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184 Cards in this Set
- Front
- Back
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Name three groups of beta-lactam antibiotics:
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1) Penicillins
2) Cephalosporins 3) Carbapenems |
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What are glycopeptides?
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The glycopeptides are a group of cell wall synthesis-inhibting antibiotics that include vancomycin.
Don't confuse glycopeptides with peptidoglycan, the polymer that forms the bacterial cell wall. |
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Name three macrolide antibiotics:
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1) Erythromycin
2) Clarithromycin 3) Azithromycin |
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Which group of antibiotics does azithromycin belong to?
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Azithromycin is a macrolide antibiotic.
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Which group of antibiotics does clarithromycin belong to?
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Clarithromycin is a macrolide antibiotic.
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Which group of antibiotics does erythromycin belong to?
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Erythromycin is a macrolide antibiotic.
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Name a commonly-used lincosamide antibiotic:
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Clindamycin
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Which group of antibiotics does clindamycin belong to?
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Clindamycin is a lincosamide antibiotic.
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What is the mechanism of action of macrolide antibiotics?
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Macrolides bind to the 50s subunit of the bacterial ribosome and inhibit bacterial protein synthesis.
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What is the mechanism of action of lincosamide antibiotics?
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Lincosamides such as clindamycin bind to the 50s subunit of the bacterial ribosome and inhibit bacterial protein synthesis.
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What is the mechanism of action of aminoglycoside antibiotics?
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The aminoglycosides, such as gentamicin, bind to the 30s subunit of the bacterial ribosome, thereby inhibiting protein synthesis.
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What's the difference between glycopeptides, peptidoglycans, and aminoglycoside?
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Glycopeptide
-group of cell wall synthesis inhibitors that includes vancomycin Peptidoglycan -polymer that comprises the bacterial cell wall Aminoglycoside -group of protein synthesis inhibitors |
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Name three aminoglycoside antibiotics:
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Gentamicin
Tobramicin Streptomycin |
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Which group of antibiotics does gentamicin belong to?
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Gentamicin is an aminoglycoside antibiotic.
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Which group of antibiotics does tobramycin belong to?
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Tobramycin is an aminoglycoside antibiotic.
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Which group of antibiotics does streptomycin belong to?
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Streptomycin is an aminoglycoside antibiotic.
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What environmental requirement is aminoglycoside efficacy dependant on? Why?
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Aminoglycosides need an aerobic environment to function because their uptake into bacterial cells occurs via an oxygen and energy-dependant process.
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Name two streptogramin antibiotics:
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Quinupristin
Dalfopristin Available in combination as quinupristin/dalfopristin. |
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What is the mechanism of action of streptogramin antibiotics?
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The streptogramins (quinupristin/dalfopristin) are protein synthesis inhibitors, binding at various points the bacterial ribosome to accomplish the feat.
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Which group of antibiotics does quinupristin/dalfopristin belong to?
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Quinupristin and dalfopristin are streptogramin antibiotics.
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Name two tetracycline antibiotics:
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Tetracycline
Doxycycline |
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What is the mechanism of action of the tetracyclines?
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The tetracyclines bind to the 30s ribosomal subunit and inhibit bacterial protein synthesis.
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Which group of antibiotics does tetracycline belong to?
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Tetracycline is a tetracycline protein synthesis inhibitor.
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Which group of antibiotics does doxycycline belong to?
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Doxycycline is a tetracycline protein synthesis inhibitor.
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What is the mechanism of action of chloramphenicol?
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Chloramphenicol binds to the 50s subunit of the bacterial ribosome and inhibits protein synthesis.
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What is the mechanism of action of linezolid?
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Linezolid binds to the 50s subunit of the bacterial ribosome, inhibiting protein synthesis
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Name 6 groups of protein synthesis-inhibting antibiotics:
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1) Aminoglycosides
-gentamicin, tobramicin, streptomycin 2) Macrolides -erythromycin, clarithromycin, azithromycin 3) Lincosamides -clindamycine 4) Tetracyclines -tetracycline, doxycycline 5) Streptogramins -quinupristin/dalfopristin 5) Chloramphenicol 6) Linezolid |
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Which 5 questions should a physician be able to answer about a specific antibiotic before prescribing it?
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1) How does this antibiotic work?
2) What are the potential toxicities and should they be monitored? 3) How is the drug metabolized? Does a dosing schedule need to be modified in patients with renal dysfunction? 4) How broad is the spectrum? 5) How much does this drug cost? |
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How are aminoglycosides cleared from the body?
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Aminoglycosides are cleared renally and can damage the kidney.
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Name two serious adverse effects of aminoglycoside therapy:
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1) Vestibulocochlear nerve (CN VIII) toxicity
-results in irreversible hearing loss and vertigo 2) Kidney toxicity -can induce renal failure, follow BUN and creatinine |
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Which group of antibiotics does amikacin belong to?
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Amikacin is an aminoglycoside antibiotic.
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What bloodwork should be monitored durining aminoglycoside therapy?
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Kidney: BUN/creatinine
Serum aminoglycoside levels should also be monitored once steady state has been achieved. |
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What is the clinical indication for quinupristin/dalfopristin?
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Infection with vancomycin-resistant enterococci, specifically E. faecium and NOT E. faecalis
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What are the adverse effects of quinupristin/dalfopristin?
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This is a nasty drug that causes hyperbilirubinemia and myalgias/arthralgias.
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What is the main clinical indication for aminoglycoside therapy?
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Treatment of the gram-negative enterics plus pseudomonas infection.
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Describe the spectrum of chloramphenicol:
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Chloramphenicol has a very wide spectrum and kills most clinically-important Gram-positives, Gram-negatives, and anaerobes.
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What rare but severe adverse effect of chloramphenicol causes this otherwise-excellent antibiotic to be used only when no other option is available?
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Chloramphenicol can cause bone marrow depression and fatal irreversible aplastic anemia.
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Which antibiotic can cause fatal aplastic anemia?
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Chloramphenicol, though this adverse effect is very rare.
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What is the principle clinical use of clindamycin?
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Clindamycin, a lincosamide antibiotic, covers anaerobic bacteria, including Bacteroides fragilis.
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Name a common adverse effect to clindamycin therapy:
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Pseudomembranous colitis.
Clindamycin is a potent antibiotic against gut flora and can clear the way for C. dificile overrun. To treat C. dificile use metronidazole or oral vancomycin. |
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What's the biggest downside to linezolid therapy?
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Linezolid is extremely expensive.
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Why is aminoglycoside therapy often combined with penicllin therapy?
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Aminoglycoside must cross the cell wall to begin working. Penicllins break down this cell wall, allowing aminoglycosides to do their job better.
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What is the principal clinical use of aminoglycosides?
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Infection with Gram-negative enterics.
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Why should bacteriostatic antibiotics not be combined with beta-lactam antibiotics?
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The activity of all beta-lactam antibiotics requires active bacterial growth and active cell wall synthesis. Therefore, bacteria in a dormant or static phase will not be killed, but those in an active log phase of growth are quickly lysed.
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What is penicillin V?
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Penicillin V is phenoxymehtylpenicillin.
This is an orally active version of penicillin. |
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What are the aminopenicillins?
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The aminopenicillins are ampicillin and amoxicillin.
They are also available in combination with with beta-lactamase inhibitors as: 1) Amoxicillin-clavulanate 2) Ampicillin-sulbactam |
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Name the beta-lactamase inhibitor that is often combined with amoxicillin.
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Clavulanate
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Name the beta-lactamase inhibitor used in conjunction with ampicillin.
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Sulbactam
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What is ampicillin meant to cover in the common antibiotic combination "amp-gent"?
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Aminopenicillins (ampicillin and amoxicillin) are some of the few drugs effective against Gram-positive enterococci.
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What is the clinical indication for the penicillinase-resistant penicillins?
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These PCNs are used against MSSA.
The natural penicillins do not cover S. aureus. The penicillinase-resistants cover MSSA. From here you're dealing with MRSA and move to vancomycin. |
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Name 4 penicillinase-resistant penicllins.
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Nafcillin
Oxacillin Cloxacillin Methicillin |
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What are the four main classes of penicillins in order from narrowest to broadest spectrum?
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1) Natural penicillins
-indicated for streptococcal infections -Penicillin G -Penicillin V 2) Penicillinase-resistant penicillins -these do not hava broader spectrum than the natural penicillins but cover organisms RESISTANT to penicillin due to the development of penicillinase -indicated for streptococcal and MSSA infections -methicillin (no longer available) -nafcillin -oxacillin -cloxacillin 3) Aminopenicillins -spectrum broadened to include E. faecalis and some Gram-negative (selective enterics, H. influenzae) -ampicillin -ampicillin-sulbactrum -amoxicillin 4) Carboxy/ureidopenicillins, also known as the anti-pseudomonal penicillins -Strep, E. faecalis, Gram-negative enterics, Pseudomonas |
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Which class of antibiotics is first line against MSSA?
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First-line treatment against MSSA include the penicillinase-resistant PCNs.
-methicillin (now discontinued) -nafcillin -oxacillin -cloxacillin/dicloxacillin |
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Which are the so-called anti-pseudomonal penicillins (PCNs)?
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The antipseudomonal penicillins are also called the carboxy/ureidopenicillins.
They include: -piperacillin-tazobactam -ticaracillin-tazobactam |
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Describe the spectrum of the natural penicillins.
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The natural penicillins have a very narrow spectrum, being used mostly for streptococcal infections.
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Describe the spectrum of the penicillinase-resistant penicillins.
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The penicillinase-resistant penicillins, like the natural penicillins, have a very narrow spectrum. They are used for to treat MSSA infections.
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Describe the spectrum of the aminopenicillins.
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The aminopenicillins have a broader spectrum than the natural penicillins. In addition to streptococci they cover some enterococci (E. faecalis only) and some gram-negatives (enterics and H. influenzae).
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Describe the spectrum of the carboxy/ureido aminopenicillins.
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These antibiotics have a very wide spectrum that includes streptococi, E. faecalis, gram-negative enterics, pseudomonas, and some anaerobic bacteria.
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Does ertapenem cover Pseudomonas?
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No.
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Does meropenem cover Pseudomonas?
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Yes!
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Does imipenem cover Pseudomonas?
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Yes!
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State the natural source for each of the following classes of beta-lactam antibiotics:
1) Penicillins 2) Cephalosporins 3) Carbapenems |
1) Penicillins
-Penicillium (fungi) 2) Cephalosporins -Acremonium, formerly Cephalosporium (fungi) 3) Carbapenems -Streptomyces (bacteria) |
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Describe the spectrum of coverage of the first generation cephalosporins.
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The first-generation cephalosporins cover mainly Gram-positives:
1) Streptococci 2) Staphylococci --> not MRSA Some Gram-negative coverage: -E. coli/Klebsiella/Proteus Note that first-gen. cephalosporins do not cover H. influenza, anaerobes, or Pseudomonas. |
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Jumping from first to second generation cephalosporin adds what coverage at the expense of what? Be specific.
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Second generation cephalosporins are less effective against streptococci and staphylococci and more effective against Gram-negatives and anaerobes.
There is variation between the specific different second-generation cephalosporins in terms of coverage. |
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Name 2 first-generation cephalosporins.
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Cefazolin (Ancef)
Cephalexin (Keflex) |
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Which two genera of Gram-positive bacteria are not covered by any cephalosporin?
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Enterococcus
Listeria |
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Name 3 second-generation cephalosporins
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Cefuroxime (actually a cephalosporin)
Cefotetan (actually a cephomycin) Cefoxitin (actually a cephomycin) |
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Which class of antibiotics do cefoxitin and cefotetan belong to?
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Strictly speaking these are cephamycin antibiotics but they are often grouped with the second-generation cephalosporin.
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Name a cephalosporin that covers Pseudomonas.
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Ceftazidime, a third-generation cephalosporin.
Cefotazime and Ceftriaxone do not cover Pseudomonas. |
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Name 3 third-generation cephalosporins.
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Ceftazidime
-covers pseudomonas Ceftriaxone -no Pseudomonas coverage Cefotaxime -no Pseudomonas coverage |
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What drugs block cell wall synthesis by inhibiting peptidoglycan cross-linking?
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Penicillin, methicillin, ampicillin, pippericillin, cephalosporings, aztreonam, imipenem
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What blocks peptidoglycan synthesis?
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Bacitracin and vancomycin
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Blocks DNA topoisomerase
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fluoroquinolones
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blocks mRNA synthesis
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rifampin
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damages bacterial DNA
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metronidazole
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1st gen cephalosporins
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cefazolin and cephalexin
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targets of 1st gen cephalosporins
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PEcK
Proteus, E Coli, Klebsiella; gram positive cocci, strep and MSSA |
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2nd gen cephalosporins
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Cefoxitin, cefaclor, cefuroxime
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Targets of 2nd gen cephalosporins
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HEN PEcKS
Hemophilus, Enterobacter, Neisseria spp Proteus, E. Coli, Klebsiella, Serratia |
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3rd gen cephalosporins
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ceftriaxone, ceftazidime, cefotaxime
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Ceftazidime targets...?
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pseudomonas
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Ceftriaxone targets...?
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meningitis and gonorrhea
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4th generation cephalosporin?
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Cefepime
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Cefepime targets...?
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Pseudomonas and gram positives
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Toxicity of Cephalosporins?
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Vit K deficiency, hypersensitivity,
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Aztreonam
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Monobactam, resists bata-lactamases; used with aminoglycosides (gentimicin).
Targets gram negative rods only |
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Imipenem
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Beta-lactamase resistant carbapenem;
Given with cilastatin to inhibit renal dehydropeptidase I (inactivates drug) |
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Uses of imipenem
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Gram positive cocci
gram negative rods |
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Vancomycin mechanism of action
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inhibits cell wall peptidoglycan formation;
binds D-ala D-ala of cell wall precursors= bactericidal gram positives only |
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Vancomycin toxicity?
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Nephrotoxicity
Ototoxicity Thrombophlebitis= red man syndrome/flushing |
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Vancomycin resistance?
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If bacteria D-ala D-ala to D-ala D-lac
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30 S inhibitors
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Aminoglycosides= gentimicin, tobramycin, streptomycin
Tetracyclines= tetracycline and doxycycline |
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Demeclocycline importance?
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Demclocycline is a tetracycline and a ADH antagonist. Used as diuretic in SIADH.
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Tetracyclines toxicities?
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Discoloration of teeth, inhibition of bone growth, photosensitivity; contraindicated in pregnancy
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Macrolide toxicity
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MACRO
Motility issues, Arrhythmias (long QT), acute Cholestatic hepatitis, Rash and eOsinophilia. |
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Clindamycin is used for ?
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anaerobic infections (bacteriodes fragilis and C. perfringens)
Class is lincosamine |
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What are the Sulfonamides?
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Sulfamethoxazole (SMX), Sulfisoxazole and sulfadiazine
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How do sulfa drugs work?
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Bacteriostatic.
PABA antimetabolites inhibit dihydropteroate synthase |
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Use of sulfa drugs?
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Gram pos, Gram Negative, nocardia and chlamydia
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Trimethoprim or TMP
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inhibits bacterial dihydrofolate reductase
bone marrow suppression |
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Fluoroquinolones
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Ciprofloxacin, Norfloxacin, Levofloxacin, Ofloxacin
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Mechanism of Fluoroquinolones
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Inhibits DNA topoisomerase II
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Targets of Fluoroquinolones
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Gram negative rods, including pseudomonas
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Fluoroquinolone toxicity
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Tendon rupture, contraindicated in pregnancy, long QT
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Metronidazole
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Damages bacterial DNA
GET GAP Giardia, Entamoeba, Trichomonas, Gardnerella, Anaerobes and h. Pylori |
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Toxicity of metronidazole
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Disulfiram-like reaction with alcohol
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Tuberculosis treatment
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RIPE
Rifampin Isoniazid Pyrazinamide Ethambutol |
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Isoniazid
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Decreases synthesis of mycolic acids
Injury to neurons and hepatocctes. Give B6 (pyridoxine) to prevent neurotoxicity. |
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Rifampin
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Inhibits DNA dependent RNA polymerase.
4 R's RNA polymerase inhibitor REvs up microsomal P450 Red/orange body fluids Rapid resistance if used alone |
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Pyrazinamide
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unknown mechanism; hepatotoxic
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Ethambutol
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Decreases carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase.
Risk of optic neuropathy |
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How do you treat VRE?
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Linezolid or Streptogramins
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Antimicrobial prophylaxis of meningococcal infection
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ciprofloxacin
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prophylaxis for gonorrhea
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ceftriaxone
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prophylaxis for syphilis
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penicillin G
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prophylaxis for recurrent UTIs
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TMP-SMX
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prophylaxis for endocarditis (surgical/dental procedures)
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penicillins
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prophylaxis for pregnant woman w/ group B strep
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ampicillin
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prophylaxis for strep pharyngitis in child w/ prior rheumatic fever
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oral penicillin
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prevention of postsurgical infection due to S. aureus?
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Cefazolin (first generation cephalosporin)
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Prevention of gonococcal or chlamydial conjunctivitis in newborn?
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Erythromycin ointment
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What antifungal inhibits membrane function?
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Amphotericin B and Nystatin
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What antifungal inhibits cell wall synthesis?
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Caspofungin and Anidulfungin
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What antifungal inhibits nucleic acid synthesis?
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5-Flucystosine 5FU
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What antifungal inhibits lanosterol synthesis?
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Naftifine and terbinafine
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What antifungal inhibits ergosterol synthesis?
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Fluconazole, Itraconazole and Voriconazole
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Mechanism of Amphotericin B?
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Binds ergosterol, forms membrane pores to allow electrolyte leakage.
"Tears" hole in fungal membrane |
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Use of Amphotericin B?
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Systemic Mycoses
Cryptococcus, Blastomyces, Coccidiodes, Histoplasma, Candida and Mucor. |
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Amphotericin B toxicities?
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"Amphoterrible"
"Shake and Bake"= fever/chills Hypotension Arrhythmias because loss of K and Mg Nephrotoxicity |
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Nystatin
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Similar to Amphotericin B; topical form only.
"Swish and swallow" for oral candida (thrush) |
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Azoles
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Fluconazole, ketoconazole, Clotrimazole, miconazole
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Mechanism of Azoles?
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Inhibit fungal ergosterol synthesis = inactivates P450 enzyme that converts lanosterol to ergosterol.
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Use of Azoles?
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Local and moderate systemic mycoses.
Fluconazole for chronic cryptococcal meningitis in AIDS pts and candida. Itraconazole for blasto, coccidiodes, histoplasma Cltrimazole for topica fungal infection |
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Azole toxicity
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Inhibited testosterone synthesis (gynecomastia)
Liver dysfunction (Cyt P450 inhibited) |
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Mechanism of Flucytosine?
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Inhibits DNA and RNA biosynthsis by becoming 5FU via cytosine deaminase.
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Use of Flucytosine?
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Systemic fungal infections (cryptococcus meningitis)
used with Amphotericin B |
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Flucytosine toxicity?
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Bone marrow suppression
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Caspofungin and micafungin mechanism?
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Inhibits cell wall synthesis by inhibiting Beta-glucan synthesis.
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Clinical use of caspofungin and micafungin?
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Invasive aspergillosis and candida
get flushing and GI upset |
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Mechaism of Terbinafine?
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Inhibits fungal enzyme squalene epoxidase
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Use of terbinafine?
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Treat dermatophytoses (onychomycosis is fungal infection of finger/toe nails),
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Terbinafine toxicity?
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abnormal LFTs, visual disturbances
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Mechanism of Griseofulvin?
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Interferes with microtubule function; disrupts mitosis; deposits in keratine-containing tissues (nails)
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Use of Grseofulvin?
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teratogenic, carcinogenic, confusion, headaches; increased P450 and warfarin metabolism
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Antiprotozoan therapy
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pyrimethamine, suramin and melarsoprol
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Chloroquine Mechanism?
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Blocks detoxification of heme into hemozoin. Heme accumulates and is toxic to plasmodia
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Chloroquine clinical uses?
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Treatment of plasmodial species other than P. falciparum. Resistance seen when membrane pump decreases intracellular concentration of drug.
Treat P. Falciparum with atovaquone/proguanil. Toxicity is retinopathy |
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Antihelminthic therapy
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Mebendazole, pyrantel pamoat, ivermectin, praziquantel to immobilize helminths.
Praziquantel for flukes like schistosoma. |
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Antiviral therapy
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Yup
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What antiviral prevents viral adsorption into cell?
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Gama globulins
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What antiviral blocks nucleic acid synthesis of virus in cell?
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Purine and pyrimidine analogs.
Reverse transcriptase inhibitors |
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What antiviral blocks late protein synthesis and processing?
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Protease inhibitors
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What antiviral blocks viral packaging and assembly?
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Rifampin
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What antiviral blocks viral release from the cell?
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Neuraminidase inhibitors
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Zanamivir and oseltamivir?
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Inhibit influenza neuraminidase, decreases release of progeny virus
treats/prevents influenza A and B |
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Ribavirin
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Inhibits synthesis of guanine nucleotides by inhibting IMP dehydrogenase
RSV and Chronic Hep C |
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Ribavirin toxicity?
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Hemolytic Anemia and teratogen
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Acyclovir mechanism?
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Monophosphorylated by HSV/VZV thymidine kinase;
Acts as guanosine analog. Triphosphate formed by cellular enzymes; inhibits viral DNA polymerase by chain termination |
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Clinical use of Acyclovir?
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HSV and VZV; no effect on latent HSV/VZV
weak activity against EBV; no effect on CMV Valacyclovir has better oral bioavailability |
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Resistance to acyclovir?
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mutated viral thymidine kinase
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Ganciclovir mechanism?
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5'-monophosphate formed by CMV viral kinase; guanosine analog;
inhibits viral DNA polymerase |
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Ganciclovir use?
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CMV in immunocompromised pts.
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Ganciclovir toxicity?
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Leukopenia, neutropenia, thrombocytopenia and renal toxicity. More toxic than acyclovir
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Ganciclovir resistance?
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CMV DNA polymerase mutation or lack of viral kinase.
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Foscarnet
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Viral DNA polymerase inhibitor. Binds pyrophosphate-binding site of enzyme; doesn't need viral kinase to activate.
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Use of foscarnet?
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CMV retinitis in immunocompromised.
Acyclovir-resistant HSV |
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Foscarnet toxicity?
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nephrotoxic
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Cidofovir
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Inhibits Viral DNA polymerase, doesn't need viral kinase phosphorylation.
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Use of Cidofovir
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CMV retinitis and acyclovir resistant HSV
nephrotoxic |
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Antibiotics to avoid in pregnancy
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SAFe Children Take Really Good Care
Sulfonamides = kernicterus Aminoglycosides= ototoxicity Fluoroquinolones = cartilage damgage Clarithromycin = embryotoxic Tetracyclines = discolored teeth/ inhibit bone growth Ribavirin =teratogen Griseofulvin =teratogen Chloramphenicol= "gray baby" |
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Principles of HIV therapy
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Highly active antiretroviral therapy HAART; initiated when pts present with AIDS-defining illness, low CD4 count (below 500) or high viral load.
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What are three drugs of HAART?
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2 nucleoside reverse transcriptase inhibitors (NRTI's)
AND 1 non-nucleoside reverse transcriptase inhibitor NNRTI OR 1 Protease inhibitor OR 1 integrase inhibitor |
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Protease inhibitors
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"Navir tease a protease"
All end in "-navir" Lopinavir, Atazanavir, Indinavir, etc. HIV-1 protease (pol gene) cleaves polypeptide produces of HIV mRNA into functional parts. If you stop the proteases, can't make new viruses. |
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Toxicity of protease inhibitors
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hyperglycemia, lipodystrophy, nephropathy, hematuria
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NRTIs
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Tenofovir, Abacavir, Zidovudine
Have you dined with my nuclear family? (Zidovudine----nucleoside) |
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Mechanism of NRTI's
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Competitively inhibit nucleotide binding to reverse transcriptase and terminates DNA chain (lack 3'OH group).
Tenofovir is nucleotide analog, doesn't need activation. Others must be phosphorylated. Zidovudine (ZDV) is used for prophylaxis and in pregnancy. |
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NRTI toxicity
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Bone marrow suppression (treat with G-CSF and EPO).
Peripheral neuropathy, lactic acidosis, anemia (ZDV) |
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NNRTIs
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Nevirapine, Efavirenz, Delavirdine
Bind to reverse transcriptase and different sites than NRTIs. No phosphorylation needed. |
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Integrase inhibitors
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Raltegravir
Inhibits HIV genome integration into host chromosome by inhibiting HIV integrase. |
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Interferons
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Glycoproteins synthesized by virus infected cells; blocks replication of RNA and DNA viruses
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Use of IFN alpha
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Chronic Hep B and Hep C and Kaposi's sarcoma
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use of IFN beta
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Multiple Sclerosis
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Use of IFN gamma
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NADPH oxidase deficiency
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IFN toxicity
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neutropenia, myopathy
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