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Antibiotics Flashcards

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1
Q

which penicillins are penicillinase sensitive (3)

A

penicillin G and V
ampicillin
amoxicillin

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2
Q

which penicillins are penicillinase resistant (3)

A

oxacillin
naficillin
dicloxacillin

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3
Q

mechanism penicillin

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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4
Q

clinical use penicillin (3)

A
  1. gram positive (S. pneumo, S. pyogenes, Actinomyces)
  2. N. meningitidis
  3. Syphillis
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5
Q

is penicillin bactericidal or bacteriostatic?

A

bactericidal

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6
Q

side effects penicillin (2)

A
  1. hypersensitivity

2. hemolytic anemia

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7
Q

mechanism of resistance to penicillin

A

penicillinase (beta-lactamase) cleaves beta-lactam ring

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8
Q

ampicillin / amoxicillin mechanism

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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9
Q

what do you combine ampicillin / amoxicillin with?

A

clavulanic acid (protect against beta-lactamase)

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10
Q

which has greater oral bioavailability, amoxicillin or ampicillin?

A

amoxicillin

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11
Q

which has wider spectrum, penicillin or ampicillin/amoxicillin?

A

ampicillin/amoxicillin

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12
Q

clinical use ampicillin / amoxicillin

A 
H. influenzae
E. coli
Listeria
Proteus
Salmonella
Shigella
Enterococci
(HELPSS kill enterococci)
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13
Q

side effects ampicillin / amoxicillin (2)

A
  1. hypersensitivity

2. pseudomembranous colitis

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14
Q

mechanism of resistance to ampicillin / amoxicillin

A

penicillinase (beta-lactamase) cleaves beta-lactam ring

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15
Q

what are three penicillinase-resistant penicillins?

A
  1. oxacillin
  2. nafcillin
  3. dicloxacillin
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16
Q

mechanism of penicillinase-resitstant penicillins

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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17
Q

which has a wider spectrum, penicillin or penicillinase-resistant penicillins?

A

penicillin

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18
Q

why are penicillinase-resistant penicillins resistant to penicillinase?

A

bulky R group blocks beta-lactamase access to ring

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19
Q

clinical use penicillinase-resistant penicillins

A

S. aureus (except MRSA)

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20
Q

how is MRSA resistant to penicillinase-resistant penicillins?

A

altered penicillin-binding protein target site

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21
Q

side effects penicillinase-resistant penicillins

A
  1. hypersensitivity

2. interstitial nephritis

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22
Q

what two drugs are antipseudomonals?

A
  1. ticarcillin

2. piperacillin

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23
Q

mechanism antipseudomonals

A

blocks cross-linking of peptidoglycan by binding penicillin-binding proteins (transpeptidases)

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24
Q

which has a wider spectrum, penicillin or antipseudomonals?

A

antipseudomonals

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25
clinical use antipseudomonals (2)
1. Pseudomonas | 2. gram-negative rods
26
what do you give antipseudomonals with?
beta-lactamase inhibitors (antipseudomonals are susceptible to penicillinase)
27
side effect antipseudomonals
hypersensitivity
28
what are three beta-lactamase inhibitors?
1. clavulanic acid 2. sulbactam 3. tazobactam (CAST)
29
what do beta-lactamase inhibitors do
protect penicillin antibiotics from destruction by beta-lactamase (penicillinase)
30
cephalosporin mechanism
beta-lactam drugs --> inhibit cell wall synthesis | less susceptible to penicillinases
31
are cephalosporins bacteriostatic or bactericidal?
bactericidal
32
organisms not covered by cephalosporins
``` Listeria Atypicals (chlamydia, mycoplasma) MRSA Enterococci (LAME) ```
33
what cephalosporin covers MRSA?
ceftaroline
34
what are two 1st generation cephalosporins?
1. cefazolin | 2. cephalexin
35
what are three 2nd generation cephalosporins?
1. cefoxitin 2. cefaclor 3. cefuroxime
36
what are three 3rd generation cephalosporins?
1. ceftriaxone 2. cefotaxime 3. ceftazidime
37
what is one 4th generation cephalosporin?
cefepime
38
what is one 5th generation cephalosporin?
ceftaroline
39
clinical use 1st generation cephalosporins (5)
1. gram positive cocci 2. Proteus 3. E. coli 4. Klebsiella 5. prior to surgery to prevent S. aureus wound infections PEcK
40
clinical use 2nd generation cephalosporins (7)
1. H. influenzae 2. Enterobacter 3. Neisseria 4. Proteus 5. E. coli 6. Klebsiella 7. Serratia
41
clinical use 3rd generation cephalosporins
serious gram-negative infections (resistant to other things
42
clinical use ceftriaxone (2)
1. meningitis | 2. gonorrhea
43
clinical use ceftazidime
Pseudomonas
44
clinical use 4th generation cephalosporins
1. greater activity against Pseudomonas | 2. greater activity against gram positive
45
clinical use 5th generation cephalosporins
broad coverage, including MRSA | does NOT cover Pseudomonas
46
side effects cephalosporins
1. hypersensitivity 2. vitamin K deficiency 3. increases nephrotoxicity of aminoglycosides (low cross-reactivity with penicillins
47
mechanism aztreonam
prevents peptidoglycan cross-linking by binding penicillin-binding protein 3 --> resistant to beta-lactamases
48
does aztreonam have any cross-allergenicity with penicillins?
NO!!!
49
what other antibiotic is aztreonam synergistic with?
aminoglycosides
50
what two groups of people is it useful to use aztreonam for?
1. penicillin allergies | 2. renal insufficiency who can't use aminoglycosides
51
is aztreonam susceptible to beta-lactamases?
NO!!
52
clinical use aztreonam
ONLY gram negative rods
53
side effect aztreonam
GI upset
54
what are four carbapenems?
1. imipenem 2. meropenem 3. ertapenem 4. doripenem
55
mechanism imipenem
broad-spectrum, beta-lactamase resistant carbapenem
56
what do you administer imipenem with?
cilastatin (inhibits renal dehydropeptidase I to decrease inactivation of drug in renal tubules)
57
what is cilastatin?
inhibits renal dehydropeptidase I to decrease inactivation of imipenem in renal tubules
58
clinical use carbapenems (3)
1. gram-positive cocci 2. gram-negative rods 3. anaerobes ONLY use in life-threatening infections b/c of side effects
59
which carbapenem has a decreased risk of seizures
meropenem
60
side effects carbapenems (3)
1. GI distress 2. rash 3. CNS toxicity (seizures)
61
vancomycin mechanism
inhibits cell wall peptidoglycan formation by binding D-ala D-ala
62
is vancomycin bacteriostatic or bactericidal?
bactericidal
63
clinical use vancomycin
gram-positive ONLY | use for multidrug-resistant organisms (i.e. MRSA, enterococci, and C. difficile)
64
how do you administer vancomycin to treat pseudomembranous colitis?
oral
65
side effects vancomycin (4)
1. Nephrotoxicity 2. Ototoxicity 3. Thrombophlebitis NOT 4. red man syndrome
66
what drug causes red man syndrome
vancomycin
67
how do you prevent red man syndrome
pretreatment with antihistamines | slow infusion rate
68
mechanism of resistance to vancomycin
modification of D-ala D-ala to D-ala D-lac in cell wall precursors
69
what protein synthesis inhibitors act on the 30S subunit?
Aminoglycosides | Tetracyclines
70
are aminoglycosides bacteriostatic or bactericidal?
bactericidal
71
are tetracyclines bacteriostatic or bactericidal?
bacteriostatic
72
what protein synthesis inhibitors act on the 50S subunit?
Chloramphenicol Clindamycin Erythromycin (macrolides) Linezolid
73
is chloramphenicol bacteriostatic or bactericidal?
bacteriostatic
74
is clindamycin bacteriostatic or bactericidal?
bacteriostatic
75
is erythromycin bacteriostatic or bactericidal?
bacteriostatic
76
what are five aminoglycosides?
1. Gentamicin 2. Neomycin 3. Amikacin 4. Tobramycin 5. Streptomycin GNATS
77
mechanism aminoglycosides
inhibit formation of initiation complex cause misreading of mRNA block translocation
78
are aminoglycosides useful against anaerobes?
NO!! | require O2 for uptake into cells
79
are aminoglycosides bacteriostatic or bactericidal?
bactericidal
80
clinical use aminoglycosides
severe gram-negative rods
81
what are aminoglycosides synergistic with?
beta-lactam antibiotics
82
what drug is useful for bowel surgery?
neomycin
83
side effects aminoglycosides (4)
1. Nephrotoxicity (esp. if use with cephalosporins) 2. Neuromuscular blockade 3. Ototoxicity (esp. if use with loop diuretics) 4. Teratogen
84
mechanism of resistance to aminoglycosides
bacterial transferase enzymes inactivate the drug (via acetylation, phosphorylation, or adenylation)
85
what are three tetracyclines?
1. tetracycline 2. doxycycline 3. minocycline
86
are tetracyclines bacteriostatic or bactericidal?
bacteriostatic
87
mechanism tetracyclines
prevent attachment of aminoacyl-tRNA
88
do tetracyclines enter the CNS well?
NO!!!
89
what type of patients is doxycycline useful for?
renal failure (doxycycline is fecally eliminated)
90
what should you not eat when taking tetracyclines?
milk (Ca), antacids (Ca or Mg), or iron-containing preparations divalent cations inhibit tetracycline absorption from gut
91
clinical use tetracyclines (3)
1. Borrelia burgdorferi 2. M. pneumoniae 3. Chylamydia and Rickettsia (accumulates intracellularly)
92
side effects tetracyclines (3)
1. GI distress 2. discoloration of teeth and inhibition of bone growth in children 3. photosensitivity
93
who are tetracyclines contraindicated in?
pregnancy
94
mechanism of resistance to tetracyclines
decrease uptake or increase efflux out of bacterial cells by plasmid-encoded transport pumps
95
how is resistance to tetracyclines encoded?
plasmid
96
what are three macrolides
1. azithromycin 2. clarithromycin 3. erythromycin
97
mechanism macrolides
block translocation | bind to the 23S rRNA of the 50S ribosomal subunit
98
are macrolides bacteriostatic or bactericidal?
bacteriostatic
99
clinical use macrolides (3)
1. atypical pneumonia (Mycoplasma, Chlamydia, Legionella) 2. STDs (Chlamydia) 3. gram-positive cocci (strep in pts allergic to penicillin)
100
side effects macrolides (5)
1. GI Motility issues 2. Arrhythmias (prolonged QT 3. acute Cholestatic hepatitis 4. Rash 5. eOsinophilian MACRO
101
what do macrolides increase the serum concentration of?
theophyllines (oral anticoagulants)
102
mechanism of resistance to macrolides
mehylation of 23S rRNA binding site
103
mechanism chloramphenicol
blocks peptidyltransferase
104
is chloramphenicol bacteriostatic or bactericidal?
bacteriostatic
105
clinical use chloramphenicol (2)
1. meningitis (H. influenzae, N. meningitidis, S. pneumo) | 2. Rocky Mountain spotted fever
106
where is chloramphenicol used?
developing countries (side effects)
107
side effects chloramphenicol
1. anemia (dose dependent) 2. aplastic anemia (dose independent) 3. gray baby syndrome (premature babies lack liver UDP-glucoronyl transferase)
108
can you use chloramphenicol in premature babies?
NO!! | gray baby syndrome (premature babies lack liver UDP-glucoronyl transferase)
109
mechanism of resistance to chloramphenicol
plasmid-encoded acetyltransferase inactivates the drug
110
how is resistance to chloramphenicol encoded?
plasmid
111
mechanism clindamycin
blocks peptide transfer (translocation)
112
is clindamycin bacteriostatic or bactericidal?
bacteriostatic
113
clinical use clindamycin (2)
1. anaerobic infections (i.e. Bacteroides, Clostridium perfringens) 1a. aspiration pneumonia 1b. lung abscesses 1c. oral infections 2. invasive group A strep
114
which part of the body do you treat anaerobes with clindamycin?
above the diaphragm
115
which part of the body do you treat anaerobes with metronidazole?
below the diaphragm
116
side effects clindamycin (3)
1. pseudomembranous colitis (C. difficile) 2. fever 3. diarrhea
117
mechanism sulfonamides
inhibit folate synthesis | PABA antimetabolites inhibit dihydropteroate synthase
118
are sulfonamides bacteriostatic or bactericidal?
bacteriostatic
119
clinical use sulfonamides
1. gram positive 2. gram negative 3. Nocardia 4. Chlamydia 5. simple UTI (triple sulfas or SMX)
120
side effects sulfonamides
1. hypersensitivity 2. hemolysis if G6PD deficient 3. nephrotoxicity (tubulointerstitial nephritis) 4. photosensitivity 5. kernicterus in infants
121
what do sulfonamides do to other drugs?
displaces other drugs from albumin (i.e. warfarin)
122
see person take an antibiotic and then get hemolysis, think....
sulfonamides in a G6PD deficient person!
123
mechanism of resistance to sulfonamides
altered enzyme (bacterial dihydropteroate synthase) decreased uptake increased PABA synthesis
124
mechanism trimethoprim
inhibits bacterial dihydrofolate reductase
125
is trimethoprim bacteriostatic or bactericidal?
bacteriostatic
126
how do you sequentially block folate synthesis?
trimethoprim in combo with sulfonamides (TMP-SMX)
127
clinical use TMP-SMX
1. UTIs 2. Shigella 3. Salmonella 4. Pneumocystic jirovecii pneumonia 5. toxoplasmosis prophylaxis
128
side effects trimethoprim
1. megaloblastic anemia 2. leukopenia 3. granulocytopenia - -> may alleviate with folic acid
129
what are some fluoroquinolones?
``` -oxacin ciprofloxacin norfloxacin levofloxacin ofloxacin sparfloxacin moxifloxacin gemifloxacin enoxacin ```
130
what drug is a quinolone?
nalidixic acid
131
mechanism fluoroquinolones
inhibit DNA gyrase (topoisomerase II) and topoisomerase IV
132
are fluoroquinolones bacteriostatic or bactericidal?
bactericidal
133
what should you not take with fluoroquinolones?
antacids
134
what two drugs would you not take with antacids?
1. fluoroquinolones | 2. tetracycline
135
clinical use fluoroquinolones (3)
1. gram negative rods of urinary and GI tracts (including Pseudomonas) 2. Neisseria 3. some gram positive
136
side effects fluoroquinolones (7)
1. GI upset 2. superinfections 3. rash 4. headache, dizziness 5. tendonitis/tendon rupture (esp. in >60 or pts on prednisone) 6. leg cramps and myalgias 7. prolonged QT
137
who are fluoroquinolones contraindicated in?
pregnant women nursing mothers children < 18 (damage to cartilage)
138
who are at risk of tendon rupture on fluoroquinolones?
pts > 60 | pts taking prednisone
139
mechanism of resistance to fluoroquinolones
chromosome-encoded mutation in DNA gyrase plasmid-mediated resistance efflux pumps
140
how is resistance to fluoroquinolones encoded?
chromosome and plasmids
141
mechanism metronidazole
forms free radical toxic metabolites in the bacterial cell --> damages DNA
142
is metronidazole bacteriostatic or bactericidal?
bactericidal
143
clinical use metronidazole
1. Giardia 2. Entamoeba 3. Trichomonas 4. Gardnerella vaginalis 5. anaerobes (Bacteroides, C. difficile) 6. H. pylori GET GAP
144
what is triple therapy for H. pylori
1. metronidazole 2. proton pump inhibitor 3. clarithromycin
145
what is M. tuberculosis prophylaxis?
isoniazid
146
what is M. avium-intracellulare prophylaxis?
azithromycin, rifabutin
147
what is M. tuberculosis treatment?
``` Rifampin Isoniazid Pyrazinamide Ethambutol RIPE ```
148
what is M. avium-intracellulare treatment?
azithromycin OR clarithromycin + ethambutol | can add rifabutin or ciprofloxacin
149
what is M. leprae treatment (tuberculoid)?
long-term dapsone and rifampin
150
what is M. leprae treatment (lepromatous)?
long-term dapsone and rifampin PLUS clofazimine
151
mechanism isoniazid
decrease synthesis of mycolic acids | bacterial catalase-peroxidase (encoded by KatG) needed to convert INH to active metabolite
152
what is needed to activate isoniazid?
bacterial catalase-peroxidase (encoded by KatG) needed to convert INH to active metabolite
153
clinical use isoniazid
M. tuberculosis
154
how does INH half-life vary?
different in fast vs. slow acetylators
155
side effects isoniazid
1. neurotoxicity 2. hepatotoxicity 3. lupus INH Injures Neurons and Hepatocytes
156
how can you prevent neurotoxicity and lupus from isoniazid?
pyridoxine (vitamin B6)
157
what are two rifamycins?
1. rifampin | 2. rifabutin
158
mechanism rifamycins
inhibits DNA-dependent RNA polymerase
159
clinical use rifamycins (3)
1. M. tuberculosis 2. M. leprae (delays resistance to dapsone) 3. prophylaxis in meningococcus and contacts of kids with H. influenzae type B
160
side effects rifamycins
1. minor hepatotoxicity 2. induces P450 3. orange body fluids rapid resistance if used alone!
161
which rifamycin is better to use in patients with HIV?
rifabutin (better than rifampin) because less cytochrome P450 stimulation
162
mechanism pyrazinamide
uncertain may acidify intracellular environment via conversion to pyrazinoic acid effective in acidic pH of phagolysosomes (where TB eaten by macrophages is)
163
clinical use pyrazinamide
M. tuberculosis
164
side effects pyrazinamide (2)
1. hyperuricemia | 2. hepatotoxicity
165
mechanism ethambutol
decrease carbohydrate polymerization of mycobacterium cell wall by blocking arabinosyltransferase
166
clinical use ethambutol
M. tuberculosis
167
side effect ethambutol
optic neuropathy (red-green color blindness)
168
prophylaxis for endocarditis with surgical or dental procedures
penicillins
169
prophylaxis for gonorrhea
ceftriaxone
170
prophylaxis for history of recurrent UTIs
TMP-SMX
171
prophylaxis for meningococcal infection
ciprofloxacin (drug of choice) | rifampin (children)
172
prophylaxis for pregnant women with group B strep
ampicillin
173
prophylaxis for prevention of gonococcal or chlamydial conjunctivitis in newborn
erythromycin ointment
174
prophylaxis for prevention of postsurgical infection due to S. aureus
cefazolin
175
prophylaxis for strep pharyngitis in child with prior rheumatic fever
oral penicillin
176
prophylaxis for syphilis
benzathine penicillin G
177
prophylaxis for CD4 < 200
TMP-SMX (to prevent Pneumocystis pneumonia)
178
prophylaxis for CD4 < 100
TMP-SMX (to prevent Pneumocystis pneumonia and toxoplasmosis)
179
prophylaxis for CD4 < 50
azithromycin (to protect against M. avium)
180
MRSA treatment (5)
1. vancomycin 2. daptomycin 3. linezolid (can cause serotonin syndrome) 4. tigecycline 5. ceftaroline
181
VRE treatment (2)
1. linezolid | 2. streptogramins (quinupristin/dalfopristin)

Pharmacology (8 decks)

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