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102 Cards in this Set
- Front
- Back
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Natural Penicillins
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-Benzylpenicillin (Pen G)
-Phenoxymethyl penicillin (Pen VK) |
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Penicillinase Resistant (Antistaphylococcal) Penicillins
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-Methicillin
-Nafcillin -Oxacillin -Dicloxacillin |
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Aminopenicillins
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-Ampicillin
-Bacampicillin -Amoxicillin |
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Carboxypenicillins
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-Carbenicillin
-Carbenicillin indanyl sodium -Ticarcillin |
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Ureidopenicillins
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-Azlocillin
-Mezlocillin -Piperacillin |
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Natural Penicillins' Activity
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-primarily gram (+)
-gram (-) limited to N. gonorrhaea & P. multocida -Clostridium (not C. difficile) -Actinomyces -T. pallidum |
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Penicillinase Resistant (Antistaphylococcal) Penicillins' Activity
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- < activity vs. streptococci then naturals
- < activity vs. enterococci & gram (-) -NOT active vs. anaerobic bacteria -[sacrifice activity for resistance] |
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Aminopenicillins' Activity
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-retain streptococci activity
- > activity to enterococci & L. monocytogenes -improved gram (-) activity |
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Carboxypenicillins' Activity
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-resembles that of ampicillin
-enhanced gram (-) activity -minimal activity to enterococci |
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Ureidopenicillins's Activity
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-resembles that of carboxypenicillins
-increased anaerobic coverage -slightly < activity to streptococci then natural PCN and ampicillin |
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B-Lactamase Inhibitors
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-Clavulanic Acid
-Sulbactam -Tazobactam |
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B-Lactamase Inhibitors' Activity
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"suicide inhibitors" that protect other B-lactams from hydrolytic activity of B-lactamases thus are active vs. B-lactamase producing bacteria (except Richmond Skyes/Bush Class I bacteria)
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1st Generation Cephalosporins
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-Cefazolin
-Cephalexin |
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1st Generation Cephalosporins' Activity
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-very active vs. gram (+) cocci
-moderate activity vs. community acquired infections -unpredictable activity vs. enterobacteriaceae -active vs. PCN susceptible oral cavity anaerobes (except B. fragilis) |
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2nd Generation "True" Cephalosporins
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-Cefuroxime
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2nd Generation "True" Cephalosporins' Activity
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- > activity vs. staphylococci & non-enteric streptococci
-improved activity against gram (-) |
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2nd Generation Cephamycin Cephalosporins
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-Cefotetan
-Cefoxitin |
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2nd Generation Cephamycin Cephalosporins' Activity
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- < activity vs. staphylococci & streptococci
- > activity vs. selected enterobacteriaceae - most active cephalosporin vs. Bacteroides sp. - good anaerobic coverage |
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3rd Generation Anti-pseudomonal Cephalosporins
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-Ceftazidime
-Cefoperazone |
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3rd Generation Cephalosporins
(No Activity vs. P. aeruginosa) |
-Cefotaxime
-Ceftriaxone -Cefpodoxime -Cefixime -Cefditoren |
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3rd Generation Cephalosporins' Activity
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-most active vs. facultative gram (-) bacilli
-superior activity vs. S. pneumoniae, S. pyognes, & other streptococci (except Ceftazidime) -modest activity vs. S. aureus (except Ceftazidime) |
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4th Generation Cephalosporins
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-Cefepime
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4th Generation Cephalosporins' Activity
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-similar gram (-) activity as Ceftazidime
-enhanced activity vs. SPICE -enhanced gram (+) activity compared to Ceftazidime: Streptococci & MSSA |
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5th Generation Cephalosporins
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-Ceftibiprole
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5th Generation Cephalosporins' Activity
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-similar gram (-) activity as Ceftazidime & Cefepime
-enhanced gram (+) activity compared to Cefepime: MRSA |
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Organisms Cephalosporins Lack Activity Against
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-Enterococcus sp.
-MRSA (except 5th generation) -PCN resistant S. pneumoniae -Listeria monocytogenes -Stenotrophomonas maltophilia -Atypical organisms |
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Carbapenems
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-Thienomycin
-Imipenem -Meropenem -Ertapenem |
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Cilastatin
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drug that blocks the metabolism of Imipenem by inhibiting kidney dipeptidase
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Carbapenem's Activity
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-gram (-), gram (+), anaerobes
-Ertapenem has NO activity against gram (-) aerobes P. aeruginosa & Acinetobacter sp. -NOT susceptible to plasmid mediated B-lactamase -strong inducers that do not alter activity |
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Organisms Carbapenem Lack Activity Against
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-MRSA
-E. faecium -Stenotrophomonas maltophilia -Flavobacterium meningoseptium -Atypical organism |
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Monobactams
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-Aztreonam
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Monobactams' Activity
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-limited to gram (-) aerobic bacteria
-similar activity as 3rd Generation Cephalosporins -poor activity vs. gram (+) & anaerobes |
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Polypeptide Antibiotics
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-Vancomycin
-Teicoplanin |
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Cyclopeptide Antibiotics
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-Bacitracin A: gram (+)
-Colistin A: gram (-) -Polymyxin B: gram (-) -Daptomycin: gram (+) |
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Polypeptides' Activity
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-gram (+)
-NO gram (-) activity -bactericidal vs. staph & strep sp. including those resistant to B-lactams -bacteriostatic vs. enterococci |
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B-Lactam Resistant Pathogens
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-MRSA
-MRSE -PRSP -Ampicillin resistant enterococcus |
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Aminoglycosides Naturally Occuring via Streptomyces sp.
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-Streptomycin
-Spectinomycin -Neomycin -Kanamycin -Tobramycin -Paromomycin |
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Aminoglycosides Naturally Occuring via Micromonospora sp.
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-Gentamicin
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Semi-Synthetic Aminoglycosides
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-Amikacin
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Aminoglycosides' Activity
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-serious gram (-) infections (used in combo with B-lactam)
-synergy vs. gram (+) infections such as staphylococi, enterococci, & viridans streptococci -Mycobacterium tuberculosis (1st line: Streptomycin; 2nd line: Amikacin, Kanamycin) |
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Tetracyclines
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-Tetracycline
-Minocycline -Doxycycline |
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Glycylcycline Tetracyclines
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-Tigecycline
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Tetracyclines' Activity
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-broad spectrum
-bacteriostatic |
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Macrolides
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-Erythromycin
-Clarithromycin -Dirithromycin -Roxithromycin -Azithromycin |
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Ketolide Macrolides
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-Telithromycin
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Atypical Organisms
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-Mycoplasma pneumoniae
-Legionella pneumophila -Chlamydia pneumoniae |
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Gram (+) Pathogens
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-Staphylococcus aureus: MSSA & MRSA
-Enterococcus: VSE & VRE -Streptococcus pneumoniae: PCN-S & PCN-R -Group A Streptococus -S. pyogenes |
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Gram (-) Pathogens
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-Haemophilus influenzae
-Atypical respiratory organisms |
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Antibiotics that Bind 30S Subunit
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-Aminoglycosides
-Tetracyclines -Glycylcycline Tetracyclines (-Polypeptide Antibiotics) |
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Antibiotics that Bind 50S Subunit
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-Macrolides
-Ketolide Macrolides -Lincosamides -Streptogramins -Oxazolidinones -Chloramphenicols |
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Causes of Community Acquired Lower Respiratory Tract Infections
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-S. pneumoniae
-H. influenzai -Atypicals |
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Causes of Community Acquired Upper Respiratory Tract Infections
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-Group A Streptococcus
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Types of Resistant gram (+)
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-MRSA
-PCN-R S. pneumoniae -VRE |
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Types of Sexually Transmitted Diseases
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-Neisseria gonorrhea
-Chlamydia trachomatis |
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Types of Peptic Ulcer Diseases
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-Helicobacter pylori
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Treatment of Community Acquired Repiratory Tract Infections
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-Macrolides
-Ketolides -Tetracyclines |
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Treatment of Resistant Gram (+)
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-Oxazolidinones
-Streptogramins -Glycylcylines Tetracyclines -Chloramphenicol |
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Treatment of Sexually Transmitted Diseases
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-Macrolides
-Tetracyclines |
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Treatment of Peptic Ulcer Disease
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-Macrolides
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Lincosamides
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-Lincomycin
-Clindamycin |
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Streptogramins
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-Quinupristin/Dalfopristin (Synercide)
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Oxazolidinones
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-Linezolid
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Chloramphenicols
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-Chloramphenicol
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Therapeutic Uses of Tetracyclines
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-CAP
-URI -STDs (-bacteriostatic) |
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Therapeutic Uses of Macrolides
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-CAP
-URI -STDs -PUD (-bacteriostatic) |
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Therapeutic Uses of Ketolide Macrolides
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-URI
-CAP: mild to moderate severity only -PCN-R S. pneumoniae (-bacteriostatic) |
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Therapeutic Uses of Lincosamides
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-anaerobes (NOT C. difficile b/c actually causes it)
-MSSA (-bacteriostatic) |
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Therapeutic Uses of Oxazolidinones
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-MRSA
-PCN-R S. pneumoniae -VRE (-bacteriostatic) |
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Therapeutic Uses of Chlorampheicols
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-MRSA
-PCN-R S. pneumoniae -VRE |
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Therapeutic Uses of Streptogramins
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-MRSA: bacteriocidal
-VRE (E. faecium only): bacteriostatic |
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Therapeutic Uses of Glycylcycline Tetracyclines
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-complicated skin infections & skin structure infections (cSSSIs)
-complicated intra-abdominal infections -gram (+) including MRSA -gram (-) -anaerobes -NO activity vs. Pseudomonas (-bacteriostatic) |
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Treatment of MRSA
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-DOC: Vancomycin
-Alternatives: 1.Linezolid 2. Streptogramins 3. Glycylcyline Tetracyclines -Maybe susceptible: Tetracyclines |
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Treatment of VRE
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-DOC: Linezolid
-Alternatives: Streptogramins (E. faecium only) -Maybe susceptible: Tetracyclines |
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Treatment of PCN-R S. pneumoniae
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-DOC: Flouroquinolones, Vancomycin
-Alternatives: Ketolide Macrolides, Linezolid, Streptogramins |
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Macrolide Resistance
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-Efflux pump
-Methylase production -Esterases |
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Macrolide Resistance due to Efflux Pumps
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-mrsA gene in staphylococci
-mefA gene in Group A streptocci -mefE gene in Streptococcus pneumoniae (NOT with Telithromycin) |
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Macrolide Resistance due to Methylase Production
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-inducible (NOT Telithromycin) or constitutive
-genes: ermA, ermB, ermC |
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MLSb Resistance
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resistance due to methylase production that acts against Macrolides, Lincosamides, & Type B Streptogramins
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Tetracyclines Resistance
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-plasmid or transposon mediated efflux pumps
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Chloramphenicols Resistance
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-chloramphenicol acetyltransferase modifies binding site
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Oxazolidionones Resistance
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-mutation of ribosomal binding site
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Macrolides Alternative Effects
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-influence neutrophil cells functions
-anti-inflammatory effects -decrease production & viscosity of biofilm below MIC levels |
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Macrolide Effects on Neutrophils Functions
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-promotes neutrophil cell degranulation
-decrease neutrophil cell phagocytosis -increase neutrophil cell migration |
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MLS (Macrolides, Lincosamides, Streptogramins) MOA
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prevents transfer of the growing polypeptide chain from the "A" site to the "P" site
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Ketolide Macrolides MOA
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blocks protein synthesis by binding to domain II and V of the 23S rRNA of teh 50S subunit
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Tetracyclines MOA
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reduces the affinity of tRNA for the mRNA ribosome complex
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Chloramphenicols MOA
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prevents binding of the amino acid containing tRNA to the "A" transferase site
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Oxazolidinones MOA
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binds to a site on the 50S ribosomal subunit near its interface with the 30S unit prevents the formation of a 70S initiation complex
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Glycylcycline Tetracyclines MOA
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binds to 30S subunit & blocks entry of tRNA into the A site of the ribosome
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Aminoglycosides MOA
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irreversibly binds to the 30S ribsome subunit (bacteriacidal):
-blocks initiation of protein synthesis -blocks further translation and elicits premature termination -incorporation of incorrect amino acids |
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Aminoglycosides Resistance
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-decreased AG uptake and accumulation
-ribosomal target modification to decrease affinity for the 30S subunit (esp. with Streptomycin) -AG modifying enzymes (gentamicin = tobramycin >amikacin) |
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Decreased Aminoglycoside Uptake & Accumulation Resistance
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-instrinsic to species or acquired by chromosomal mutation
-due to membrane impermeability (P. aeruginosa & other non-fermenting gram (-) bacilli) -efflux pumps |
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Aminoglycoside Modifyng Enzymes
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-AG acetyltransferases (aac)
-AG nucleotidyltransferases (ant) -AG phosphotransferases (aph) |
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Vancomycin MOA
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inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of peptidoglycan pentapeptides preventing elongation and cross-linking
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Vancomycin Resistance
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-modifaction of D-Ala-D-Ala terminal D-Ala-D-Lactate terminal
-3 phenotypes: vanA, vanB, vanC |
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B-Lactams MOA
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-analog of D-Ala-D-Ala N-terminal and thus inhibits bacterial cell wall synthesis by binding to PBP, inducing a bacterial autolytic effect (bactericidal)
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B-Lactams Resistance
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-inactivation by B-lactamases
-altered permeability to PCN (gram (-) only) -active efflux -altered PBP |
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SPICE
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-Serratia sp.
-P. aeruginosa -Indole + Proteus sp. -Citrobacter (-Bush 1 enzymes) -Enterobacter sp. |
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High Potential for Induction of B-lactamases
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Cefoxitin
Imipenem |
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ESBLs
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-K. pneumoniae
-E. coli (-Bush 2be enzymes) (-plasma mediated) |
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Treatment Options for SPICE
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-Cefepime
-Carbapenems |
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Treatment Options for ESBLs
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-Carbapenems
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