E2 Erdman MSC antibiotics Flashcards
tetracyclines in lecture (3)
tetracycline
doxycycline
minocycline
Tetracycline analogs in lecture (3)
Tigecycline
eravacycline
Omadacyline
Sulfonamide in lecture (1)
TMP-SMX
2 polymyxins in lecture
Colistin
Polymyxin b
Lincosamide in lecture (1)
clindamycin
Nitroimidazole in lecture (1)
metronidazole
tetra MOA
reversibly bind 30S
Tetra static or cidal
static, but cidal when at high conc against very susceptible organisms
3 mechs of resistance tetras
- efflux pumps
- dec access to ribosom from ribosomal protection proteins
- enzymatic inactivation of tetras
Cross-resistance is NOT observed
tetracycline
doxycycline
minocycline
mino
T or F:
tetracycline analogs are affected by the major tetra resistance mechs
false actually
which 2 are most active against GP aerobes
tetracycline
doxycycline
minocycline
Mino and doxy
highlighted GP bacteria tetras are active against
MSSA
tetra SoA
GN aerobes
Haemophilus influ
Haemophilus duc
Camplyobacter
Helocobacter
Acinetobacter
(NO ENTEROBACTERALES)
2 anaerobic bacteria for tetras
Actinomyces
Propionibacterium
Tetra SoA:
MSC bacteria
atypical bacteria such as
LEGIONELLA*
Chlamydophila pneumoniae
Mycoplasma
Ureaplasma
tetra analogs SoA:
GP aerobes (highlighted)
MSSA
MRSA
entero faecalis (VSE and some VRE)
acronym for tetra analog GN aerobes
EEACKSS
T or F:
tetra analogs are active against proteus mirabilis and pseudomonas aeruginosa
FALSE*
has higher MIC for GN aerobe Stenotrophomonas maltophilia
A. Tigecycline
B. Eravacycline
C. Omadacycline
C
1 highlighted anaerobe for tetra analogs
Bacteroides spp
have coverage against atypical bacteria
A. Tigecycline
B. Eravacycline
C. Omadacycline
B and C
which 3 tetras + analogs are available PO and IV
doxy
mino
omada
which 2 tetras + analogs are only IV
Tige
erava
which tetras + analogs have impaired absorption from dairy, zinc, mag, etc?
all orals (doxy, mino, omada)
absorption of tetras + analogs is impaired by what
di and trivalent cations
1 highlighted location for where tetras + analogs are distributed
prostate
T or F:
tetras + analogs penetrate CSF well
false, very little amounts
T or F:
tetras + analogs are removed during hemo
true BUT minimally
which two tetras do not require dose adjustment in RI
doxy
mino
which tetra analogs require dose adjustment in RI
none
which is used in outpatient use for CAP
tetracycline
doxycycline
minocycline
doxy
used for acinetobacter infections
tetracycline
doxycycline
minocycline
Mino
Used for chlamydial infections, including nongonococcal urethritis
tetracycline
doxycycline
minocycline
doxy
T or F:
tetra analogs cover proteus and psedomonas
false
Tetra + analogs AEs:
GI, which one most likely
N/V
Tigecycline*
Tetra + analogs AEs:
dermatologic
photosensitivity
T or F:
all tetras + analogs are safe in pregnancy
false, all category D
why cant the tetras + analogs be used in pregnancy?
discoloration of permanent teet and dec bone growth in children
Which antibiotic will interact with divalent/trivalent cations so that oral absorption is impaired potentially leading to clinical failure?
A. Oral levofloxacin
B. Oral doxycycline
C. Oral ciprofloxacin
D. Oral minocycline
E. All of the above
E
Which of the following antibiotics does NOT have activity against atypical bacteria (e.g., Legionella pneumophila)?
A. Azithromycin
B. Levofloxacin
C. Amoxicillin-clavulanate
D. Doxycycline
E. Moxifloxacin
C
TMP-SMX MOA
produce sequential blockade of microbial folic acid synthesis, which is necessary for production of DNA
Inhibits dihydropteroate synthesis:
A. TMP
B. SMX
B
Inhibits dihydrofolate reductase:
A. TMP
B. SMX
A
TMX and SMX are ______ alone but ______ in combination
static
cidal
mechs of resistance for TMP-SMX
- point mutations in dihydropteroate synthase and/or altered production or sensitivity of bacterial dihydrofolate reductase (wtf)
TMP-SMX SoA:
GP aerobes
S aureus (including some MRSA, especially CA-MRSA)
TMP-SMX SoA:
GN aerobes (1)
Stenotrophomonas maltophilia**
what notable GN aerobe does TMP-SMX NOT cover
pseudomonas*
“other” bacteria that makes TMP-SMX the DRUG OF CHOICE for
Pneumocystis carinii***
TMP-SMX dosage form(s)
IV and PO
how do you achieve steady-state serum conc of TMP-SMX
fixed oral or IV combo of 1:5
T or F:
TMP-SMX penetrates CSF w/ inflamed meninges
true
2 highlighted locations TMP-SMX distributes to
urine
prostatee
SMX is ___% protein bound
70
TMP-SMX elimination
both are eliminated by liver and kidney
When should you consider dose adjustment for TMP-SMX?
CrCl <30
3 highlighted clinical uses for TMP-SMX
- acute, chronic, or recurrent UTIs
- acute or chronic bacterial prostatitis
- skin infxns due to CA-MRSA
TMP-SMX AEs:
hematologic
leukopenia, thrombocytopenia
TMP-SMX AEs:
hypersensitivity
rash
TMP-SMX AEs:
CNS
headache, aseptic meningitis, seizures
TMP-SMX AEs:
other
crystalluria, hyperkalemia, inc creatinine
T or F:
TMP-SMX is safe in pregnancy and breastfeeding
false, can cause kernicterus in newborn
TMP-SMX drug interactions
warfarin
inc anticoagulation effect
TMP-SMX dosage forms and dosing, oral tabs:
Single strength: __mg TMP and ___mg SMX
double strength: ___mg TMP and ___mg SMX
- 80, 400
- 160, 800
_____ are cationic cyclic decapeptides linked to a fatty acid chain by an a-amide linkagee
Polymyxins
is a prodrug:
A. colistin
B. polymyxin B
A
Polymyxin MOA
cationic detergents that binds to anionic lipopolysaccharide molecules in the outer cell membrane of Gram-negative bacteria causing displacement of Ca and Mg induces changes in permeability and leakage of cellular contents, leading to cell death
Polymyxins display (time/conc) dependent and (static/cidal) activity
conc
cidal
1 resistance mech for polymyxins
alteration of outer cell membrane
Polymyxins SoA:
GP aerobes
none
Polymyxins SoA:
GN aerobic bacilli
(2 highlighted options)
Acinetobacter spp
Pseudomonas aeruginosa
Polymyxins SoA:
anaerobes
none
Polymyxins Absorption
only IV not absorbed like that ig
Polymyxin elimination
Colistin and polyB are eliminated by nonrenal routes
HOWEVER
50% of CMS is eliminated unchanged by the kidney
requires dose adjustment in RI when CrCl <80
A. colistin
B. polyB
A
Polymyxins clinical uses
infections caused by GN bacteria that are resistant to other antibiotics
Pref for systemic infections
A. colistin
B. polyB
A
pref for UTI
A. colistin
B. polyB
B
polymyxins AEs:
(2)
nephrotox - reversible
neurotox - reversible
use what BW for colistin IV
IBW
use what BW for polyB
TBW
can both polymyxins be used for inhalation
yes
True/False:Colistin is often used for the treatment of infections due to Gram-negative aerobes because it is not associated with serious adverse effects
false, only for tx of infections due to MDR GN aerobes bc it is nephro and neurotoxic
best for ADA; except for treatment in brain abscesses:
A. Clindamycin
B. Metronidazole
A
best for BDA; useful for brain abscesses due to CNS/CSF pen:
A. Clindamycin
B. Metronidazole
B
clindamycin MOA
50s
clinda is (time/conc) dependent and (cidal/static)
time
static
mechs of resistance for clinda
- altered target sites
is active efflux effective against clindamycin
no
Clinda SoA:
GP aerobes
(highlighted)
PSSP
CA-MRSA
MSSA
clinda is active against many GP and GN anaerobes, but is most useful for anaerobes ________ ____ _______
above the diaphragm
clinda SoA:
anaerobes (highlighted)
some bacteroides spp
T or F:
clinda has activity against C diff
false
clinda absorption
rapidly and completely absorbed, food has minimal effect
Clinda distribution
good tissue penetration including bone, minimal CSF pen
clinda elimination
primarily metabolized by liver
T or F:
clinda is removed during hemo
FALSE IT IS NOT
clindamycin clinical uses
- infections due to anaerobes OUTSIDE THE CNS
- pulmonary
- diabetic foot infections
- penicillin-allergic pts
- infections due to CA-MRSA*(
clinda AEs:
worst inducer of?
C diff
clindamycin AEs:
highlighted and not Gi
hepatotoxicity - rare
metronidazole MOA
ultimately, inhibits DNA synthesis
T or F:
both colistin and metronidazole are prodrugs
true
Metronidazole displays (time/conc) dependent and (cidal/static) activity
conc
cidal
2 mechs of resistance for metro
altered growth requirements
and
altered ferredoxin levels
metronidazole SoA:
anaerobes *
ADA: peptococcus
BDA: bacteroides
C diff
metro is the antianaerobic agent most reliably active against what bacteria
bacteroides fragilis
metronidazole SoA:
GP anaerobes
Clostridium spp including C diff
T or F:
metro is inactive against all common aerobic bacteria
true
T or F:
metro penetrates CSF well
true
metronidazole elimination
primarily metabolized by liver
T or F:
metro is removed during hemo
true
metro clinical uses
- anaerobic infections*
- pseudomembranous colitis due to C diff
- trichomonas
- giardia
metro AEs:
GI
stomatitis
metallic taste
metro AEs:
CNS- most serious btw
peripheral neuropathy**
Metro AEs:
other significant highlighted one
mutagenicity, carcinogenicity (avoid during pregnancy and breastfeeding)
2 notable drug interactions with metro
warfarin
alcohol
Which of the following antibiotics will NOT interact with warfarin?
A. TMP-SMX
B. Metronidazole
C. Ciprofloxacin
D. Clindamycin
E. Clarithromycin
D
Which of the following antibiotics can be safely used during pregnancy?
A. Ampicillin
B. Levofloxacin
C. Doxycyclline
D. Metronidazole
E. Telavancin
A
Which of the following antibiotics does NOT require dosage adjustment in renal insufficiency?
A. Trimethoprim-sulfamethoxazole
B. Vancomycin
C. Gentamicin
D. Cefazolin
E. Nafcillin
E, even tho it can cause nephrotox?
Which of the following antibiotics is NOT associated with the development of nephrotoxicity?
A. Metronidazole
B. Vancomycin
C. Tobramycin
D. Colistin
E. Nafcillin
A