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FOM Antibiotics Flashcards

1
Q

Name the Beta-Lactams

Bactericidal vs bacteristatic

A

Penicillins, Cephalosporins, Carbapenems, Azteronam

bactericidal

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2
Q

What are Penicillin Binding Proteins

A

Transpeptidases that catalyze cell wall synthesis

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3
Q

What site do penicillins occupy on PBPs? What does this do?

A

D-alanyl-D-alanine
Block cell wall synthesis leading to an increase in cell wall precursors and autolytic enzymes. In hypotonic solutions, the cell will swell and burst.

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4
Q

What type of clearance does penicillin have?

A

Renal

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5
Q

Penicillin Spectrum?

A

Gram (+) & Few Gram (-)

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6
Q

What is Penicillin administered with to increase its half-life and how does it work?

A

Probenecid - impairs renal secretion of weak acids

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7
Q

Penicillin in high doses causes what reaction?

A

seizures

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8
Q

Oral Penicillin

A

Penicillin V

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9
Q

IV penicillin

A

Penicillin G

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10
Q

What is benzathine? Describe administration and side effects.

A

Long acting form of Penicillin
IM administration for slow absorbance
Irritation and Local Pain

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11
Q

Penicillin side effects

A

Hypersensitivity (rash -> anaphylaxis)
Seizures (crosses BBB)
Nausea
Diarrhea

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12
Q

List Penicillinase Resistant Penicillins (Structural Change) and how they are resistant

A

Nafcillin, Dicloxacillin, and Methicillin (no longer used)

larger R-groups so that penicillinases cannot inhibit

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13
Q

Penicillinase Resistant Penicillin (structural change) spectrum?

A

MSSA (methicillin susceptible Staphylococcus Aureus)

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14
Q

List Penicillinase Resistant Penicillins (inhibitors) and how they are resistant

A

Clavulanate (Taken in Combination with Penicillin because binds irreversibly with penicillinase allowing penicillin to be an effective drug)
Sublactam
Tazobactam

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15
Q

List Aminopenicillins and the Penicillinase Resistant Penicillins they are administered with

A

Ampicillin (+ Sublactam)

Amoxicillin (+Clavulanate)

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16
Q

Describe Aminopenicillins (including spectrum and mode of action)

A

Penicillinase susceptible, works on Gram (-) bacteria which are intrinsically resistant to penicillin due double membrane/decreased uptake
Aminopenicillins are water soluble and pass through porin channels
H. Influenza, E. Coli, Lysteria, Salmonella

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17
Q

List Antipseudomonals and the PRP’s they are administered with

A

Ticarcillin (+clavulanate)

Piperacillin (+tazobactam)

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18
Q

Antipseudomonal spectrum

A

Broad activity of both gram positive and gram negative including gram (-) bacilli
Pseudomonas

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19
Q

Which Beta-lactams are penicillinase susceptible

A

Penicillin V, Penicillin G, Benzathine, Ampicillin, Amoxicillin, Ticarcillin, Pipercillin

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20
Q

Which Beta-lactams are extended spectrum Beta-lactamase sensitive

A

Aztreonam, Cephalosporins

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21
Q

Which Beta-lactams are cephalosporinase sensitive?

A

Cephalosporins

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22
Q

Which Beta-lactams are Carbapenemase susceptible?

A

Carbapenems

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23
Q

Ampicillin is associated with which condition?

A

Pseudomembranous Colitis

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24
Q

Which antibiotic should be used for penicillin all penicillin allergies?

A

Aztreonam

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25
Q

What causes a pencillin allergic reaction in patients?

A

Formation of a hapten-protein from B-lactams combining with patient’s proteins and stimulating an immune response

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26
Q

How common is penicillin induced anaphylaxis?

A

0.05% of the population

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27
Q

How do beta-lactamases work?

A

Inhibit the beta-lactam ring

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28
Q

What are subcategories of Beta-lactamases?

A

cephalosporinases, penicillinases, carbapenimases

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29
Q

What are extended spectrum beta-lactamases?

A

recognize most beta-lactams and are common in gram negative bacteria

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30
Q

What antibiotic can be used for patients with a mild penicillin allergy?

A

Cephalosporinase

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31
Q

What is the structure of Aztreonam?

A

monocyclic beta-lactam

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32
Q

What is Aztreonam’s spectrum?

A

Gram negative rods

klebsiella, pseudomonas, serratia

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33
Q

What are cephalosporins susceptible to?

A

cephalosporinases and extended spectrum beta lactamases

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34
Q

What is aztreonam susceptible to?

A

extended spectrum beta-lactamases

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35
Q

In what format is cephalosporin administered?

A

oral

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36
Q

where are cephalosporins excreted?

A

kidney

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37
Q

Describe 1st generation cephalosporins

A

Cephlexin
Gram (+) cocci
surgical prophylaxis
don’t use for CNS infections - crosses BBB

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38
Q

Describe 2nd generation cephalosporins

A

Cefoxitin
Gram (-) activity (limited Gram (+) activity)
use immediately prior to surgery to prevent infection
doesn’t cross BBB
inhibits clotting factors and can prolong bleeding
causes disulfram-like (hangover) symptoms when co-administered with ethanol

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39
Q

Describe 3rd generation cephalosporins

A

Ceftriaxone
streptococci and more serious gram (-) infections resistant to other beta-lactams
crosses BBB
used in meningitis
interacts with calcium containing medications to form crystals that precipitate in the lungs and kidneys

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40
Q

Describe 4th generation cephalosporins

A

cefepime
broadest spectrum
gram (+) & (-) including pseudomonas

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41
Q

Describe 5th generation cephalosporins

A

ceftaroline
binds to penicillin binding protein 2a present in MRSA which has low affinity for other beta-lactams
hospital acquired pneumonia
acute bacterial skin infections

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42
Q

Name the carbapenems

A

Imipenem/Cilastatin (administered together)

meropenem

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43
Q

Why are imipenem and cilastatin always adminstered together?

A

imipenem can be broken down to a toxic nephrotoxic metabolite
cilastatin prevents this break down by decreasing cleavage of the B-lactam ring by renal dehydropeptidase

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44
Q

Carbapenem Spectrum

A

broad spectrum

MRSA is resistant

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45
Q

Carbapenem is administered…

A

parenterally

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46
Q

What are possible side effects:

A

With renal dysfunction: seizures

GI distress can occur

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47
Q

Resistance to Carbapenem?

A

Carbapenemase
Klebsiella pneumonia transmits carbapenemase through horizontal gene transfer and is spreading across the country. The plasmid contains genes knocking out aminoglycosides, fluorquinolines, bactrim

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48
Q

List non beta-lactam cell wall synthesis inhibitors

A

Vancomycin, bacitracin, polymixin B, Daptomycin

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49
Q

Vancomycin mechanism

A

binds D-alanyl-D-alanine terminus of cell wall precursor and inhibits release from the bactophrenol carrier
prevents transglycosylase reaction and cell wall synthesis

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50
Q

Vancomycin spectrum

A

gram positive – NARROW

MRSA & c. diff

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51
Q

Vancomycin absorption

A

poor absorption: oral vanco should only be used for c. diff

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52
Q

Vancomycin side effects

A

red man syndrome (hypersensitivity)
nephrotoxicity
dosage adjusted in renal insufficiency

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53
Q

Vancomycin resistance

A

Enterococci
replaces alanine with serine or lactate to prevent binding
some staphylococci have learned vanco-resistance

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54
Q

Bacitracin mechanism

A

prevents dephosphorylation of bactophrenol carrier needed for elongation
cell wall precursors aren’t flipped out of the cytosol

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55
Q

Bacitracin is administered…

A

topical opthalmic and derm preps

poor bioavailability

56
Q

Bacitracin side effects

A

nephrotoxic when given IM

57
Q

Bacitracin Resistance

A

Resistance is rare

58
Q

Polymixin B Mechanism

A

binds to LPS in the membrane and creates holes which release cell contents

59
Q

Polymixin B Spectrum

A

Multidrug Gram negative Bacilli
pseudomonas aeruginosa
klebsiella pneumoniae
Used in combo with other antibiotics to facilitate entry

60
Q

Polymixin B side effects

A

severe nephrotoxicity

61
Q

Polymixin B resistance

A

infrequent to develop resistance and no cross-resistance

62
Q

Daptomycin Mechanism

A

binds to the cell membrane, aggregates, membrane depolarizes, cell dies

63
Q

Daptomycin Spectrum

A

gram-positive organism

vanco resistant and MRSA

64
Q

Daptomycin side effects

A

pneumonia binds pulmonary surfactant and accumulates in pulmonary spaces

65
Q

Daptomycin Resistance

A

addition of a positive charged lysine to the cell surface repels the positively charged drug

66
Q

Rifampin Mechanism

A

Bactericidal

binds bacterial RNA Polymerase abd block mRNA elongation

67
Q

Rifampin spectrum

A

mycobacteria TB

68
Q

Rifampin resistance

A

intrinsic: drug can’t bind the beta subunit of RNA-P
acquired: mutations in rpoB gene

69
Q

Rifampin side effects

A

GI
metabolite turns body fluids orange
CYP3A4 induces metabolism of other medicine leading to organ rejection, seizure loss of control, and risk of pregnancy

70
Q

Fidoxamicin mechanism

A

bactericidal inhibits RNA P

71
Q

Fidoxamicin spectrum

A

gram positive anaerobes (c. diff)

72
Q

Fidoxamicin side effects

A

few due to low absorption

73
Q

Fidoxamicin resistance

A

point mutations in RNA-P

74
Q

Fluoroquinolones List

A

ciprofloxacin, levofloxacin, moxifloxacin

75
Q

Fluoroquinolones mechanism

A

bactericidal
creates DS breaks
bind and inhibit topoisomerase II (gram -) and IV (Gram + – during mitosis)

76
Q

Fluoro spectrum

A

gram (+) & (-) and mycoplasma

77
Q

fluoro is prescribed for….

A

hospital acquired pneumonia

UTI

78
Q

fluoro resistance

A

overprescribed
active drug efflux
mutations in topoisomerase

79
Q

Ciprofloxacin public use

A

biological warfare

80
Q

Fluoro side effects

A

GI
confusion
C. diff and Candida vaginitis
contraindicated in pregnant and breasting feeding women as well as children (arthoropathy)

81
Q

fluoro should not be taken with…

A

chelates cations so don’t take with calcium, aluminum, iron, and zinc
avoid dairy products

82
Q

Sulfondamide list

A

sulfamethoxazole, sulfisoxazole

83
Q

Sulfonamide spectrum and action

A

acts on bacteria/fungi/protozoa that make their own FH4
bacteriostatic
PABA analog and competitively inhibits dihydropteroate synthetase

84
Q

sulfonamide resistance

A

change dihydropteroate synthase, increase PABA, increase drug effluxf

85
Q

Sulfonamide side effects

A

hypersensitivity: rash, cross reaction
crystalluria leading to acute renal failure
hemolysis of RBCs if G6P dehydrogenase is deficient
kernicterus: neurologic condition where sulfonamides compete for albumin in newborns causing bilirubin buildup in the brain

86
Q

Trimethoprim mechanism

A 
bacteriostatic
inhibits DHFR (dihydrofolate reductase)
87
Q

trimethoprim resistance

A

altered DHFR, increased DHFR, alternative metabolic pathway

88
Q

trimethoprim side effects

A

GI

89
Q

What is Bactrin and what is the mechanism?

A

Trimethoprim & sulfamethoxazole

bactericidal

90
Q

Bactrin treats…

A

UTI, pneumocystis

91
Q

Metronidazole mechanism

A

bactericidal

when it is reduced, it generates free radicals leading to DS breaks and cell death

92
Q

Metronidazole spectrum

A

anaerobic bacteria

93
Q

Metronidazole resistance

A

down regulation of pyruvate:ferredoxin oxidoreductase that reduces metronidazole to its toxic radical state

94
Q

Metronidazole side effects

A

nausea, diarrhea, headache, metallic taste
avoid during pregnancy
disulfram-like reaction with alcohol
build up of acetaldehyde due to inhibition of acetaldehyde dehydrogenase

95
Q

Nitrofurantoin mechanism

A

bactericidal
reduced by bacterial flavoproteins to reactive intermediates which inactivate or alter bacterial ribosome proteins to inhibit DNA, RNA, protein, and cell wall synthesis

96
Q

Nitrofurantoin spectrum

A

broad

rapidly excreted so used for UTI’s

97
Q

Nitrofurantoin resistance

A

no resistance because it inhibits so many different mechanisms

98
Q

nitrofurantoin adverse effects

A

vomiting and rash

99
Q

Oxazolidinone main antibiotic

A

Linezolid

100
Q

Linezolid Mechanism

A

Bacteriostatic
Binds 50S ribosome at the P-site
Binds 23S rRNA & inhibits the initiation complex

101
Q

Linezolid Spectrum

A

Gram (+)

MRSA and Vancomycin Resistant Enterococci

102
Q

Linezolid Resistance

A

Mutation in 23S rRNA

Not much cross resistance because of its unique binding site

103
Q

Linezolid Side Effects

A

Bone Marrow Suppression
Inhibits Monoamine Oxidase which can lead to Serotonin Syndrome if taken with Selective Serotonin Reuptake Inhibitor (SSRI).
- SYMPTOMS: anxiety, hallucinations, nausea, increased heartbeat

104
Q

List the aminoglycoides

A

Gentamicin, Tobramycin, Amikacin

105
Q

Aminoglycoside mechanism & discuss their ability to enter the cell

A

Bactericidal
Binds 30S Ribosomal Subunit
Inhibits initiation, increase mRNA misreading, induces early termination
NEEDS ATP to get into the cell –> aminoglycosides are cations and polar so they don’t cross the PM well. Additionally, they cannot enter the CSF

106
Q

Aminoglycoside Spectrum

A

Broad Spectrum

107
Q

Aminoglycoside Resistance

A

Intrinsic: Aminoglycosides cannot cross the PM in anaerobes and in high pH environments – must be administered with cell wall synthesis attacking antibiotics

Acquired: adenylation, phosphorylation, or acetylation of aminoglycosides for inactivation

108
Q

Amikacin Resistance

A

Are immune to enzymatic inactivation and are a broader spectrum than most other aminoglycosides (can be used for pseudomonas infections)

109
Q

Aminoglycoside Side Effects

A

Tubular Necrosis
Nephrotoxic (should not be given with vancomycin or loop diuretics)
Ototoxicity - vestibular and auditory disfunction
Pregnancy Class D (deafness in fetus)

110
Q

List the Tetracyclines

A

Tetracycline, Doxycycline, minocycline, demeclocycline

111
Q

Concentration Dependent Antibiotics

A

Aminoglycosides, fluoroquinolones

112
Q

Time Dependent Antibiotics

A

Beta-lactams, vancomycin

113
Q

Describe the Persister Phenotype

A

Drug tolerance distinct from resistance
Genetically homogenous forms of bacteria shift between phenotypes
Go into hibernation phenotype while the drug is being administered

114
Q

Tetracycline Mechanism

A

Bacteriostatic
Binds the 30S ribosome at the A-site
prevent attachment of aa-tRNA

115
Q

Tetracycline Spectrum

A

Broad including H. Pylori, B. Burgdorferi, chlamydia, mycoplasma

116
Q

Tetracycline Resistance

A

Increased Efflux

Ribosomal Protection Proteins block the A-site so tetracyclines can’t bind

117
Q

Tetracycline Side Effects

A

Forms stable chelates with Al, Mg, Fe, & Ca
should be taken without food
GI
phototherapy sensitive
teeth discoloration and inhibition of long bone growth in children
pregnancy class D

118
Q

Chloramphenicol Mechanism

A

Bacteriostatic

Binds 50S and inhibits peptidyltransferase and peptide bond formation

119
Q

Chloramphenicol Spectrum

A

Broad but limited use due to side effects

120
Q

Chloramphenicol Resistance

A

Inactivated by acetyltransferases

Decreased membrane permeability

121
Q

Chloramphenicol Side Effects

A

Bone marrow depression
aplastic anemia
Gray Baby Syndrome (infants don’t have glucuronidyl transferase or hepatic enzymes leading to high levels of drug accumulation – cardiovascular and respiratory collapse)

122
Q

List the Macrolides

A

Erythromycin, Azithromycin, Clarithromycin

123
Q

Macrolides Mechanism

A

Bacteriostatic
Bind 50s P-site (prohibits translocation during elongation)
bind 23s rRNA

124
Q

Macrolides Spectrum

A

Respiratory pathogens
pharyngitis, pneumonia, otitis media
chlamydia (one dose)

125
Q

Macrolides Resistance

A

Methylation of 23s rRNA (cross resistance with lincosamides & streptogramins)
increased efflux
hydrolysis by esterases

126
Q

Macrolides Side effects

A
  • GI upset
  • Erythromycin and Clarithromycin inhibit CYP3A4 leading to a decrease in drug metabolism and hepatic failure
  • clarithromycin - class D pregnancy
  • Azithromycin - pyloric stenosis in children under 6 months old
127
Q

What antibiotics should be used to treat mycoplasma?

A

Levofloxacin, azithromycin, doxycycline

128
Q

what is the regiment for treating lymes disease?

A

Adults: 10 days of doxycycline
Children: 5 days of doxycycline

129
Q

Lincosamide main antibiotic

A

Clindamycin

130
Q

Clindamycin Mechanism

A

Bacteriostatic
Bind 50S P-site (inhibits translocation during elongation)
23s rRNA

131
Q

Clindamycin Spectrum

A

Gram (+)
include anaerobes
skin infections
acne

132
Q

Clindamycin Resistance

A

Methylation of 23s rRNA (Cross resistance with macrolides and streptogramins)
Adenylation inactivates
ribosomal mutation

133
Q

Clindamycin Side Effects

A

GI discomfort, abdominal pain, blood and mucus in stool, diarrhea, superinfection with C. diff, hypersensitivity: rash

134
Q

Streptogramins major antibiotics

A

Quinupristin, Dalfoprisitin (should be taken together)

135
Q

Streptogramins Mechanism

A

bactericidal for some organisms
bind 50s P-site (inhibit translocation during elongation)
bind 23s rRNA

136
Q

Streptogramins Resistance

A

methylation of 23s rRNA (cross resistance with macrolides and clindamycin)
enzyme inactivation
increased efflux

137
Q

Streptogramins side effects

A 
inhibit CYP3A4 (can't metabolize -- can lead to renal failure)
arthralgias (joint pain)

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