antibacterials Flashcards
1
Q
folic acid synthesis and reduction
A
DNA methylation,
PABA inhibitors: sulfonamides,
DHF inhibitor: trimethoprim
2
Q
peptidoglycan synthesis inhibitors
A
glycopeptides ( vancomycin, bacitracin)
3
Q
peptidoglycan x-link inhibitors
A
pencillinase-sensitive, pencillinase-resistant, antipseudomonals, cephalosporin (I-V), Carbapenems, Monobactams
4
Q
Pencillinase sensitive
A
pencillin G,V; ampicillin; amoxicillin
5
Q
penicillinase resistant
A
oxacillin, nafacillin, dicloxacillin
6
Q
antipseudomonals
A
ticarcillin, pipercillin
7
Q
cephalosporin I
A
cefazolin
8
Q
cephalosporin II
A
cefoxitin
9
Q
cephalosporin III
A
ceftriaxone
10
Q
cephalosporin IV
A
cefepime
11
Q
cephalosporin V
A
ceftaroline
12
Q
Carbapenems
A
imipenem, meripenem, ertapenem, doripenem,
13
Q
monobactam
A
aztreonam
14
Q
DNA integrity inhibitor (via free radicals)
A
metronidazole
15
Q
mRNA synthesis inhibitor (via RNA polymerase)
A
rifampin
16
Q
DNA gyrase inhibitor
A
FQN, quinolone
17
Q
FQN
A
ciprofloxacin, levofloxacin
18
Q
quinolone
A
nalidixic acid
19
Q
50s protein synthesis inhibitors
A
chloramphenicol, clindamycin, linezolid, macrolides, streptogramins
20
Q
macrolides
A
azmycin, cymcin, emycin
21
Q
streptogramins
A
quinupristin, dalfopristin
22
Q
30s subunit inhibitors
A
aminoglycosides, tetracyclines
23
Q
aminoglycosides
A
gentamicin, neomycin, amikacin, tobramycin, streptomycin
24
Q
PCN G/V mechanism
A
D-ala-D-ala structural analog. Binds PBP.
blocks PBP xlink of peptidoglycan in cell wall.
activates autolytic enzymes
25
PCN G/V use
G+ organisms, syphilis and gonorrhea
bacteriocidal
26
PCN G/V ADR
hypersensitivity rxns, direct Coombs + hemolytic anemia
27
PCN G/V resistance
pencillinase in bacteria cleaves b-lactam ring
28
penicillinase-resistant PCN MOA
same as PCN; narrow spectrum
pencillinase resistant b/c bulky R group blocks access of B-lactamases
29
penicillinase-resistant PCN use
MSSA
30
penicillinase-resistant PCN ADR
hypersensitivity rxns, ***interstitial nephritis***
31
penicillinase-sensitive PCN MOA
same as PCN, wider spectrum
pencillinase sensitive. also combine with clavulanic acid to protect against destruction by b-lactamase
32
penicillinase-sensitive PCN use
extended-spectrum pencillin
H. influenzae, H pylori, E. coli, listeria monocytogenes, Proteus mirabilis, salmonella, shigella, enterococci
"Ampicillin/amoxicillin HHELPSS kill enterococci"
33
penicillinase-sensitive PCN ADR
pseudomembranous colitis, rash, hypersensitivity rxns
34
penicillinase-sensitive PCN mechanism of resistance
penicillinase in bacteria cleaves b-lactam ring
35
antipseudomonal PCN MOA
same as pcn, extended specturm
36
antipseudomonal PCN ADR
pseudomonas, gram - rods
37
antipseudomonal PCN codrug
susceptible to penicillinase. need B-lactamase inhibitors
38
antipseudomonal PCN ADR
hypersensitivity rxns
39
B-lactamase inhibitors
clavulanic acid, sulbactam, tazobactam
40
cephalosporin MOA
b-lactam drugs that inhibit cell wall synthesis, but are less susceptible to penicillinase
bactericidal
41
organisms not covered by 1-4 generation
("Lame")
Listeria, Atypicals (chlamydia, mycoplasma), MRSA, and Enterococci
42
1st generation cephalosporin use
cefazolin, cephalexin
gram + cocci; PEK
43
Cefazolin surgical use
prophylaxis to prevent S aureus wound infections
44
2nd generation cephalosporin use
cefaclor, cefoxitin, cefuroxime ("Fake fox fur")
gram + cocci; HENS PEK
45
HENS
H influenzae, Enterobacter aerogenes, Neisseria, Serratia
46
PEK
proteus mirabilis, E coli, Klebsiella pneumoniae
47
3rd generation cephalosporin use
ceftriaxone, cefotaxime, ceftazidime
serious gram - infections resistant to other B-lactams
48
Ceftriaxone use
meningitis, gonorrhea, disseminated Lyme disease
49
Ceftazidime use
pseudomonas
50
4th generation cephalosporin use
cefepime
gram - organisms, inc activity against Pseudomonas and gram + organisms
51
5th generation cephalosporin use
ceftaroline
broad +/- coverage, including MRSA; **no pseudomonas**
52
cephalosporin ADR
hypersensitivity rxns, autoimmune hemolytic anemia, disulfiram-like rxn, vitamin K deficiency.
53
cephalosporin drug interactions
exhibit x-rxn with PCN
inc nephrotoxicity with aminoglycosides
54
cephalosporins mechanism of resistance
structural changes in PBP
55
Imipenem (carbapenems) MOA
broad-spectrum, B-lactamase-resistant.
| **always administered with cilastatin to decrease inactivation of drug in renal tubules**
56
imipenem use
G+ cocci, G - rods, and anaerobes.
wide spectrum, but significant ADR limit use
57
meropenem
dec risk of seizures and is stable to dehydropeptidase I
58
carbapenem adr
GI distress, skin rash, seizures at high plasma levels
59
monobactams MOA
prevents peptidoglycan x-linking by binding to PBP 3. synergistic w/ aminoglycosides.
***no cross allergenicity w/ PCN***
60
monobactam use
***G- only***
used in PCN allergic pts, and those with renal insufficiency
61
vancomycin MOA
inhibits cell wall peptidoglycan formation by binding to D-ala-D-ala precursor.
Bacteriocidal (except C. Diff --> bacteriostatic)
62
vanc use
gram + only
63
vanc ADR
red man sx; nephrotoxicity, ototoxicity, thrombophlebitis
64
vanc resistance
bacteria change walls to d-ala-d-lac
65
protein synthesis inhibitors
specifically target smaller bacterial ribosome (70s, made of 30s and 50s), leaving human ribosomes unaffected
66
30s inhibitors
aminoglycosides (bactericidal); tetracyclines (bacteriostatic)
67
50s inhibitors
Chloramphenicol, Clindamycin (bacteriostatic)
Erythromycin (bacteriostatic)
Linezolid (variable)
68
protein synthesis inhibitors mnemonic
Buy AT 30, CCEL at 50
69
aminoglycosides MOA
bactericidal;
irrev. inhibition of initiation complex thru binding of 30s subunit.
Can cause misreading of mRNA; block translocation.
Require O2 for uptake-->INACTIVE AGAINST ANAEROBES
70
aminoglycosides use
severe G- rod infections. synergistic w/ b-lactam abx
71
neomycin
prophylaxis for bowel surgery
72
aminoglycoside ADR
nephrotoxicity, neuromuscular blockade, ototoxicity
teratogen
73
aminoglycoside method of resistance
bacterial transferase enzymes inactivate drug by acetylation, phosphorylation, or adenylation
74
tetracyclines
(bacteriostatic) bind 30s and prevent attachment of aminoacyl-tRNA;
limited CNS penetration
75
Doxycycline pts
can be used in pts with renal failure due to fecal elimination
76
Tetracycline drug interactions
milk, antacids, iron preparations b/c divalent cations inhibit drugs absorption in drugs
77
tetracycline use
Borrelia burgdorferi, M pneumoniae
accumulates intracellularly --> Rickettsia, Chlamydia
acne tx
78
tetracycline ADR
discoloration of teeth and inhibition of bone growth in children
photosensitivity
***contraindicated in pregnancy***
79
Chloramphenicol MOA
blocks peptidyltransferase at 50s (bacteriostatic)
80
Chloramphenicol use
Meningitis, Rocky mounted spotted fever
81
chloramphenicol ADR
anemia, aplastic anemia, ***gray baby syndrome**
82
gray baby sx cause
premie infants bc lack liver UDP-glucuronyl transferase
83
Chloramphenicol mech. of resistance
plasmid-encoded acetyltransferase inactivates drug
84
Clindamycin MOA
blocks peptide transfer (translocation) at 50s (bacteriostatic)
85
Clindamycin use
anaerobic infections (aspiration pneumonia, lung abscesses, oral infections)
invasive GAS infection
86
Clindamycin versus metronidazole
clindamycin treats ABOVE diaphragm
metronidazole BELOW diaphragm
87
Clindamycin ADR
pseudomembranous colitis, fever, diarrhea
88
Linezolid MOA
inhibit protein synthesis by binding 50s and preventing formation of initiation complex
89
Linezolid use
G+ including MRSA and VRE
90
Linezolid ADR
bone marrow suppression (thrombocytopenia); peripheral neuropathy; serotonin syndrome
91
linezolid mech of resistance
pt mutation of ribosomal RNA
92
macrolides MOA
inhibit protein synthesis by blocking translocation; bind to 23s rRNA of 50s (bacteriostatic)
93
macrolides use
atypical pneumonia (Mycoplasma, Chlamydia, Legionella), STIs (chlamydia), gram + cocci, B pertussis
94
Macrolides ADR
GI motility issue; arrhythmia (prolonged QT interval); acute cholestatic hepatitis; rash; eosinophilia
95
Macrolides drug interactions
increases serum concentration of theophylline, oral anticoag.
Clarithromycin and emycin inhibit cyp450
96
Macrolides mechanism of resistance
methylation of 23S rRNA-binding site prevents binding of drug
97
Sulfonamides MOA
inhibit dihydropteroate synthesis, thus inhibiting folate synthesis (bacteriostatic)
98
when does sulfonamide become bacteriocidal?
combined with trimethoprim
99
sulfonamide use
G+/-, nocardia, chlamydia
100
SMX use
simple UTI
101
Sulfonamide mech of resistance
altered enzyme (bacterial dihydropteroate synthase), dec uptake, inc PABA synthesis
102
Dapsone MOA
similar to sulfonamides, but structurally distinct agent
103
Dapsone use
leprosy, pneumocystis jirovecii prophylaxis
104
Dapsone ADR
hemolysis if G6PD deficient
105
Trimethoprim MOA
inhibits bacterial dihydrofolate reductase (bacteriostatic)
106
Trimethoprim use
used in combo with SMX, causing sequential block of folate synthesis
combo tx: UTI, shigella, salmonella, pneumocystis tx and prophylaxis, toxo prophylaxis
107
trimethoprim ADR
megaloblastic anemia, leukopenia, granulocytopenia
108
FQN MOA
inhibit prokaryotic enzymes Topoisomerase II (dna gyrase) and topoisomerase IV. (bacteriocidal)
109
FQN drug interaction
CANT use antacids
110
FQN use
G - rods of urinary and GI tracts, Neisseria, some + positive organisms
111
FQN ADR
contraindicated in pregnant women, nursing mothers, and kids under18 for cartilage damage
tendonitis in 60+ and in pts taking pred
112
FQN mechanism of resistance
Chromosome-encoded mutation in DNA gyrase, plasmid-mediated resistance, efflux pumps.
113
Daptomycin MOA
lipopeptide that disrupts cell membrane of gram + cocci
114
daptomycin use
MRSA skin infections, bacteremiam endocarditis, VRE
115
Daptomycin cant be used in what dx?
pneumonia, inactivated by surfactant
116
Daptomycin ADR
myopathy, rhabdomyolysis
117
Metronidazole use
forms toxic free radical metabolites in the bacterial cell that damage DNA. (bactericidal, antiprotozoal)
118
Metronidazole use
Tx Giardia, Entamoeba, Trichomonas, Gardnerella vaginalis, anaerobes (Bacteroides, C diff).
Used with PPI and clarithromycin for triple therapy against H pylori
119
Metronidazole ADR
disulfiram-like rxn (severe flushing, tachycardia, hypotension)
HA, metallic taste
