LEC 16,17 - Inhibitors of Cell Wall Synthesis Flashcards

1
Q

What are the beta-lactam antibiotics?

A

Penicillin

Cephalosporin

Carbapenems

Monobactams

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2
Q

What is polymixin used for?

A

Topically to treat Gram (-) infections in skin + eye + ear

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3
Q

What are the five ways that a bacteria can become resistant to pencillin?

A

Inactivation

Decreased permeability

Alteration to PBP

Autolytic enzymes not activated

Lack of Cell wall

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4
Q

What must imipenem be given with? Why?

A

Cilastatin

Rapidly inactivated by renal tubule dehydropeptidases. Cilastatin is a dehydropeptidase inhibitor

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5
Q

What is the general activty of ertapenem?

A

Wide variety of

gram+

gram-

anaerobic

Eneterobateriaceae

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6
Q

bacterial target of pencillinase resistant penicillins

A

Low activity againse certain gram +’s

Resistant to penicllinase

DOC - penicillinase producing Staphylocccocus areus

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7
Q

Which of the natural penicillins are resistant to gastric acid?

A

Penicillin V

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8
Q

How does B-lactamase stop B-lactams from being active?

A

Cleaves the B-lactam ring

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9
Q

What is the general activity of carbaenems?

A

Broad spectrum

Anaerobes

Gram (+)

Gram (-) rods

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10
Q

Antipseudomonal penicillins (2)

A

Piperacillin

Ticarcillin

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11
Q

How are cephalosporins excreted?

A

Unchanged by the kindey

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12
Q

What are your two atypical bacteria?

A

Chlamydia

Mycoplasma

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13
Q

What are the specific bacteria that 1st gen cephalosporins are good against?

A

E. Coli

Klebsiella pneumoniae

Proteus mirabilis

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14
Q

How do the glycopeptides work?

A

Sterically inhibit addition of subunits to the peptidoglycan backbone

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15
Q

What are the bacterial targets of antipseudomonal penicillins?

A

Those covered by extended spectrum penicillins + addition gram negative bacilli

NO KLEBSIELLA

Major treatment for Pseudomonas aeruginosa

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16
Q

What is the function of the cell wall in bacteria?

A

Bacteria are hyperosmolar to their environment. The cell wall prevents osmotic rupture

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17
Q

What is the adverse effects of imipenem?

A

Seizures can occur with high levels

Use carefully in patients with brain lesion, head trauma , or hx of CNS disorders

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18
Q

What is the general structure of gram positive bacteria?

A

Only layered structure external to cell membrane and is thick

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19
Q

Route of Admin - Pen G procaine

A

IM

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20
Q

What cephalosporin is the only one allowed in food animals?

A

Cephapirim

Cows, pigs, turkey, and chickens

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21
Q

Use - Ceftiofur

A

Respiratory infections

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22
Q

What is the big difference between bacteria and mammialian cells?

A

Rigid cell wall external to the cell membrane

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23
Q

How is vancomycin excreted?

A

Primarily unchanged via the kidney

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24
Q

What is Penicillin G not effective against?

A

Amoebae

Plasmodia

Rickettsiae

Fungi

Virus

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25
Route of Admin - Pen G potassium
IV + IM
26
What is the real reason behind the loss of cell-wall integrity following treatment of CWSi?
Bacteria's own cell wall remodeling enzymes aka autolysins Cleave peptidoglycan bonds
27
If choosing carbapenems for a pseudomonas infection how is recommended to be given? WHy?
resistance occurs quickly Give with aminoglycoside
28
Carbapenems (3)
Imipenem Meropenem Ertapenem
29
What is the rank of antipseudomonal activity?
Piperacillin \> Ticarcillin
30
When should doses of cephalosporin be adjusted?
Renal impairment
31
Penicillinase ressitant penicillins (3)
Oxacillin Cloxacillin Methicillin
32
How does bacitracin work?
Inhibits the conversion to its active form of the lipid carrier that moves water soluble cytoplasmic peptidoglycan subunits through cell membrane to cell exterior
33
Use - Cefovecin
Skin and soft tissue infections
34
What is a very important thing to remember about monobactams (aztreonam) when it comes to theraputic use?
No cross sensitivty with penicillin, can give it to those who are allergic
35
B-lactamase inhibitor combo - Piperacillin
Tazobactam
36
What are the adverse effects of monobactams?
Phlebitis Skin rash Abnormal liver function
37
Route of Admin - Penicillin V
Oral
38
Use - Cefpodoxime
Skin and soft tissue infections in dogs
39
Natural penicillins (4)
Penicillin G potassium Penicillin G benzathine Penicillin G procaine Pencillin V
40
How are natural penicillins excreted?
Active transport in the kidney
41
What is vancomycin useful against?
Penicillin + methicillin resistant staphylococcus aureus Treating gram (+) infections in penicillin allergic patients
42
how can you prolong the time penicillin stays in the body? How does it work?
Give probenecid Tubular secretion partially blocked by probenecid Used for severe infections
43
Can you take antipseudomonals orally?
Acid sensitive
44
Where is PBP located?
On the cytoplasmic membrane
45
What are the three groups of polymyxins?
Monobactams Carbapenems Others...
46
Where is the antibacterial activity located in penicillin?
Intact B-lactam ring
47
What are the symptoms of penicillin toxicity?
Mostly just allergic reactions Anaphylactic Cytotoxic Arthus Cell mediated
48
What are the the six major groups of drugs that inhibit cell wall formation?
Polymyxins Natural penicillins Penicillinase Resistant penicillins Extended spectrum penicillins Antipseudomonal penicillins Cephalosporins
49
1st gen cephalosporins (4)
Cefazolin Cefadroxil Cephalexin Cephapirim
50
What is the general activty of 4th gen cephalosporins?
More resistant to B-lactamases
51
What do B-lactamase inhibitors not work against?
Methicillin-resistant, penicillinase-producing, Staphylococci
52
What is the structure of the bacterial cell wall?
Resistant to osmotic lysis in both gram positive and gram negative due to peptidoglycan Convalently linked sacculus that surrounds bacterium
53
What are the two ways vancomycin inhibits cell wall synthesis?
1 - binding to D-ala-D-ala terminus of peptidoglcan peptide = prevention of crosslinking 2- inihibits transglycosylation which inhibits elongation of peptidoglycan and chain
54
What does resistance form against vancomycin?
1 - D-ala-D-ala replaced with D-ala-D-lactate
55
B-lactamase inhibitor combo - Amipicillin
Sulbactam
56
What is the upside to using ertapenem?
Highly stable against beta-lactamases
57
What are the gram - bacteria that are targeted by extended spectrum penicillins? (5)
E. Coli Salmonella Shigella H. influenzae Proteus
58
What is the major characteristic of penicillin excretion?
one of the fastest drugs to be excreted renally
59
Why is polymixin not used parenteral?
Too nephrotoxic
60
Use for cefazolin
surgical prophylaxis
61
What is the mechanism by which bacitracin works?
Interferes with final dephosphorylation step in the phospholipid carrier cycle Impedes on mucopeptide transder to growing cell wall
62
Why is parenteral bacitracin used with extereme caution?
Serious nephrotoxicity
63
What is the general structure of gram negative bacteria?
Outer membrane external to very thin peptidoglycan layer
64
How is bacitracin most commonly used?
Prevent superficial skin + eye infections following minor injuries
65
What is polymixin B normally combined with?
Bacitracin for broad spectrum antibacterial effects
66
What are the gram + exceptions to 1st gen cephalosporin susceptibility?
Enterococci MRSA
67
What is the requirement for biological activity of penicillin?
Penicillin nucleus
68
What are the extra bacterial targets of the antipseudomonal pencillins?
Proteus Enterobacter
69
What is the general activity of 2nd gen cephalosporins?
Increased activity against gram (-)
70
4th gen cephalosporin (1)
Cefepimes
71
What drugs are contraindicated when using CWSi?
Protein synthesis inhibitors
72
What is the general activity of 1st gen cephalosporins?
good activity - gram + (cocci most) moderate activity - gram -
73
What is the mechanism of action for polymixin B?
Interacts with phospholipids in bacterial cell wall membrane to produce a detergent-like effect + membrane disruption
74
What are the four things that cephalosporins do not work against?
MRSA Listeria monocytogene s Enterococci Atypicals
75
What group of bacteria are ICWS most effective against?
Gram +
76
How is penicillin excreted?
10% glomerular filtration 90% tubular secretion
77
B-lactamase inhibitor combo - Ticarcillin
Calvulanic Acid
78
When is polymixin B administered orally?
Cattle + Swine Treatment of Gram (-) enteric infections
79
When can polymixin B be used parenterally?
Severe cases in horses
80
Extended spectrum penicillins (2)
Ampicillin Amoxicillin
81
How is resistance to b lactamase inhibitors occurring?
Develope independently upon b-lactamase production altered PBP production
82
What is the general activity of 3rd gen cephalosporins?
less active against gram + cocci more active against Enterobacteriaceae
83
How do b-lactams function?
Prevent cross-linking reaction called transpeptidation
84
How do the CWS inhibitors cause cell death?
Osmotic lysis
85
Route of Admin - Pen G bezathine
IM
86
What is the general activity of Bacitracin?
Gram (+)
87
What bacteria lack a cell wall?
Mycoplasma L forms Chlamydia
88
What are the regulations of vancomycin use in food animals
89
Monobactams (1)
Aztreonam
90
2nd gen cephalosporin
Cefoxitin Cefaclor
91
What are the bacterial targets of extended spectrum penicillin?
Lower gram + coverage Extended gram - coverage Anaerobic coverage (w/ penicillinase inhibitors)
92
What are the adverse reactions to vancomycin?
Hypersensitivty Ototoxic Nephrotoxic Uremia
93
What are the bacteria that do not have the autolytic enzymes activate and therefore are tolerant to penicillin?
Listeria Staphylococci
94
What does vancomycin have synergistic effects against?
Aminoglycosides
95
What are the glycoeptides?
Vancomycin
96
Use - Cefixime
Skin + Soft tissue + Urinary infections
97
What is the general activity of monobactams?
Relatively resistant to beta-lactamases Active against gram(-) rods (pseudomonas) No activity against gram + or anaerobes
98
What are the drugs the b lacatamase inhibitors are added with?
Ampicillin Amoxicillin Ticarcillin Pipercillin
99
What specific bacteria do ICWS work the best against?
Pseudomonas aeruginosa
100
B-lactamase inhibitor combo - Amoxicillin
Clavulanic acid
101
When is polymixin B bactericidal?
Gram (-) organism
102
What are the three B-lactamase inhibitors?
Clavulanic acid Sulbactam Tazobactam
103
Two other cell wall synthesis inhibitors that are not in groups
Vancomycin Bacitracin
104
3rd gen cephalosporins
Ceftiofur Cefovecin Cefixime Cefpodoxime