
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mycobacterium TB
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Is cycloserine bacteriocidal or bacteriostatic?
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bacteriocidal
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What is the drug polymixin B used for?
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Gram- bacteria except for Proteus
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Is polymixin B bacteriocidal or bacteriostatic?
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bacteriocidal
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How specifically does polymixin B work?
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detergent that disrupts lipoproteins in bacterial cell walls, increasing membrane permeability
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Name 2 aminoglycosides
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amikacin, gentamicin
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What is mechanism for aminoglycosides?
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binds to bacterial 30s subunit; interferes with formation of complex. and causes ribosome to separate from the mRNA
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What tissue(s) is toxicity to aminoglycosides seen?
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eyes and kidneys
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What are resistance mechanisms for aminoglycosides?
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alterations in receptor proteins on ribosomes; enzymatic alteration of AGs by the bacteria
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What bacteria are aminoglycosides used to treat?
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G-
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What is route for aminoglycosides?
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IV
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Name 2 macrolides
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erythromycin, clarithromycin and azithromycin
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What is important to remember about erythromycin?
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CYP450 inhibitor and can prolong the QT interval
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What is mechanism for macrolides?
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binds to 50S subunit and prevents translocation of incoming AA from the A site to the P site
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What adverse effect(s) are associated with erythromycin?
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GI distress and therefore should be taken with food; CYP inhibition
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What is the resistance mechanism for macrolides?
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methylation of the 50S subunit or enzymatic ability to destroy the drug
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What is important to remember about tetracyclines?
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can be inhibited by chelation with milk; take on an empty stomach
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What kind of bacteria are tetracyclines used for?
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G- and G+
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Name 2 tetracyclines
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-tetracycline -doxycyclin
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Are tetracyclines bacteriocidal or bacteriostatic?
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bacteriostatic
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What is the mechanism of action for tetracyclines?
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inhibit protein synthesis through reversible binding to 30S subunit; prevents binding of new incoming AAs
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Which tetracyline is best for patients with renal dysfunction?
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doxycycline
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What is resistance mechanism for tetracyclines?
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efflux / pumped out of the cell (in G+)
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What is the drug chloramphenicol used for?
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anaerobic bacteria
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Is chloramphenicol bacteriocidal or bacteriostatic?
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bacteriostatic
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What is complication is patients with hepatic disease on chloramphenicol?
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gray color, "gray baby"
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Clindamycin is what kind of drug?
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lincosamide
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What is mechanism of action for chloramphenicol?
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binds to 50S subunit and blocks linkage of incoming AAs; interferes with peptidyl transferase
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Name an important lincosamide
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clindamycin
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Clindamycin is used to treat what kind of bacteria?
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anaerobic
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What is the route for clindamycin?
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topical
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Is clindamycin bacteriocidal or bacteriostatic?
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bacteriostatic
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What is the mechanism of action for clindamycin?
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binds to 50S subunit and prevents translocation of the incoming AA from the A site to the P site
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What is 1 example of a ketolide?
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telithromycin
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What are ketolides / telithromycin used to treat?
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MDR streptococci
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What is mechanism of action for telithromycin?
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binds to 2 location on the 50S subunit; resistant to mutations
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What is the route for mupirocin?
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topical
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What is brand name for mupirocin?
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Bactroban
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What is mechanism of action for mupirocin?
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inhibits the tRNA that transports isoleucine
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What is mechanism of action for linezolid?
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binds to 50S subunit and prevents formation of the 70S complex
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What is the target organism of streptogramins?
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VRA and MRSA
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Name an example of a streptogramin
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quinupristin / dalfopristin (given together)
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What is the mechanism for quinupristin / dalfopristin?
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quin -- blocks late phases of protein synthesis dalf -- inhibits early phases of protein synthesis
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Name 2 drug classes of folic acid synthesis inhibitors?
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1) sulfonamides 2) trimethoprim
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Name an example of a sulfonamide?
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sulfamethoxazole -- they all begin with "sulfa"
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Are sulfonamides bacteriostatic or bacteriocidal?
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bacteriostatic
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Is trimethoprim bacteriostatic or bacteriocidal?
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bacteriostatic
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What is the mechanism of action for sulfonamides?
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interfere with the 1st step of folic acid synthesis -- compete with para-aminobenzoic acid and inhibit dihydropteroate synthetase
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What is the mechanism of action for trimethoprim?
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interfere with the 2nd step of folic acid synthesis -- inhibits dihydrofolate reductase (DHFR)
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Trimethoprim -- take with or without food?
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without -- food may inhibit absorption
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Name 2 fluoroquinolones
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ciprofloxacin, moxifloxacin (ends in -floxacin)
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Are fluoroquinolones bacteriocidal or bacteriostatic?
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bacteriocidal
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What is mechanism for fluoroquinolones?
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inhibits DNA gyrase and DNA topoisomerase and therefore prevents DNA from replicating
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Name 1 lipopeptide
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daptomycin
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Is daptomycin bacteriocidal or bacteriostatic?
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bacteriocidal
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What is the mechanism of action for lipopeptides / daptomycin?
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rapidly depolarizes the cell membrane
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What is another name for metronidazole?
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Flagyl
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What is the target of metronidazole?
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anaerobic bacteria especially in meningitis
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What is the mechanism of action for metronidazole?
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the enzyme pyruvate ferridoxin oxidoreductase generates ferredoxin which reacts with the drug and generates toxins
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What is the target for nitazoxanide?
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inhibits electron transfer reaction
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What is ADE associated with metronidazole?
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mutagenic and possibly carcinogenic
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What is mechanism of action for tinidazole?
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damages DNA and inhibits DNA synthesis
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What is the name of a drug that inhibits mRNA synthesis by binding to RNA polymerase?
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rifaximin
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Name 3 anti-mycobacterials?
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rifampin, isoniazid and ethambutol
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What is mechanism for rifampin?
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inhibits the bacterial RNA polymerase
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What is the mechanism for isoniazid?
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inhibits components of the mycobacterial cell wall
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What is the mechanism for clofazimine?
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inhibits RNA polymerase
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Why are there many drug interactions associated with rifampin?
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rifampin induces drug metabolism and binds to plasma proteins
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