Antibiotics I Flashcards

1
Q

What do all β-lactam Superfamily of antibiotics target?

A

1) Prevent Crosslinking of peptidoglycan

2) Prevent stable cell wall formation

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2
Q

What is the final outcome of β-lactam’s targeting the bacterial cell wall?

A
  • “popping”

- Due to osmotic differences between the interior/extracellular environment

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3
Q

What are the four major groups of β-lactam’s ?

A

1) Penicillin
2) Cephalosporins
3) Monbactams
4) Carbapenems

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4
Q

What causes β-lactam resistance?

A

1) Changes in the Transpeptidase (PBP) receptor
- Gram + bacteria
- Mechanism of resistance in MRSA

2) Production of beta-lactamase enzymes
- Gram - bacteria

3) Decrease permeability of target bacteria
- Modifications of porins
- Efflux pumps (Pseudomonas)

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5
Q

What do β-lactam antibiotics inhibit?

A
  • Transpeptidase (PBP)

- Thus inhibiting transpeptidation necessary to strengthen cell wall

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6
Q

What is the target of β-lactam antibiotics?

A
  • Transpeptidase (PBP)
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7
Q

T of F

Natural Penicilin has the narrowest spectrum and highly sensitive to Beta Lactamase?

A
  • True
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8
Q

What is Methicillin used for?

A
  • AntiStaphylococcal
  • Not used for Tx
  • Used to ID MRSA
  • Test for Penicillin resistance
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9
Q

What are some adverse effects of Penicillin G, V and Methicillin?

A
  • Hypersensitivity
  • Maculopapular rash
  • GI irritation (Secondary infections C. Diff)
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10
Q

What is Probenecid used for in pharmacology?

A
  • Increases the plasma half life of many antibiotics
  • Blocks the Organic Anion Transport (OAT) in the kidneys
  • Prevents excretion
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11
Q

Why is Pseudomonas resistance to antibiotics?

A
  • Due to efflux pumps
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12
Q

Only Penicillin that could be given PO with food?

A
  • Amoxicillin (Aminopenicillin)
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13
Q

Amoxicillin (Aminopenicillin) commonly prescribed for?

A
  • ENT and UTI infections
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14
Q

What type of infections does Amoxicillin (Aminopenicillin) treat?

A
  • All Gram positive
  • Some Gram Negative (Where Beta Lactamase not expected)
  • Anaerobic infections
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15
Q

What does Clavulanic Acid do?

A
  • Turns off Beta Lactamase allowing for antibiotic to work

- Extends Gram - Spectrum

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16
Q

What are other names for Clavulanic Acid?

A
  • β-clavulanic acid
  • Clavulanate (Augmentin)
  • Beta Lactamase inhibitor
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17
Q

What does the combination Tx of

Amoxicillin + Clavulanic acid

fight off?

A
  • All Gram positive
  • All Gram Negative
  • All Anaerobic infections
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18
Q

T of F

Amoxicillin + Clavulanic acid will fight off Pseudomonas infections?

A
  • False

- Because Pseudomonas has Efflux pumps

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19
Q

What medication is an Antipseudomonal penicillin?

A
  • Piperacillin + Tazobactam (Zosyn)
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20
Q

What does Tazobactam (Zosyn) do to Pseudomonas?

A
  • Inhibits Beta Lactamase
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21
Q

What penicillin has the broadest spectrum and used empirically with organism is not known?

A
  • Piperacillin + Tazobactam (Zosyn)
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22
Q

When is - Piperacillin + Tazobactam (Zosyn) usually use?

A
  • Empirical treatment of serious or life-threatening infections
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23
Q

What coverage does Piperacillin + Tazobactam have?

A
  • Widest spectrum
  • Gram +
  • Gram -
  • Pseudomonas
  • Anaerobes
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24
Q

T of F

Patients with penicillin allergies will be able to take cephalosporins?

A
  • True
  • 90% no reactions
  • 10% might have a reaction administer with caution
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25
Q

What do cephalosporins inhibit?

A
  • Cell wall syn

- Works on Transpeptidase (PBP)

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26
Q

What are Cephalosporins commonly used for?

A
  • Very commonly given as presurgical prophylaxis
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27
Q

Cephalosporins are classified as?

A
  • Bactericidal

- Absolute Selectively Toxic

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28
Q

Cephalosporins first gen treats?

A
  • Gram +

- Some Gram -

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29
Q

What are Cephalosporins inactive against?

A

LAME

  • Listeria
  • Atypicals
  • MRSA
  • Enterococci
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30
Q

T of F

The higher the Cephalosporins generation the wider the spectrum?

A
  • True
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31
Q

What are fourth gen Cephalosporins used for?

A
  • Nosocomial infections
  • IV only
  • Where Beta Lactamase resistance is expected
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32
Q

T of F

3rd and 4th Gen Cephalosporins penetrate the CNS?

A
  • True

- Treats bacterial meningitis

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33
Q

Only monobactam that treats Gram - Rods Pseudomonas Aeruginosa ?

A
  • Aztreonam (Azactam)
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34
Q

Aztreonam (Azactam) is safe to use in pt’s with a penicillin allergy? \

T or F

A
  • True
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35
Q

Aztreonam (Azactam) can penetrate the CNS ?

T or F

A
  • True
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36
Q

What is Imipenem + Cilastatin (Primaxin) used for?

A
  • Treats serious infections

- Broadest spectrum among the Beta Lactam’s

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37
Q

Why is Imipenem given in combination with Cilastatin (Primaxin)?

A
  • Prevents metabolism by renal Dehydropeptidase

- Stabilizes the drug in circulation

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38
Q

T of F

Imipenem + Cilastatin (Primaxin) penetrate the CNS system?

A
  • True
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39
Q

Serious side effect of Imipenem (Carbapenems) ?

A
  • Seizures
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40
Q

Glycopeptides do not treat Gram - bacteria because?

A
  • Very large
  • Too big to cross through porins (transporters) in Gram- bacterial
  • Cannot access the peptidoglycan layer of Gram - bacteria
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41
Q

Most common resistance of cell wall disruptions in bacteria?

A
  • Overproduction of D-ala – D-ala by the bacterium

- Acts as a sponge for the drug

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42
Q

Least common resistance of cell wall disruptions in bacteria?

A
  • Formation of cell walls using D-ala – D-lactate
  • Instead of D-ala – D-ala
  • D-lactate cannot be bound by the drug
43
Q

Vancomycin (Vancocin) binds to what on the bacteria?

A
  • Binds directly to D- Ala - D- Ala Peptid
  • Forms a cap, blocks cross linking
  • Downstream effect, preventing Transpeptidation
  • Now cell susceptible to Osmotic pressure = Cell Lysis
44
Q

Last resort drug from life threatening Gram + bacteria?

A
  • Vancomycin

- Bactericidal

45
Q

What does Vancomycin treat ?

A
  • MRSA Endocarditis

- Bacteremia

46
Q

Can Vancomycin treat Gram - bacteria?

A
  • No

- Too big to cross through Gram - Porins

47
Q

T of F

Vancomycin given PO can treat C. Diff ?

A
  • True
  • Only reason its given PO
  • Usually IV
48
Q

Vancomycin can penetrate the CNS and treat Meningitis?

T of F

A
  • True

- Even treats MRSA Endocarditis

49
Q

What are the two resistance methods of Vancomycin?

A

1) D- Ala - D- Lactate mutation (Least Common)

2) Over production of D- Ala D- Ala (Most Common)

50
Q

What are the three adverse effects of Vancomycin?

A
  • Nephrotoxicity (Most Common)
  • Ototoxcitiy
  • Red Man syndrome (Erythematous rash Face, neck, and upper torso) (Most Obvious)
51
Q

What causes Red man syndrome?

Is it a true allergic reaction? No

A
  • Vancomycin
  • No, its caused by the release of Histamine from Mast Cells
  • Hypotension occurs as well
52
Q

How can you reduce the risk of red man syndrome?

A
  • Slow infusion rate > 60 mins

> 90 mins for high doses

53
Q

How can you counter red man syndrome?

A
  • Antihistamine
54
Q

Where do Protein Syn inhibitors act on?

A
  • Act on the Ribosome sub-units

- Either 30s or 50s

55
Q

What are the three sites of the ribosome?

A

A Site = Docking station

P Site = Reading station

E Site = Exit station, cleaved

56
Q

All Protein syn inhibitors are bacteriostatic except for one class, which one?

A
  • Amnioglycosides which is Bactericidal
57
Q

T of F

Protein syn inhibitors are relatively selective? toxic?

A
  • True
58
Q

How do Protein syn inhibitors work?

A
  • Stick to Teichoic and Lipoteichoic acids present in the peptidoglycan cell wall
  • Disrupt cell wall syn
59
Q

Where does Tetracycline (Doxycycline) bind to on the bacteria?

A
  • 30s subunit
  • A site
  • Prevents binding of incoming tRNA on the mRNA template
60
Q

Why are Tetracycline’s (Doxycycline) contraindicated in pregnant woman and children < 8?

A
  • Co-deposit with calcium in Bone/Teeth

- Causes weaknesses, discoloration, and deformities

61
Q

What blocks the absorption of tetracyclines?

A
  • Divalent cations (Mg2+, Ca2+, Fe2+, Al2+)
  • Antacids, Tums
  • Dairy
62
Q

T of F

Dose adjustments need to be made on pt’s with kidney issues if taking Doxcycline?

A
  • True
63
Q

Where does Doxycycline accumulate ?

A
  • Bile
64
Q

What does Doxycycline treat?

A
  • ENT infections
  • Bronchitis
  • Bladder infections
  • Chlamydia
  • Gonorrhea
  • CA Pneumonia
65
Q

MOA of the microlide Azithromycin ?

A
  • Binds 50S
  • Blocks exit tunnel, E Site
  • Preventing escape of growing polypeptide chain
66
Q

Azithromycin is consider bacteriostatic and relatively toxic?

T or F

A
  • True
67
Q

How is Azithromycin excreted?

A
  • Cleared entirely through the feces

- Useful in pt’s with renal failure

68
Q

What is the drug of choice to treat Chlamydia?

A

-Azithromycin (Macrolide)

69
Q

Why does Azithromycin need to be enteric coated?

A
  • Gastric Ph disables the medication

- Do not give with food either

70
Q

T of F

Azithromycin inhibits CYP450 enzymes?

A
  • False

- Only Macroglide that does not

71
Q

Because Azithromycin does not modify CYP450 what caution must you take?

A
  • Increases serum levels of other drugs
  • Thephylline
  • Warfarin
  • Cyclosporine
  • Methylprednisolone
  • Digoxin
72
Q

What is Azithromycin usually prescribed for?

A
  • Chlamydia (DOC)
  • Respiratory tract infections
  • Travelers Diarrhea
  • Skin infections
73
Q

Major adverse effect of Azithromycin?

A
  • Cardiac Arrhythmia’s
  • QT prolongation
  • Torsades de pointes
74
Q

T of F

Azithromycin is safe during pregnancy?

A
  • False

- Crosses the placenta and breast milk

75
Q

T of F

Almost all MRSA strains are already resistant to macrolides?

A
  • True

- Because they were next in line after Beta lactams

76
Q

What antibiotic is multimodal interfering with several processes all through the 30S sub-unit?

A
  • Gentamicin (Aminoglycoside)
77
Q

What are the actions of Gentamicin?

A

1) Blocks complex 30S and 50S association
2) Promotes translation errors
3) Blocks translocation

78
Q

What antibiotic has synergistic effects with cell wall inhibitors?

A
  • Gentamicin + Beta Lactams

- Enhances uptake of Gentamicin, increasing efficacy

79
Q

What does Gentamicin + Beta Lactams treat?

A
  • Endocarditis and Sepsis
80
Q

What Aminoglycoside displays both

Concentration dependent killing & Significant post antibiotic effects ?

A
  • Gentamicin
81
Q

T of F

You need to adjust Gentamicin doses for pt’s with renal disease?

A
  • False

- Only excreted in the feces

82
Q

What is Gentamicin used to treat?

A
  • Mainly Aerobic Gram -

- But has coverage for both Gram - & +

83
Q

What are the two toxicities associated with Gentamicin at high doses and extended use?

A
  • Nephrotoxicity

- Ototoxicity

84
Q

T or F

Gentamicin can be given to pregnant women?

A
  • False

- It crosses the placenta and into breast milk

85
Q

Lincosamide (Cindamycin) MOA?

A
  • Slow down / Stop bacteria growth
  • Binds to the 50s subunit
  • Causes peptidyl tRNA dissociation from ribosome
  • Blocks the polypeptide exit tunnel
86
Q

T of F

No need to adjust doses for renal and hepatic impairment pt’s when treating with Lincosamide (Clindamycin) ?

A
  • True

- Excreted in the Urine and Feces

87
Q

Whats adverse effect of Lincosamide?

A
  • C. Diff associated Diarrhea
  • (Black Box warning)
  • Clears out gut flora. Only use for serious infections
88
Q

What does Lincosamide treat?

A
  • Treats MRSA
  • MRSA associated soft tissue infections
  • Gynecological infections (PID)
89
Q

T or F

You can administer Licosamide and Microglides together?

A
  • False
  • They complete with one another for the same binding site
  • Cancel each other out
90
Q

Tetracycline bind’s where and interfere with what?

A
  • 30s

- Interferes with binding of tRNA to the ribosomal complex

91
Q

Aminoglycosides bind where and interfere with what?

A
  • 30s
  • Causes mRNA to be misread
  • Interferes with initiation complex of 30s and 50s with mRNA
92
Q

Linezolid binds where and prevents what?

A
  • 50s P site

- Prevents formation of the 50/30s complex

93
Q

Macroglides, Clindamycin and Streptogramins binds where and prevents what?

A
  • Block the polypeptide exit tunnel of 50s

- prevent peptide chain elongation

94
Q

What does Linezolid treat?

A
  • Treats Vancomycin resistant (MRSA) enterococcal infections (VRE)
95
Q

If a drug binds the 50s unit A site and the other drug binds the 50s unit E site there will be no cross resistance?

T of F

A
  • True
  • Linezoild 50s P site and Macrolides 50s E site
  • No cross resistance
96
Q

What mediation lowers the seizure threshold and has strong serotoninergic effects with SSRI’s and Serotonin Rx’s?

A
  • Linezolid (Oxazolidinones)
97
Q

Where is Chloramphenicol cleared by ?

A
  • UDP-glucouronidation in the liver (90% Phase II)

- Adjust doses for pt’s with liver disease

98
Q

What is Chloramphenicol used to treat?

A
  • Last-resort treatment against VRE

Can treat

  • Rickettsial infections -Typhus
  • Rocky mountain spotted fever
99
Q

T or F

Chloramphenicol is rarely used in the US due to its toxicities?

A
  • True
100
Q

What are important adverse effects of Chloramphenicol ?

A
  • Leukemia’s
  • Aplastic Anemias
  • Grey baby syndrome
101
Q

Why do infants develop grey baby syndrome with Chloramphenicol ?

A
  • Neonates have not yet developed efficient phase II metabolism
  • Drug can build up to unsafe levels
  • Inhibits electron transport chain
  • Reduces energy production
  • Ashen skin color
  • Hypotension
  • Hypothermia
  • Used in caution with infants LOW DOSES
102
Q

What are the three mechanisms for protein sys inhibitors resistance?

A

1) Decreased accumulation (Reduced permeability of Increased Efflux pumps)
2) Chemical modifications that inactive the drug
3) Changes in biding site on Ribosome (Antibiotic protection proteins, Ribosomal subunit mutations)

103
Q

What is the most common mechanism for protein syn inhibitor resistance?

A
  • Changes in biding sites on ribosome

- Ex rpsL mutation on 50s prevents binding of Aminoglycoside Streptomycin

104
Q

masAB ToIC exporter pumps out Macroglides in many Gram - bacteria, what resistance mechanism is this an example of?

A
  • Decreased accumulation