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Antimicrobials Flashcards

1
Q

MOA of PCNs

A

bind PBPs–> inhib. transpeptidation–> inhib. crosslinking of bacterial cell walls

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2
Q

Mech. of Resistance for PNCs

A

penicillinases (B lactamases); structural change in PBP, change in porin structure

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3
Q

how do you treat MRSA?

A

vancomycin

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4
Q

how do you treat syphillis?

A

PCN G or V

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5
Q

what are the narrow spectrum PCNs?

A

PCN G and V

*B lactamase sensitive

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6
Q

List the lactams

A

PCNs, cephalosporins, imipenem, meropenem, aztreonam

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7
Q

what are the very narrow spectrum PCNs? what do they treat?

A

methicillin, nafcillin, oxacillin
staph aureus (not MRSA)
*B lactamase resistant

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8
Q

what are the broad spectrum PCNs?

A

amoxicillin, ampicillin

tx: gram + cocci, not staph, listeria, E. coli, H influenza, borrelia, H. pylori
* B lactamase sensitive

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9
Q

what are the extended spectrum PCNs?

A

ticarcillin, piperacillin, azlocillin

tx: gram neg rods, pseudomonas
* B lactamase sensitive
* *synergy with aminoglycosides

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10
Q

how are most PCNs excreted?

A

kidney

*dose reduction in kidney disease

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11
Q

What two PCNs are NOT excreted in the kidney?

A

nafcillin, oxacillin (bile excretion)

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12
Q

If a person is allergic to one PCN, can you give them a different one?

A

NO, assume allergy to all PCNs

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13
Q

What is the most unique side effect of PCNs?

A

Jarish-herxheimer rxn - when tx syphilis

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14
Q

What part of a PCN tends to cause hypersensitivity?

A

sulfur group

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15
Q

What is a side effect of methicillin?

A

interstitial nephritis

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16
Q

What is a common side effect of PCNs?

A

GI distress

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17
Q

how do you enhance PCN activity?

A

add Clavulanic acid or sulbactam

they are B lactamase inhib.

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18
Q

what drug increases PCN and cephalosporin concentration?

A

probenecid

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19
Q

What is the MOA of cephalosporins?

A

same as PCNs: bind PBPs–> inhib. transpeptidation–> inhib. crosslinking of bacterial cell walls
same resistance mech too.

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20
Q

first generation cephalosporins

A

cefazolin

cePHalexin

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21
Q

what are first generation cephalosporins used for?

A 
surgical prophylaxis
gram +
E. coli
klebsiella
proteus
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22
Q

second generation cephalosporins

A

cefotetan, cefaclor,

cefuroxime–> crosses BBB

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23
Q

What are second generation cephalosporins used for?

A

gram neg.

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24
Q

third gen. cephalosporins

A

ceftriaxone, cefotaxime, cefdinir, cefixime, cefoperazone

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25
what do you use third gen. cephalosporins for?
empirical tx of sepsis and meningitis | NO ACTIVITY AGAINST LAME: listeria, atypicals, MRSA, enterococci
26
How do you treat listeria?
amoxicillin
27
How do you treat atypicals?
macrolides or tetracyclines
28
How do you treat enterococci?
amoxicillin with aminoglycosides
29
4th gen. cephalosporins
cefepime IV only! - wider spectrum * B lactamase resistant * *enters CNS
30
What is the mode of excretion for most cephalosporins?
Kidney
31
What cephalosporins are not excreted through the kidney?
cefoperazone, ceftriaxone --> bile
32
Cephalosporin Side Effects
hypersensitivity, GI distress, Disulfiram-like effect
33
What drug should you use if a pt is allergic to cephalosporins?
macrolides (gram+), or aztreonam (gram-)
34
MOA of imipenem and meropenem?
same as PCN but resistant to B lactamases
35
What doe you use imipenem and meropenem for?
gram + cocci, gram - rods, empiric use in nosocomial infections
36
What drug must you give with imipenem? Why?
cilastatin | prevent kidney from metabolizing it too quickly
37
SE of imipenem and meropenem?
GI distress, drug fever, CNS | **1/2 of pts have seizures with imipenem
38
MOA for aztreonam? Use? SE?
same as PCNs + B lactamase RESISTANT ONLY IV use: gram neg. rods **no cross allergenicity with cephalosporins and PCNs
39
MOA vancomycin
binds d-ala-d-ala muramyl pentapeptide--> blocks transglycosylation--> prevents elongation of peptidoglycan cell wall
40
What do you use vancomycin for?
MRSA enterococci c. diff
41
What is the first line tx for C. difficile?
metronidazole
42
What are VRSA and VRE microbes? how do they develop resistance?
vancomycin resistant staph aureus vancomycin resistant enterococci *change in muramyl pentapeptide target to d-lactate
43
how do you treat VRSA and VRE?
linezolid and streptogramins
44
How is vancomycin delivered?
IV | orally only for colitis
45
SE of vancomycin?
Red man syndrome (histamine induced vasodilation) ototoxicity nephrotoxicity
46
MOA of aminoglycosides
inhibits initiation of protein synthesis (30S subunit)--> BACTERIOSTATIC can also cause misreading of genetic code-> BACTERIOCIDAL
47
Name the aminoglycosides
gentamycin, tobramycin, amikacin, streptomycin
48
What do you use aminoglycosides for?
TB, bubonic plague, tularemia gram neg rods: pseudomonas CANT BE USED ON ANAEROBES
49
Excretion of aminoglycosides?
water soluble--> KIDNEY
50
Side effect of aminoglycosides?
nephrotoxicity, ototoxicity, neuromuscular blockade
51
What is neomycin and what is it known for?
aminoglycoside in neosporin, known for contact dermatitis (hypersensitivity)
52
How are aminoglycosides given?
1xday dosing: bacteriocidal so only need a spike once a day | decreases SE
53
aminoglycosides resistance?
conjugating enzymes--> eliminates it too fast to be effective
54
MOA of chloramphenicol?
inhibits peptides transferase (50S) | bacteriostatic
55
What is chloramphenicol used for?
backup for salmonella, b. fragillis, rickettsia, bacterial meningitis
56
Where is chloramphenicol broken down?
LIVER; does reduction in liver dysfunction and in neonates | INHIBITS CYP450
57
SE of chloramphenicol?
dose dependent bone marrow suppression (hypersensitivity), grey baby syndrome and kernicterus
58
Resistance of chloramphenicol?
changes in peptidyl transferase
59
Macrolides MOA?
``` inhibit translocation (50S) **inhib. CYP450 ```
60
Names of Macrolides?
erythromycin, azithromycin, clarithromycin, clindamycin
61
What are the Macrolides used for?
gram pos. cocci: staph aureus and anaerobes also goes into bones for osteomyelitis atypicals (chlamydia, mycoplasma, ureaplasma) legionella campylobacter mycobacteria avium-intracellular
62
SE of Macrolides?
GI distress, reversible deafness
63
how do you treat macrolide resistant s. pneumo?
telithromycin
64
Macrolides resistance?
methylation of rRNA by methyltransferase of bug--> unable to recognize binding site
65
Tetracylines MOA?
``` inhibits elongation (30S) bacteriostatic ```
66
What abx cannot be used in pregnant women?What do you use tetracyclines for?
aminoglycosides, fluoroquinolones, sulfonamides, tetracylcines
67
What do you use tetracyclines for?
chlamydia, mycoplasma, H. pylori, rickettsia, borrelia burgdorferi, brucella, vibrio, treponema
68
name the tetracyclines
doxycycline, minocycline, demeclocycline
69
what do you use doxycycline for?
prostatitis
70
what do you use minocycline for?
gingivitis
71
what do you use demeclocycline for?
SIADH (blocks ADH receptors)
72
SE of tetracyclines
tooth enamel dysphagia, decreased bone growth, phototoxicity, GI distress, superinfection with candidiasis, vestibular dysfunction
73
tetracycline resistance
pumps drugs out of cells
74
excretion of tetracyclines
most through kidneys, doxycyline goes through liver
75
What is unique about the tetracyclines in regard to divalent cations?
they are chelators | so they shouldn't be taken with food or with vitamins
76
streptogramins moa?
inhibit elongation 50S by blocking acceptor site and decreases release of completed peptide
77
what are the streptogramins?
quinipristin and dalfopristin
78
What do you use streptogramins for?
VRE and VRSA
79
Linezolid MOA?
inhibits initiation (50S)
80
What do you use Linezolid for?
VRE, VRSA, drug resistant pneumococci
81
SE of Linezolid?
bone marrow suppression
82
Fluoroquinolones MOA?
inhib. NA synthesis by inhib. topoisomerase 2 and 4 (DNA gyrase)
83
Name the Fluoroquinolones?
norfloxacin, ciprofloxacin, ofloxacin
84
What do you use Fluoroquinolones for?
UTI, STD (chlamydia, gonorrhea), skin and soft tissue infection with gram neg., shigella, salmonella, E. coli, campylobacter, drug resistant pneumo
85
Why do you have to take Fluoroquinolones without food?
it binds to iron and calcium which inhibits its absorption
86
Excretion of Fluoroquinolones
kidney
87
SE of Fluoroquinolones
tendonitis, tendon rupture, phototoxicity, rash, CNS effects (increase QT interval, Seizures with IV), contraindicated in kids and preg
88
MOA of sulfonamides?
inhib. dihydropteroate synthetase (indirectly inhib. NA synth.)
89
SE of sulfonamides?
hypersensitivity, Stevens-Johnson syndrome (aka exfoliating dermatitis), hemolysis in G6PD deficiency, phototoxicity
90
MOA of trimethoprim and pyrimethamine?
inhib. dihydrofolate reductase (also in humas) - indirectly inhib NA synth.
91
How does trimethoprim and pyrimethamine have anti-neoplastic activity?
because its inhib. dihydrofolate reductase, which is in the microbe and human!
92
SE of trimethoprim and pyrimethamine?
bone marrow suppression | *worrisome because it is used for tx in HIV pts and can worsen leukoplakia
93
What is trimethoprim-sulfamethoxazole used for?
nocardia, listeria, gram neg. and gram pos., pneumocystis jiroveci (prophylaxis in HIV)
94
Pyrimethamine-sulfadiazine use?
toxoplasma gondii (prophylaxis in HIV)
95
Metabolism of trimethoprim and pyrimethamine?
acetylation by liver, excreted in kidney--> can cause kidney stones because its conjugate is less water soluble
96
Why do trimethoprim and pyrimethamine cause drug interactions?
high protein binding, causes kernicterus in neonates
97
Metronidazole MOA?
produces free radicals, bactericidal
98
What is Metronidazole used for?
drug of choice for giardia, trich, entamoeba, C. diff, gardernella, H. pylori
99
SE of Metronidazole?
metallic taste! | disulfiram-like effect
100
What combos are usually used for H. pylori?
BMT= bismuth + metronidazole + tetracycline OR | clarithromycin + amoxicillin + omeprazole
101
Antitubercular drugs
isoniazid, rifampin, ethambutol, pyrazinamide, streptomycin
102
How do you prevent resistance in antitubercular drugs?
combination therapy
103
isoniazid MOA?
cell wall synth inhib. - mycolic acid synth.
104
isoniazid is a prodrug, what allows it to become activated?
conversion by catalase
105
isoniazid resistance?
if the microbe is missing the catalase gene
106
isoniazid use?
mycobacterium only
107
SE of isoniazid?
hepatitis, peripheral neuritis, sideroblastic anemia (B6 def., increased iron), SLE, hemolysis in G6PD def.
108
Rifampin MOA?
inhib. DNA dependent RNA polymerase (transcription)
109
SE of Rifampin?
hepatitis, induction of P450, red-orange metabolites in urine, saliva, tears
110
Ethambutol MOA?
inhib. cell wall synth. by blocking arabingalactan
111
SE of Ethambutol?
dose dependent optic neuritis --> loss of color vision
112
Pyrazinamide MOA?
UNKOWN, prodrug
113
SE of Pyrazinamide?
hepatitis, hyperuricemia
114
Streptomycin MOA?
inihib protein synthesis
115
SE of Streptomycin?
deafness, vestibular dysfunction, nephrotoxicity, neuromuscular blockade vie decreased ach release

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