Term
2nd Generation Penicillins |
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Definition
methicillin
naficillin
oxacillin
dicloxacillin
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Term
2nd Generation Penicillins
Special features |
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Definition
resist inactivation by beta-lactamase
used to treat MSSA
not active against Gram (-) bacteria
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Term
3rd Generation Penicillins |
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Definition
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Term
3rd Generation Penicillins
Special Features |
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Definition
for Gram (-) bacteria w/out penicillinase
aka aminopenicillins
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Term
4th Generation Penicillins |
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Definition
piperacillin
carbenicillin
ticarcillin
mezlocillin
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Term
4th Generation Penicillins
Special Features |
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Definition
for Gram (-) like Pseudomonas
SE: can cause large salt load
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Term
Monobactam Abx & Characteristics |
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Definition
Aztreonam!!!
for factultative Gram (-) bacteria
renal excretion[image]
resistant to many beta-lactamases (not Pseudo,Acineto, or Enterobacter
parenteral[image]
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Term
Carbapenems & Relative Activity |
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Definition
imipenem (more against GPC)
ertapenem (less against Pseudomonas & Enterococcus
meropenem (more against GNR)
parenteral [image]
imipenem: renal tubular hydrolysis [image]
Pseudo can become resistant
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Term
Beta-lactamase Inhibitors |
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Definition
clavulanic acid
sulbactam
tazobactam
work against Gram (-) & S. aureus
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Term
Vancomycin
(click word for mechanism) |
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Definition
- for Gram (+) only
- used for
- MRSA
- C. difficile
- beta-lactam resistant pneumococci
- SE: Red Man Syndrom, ototoxic, nephrotoxic (w/ AGs)
- glomerular filtration[image]
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Term
Inhibitors of Protein Synthesis
(5 Classes) |
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Definition
Aminoglycosides
Tetracyclines
MSL group
Chloramphenicol
Oxazolidinones
(Click words for mechanism)
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Term
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Definition
Streptomycin
Gentamicin
Tobramycin
Amikacin
(Click drugs for uses)
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Term
Aminoglycoside Characteristics |
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Definition
administered IM or IV [image]
very polor (don't enter CSF, eye, or bile
glomerular filtration [image]
low toxic:therapeutic ratio (monitor levels)
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Term
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Definition
tetracycline
oxytetracycline
minocycline
doxycycline
demeclocycline
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Term
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Definition
Chlamydia
M. pneumonia
Rickettsia
Brucella
Leptospire
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Term
Tetracycline
Side Effects, Availability, & Metabolism |
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Definition
Side Effects:
Binds new bone and discolors teeth
Photosensitizing skin rash
Vertigo (Minocycline)
Yeast infxns post tx
Availability:
Oral administration [image]
Dairy products inhibit absorption
Metabolism:
Tetracyclines: Renal[image] & hepatic[image] excretion
Doxycycline & Minocycline: hepatic only[image]
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Term
MSL Group Members (6)
Mnemonic Help |
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Definition
telithromycin
erythromycin
clarithromycin
clindamycin
streptogramins
azithromycin
(Click drugs for uses)
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Term
Erythromycin
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
cholestatic hepatitis
nausea & diarrhea
ototoxic at high doses
inhibits P450
QT prolongation w/ IV [image]
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Availability:
given orally [image]
enters placenta, milk, & prostate (not CSF)
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Metabolism & Excretion:
Liver [image]
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Term
Clarithromycin
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
Teratogenic
Ototoxic in high doses [image]
inhibits P450s
fewer GI probs than erythromycin
Availability:
2 doses per day
well-absorbed orally[image]
Metabolism & Excretion:
concentrates in some organs like the lung[image]
30% excreted renally unchanged [image]
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Term
Azithromycin
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
allergic reactions
epidermal necrolysis (rare)
Availability:
1 dose per day
prolonged levels in lungs, PMNs and macrophages
Metabolism & Excretion:
75% unchanged in feces [image]
10% renally excreted [image]
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Term
Clindamycin
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
pseudomembranous colitis
Availability:
orally [image]
IM or IV [image]
Metabolism & Excretion:
mostly biliary excretion [image]
NOTE: Bacteroides is becoming increasingly resistant.
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Term
Streptogramins (Synercid)
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
Thrombophlebitis
increase in conj. bilirubin
arthralgias & myalgias
increase P450
Availability:
IV only [image]
Metabolism & Excretion:
Metab in liver, excrete in bile [image]
Resistance:
mediated by methylation of binding site or acquisition of acetyltransferases
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Term
Telithromycin (Ketek)
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
GI effects
prolonged QT & potential arrhythmias [image]
CYP3A4 inhibition--> discontinue statins
exacerbate myasthenia gravis
blurry vision
Availability:
orally [image]
Metabolism & Excretion:
metab by liver, excreted in bile [image]
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Term
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Definition
Plasmid-encoded resist = resist to ALL
multi-drug transporters affect macrolides but NOT CLINDAMYCIN
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Term
Chloramphenicol
Mechanism & Uses |
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Definition
Mechanism:
Binds 50s ribo subunit & prevents transfer from A to P site
BACTERIOSTATIC
Uses:
broad spectrum
not used in U.S. due to side effects
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Term
Chloramphenicol
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
aplastic anemia
grey baby syndrome
hemolysis w/ G6PD deficiency
Availability:
good concentrations everywhere
Metabolism & Excretion:
glucuronidated in liver [image]
renally excreted [image]
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Term
Oxazolidinones (Linezolid)
Mechanism & Uses |
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Definition
Mechanism:
binds 50s ribo subunit and blocks peptide transfer
Uses:
all Gram (+) cocci and P. multocida
can be used for VRE, MRSA, and beta-lactam resistant pneumococcus
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Term
Oxazolidinones (Linezolid)
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
MAO-inhibitor
Thrombocytopenia (~3%) and bone marrow suppression
Availability:
oral availability same as IV [image]
Metabolism & Excretion:
metab by renal and non-renal routes [image]
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Term
Quinolones
Mechanism & Uses |
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Definition
Mechanism:
- interfere w/ DNA gyrase
- BACTERIOCIDAL
Uses:
- Enterobacteriaceae
- Pseudomonas (Cipro)
- Newer floroquinolones: Gram + & -, anaerobes, intracellular (Chlamydia), and Mycoplasma.
- Floroquinolones
- UTIs
- pneumonia & atypical pneumonia
- bacterial gastroenteritis
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Term
Quinolones
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
idiosyncratic hepatotoxicity
inhibit P450 --> raise blood methyl-xanthines
neurotoxic at high doses
tendon damage w/ prolonged use
NOT FOR CHILDREN OR LACTATING WOMEN
Availability:
Oral [image] or IV [image]
good distrib to prostate, CSF, & eye
food and anti-HM delay absorption
Metabolism & Excretion:
depends on drug
Grepafloxacin & trovafloxacin are excreted by liver [image]
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Term
Metronidazole
Mechanism & Uses |
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Definition
Mechanism:
inhibits bacterial DNA synth in a reducing environment (only in anaerobes)
BACTERIOCIDAL
Uses:
obligate anaerobes (not Actinomyces, protazoa,H. pylori)
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Term
Metronidazole
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
metalic taste in mouth
peripheral neuropathy, seizures,& ataxia (w/ prolonged use)
increased PT when taking warfarin
Availability:
Oral [image] or IV [image]
gets into eye and CSF
Metabolism & Excretion:
metab by liver [image]
excreted in urine [image]
Resistance:
Actinomyces intrinsically
B. fragiis rarely by plasmid
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Term
Rifamycins (Rifampin)
Mechanism & Uses |
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Definition
Mechanism:
inhibits DNA-dependent RNA polymerase, inhibiting initiation
BACTERIOCIDAL
Uses:
TB & mycobacterial infxns
used with other Abx for refractory infxns
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Term
Rifamycins (Rifampin)
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
turns urine, tears, & sweat orange
flu Sx on start and stop
induces P450s
causes uveitis & arthralgias (w/ prolonged use)
Availability:
Once per day
Oral [image]
gets into CSF, prostate, eye
Metabolism & Excretion:
excreted by liver [image]
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Term
Daptomycin
Mechanism & Uses |
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Definition
Mechanism:
disruption of Gram (+) cell membrane function
alters PDG synth, lipoteichoic acid synth,& membrane potential
concentration dependent BACTERIOCIDAL
Uses:
aerobic Gram (+), including MRSA and VRE
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Term
Daptomycin
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
muscle weakness and elevated CPK (at high doses)
Availability:
not orally absorbed [image]
Metabolism & Excretion:
80% in urine [image]
5% in feces [image]
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Term
Sulfonamides & Trimethoprim
Mechanism & Uses |
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Definition
Mechanism:
inhibit folate synthesis
BACTERIOCIDAL in combo
Uses:
community acquired UTIs (but 20% of E. coli are resistant)
Pneumocystis carinii prophylaxis in AIDS
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Term
Sulfonamides & Trimethoprim
Side Effects, Availability, & Metabolism |
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Definition
Side effects:
allergic rash
megaloblastic anemia
reversible hepatitis in AIDS patients
kernicterus in newborns [image]
Availability:
Oral [image]
Metabolism & Excretion:
renal excretion [image]
metabolized in liver [image]
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