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46 Cards in this Set

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Penicillin G
1st B-lactam abx, 1st gen (narrow spectrum); acid labile, penicillinase-sensitive

activity: G+, G- cocci
Penicillin V
B-lactam, 1st gen (narrow spectrum); acid STABLE (1st oral), penicillinase-sensitive

Activity: G+, G- cocci
Ampicillin
B-lactam, 2nd gen (broader spectrum); acid stable, penicillinase-sensitive

Activity: G+, G- enteric bacilli
Amoxicillin
B-lactam, 2nd gen (broader spectrum); acid stable, 2x more serum levels, penicillinase-sensitive

Activity: G+, G- enteric bacilli
Carbenicillin
B-lactam, 2nd gen (broader spectum); 1st B-lactam active against Pseudomonas aeruginosa
Ticarcillin
B-lactam, 2nd gen (broader spectrum); like carbenicillin, active against Pseudomonas aeruginosa, but 2x as active
Methicillin
B-lactam, 3rd gen (narrow-spec/pen-ase resistant); acid labile, 1st antistaph penicillin, no longer used (Staph aureus is B-lactamase +)
Oxacillin, cloxacillin, dicloxacillin, nafcillin
B-lactam, 3rd gen (narrow-spec/pen-ase resistant);
like Methicillin
Piperacillin
B-lactam, 4th gen (extended-spec/anti-pseudomonas penicillin); active against a wide variety of G- bacilli, incl. pseudomonas aeruginosa, less active against G+ cocci
B-lactam antibiotics
D-ala:D-ala analogue, bind to PBP, inhibits the transpeptidase activity, preventing cross-linking, and thereby preventing cell wall maintenance
Cephalosporins
Similar in activity to B-lactams (prevent cell wall maintenance via inhibition of transpeptidase activity); more acid stable, penicillinase resistant, cephalosporinase-sensitive; 5-15% cross-reactivity w/ penicillin
cefazolin, cephalexin
1st gen cephalosporins (resistant to S. aureus B-lactamase, but sensitive to normal cephalosporinases); most active against G+, active vs some G-, not pseudomonas aeruginosa
cefoxition, cefotetan
2nd gen cephalosporin; improved resistance to normal cephalosporinases, still resistant to B-lactamase; more effective against Bacteroides, anaerobes, G- enterics, but still not towards Pseudomonas aeruginosa
ceftriaxone, ceftazidime, cefoperazone, cefotaxime
3rd gen cephalosporin; improved B-lactamase resistance, broader G- spectrum, effective against P. aeruginosa
Cefepime (maxipime)
4th gen cephalosporin, active against those G- resistant to ceftriaxone & cefotaxime, also active against Enterobacter & Citrobacter resistant to ceftazidime; superior to ceftazidime in coverage of G+
Aztreonam
Monobactam (activity similar to B-lactam abx); activity limited to aerobic G- bacilli, resistant to most B-lactamases, minimal cross-reactivity w/ other B-lactams
Imipenem (& meropenem & ertapenem)
Carbapenem - resistant to B-lactamases (and have similar action mechanism to other B-lactamases), perhaps the broadest antimicrobial spectrum of any abx
Clavulanic acid
anti-B-lactamase drug, not an abx! Taken with other abx (amoxicillin + clavulinate = augmentin)
augmentin
amoxicillin _ clavulinate
Unasyn
ampicillin + sulbactam
Zosyn
piperacillin + tazobactam
Vancomycin (also, teichoplanin)
glycoprotein, activity restricted to G+ organisms; prevents transfer of the lipid-attached peptidoglycan precursors to the growing cell wall. The drug of choice for MRSA
Bacitracin
prevents transfer of peptidoglycan precursor across cell membrane by inhibiting the phosphatase that "resets" the carrier phospholipid. TOXIC, restricted to topical use
Cycloserine
2nd-line anti-TB medicine. a D-ala analogue, that inhibits the L-ala --> D-ala step and D-ala + D-ala -> D-ala-D-ala step in peptidoglycan synthesis
Polymyxin B
+ly charged polypeptides, damaging against G- rods; damaging against cell membrane (topical only, due to TOXIC organ effects)
Neomycin, gentamycin, amikacin,
aminoglycoside abx (which all work against the 30S subunit of bacterial ribosomes)-not effective against intracellular bacteria or anaerobes - VIII nerve damage, kidney damage
tetracycline, doxacycline, minocycline
Tetracyclines (active against 30S subunit by blocking aminoacyl-tRNA binding), bind to growing bones & teeth (discoloration of teeth), so don't give before 8 yrs of age
erythromycin
macrolide abx (active against 50S subunit of bacterial ribosome, dislodges amino-acyl-tRNA, terminates peptides) - spectrum similar to Pen G (G+, G-cocci), as well as mycoplasma & chlamydia
azithromycin & clarithromycin
macrolide (inhibits 50S subunit by dislodging aminoacyl-tRNA, terminates polypeptides), longer half life (70 hours)
telithromycin (Ketek)
ketolide abx (related to macrolide, but more active & works against macrolide-resistant species) - inhibits 50S subunit same as macrolides; active against most respiratory tract pathogens
clindamycin
spectrum of activity like macrolides, plus activity against anaerobes in general; bacteriostatic (prevents peptide transfer) - causes pseudomembranous colitis, from overgrowth of clostridium difficile
chloramphenicol
broad spectrum, bacteriostatic, mainly inhibits peptidyl transfer; can penetrate human mitochondria, causing bone-marrow depression, aplastic anemia!!!
quinupristin/dalfopristin (aka, Synercid)
synergistic combination of two streptogramin agents; blocks ribosome channel through which new proteins are extruded. Wide-spread G+ activity, active against MRSA, possibly against VRSA
Linezolid (Zyvox)
novel class of agents (oxazolidones)-highly active against G+ organisms (bacteriostatic); another VRSA agent candidate, but better tolerated than Synercid; blocks interaction of 50S subunit with fMet-tRNA
Rifampin
blocks initiation of transcription by RNA polymerase (thereby inhibiting RNA synthesis) - broad-spectrum bacteriocidal, but resistance quickly develops - a 1st line abx against TB, along w/ other abx
ciprofloxacin, norfloxacin
fluroquinolone - broad spectrum, bacteriocidal, inhibits DNA gyrase (thereby preventing DNA replication & synthesis) & topoisomerase IV; resistance rapidly develops due to point mutation in DNA gyrase A
Metronidazole
once activated (its a pro-drug), it binds to and breaks up DNA; useful against protozoa, broad spectrum of anaerobic & microaerophilic bacteria (bactericidal)
nitrofurantoin
Nitrofuran drug - binds covalently to proteins - active against G+ & G-, protozoa & fungi - mainly bacteriostatic - a pro-drug, restricted to UTIs
Mupirocin
binds reversibly & specifically to leucyl-tRNA synthetase; used topically to tx S. aureus in nares, and impetigo in children
list the anti-mycobacterium agents
isoniazid
pyrazinamide
ethionamide
ethambutol
cycloserine

all 5 work to inhibit the mycobacterium's cell wall from forming
amphotericin B & nystatin
polyene antibiotics - are important ANTIFUNGALS, not effective against bacteria - used topically, they bind ergosterols (found in fungal & plant membranes only), damaging the cell membrane
Ketoconazole
systemic antifungal agent (member of the "azole" derivatives) - blocks CYP-dependent demethylation of lanosterol (precursor to ergosterol), disturbing the fungal cell membrane properties; inhibits hyphae synthesis, enabling easy phagocytosis by PMNs and macrophages - the Azoles have higher affinity for fungal CYP than human CYP
Fluconazole & Itraconazole
triazoles, similar action to azoles (CYP inhibition), but less specific for fungal CYP, therefore more side effects
Voriconazole
azole agent, higher activity against aspergillus
Caspofungin
echinocandin (a new class of antifungal), inhibits synthesis of 1-3-beta-D-glucan, used in fungal cell wall - fungicidal for candida & active against aspergillus
Griseofulvin
FUNGISTATIC against dermatophytes; oral route, delivered to skin bound to keratin; inhibits microtubule formation, blocking mitosis & cell wall synthesis