Antibiotics I & II Review Flashcards
- fungal overgrowth
- most common type of superinfection
- continue administration of antibacterial agent
- treat w/ antifungal , ex: oral nystatin for GI
intestinal candidiasis
- life threatening
- discontinue admin of antibacterial agent
- treat w/ oral vancomycin (not absorbed, treats locally)
staphylococcal enterocolitis
- life threatening, caused by c/ difficile
- discontinue admin of antibacterial
- treat w/ oral metronidazole (or vancomycin)
- often caused by clindamycin
pseudomembranous colitis
-aminoglycosides, vancomycin, minocycline cause what organ directed toxicity?
ototoxicity
chloramphenicol and sulfonamides cause what organ directed toxicity?
hematopoietic
tetracyclines, macrolides, isoniazid, sulfonamides, and ampho B cause what organ directed toxicity?
hepatotoxicity
aminoglycosides, vancomycin, ampho B, cephalosporins, and sulfonamides cause what organ directed toxicity?
renal
primaquine, sulfonamides, and nitrofurantoin cause what idiosyncratic response?
hemolytic anemia (in G6PDH deficiency)
tetracyclines, sulfonamides, and fluoroquinolones cause what idiosyncratic response?
photosensitivity
sulfonamides can cause what hypersensitivity reaction?
stevens johnson
beta lactams and vanocmycin blocks enzymatic steps in the _______ space, and other ICWs (fosfomycin, cycloserine) act at _______ sites
periplasmic
intracellular
penicillins primarily useful against gram positive microbes?
pen G, pen V
nafcillin, methcillin, oxacillin, dicloxacillin are __________ penicillincs
anti-staph
ampicillin, amoxacillin, piperacillin, ticarcillin are extended spectrum penicillins with increased ________ activity
gram negative
antipseudomonal penicillins effective against proteus and pseudomonas? use in combo with aminoglycoside
piperacillin, ticarcillin
beta lactam drugs that inhibit cell wall synthesis but are less susceptible to penicillinases, bactericidal
cephalosporins
cefazolin and cephalexin are ____ generation cephalosporins
1st
- good activity against gram positive and modest gram negative
- treat staph and strep cellulitis
- DOC for surgical prophylaxis
cefazolin (1st gen)
cefaclor, cefoxitin, cefuroxime, cefotetan are _____ generation cephs
2nd (fur ox with two fac tets)
- increased activity against gram negative bacteria (Ecoli, Kelbsiella, Proteus, haemophilus, moraxella catarrhalis)
- PID, diverticulitis, surgical prophylaxis for abdominal, bronchitis
uses for 2nd gen cephalosporins (cefaclor, cefoxitin, cefuroxime, cefotetan)
-ceftriaxone, cefotaxime, ceftazidime, cefpodoxime are ______ generation cephs
3rd
- decreased gram (+) but increased gram negative (enterobacter, serratia)
- pseudomonas activity
- meningitis
- CAP, lyme disease, osteomyelitis, gonorrhea
- penetrate CNS, so many useful in meningitis
3rd gen cephalosporin use
cefipime a ____ generation cephalosporin
4th
- extensive gram positive and gram neg activity
- increased resistance to beta lactamases
- reserve for situations such as neutropenic fever
4th gen ceph (cefepime)
- MRSA activity, gram negs except pseduomonas
- approved for cSSSIs and CAP
5th gen cephalosporin (ceftaroline)
- monobactam, only gram negative activity
- no anaerobe activity
- for pseudomonas use w/ an aminoglycoside
- beta lactamase resistant
- no cross reactivity to penicillin allergies
aztreonam
- broad spectrum: gram (+), (=), and anaerobes
- beta lactamase resistant
- inactivated by renal dipeptidase (co admin cilastatin)
- cross sensitivity w/ penicillin allergies
- pseduomonas resistance rapid, so use w/ aminoglycosides
carbapenems: imipenem, meropenem, doripenem, ertapenem
vancomycin inhibits _________ by binding to D-ala D-ala terminus of petidoglycan monomer
transglycosylation
vancomycin bactericidal for _______ bacteria
gram positive
vancomycin used systemically for ______
MRSA
vancomycin enhances oto and nephro toxicity of ________
aminoglycosides
- used for infections caused by gram positive, penicillin resistant organisms
- s. aureus, MRSSA, enterococci, C diff alternative treatment
vancomycin
- newer ICWS, gram positive and negative activity
- inhibits cytoplasmic step in cell wall precursor synthesis
- actively transported by G6P transporter into bacteria
- approved for single dose therapy of UTI
- actively excreted by kidney
fosfomycin
- topical antibiotic only, for gram (+) organisms
- markedly nephrotoxic
bacitracin
-inhibit dihydrofolate synthesis, bacteriostatic (-cidal when combined with trimethoprim)
sulfonamides (sulfamethoxazole, sulfadizaine)
- inhibits dihydrofolate reductase, bacteriostatic
- combo for UTIs, shigella, salmonella, pneumocystis, toxoplasmosis
trimethoprim, pyrimethamine (protozoa), methotrexate (mammalian)
-inhibit prokaryotic enzymes topoisomerase II, bactericidal
fluoroquinolones
- prototype quinolone
- oral, rapidly glucoronidated and actively excreted in urine
nalidixic acid
all fluoroquinolones have what suffix?
-floxacin
- actively excreted in urine, blocked by probenicid
- treat gram (-) rods of urinary and GI tracts, some gram (+), otitis externa
fluoroquinolones
-excellent activity against many gram (-) bacteria (gonococcus, psuudomonas, mycobacteria, chlamydia)
2nd gen fluoroquinolones (cipro, ofloxacin)
- 3rd gen fluoroquinolone, given 2X daily
- greater gram (+) activity (strp pneumo, enterococci, MRSA), resp infections)
levofloxacin
-broadest spectrum fluoroquinolones, respiratory
4th gen (moxifloxacin, gemifloxacin)
- chronic infections with long dormant periods separating intermittent active periods
- intracellular pathogens
- requires constant prolonged treatment with multiple drugs
tuberculosis and leprosy
_______ favored over rifampin for HIV patients on HAART cocktails b/c of less DDIs
rifabutin
- may involve oxidative stress, urinary tract antiseptic
- excreted in urine 50% as active drug
- treats UTI, gram positive or negative, most effective at acidic urine pH
- adverse: headaches, anorexia, GI, hemolytic anemia if G6PDH deficient
- pseudomonas and proteus resistant
nitrofurantoin
- alter permeability and damage bacterial cytoplasmic membrane, leakage
- gram (-) only
- topically
- systemically as last resort for pseudomonas
- nephrotoxic
polymixins (colistin, polymixin E, polymixin B)
- binds cell membrane of susceptible organisms, causes rapid depolarization
- gram (+) only
- IV
- treats complicated skin infections
- used for vancomycin resistant bacteria
daptomycin
- binds bacterial isoleucyl transferase RNA synthetase, inhibits protein synthesis
- topical: for impetigo caused by s aureus and s. pyogenes
- intranasal for MRSA
mupirocin
abx of choice for:
H pylori
amoxicillin, clarithromycin, omerprazole
abx of choice for: listeria
ampicillin
abx of choice for: neisseria gonorrhea
ceftriaxone, cefexime
abx of choice for: H. influenza, klebsiella
3rd gen cephalosporins
abx of choice for: borrelia burgdorferi, Rickettsiae?
doxycycline
abx of choice for: legionella
erythromycin
abx of choice for: candida
fluconazole, miconazole, nystatin
abx of choice for: mycobacterium tuberculosis
isoniazid, rifampin, ethambutol, pyrazinamide
abx of choice for: mycoplasma pneumonia, legionella, corynebacterium diptheria, chlamydia
macrolides
abx of choice for: trichomonas, c diff
metronidazole
abx of choice for: treponema pallidum, bacillus anthracis, clostridium, bacteroides
penicillin G
abx of choice for: campylobacter, shigella
fluoroquinolones
abx of choice for: vibrio cholera
tetracycline
abx of choice for: salmonella, shigella
TMP-SMX
abx of choice for: C diff
metronidazole, vancomycin
prophylaxis for surgical procedures?
cefazolin
prophylaxis for surgery where anaerobe present?
cefoxitin, cefotetan
prophylaxis for GBS?
ampicillin, penicillin
prophylaxis for pneumocytsis, UTIs?
TMP-SMX
prophylaxis for h influenza, meningococcal infxn?
rifampin
prophylaxis for malaria?
chloroquine
prophylaxis for M. avium in AIDS?
azithromycin
prophylaxis for dental procedures?
amoxicillin, azithromycin, clindamycin
-aminoglycosides, tetracyclines, tigecycline and spectinomycin target the ______ ribosomal subunit
30S
chloramphenicol, macrolides, tilethromycin, linezolid, and quinupristin-dalfopristin target the _______ ribosomal subunit
50S
________ irreversibly inhibit the 30S subunit, making them bactericidal
aminoglycosides
- reversible binding to 30S subunit
- bacterostatic
- chelate metal ions, not absorbed so don’t admin with food/milk/antacids
- concentrates in teeth, bone, liver, bile, kidney
- cross placenta and excreted in milk
tetracyclines
- mycoplasma, chlamydia, rickettsiae, H pylori
- prophylaxis for plasmodiium falciparum
- helpful for lyme disease
- ability to accumulate intracellulary
tetracyclines
- tetracycline analog
- used for CAP, skin and suture infections, intra abdominal infxn (MRSA, E. faecalis)
- FDA black box warning for mortality
tigecycline
- cause superinfections
- impaired liver functions
- photosensitization
- calcium chelation
adverse effects of tetracyclines
- impaired influx/increased efflux by active transport protein pump
- overuse has fostered emergence of resistance
tetracyclines
- reversible inhibitor of protein synthesis (50S subunit) , bacteriostatic
- CNS levels = serum levels
- glucoronidation in liver is rate limiting step for clearance
chloramphenicol
- adverse:
- anemia due to bone marrow depression, usually reversible
- aplastic anemia: irreversible and fatal
- gray baby syndrome: newborns are poor glucoronidators
- DDIs, inhibits enzymes
chloramphenicol
- powerful antibacterial limited by toxicity
- typhoid fever, RMSF
- alternate for bacterial meningitis, topical for eye infexns
chloramphenicol
- bacteriostatic or -cidal depending on dose
- 50S IPS
- acid labile - use enteric coat or ester
- CNS, crosses placenta
- excreted in bile, half life 2-5 hours except one drug
macrolides (erythryomycin, clarithromycin, azithromycin)
- GI distress
- cholestatic jaundice
- microsomal enzyme inhibition
- used for atypical pneumonia (mycoplasma, legionnaire’s, chlamydia), back for penicillin sensitive patients
macrolides
-plasmid mediated resistance to staph, strep, pneumococci
macrolides
newer macrolide with less GI effects, given with ethambutal for m avium
clarithromycin
-macrolide with minimal P450 inteactions, tissue levels 100X plasma levels (half life 2-4 days), active against m. avium, shorter dosing period
azithromycin
- ketolide
- treatment of CAP
- may prolong QT interval
- hepatic failure, respiratory failure in myasthenia gravis
- DDIs CYP3A4
telithromycin
- lincosamide
- 50S IPS
- good for bacteroides fragilis
- with primaquine treats pneumocystis in AIDS
- with pyrimethamine for toxoplasmosis
- adverse: clostridium superinfections, hepatotoxicity
clindamycin
- significant CYP3A4 inhibitor
- complete cross resistance b/w two components
- no cross resistance with other IPS
- bacteriostatic against E faecium, cidal against others
- e. faecalis is resistant
- approved for vanco and MDR e. facium and MRSA
streptogramins (quinupristin, dalfopristin)
- binds 23S rRNA of 50S subunit
- no cross resistance with other IPS
- IV or oral
- for vanco resistant e faecium, MRSA
- adverse: bone marrow suppression, inhibits MAO
- serotonin syndrome
linezolid
gentamicin, streptomycin, tobramycin, amikacin, neomycin (topical)
aminoglycosides
- bactericidal, inactivate 30S subunit irreversibly
- interfere w/ initiation, misread mRNA, break up polysomes
aminoglycosides
- IV, no significant host metabolism
- glomerular filtration, high concentrations in proximal tubules
- rapid resistance alone
- anaerobes resistant (oxygen dependent uptake)
aminoglycosides
- once daily dosing, removes factor of time maintaining concentration
- nephrotoxic: exacerbated in vanco, cephs, ampho B, cisplatin and other nephrotoxics
- ototoxicity
- neuromuscular blockade in MG, common during surgery
aminoglycosides
- use for infections with aerobic gram negatives
- ecoli, proteus, klebsiella, serratia, enterobacter
- cell wall inhibitors are synergistic
- treats pseduomonas in combo with penicillins
- tuberculosis
aminoglycoside uses
- postantibiotic effect
- useful for non resistant gram (-) infections
- use older first
aminoglycosides
order of use of aminoglycosides for pseudomonas?
gentamycin > tobramycin > amikacin
- related to aminoglycosides and tetracyclines (30S IPS)
- useful against drug resistant gonococci and patients allergic to cephalosporins
spectinomycin