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DD Test 2 LOs > Antibacterial Agents 2: Cell-Wall Synthesis Inhibitors > Flashcards

Antibacterial Agents 2: Cell-Wall Synthesis Inhibitors Flashcards

(63 cards)

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1
Q

3 Components of the B-lactam drugs

A

Side chain, B-lactam ring, and thiazolidine ring

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2
Q

Penicillin G

A

High activity against Gram (+), low against (-)

Destroyed by B-lactamase (resistance mech)

Acid labile

Prototypical penicillin

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3
Q

Oxacillin/cloxacillin/dicloxacillin/flucloxacillin

Aka isoxazoyl penicillins

A

Acid stable

Can be taken orally

Highly protein-bound

Safe with pts w/ renal insufficiency

Narrow Spectrum (cocci)

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4
Q

Nafcillin

A

Similar to isoxazolyl penicillins, but not as strongly bound

Resistant to staph B-lactamase

More efficacious that Oxacillin fam

Narrow spectrum (cocci)

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5
Q

Ampicillin

A

Similar to penicillin G

Susceptible to B-lactamase

Acid stable, and better gram (-) activity

Extended spectrum (additional activity against g(-) bacilli)

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6
Q

Ticarcillin

A

Like carbenicillin, but higher blood levels

Active against gram (-) aerobes

Anti-pseudomonal

Not penicillinase resistant

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7
Q

Amoxicillin

A

Similar to ampicillin but higher blood levels

Extended spectrum (additional activity against g(-) bacilli)

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8
Q

Penicillin R Groups

A

Can alter function of of atbx, like

Acid stability

Renal excretion

Bacterial resistance

Spectrum variation

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9
Q

What is Stage 1 of wall formation and what atbx inhibits it

A

Synthesis of cell wall subunits in cytosol

Fosfomycin and cycloserine

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10
Q

What is Stage 2 of wall formation and what inhibits it

A

Linear polymerization of subunits at cell membrane

Bacitracin and vancomycin

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11
Q

What is Stage 3 of cell wall formation and what inhibits it

A

Cross-linking of peptidoglycan polymers at the cell wall

Penicillin and cephalosporins

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12
Q

How does penicillin interfere with the cross-linking?

A

Penicillin mimis D-al-D-al, the terminal end of the peptide that crosslinks adjacent N-actylmuramic acids

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13
Q

Penicillins are ________ to growing organisms

A

Bactericidal

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14
Q

Penicillin Binding Proteins

A

Bacterial proteins targetted by B-lactams for acetylation

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15
Q

Penicillin Mech of action:

Effect on autolytic enzymes

A

Depresses inhibitors of natural autolysins

Covalently binds to them, thus effect persist when drug is gone

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16
Q

B-lactamase

A

Generic term for enzymes that hydrolyze B-lactams, including penicillinases and cephalosporinases

Production via plasmids in response to penicillin

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17
Q

MRSA and Penicillin resistance in pneumococci resistance

A

They alter their penicillin-binding proteins

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18
Q

Penicillin:

Absorption characteristics

A

Highly water soluble (moderately acidic)

Best taken on empty stomach (lots of penicillins are acid-labile)

Oral needs higher dosage than parenteral

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19
Q

Penicillin:

Distribution characteristics

A

Throughout body

Poor tissue penetration (ionized at physiological pH)

Can enter inflamed tissues or membranes

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20
Q

Penicillins:

Metabolism and Excretion

A

Ecreted as active drug

90% tubular excretion

Excreted in breast milk

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21
Q

B-Lactamase Inhibitors

A

Clavulanic Acid, Sulbactam, Tazobactam

Irreversible inhibitors

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22
Q

Clavulanic acid combines with this amoxicillin

A

Augmentin

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23
Q

Calvulanic acid combines with this ticarcillin

A

Timentin

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24
Q

Sulbactam combines with this ampicillin

A

Unasyn

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25
Tazobactam combines with this piperacillin
Zosyn
26
Streptococci Clinical atbx uses Penicillins
Penicillin G Penicillin V Amoxicillin
27
Enterococci Clinical atbx uses Penicillins
Penicillin G and Ampicillin for bacteremia Ampicillin for UTI
28
*Staphylococcus aureus* Clinical atbx uses Penicillins
MSSA: Oxacillin MRSA: No penicillins
29
*Neisseria meningititis* Clinical atbx uses Penicillins
Penicillin G
30
*Moraxella catarrhalis* Clinical atbx uses Penicillins
Amoxicillin combined with Clavulanate
31
*Bacillus anthracis* Clinical atbx uses Penicillins
Penicillin G
32
*Corynebacterium diphtheria* Clinical atbx uses Penicillins
Penicillin G
33
All gram negative bacilli Clinical atbx uses Penicillins
Ampicillin Amoxicillin +/- Calvulanate (Includes: H-flu, E. coli, klebsiella, H. pylori)
34
*Pseudomonas aeruginosa* Clinical atbx uses Penicillins
Amoxicillin-Clavulanate Piperacillin-Tazobactam Ticarcillin-Clavulanate
35
*Clostridium perfringens* Clinical atbx uses Penicillins
Penicillin G
36
*Bacteroides fragilis* Clinical atbx uses Penicillins
Pipercillin - tazobactam Ticarcillin - clavulanate
37
*Treponema pallidum* (syphilis) Clinical atbx uses Penicillins
Penicillin G
38
*Borelia burgdorferi* (Lyme) Clinical atbx uses Penicillins
Amoxicillin
39
Penicillin G Clinical atbx uses
Streptococci Enterococci * Neisseria meningititis* * B. anthracis* * C. diphtheria* * C. perfringens* * T. pallidum*
40
Amoxicillin Clinical atbx uses
* Streptococci* * Morazella catarrhalis* (with Calvulanate) Gram Negative Bacilli (+/- Calvulanate) * P. aeruginosa* * Borrelia burgdorferi*
41
Penicillins: Toxicity and Adverse Reactions
Virtually non-toxic except hypersensitivity 10% of patients report penicillin allergy, but only 10-20% actually experience a reaction (1-2% of population) Commonly an idiopathic reaction, with a rash, type I reactions are life threatening
42
Vancomycin Mechanism of Action
Inhibits cell wall synthesis at site different than penicillin (**Stage 2**)
43
Vancomycin Pharmacokinetics (absorption and excretion)
Poor oral, IV preferred unless for GI infection Excreted by kidneys (6-10 days if renal failure)
44
Vancomycin Clinical Uses
MRSA Staphylococci and streptococci Ampicillin resistant enterococci *C. diff*
45
Vancomycin Adverse Effects
Chill-Fever-Skin rash Ototoxity for most severe
46
Daptomycin MOA
At bacterial membrane leading to loss of intracellular ions causing lysis
47
Cephalosporins
Similar to penicillins but key differences: Broader specturm v. G(-) Less suscetible to B-lactamase LEss cross-reactivity in penicillin sensitive patients
48
Cephalosporins Absoprtion
Some oral, some parenteral, depending on acid staiblity
49
Cephalosporins Distrubution
Tissue penetrant, including placenta 3rd Gen can go into CSF
50
Cephalosporins Metabolism and Excretion
Primarily renal Dose appropriately if renal insufficiency
51
Cephalosporin Generation I
Cefazolin (IV) and Cephalexin (po) Many G(+) cocci, some g(-) bacillli Spectrum like amoxicillin Great activity against MSSA
52
Cephalosporin Generation 2
Ceruroxime Greater against g(-) bacteria than Gen I Little to no activity agaisnt *pseudomonas* Activate against anaerobes (*Bacteroides fragilis)*
53
Cephalosporin Generation 3
Cefdinir, Ceftriaxone, Ceftazidime Comapred to gen 2, more activate agaisnt enteric g(-) bacilli (lkike eneterobacter) Ceftazidime has moderate antipseudomonal activity
54
Cephalosporin Generation 4
Cefepime Like gen 3 covers pseudomonas and s. pneumoniae
55
Cephalosporin Generation 5
Ceftaroline MRSA coverage
56
Cephalosporin Generation I Clinical uses
MSSA, Streptococci [cephalexin, cefazolin] * Klebisella* [cephalexin] * E. coli* [cephalexin]
57
Cephalosporin Generation II Clinical uses
Resistant *E. coli* * H. influenza* [ceruoxime for meingitis and Cefaclor for sinusitis] * M. catarrhalis* [Cefaclor]
58
Cephalosporin Generation III Clinical uses
* Streptococcus pneumoniae* [Cefotaxime, ceftriaxome] * Neisseria gonorrheae* [Ceftriaxome] * Pseudomonas aeruginosa* [Ceft] * H-flu* [Ceft] * E. coli* [Cefo, ceft] * Klebsiella* [ceft] Sespis [Ceft]
59
Cephalosporin Generation IV Clinical uses
(All Cefepime) ## Footnote * S. pneumoniae* * P. aeruginosa* * Klebsiella*
60
Cephalosporins Adverse Reactions and Toxicity
Well tolerated Do not give to patients with history of immeidate sensitivity to Penicillin Can intensify oral anticoags
61
Carbapenems MOA
Interact with penicillin binding porteins responsible for elongation B-lactamase resistance
62
Carbapenems Pharmacokinetics
Parenteral Tissue penetrant, including CSF imipenem- renal metabolism and excretion Meropenem and ertapenem not ensitive to renal dipeptidase
63
Carbapenems Clinical Uses
Active to both G(+) and G(-) Reserved for multiple resistance *P. aeruginosa, E. coli, C. perfringens,* and Becteroides

DD Test 2 LOs (10 decks)

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