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names: imipenem, meropenem, ertapenem, doripenem targets: gram positive cocci, GNR (CA and nosocomial) action: PBPs -- autolysins resistance: decreased permeability; rare due to trans-configuration of b-lactam ring in penems side effects:1-5% cross-allergenicity to penicillins; seizures notes: - not-susceptible: stenotrophomonas, burkholderia, enterococcus faecium, amp-resistant e. faecalis, MRSA - not-susceptible to ertapenem: enterococci, pseudomonas - IV, imipenem -- renal metabolite is nephrotoxic (tx. with cilastatin); renal OAT clearance (inhibited by probenecid)
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names: cefadrozil, cephalexin, cephradine, cefazolin targets: strep, MSSA, ca-enteric GNR action: binds to PBPs; autolysins resistance: b-lactamase; decreased permeability; altered PBPs side effects: 1-5% cross-allergenicity to penicillins; allergic delayed hypersensitivity; immediate hypersensitivity (IgE)l GI bleed due to inhibtion of post-translational carboxylation of glutamic acid in VitK clotting factors notes: all cephalosporins are inactive v. MRSA, listeria, enterococci - excreted by OAT (inhibited by probenecid)
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names: cefaclor, cefuroxime, cefoxatin targets: less v gram positive; more v. GNR; cefoxitin (h. inf, n. meningitides) action: binds to PBPs; autolysins resistance: b-lactamase; decreased permeability; altered PBPs side effects: 1-5% cross-allergenicity to penicillins; allergic delayed hypersensitivity; immediate hypersensitivity (IgE)l GI bleed due to inhibtion of post-translational carboxylation of glutamic acid in VitK clotting factors notes: all cephalosporins are inactive v. MRSA, listeria, enterococci - excreted by OAT (inhibited by probenecid)
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names: ceftriaxone, cefotaxime, ceflazidime, cefixime, cefpodoxime, loracarbef targets: more activity v. nosocomial GNRs action: binds to PBPs; autolysins resistance: b-lactamase; decreased permeability; altered PBPs side effects: 1-5% cross-allergenicity to penicillins; allergic delayed hypersensitivity; immediate hypersensitivity (IgE)l GI bleed due to inhibtion of post-translational carboxylation of glutamic acid in VitK clotting factors notes: all cephalosporins are inactive v. MRSA, listeria, enterococci - excreted by OAT (inhibited by probenecid) - ceftriaxone: high biliary levels // excreted in feces
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names: cefepime targets: broad activity against gram + and gram - action: binds to PBPs; autolysins resistance: b-lactamase; decreased permeability; altered PBPs side effects: 1-5% cross-allergenicity to penicillins; allergic delayed hypersensitivity; immediate hypersensitivity (IgE)l GI bleed due to inhibtion of post-translational carboxylation of glutamic acid in VitK clotting factors notes: all cephalosporins are inactive v. MRSA, listeria, enterococci - excreted by OAT (inhibited by probenecid)
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names: - pen G (IV), pen V (oral) - penicillinase resistant: methicillin, dicloxacillin, naficillin, oxacillin - aminopenicillin: ampicillin, amoxacillin - ureidopenicillin: ticaricillin, piperacillin - carboxypenicillin: carbenecillin targets: gram positive cocci; gram positive rods; gram negative cocci; gram negative rods action: binds to PBPs -- inhibits transpeptidases; causes autolysin resistance: b-lactamases; abnormal PBPs; reduced permeability side effects: - type I (IgE) -- anaphylaxis, hives, flushing, wheezes, laryngeal edema - type II (IgG/IgM) -- penicillin binds to tissue and then bound by ab; interstitial nephritis, hemolytic anemia, rashes - type III (IgG/IgM) -- circulating penicillin bound by ab before it binds to tissue: serum sickness, joint/mucosa pain notes: variable oral availability; CNS only in meningeal inflammation; 80% excreted via OAT (inhibited by probenecid) - combined with B-lactamase inhibitors: clauvanic acid, sulbactam, tazobactam
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aminopyrimidines, trimethoprim
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names: trimethoprim targets: gram positive cocci, GNR action: inhibits DHFR -- blocks formation of tetrahydrofolic acid from dihydrofolic acid resistance: side effects: notes: forms bactrim with suflamethoxazole -- synergistic effect
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names: sulfamethoxazole targets: gram positive cocci, CA-GNR action: competitlvely inhibits tetrahydropteric acid synthetase -- blocks formation of dihydrofolic acid from PABA and tetrahydropteroid acid resistance: overproduction of PABA; mutation in tetrahydropteric acid synthetase; decreased uptake side effects: erythematous rash to sulfa hypersensitivity; crystalluria/tubular deposits at high doses; hemolytic anemia; leucopenia; thrombocytopenia notes: triple sulfa; excreted in kidneys
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names: metronidazole targets: anaerobes action: reduction of nitro group -- formation of radicals resistance: unknown, rare side effects: - mild GI: nausea, vomiting, anorexia - disulfiram-like reaction notes: 100% oral, CNS distribution, urine and fecal excretion
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names: daptomycin targets: gram positive cocci action: lipid portion binds to bacterial cell membrane -- depolarizes the membrane, efflux of K+, inhibits DNA, RNA, protein synthesis resistance: unknown side effects: reversible myopathy notes: IV, no lung distribution (binds to surfactant), renal excretion
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names: linezolid targets: gram positive cocci action: binds to 23S rRNA of 50S -- prevents formations of 70S initiation complex resistance: point mutation in 23S rRNA side effects: - mild GI: nausea, vomiting, diarrhea - thrombocytopenia (w/ tx longer than 2wks) - reversible, non-selective MAO inhibition (enhance adrenergic, serotonergic agents) notes: 100% oral, hepatic metabolism; can be used for UTIs - bactericidal for strep, bacteriostatic for staph/enterococcus - reserve for resistant microbes only
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names: chloramphenicol targets: gram positive cocci, GNR, anaerobes (GN +/-), rickettsia action: binds to peptidyl transferase of 50S -- prevents binding of AA-tRNA to growing peptide chain resistance: chloramphenicol acetyl transferase -- acetylates and inactivates chloramphenicol molecules side effects: BM aplasia (anemia, low WBCs); reversible neutropenia; grey baby syndrome notes: oral (100%), IV (70-80%); CNS distribution; hepatic metabolism; can be used for UTI
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names: erythromycin, clarithromycin, azithromycin targets: atypical organisms action: reversible binding of 50S -- in areas of peptidyl transferase resistance: decreased permeability; methylation of adenine in 23S rRNA of 50S; chromosomal mutations side effects: - GI irritation (cramps, diarrhea) - cholestatic hepatitis with high doses - reversible partial deafness notes: oral (33%) or IV (azithro); no CNS; azithro -- higher tissue levels than serum; hepatic metabolism/excretion
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names: clindamycin targets: anaerobic bacteria, gram positive cocci, some protozoa action: inhibition of peptidyl transferase in 50S resistance: methylation of adenine in 23S rRNA of 50S; chromosomal mutation; inactivation by adenylation of clinda (MRSA -- different than mech of resistance to b-lactams) side effects: toxin-mediated colitis due to c. diff overgrowth notes: oral, hepatic metabolism; excreted in both urine and feces
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names: telithromycin targets: atypical organisms with greater activity for strep pneumo action: reversible binding to 50S -- at peptidyl transferase site resistance: side effects: similar to macrolides; can produce rare liver necrosis in healthy pts --> not used much anymore notes: pharmacokinetics similar to macrolides
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names: tetracycline, doxycycline, minocycline, tigecycline targets: atypical organisms; MTb (minocycline); MRSA, nosocomial GNR (tigecycline) action: binds to 30S -- prevents access of AA-tRNA to mRNA-ribosome peptide complex resistance: decreased transport + increased efflux side effects: - mild/reversible: rashes (photosensitization), phlebitis, vaginal thrush, diarrhea - staining of teeth in fetus and children (due to chelating activity to Ca2+) - fatty hepatic necrosis in preg women with high doses - demeclocycline causes nephrogenic diabetes insipidus -- used for its SE in treating refractory SIADH notes: oral (avoid food due to chelating issues), CNS distribution, renal excretion (doxy/tige -- also fecal)
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names: spectinomycin targets: GN rods and cocci action: binds to 30S resistance: side effects: notes: similar to aminoglycosides with less toxicity
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names: streptomycin, neomycin, kanamycin, gentamicin, tobramycin, amikacin targets: aerobic GNR action: reversible binding to 30S (streptomycin only); reversible binding to 30S and 50S (all others) resistance: aminoglycoside-modifying enzymes; point mutations to ribosomes side effects: - progressive non-oliguric renal insufficiency - irreversible auditory/vestibular toxicities - neuromuscular blockade -- fatal if diaphragm is involved/paralyzed notes: IM, renal excretion (adjust accordingly)
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names: ciprofloxacin, levofloxacin, moxifloxacin targets: GNR, GN cocci, gram pos cocci, atypical respiratory pathogens action: inhibition of DNA gyrase resistance: ATP-efflux pump; mutations to a/B subunits of DNA gyrase side effects: GI discomfort, HA, damage to cartilage (spont. rupture of achilles), prolonged QTc (torsades) notes: oral, variable CNS distribution, excreted via urine and feces (enough to tx uncomplicated UTIs)
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names: vancomycin targets: most gram positives including resistant ones (eg MRSA) action: inhibition of cell wall synthesis via prevention of simultaneous hydrolysis of D-ala necessary for cross-linkage to occur resistance: synthesis of D-ala penta-peptide terminus that does not bind vancomycin side effects: "red man/redneck" syndrom -- flushing of face and neck due to histamine release; can caused deafness with prolonged use notes: IV, renal excretion (adjust accordingly)
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names: aztreonam targets: aerobic GNR action: binds to PBP3 on aerobic GNRs, cause autolysin resistance: b-lactamases side effects: rashes due to delayed hypersensitivity; no cross-allergenicity to b-lactams notes: IV, excreted by kidneys (adjust levels according)
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clindamycin -- except c. difficile chloramphenicol -- most anaerobes (gn+/-) metronidazole -- enteric anaerobes (bacteroides, prevotella); misc anaerobes (clostridium, fusobacterium, gardenella); most anaerobic, microaerophilic strep; resistant anaerobes: proprionibacterium, actinomyces
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atypical organisms:: respiratory - mycoplasma - chlamydophila pneumonia - legionella - bordetella pertussis
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quinolones tetracyclines -- mycoplasma, chlamydophila, chlamydia trachomatis macrolides -- mycoplasma, chamydophila, legionella, bordetella teilithromycin -- mycoplasma, chamydophila, legionella
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GN cocci - n. meningitides - n. gonorrhea
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penicillins -- n. meningitides (not gonorrhea), t. pallidum cephalosporin (2nd gen) -- n. meningitides cephalosporin (3rd gen) -- n. meningitides, n. gonorrhea
quinolones -- gn cocci (n. meningitides?)
spectinomyces -- occasionally used to treat urethritis due to gonorrhea (not in NYC)
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gram positive cocci - staph - strep - enterococcus
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sulfonamides -- strep (except pneumo), staph (except MRSA), h. inf aminopyridimines -- strep (except pneumo), staph (except MRSA), h. inf trimethoprims -- strep (except pneumo), staph (except MRSA), h. inf
penicillins -- strep (including most step. pneumo), e. faecalis; PRPs and combo tx against MRSA cephalosporins (1st gen-4th gen) -- strep, MSSA carbapenems -- strep, MSSA, amp-susceptible enterococcus
quinolones
clindamycin -- except enterococci, MRSA chloramphenicol -- except some enterococi, MRSA
tetracyclines (tigecycline) -- MRSA vancomycin -- nearly all gram positives (including strep, enterococcus, staph) linezolid -- including penicillin resistant strep, MRSA, e. faecium/faecalis daptomycin -- including penicillin resistant strep, MRSA, e. faecium/faecalis
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sulfonamides -- e. coli, vibrio, yersinia, brucella, h. inf aminopyrimidines -- e. coli, vibrio, yersinia, brucella, h. inf trimethoprim -- e. coli, vibrio, yersinia, brucella, h. inf
penicillins -- e. coli, proteus, enterics ureidopenicillins -- pseudomonas, nosocomial organisms cephalosporins (1st gen) -- CA-enteric GNRs (e. coli, klebsiella, proteus) cephalosporins (2nd gen) -- CA-enteric GNRs (e. coli, klebsiella, proteus) cephalosporins (3rd gen) -- nosocomial GNRs (enterobacter, citrobacter, serratia) cephalosporins (4th gen) -- CA and nosocomial GNRs (including pseudomonas) carbapenems -- CA and nosocomial GNRs aztreonams -- aerobic GNRs only (e.coli, h. inf, vibrio, pseudomonaceae)
quinolones -- GNRs (including nosocomial)
aminoglycosides -- aerobic GNRs (including pseudomonas) spectinomyin -- GNRs tetracyclines (tigecycline) -- nosocomial GNR (except pseudomonas)
chrloramphenicol -- most GNRs (except pseudomonas, acinetobacter)
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gram positive bacilli - bacilli - cornyebacterium - clostridium - listeria
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penicillins -- actinomyces israeli, bacillus antracis, clostridium, diptheria, listeria monocytogenes vancomycins -- corynebacteria, bacillus, lactobacillus, listeria monocytogenes
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