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36 Cards in this Set
- Front
- Back
- 3rd side (hint)
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Penicillin
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Binds to PBP (transpeptidase), to inhibit PG cross linking; activates autolysins
Note that all cell wall synthesis inhibitors are CIDAL. |
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Clavulinic (clavunate,tazobactam)
Bonus: used with what? |
Beta-lactamase inhibitor, used in combo with penicillin
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Amoxicillin/clavunate, piperacillin/tazobactam
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Cephalosporins
Name the 4 generations. |
Inhibits PG cross-linking; induces autolysis
1st generation: used for non-life threatening, surgical prophylaxis. G+ and G- 2nd generation: effective against more G- 3rd generation: broad spectrum against many G-, anaerobes, G+s,good penetration of CNS. 4th generation: broadest spectrum; increased stability to beta-lactamases. |
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Carbapenims (imipenem)
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as other beta-lactams; resistant to most beta-lactamases
Broad spectrum against most G- and G+ |
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Monobactam (Aztreonam)
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Similar to other beta-lacatms, resistant to other beta-lactamases
Only active against G-, NOT against G+ or anaerobes. |
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Vancomycin
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Binds D-Ala-D-Ala and inhibits PG transglycosylation
Only good against G+; effective aainst MRSA (although there is now VRSA) CIDAL to actively growing bacteria, more concentration dependency |
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Teicoplanin
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Binds D-Ala-D-Ala and inhibits PG transglycosylation
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Bacitracin
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Inhibits dephosphorylation of bactoprenol phosphate, blocks transfer of PG monomers across cell membrane
G+ only Used only topicaly, as it is toxic to eukaryotic cells. |
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Cycloserine
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Blocks L-Ala -> D-Ala conversion (outcompetes D-Ala for binding to enzymes driving reaction)
Mycobacterium tuberculosis |
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Isoniazid (INH)
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Inhibits mycolic acid synthesis, a cell wall component unique to Mycobacteria species
Mycobacterium tuberculosis |
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Ethambutol (EMB)
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Inhibits arabinogalactan synthesis
Mycobacterium tuberculosis |
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Ethionamide
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Inhibits mycolic acid synthesis
Mycobacterium tuberculosis |
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Polymyxins (polymyxin B, polymyxin E)
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Binds LPS; acts as detergent by inserting into membrane and distrupting integrity, causing increased cell permeability
G- only. Used only topicall due to neprotoxicity. CIDAL. |
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Daptomycin
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incorporates into membrane in a calcium-dependent manner via lipid tail; leads to depolarization of membrane
G+ only. Can be used against MRA, MSSA, vancomycin-sensitive E. faecalis. Not yet approved for vancomycin-resistant E. faecium. (but it IS EFFECTIVE!) CIDAL. |
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Aminoglycosides (streptomycin, gentamicin, amikacin)
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Bind 30S ribosomal subunit irreversibly -> leads to misreading of mRNA and premature release of ribosome from mRNA
Broad against aerobes, usually against facultative G- rods (Vibrio, Campylobacter) in combo with penicillin. Requires O2 dependent transport, so INEFFECTIVE AGAINST ANAEROBES. CIDAL. |
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Tetracyclins (tetracycline, doxycycline, tigecycline)
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Binds 30S subunit, prevents stable binding of tRNA, blocks peptide elongation
Useful with G-, G+, intracellular bacteria STATIC. |
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Chloramphenicol
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Binds 50S subunit, inhibits peptide bond formation
May have decreased ability to enter G- cells, due to mutations in porins. STATIC |
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Macrolides
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Binds 50S subunit, blocks peptide elongation by blocking translocation and/or transpeptidation
Primarily for G+, also as an alternative for penicillin-allergic patients. STATIC. |
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Lincosamides (Clindamycin)
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Binds 50S subunit, blocks peptide bond formation
Only good for G+ anaerobes, no activity against G-. STATIC. |
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Oxazolidinones (Linezolid)
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Binds 50S subunit, inhibits initiation step in protein synthesis
Effective against Vancomycin-resistant Enterococcus, MRSA STATIC. |
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Streptogramins (dalfopristin + quinupristin = Synercid)
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Binds 50S subunit, blocks protein synthesis at two steps in elongation
(A-> tRNA binding; B -> peptide transfer) A or B alone: STATIC. A+B: CIDAL. |
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Mupirosin
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Binds isoleucyl-tRNA synthase enzyme, blocks formation of Ile-tRNA; leads to protein synthesis arrest at codons for Ile
Good for S. Aureus, including MRSA. used for impetigo and folliculitis only (toxic) CIDAL. |
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Quinolones, Fluroquinolones (ciprofloxacin, moxifloxicin, gatifloxicin)
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Binds to DNA gyrase (in G-), topoisomerase IV (in G+) in complex with DNA, promotes DNA cleavage and interferes with supercoiling of DNA
Poor against Streptococci, staphylcocci. Used towards B. Cereus, B. Anthracis, C. Jejuni, C. Fetus. N. Gonorrhea. CIDAL. |
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Metronidazole
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Bacterial nitroreductase reduces drug's nitro group; resulting compounds damage DNA (not an inhibitor of synthesis)
Only good for anaerobic infections (Clostridium difficile). Also effective for Helicobacter pylori. No activity against aerobes or facultative anaerobes. CIDAL. |
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Rifamycins (Rifampin, Rifabutin, Rifaximin)
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Binds beta-subunit of bacterial DNA-dependent RNA polymerase, inhibits transcription initiation.
Good only against G+. Usually with prophylaxs for bacteria meningitis. CIDAL. |
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Sulfonamides (sulfioxazole, sulfamethoxazole, sulfadozine, dapsone)
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Inhibits para-aminobenzoic acid conversion to dihydropteroic acid, thus stopping purine and pyrimidine synthesis
Note TMP-SMX (with Trimethoprim) for UTI STATIC. |
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Trimethoprim
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inhibits dihydrofolate reductase, blocks folic acid synthesis; synergistic with sulfamethoxazole (combined use = TMP-SMX; for UTIs, Pneumocystis pneumonia)
TMP-SMX for UTIs) CIDAL. |
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Methenamine
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at pH <6, drug is converted to ammonia and formaldehyde; formaldehyde is bactericidal by denaturing proteins and nucleic acids; ineffective against pathogens that raise urine pH
Prophylaxi fo recurrent bladder infections. CIDAL. |
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Nitrofurantoin
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Weak acid; mechanism of action poorly understood. Requires reduction inside bacterial cell for activity. Reduced form inhibits several metabolic processes, including protein synthesis, nucleic acid synthesis, respiration. Active against most bacteria that cause UTI
CIDAL. |
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G- only antibiotics
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Polymixin, Monobactam
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G+ only antibiotics
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Bacitracin, Clindamycin,Daptomycin, Vancomycin, Rifampin
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Broad
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Both 30S, 50S: Chloramphenicol, macrolides
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Aerobes only
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Aminoglycoside
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Drugs against VRE, MRSA
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Oxazolidinone (Linezolid), Streptogranin (Synercid), Daptomycin
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3 50S drugs that bind to same target
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Macrolides, Clindamycin, and Chloramphenicol
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Static drugs
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Tetracycline,
all 50S except Streptogramin A+B, Mupirosin, sulfonamide |
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