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

Antibacterial Agents 2: Cell-Wall Synthesis Inhibitors Flashcards

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
Q

Tazobactam combines with this piperacillin

A

Zosyn

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26
Q

Streptococci

Clinical atbx uses

Penicillins

A

Penicillin G

Penicillin V

Amoxicillin

27
Q

Enterococci

Clinical atbx uses

Penicillins

A

Penicillin G and Ampicillin for bacteremia

Ampicillin for UTI

28
Q

Staphylococcus aureus

Clinical atbx uses

Penicillins

A

MSSA: Oxacillin

MRSA: No penicillins

29
Q

Neisseria meningititis

Clinical atbx uses

Penicillins

A

Penicillin G

30
Q

Moraxella catarrhalis

Clinical atbx uses

Penicillins

A

Amoxicillin combined with Clavulanate

31
Q

Bacillus anthracis

Clinical atbx uses

Penicillins

A

Penicillin G

32
Q

Corynebacterium diphtheria

Clinical atbx uses

Penicillins

A

Penicillin G

33
Q

All gram negative bacilli

Clinical atbx uses

Penicillins

A

Ampicillin

Amoxicillin +/- Calvulanate

(Includes: H-flu, E. coli, klebsiella, H. pylori)

34
Q

Pseudomonas aeruginosa

Clinical atbx uses

Penicillins

A

Amoxicillin-Clavulanate

Piperacillin-Tazobactam

Ticarcillin-Clavulanate

35
Q

Clostridium perfringens

Clinical atbx uses

Penicillins

A

Penicillin G

36
Q

Bacteroides fragilis

Clinical atbx uses

Penicillins

A

Pipercillin - tazobactam

Ticarcillin - clavulanate

37
Q

Treponema pallidum (syphilis)

Clinical atbx uses

Penicillins

A

Penicillin G

38
Q

Borelia burgdorferi (Lyme)

Clinical atbx uses

Penicillins

A

Amoxicillin

39
Q

Penicillin G

Clinical atbx uses

A

Streptococci

Enterococci

  • Neisseria meningititis*
  • B. anthracis*
  • C. diphtheria*
  • C. perfringens*
  • T. pallidum*
40
Q

Amoxicillin

Clinical atbx uses

A
  • Streptococci*
  • Morazella catarrhalis* (with Calvulanate)

Gram Negative Bacilli (+/- Calvulanate)

  • P. aeruginosa*
  • Borrelia burgdorferi*
41
Q

Penicillins:

Toxicity and Adverse Reactions

A

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
Q

Vancomycin

Mechanism of Action

A

Inhibits cell wall synthesis at site different than penicillin (Stage 2)

43
Q

Vancomycin

Pharmacokinetics (absorption and excretion)

A

Poor oral, IV preferred unless for GI infection

Excreted by kidneys (6-10 days if renal failure)

44
Q

Vancomycin

Clinical Uses

A

MRSA

Staphylococci and streptococci

Ampicillin resistant enterococci

C. diff

45
Q

Vancomycin

Adverse Effects

A

Chill-Fever-Skin rash

Ototoxity for most severe

46
Q

Daptomycin

MOA

A

At bacterial membrane leading to loss of intracellular ions causing lysis

47
Q

Cephalosporins

A

Similar to penicillins but key differences:

Broader specturm v. G(-)

Less suscetible to B-lactamase

LEss cross-reactivity in penicillin sensitive patients

48
Q

Cephalosporins

Absoprtion

A

Some oral, some parenteral, depending on acid staiblity

49
Q

Cephalosporins

Distrubution

A

Tissue penetrant, including placenta

3rd Gen can go into CSF

50
Q

Cephalosporins

Metabolism and Excretion

A

Primarily renal

Dose appropriately if renal insufficiency

51
Q

Cephalosporin

Generation I

A

Cefazolin (IV) and Cephalexin (po)

Many G(+) cocci, some g(-) bacillli

Spectrum like amoxicillin

Great activity against MSSA

52
Q

Cephalosporin

Generation 2

A

Ceruroxime

Greater against g(-) bacteria than Gen I

Little to no activity agaisnt pseudomonas

Activate against anaerobes (Bacteroides fragilis)

53
Q

Cephalosporin

Generation 3

A

Cefdinir, Ceftriaxone, Ceftazidime

Comapred to gen 2, more activate agaisnt enteric g(-) bacilli (lkike eneterobacter)

Ceftazidime has moderate antipseudomonal activity

54
Q

Cephalosporin

Generation 4

A

Cefepime

Like gen 3 covers pseudomonas and s. pneumoniae

55
Q

Cephalosporin

Generation 5

A

Ceftaroline

MRSA coverage

56
Q

Cephalosporin

Generation I

Clinical uses

A

MSSA, Streptococci [cephalexin, cefazolin]

  • Klebisella* [cephalexin]
  • E. coli* [cephalexin]
57
Q

Cephalosporin

Generation II

Clinical uses

A

Resistant E. coli

  • H. influenza* [ceruoxime for meingitis and Cefaclor for sinusitis]
  • M. catarrhalis* [Cefaclor]
58
Q

Cephalosporin

Generation III

Clinical uses

A
  • Streptococcus pneumoniae* [Cefotaxime, ceftriaxome]
  • Neisseria gonorrheae* [Ceftriaxome]
  • Pseudomonas aeruginosa* [Ceft]
  • H-flu* [Ceft]
  • E. coli* [Cefo, ceft]
  • Klebsiella* [ceft]

Sespis [Ceft]

59
Q

Cephalosporin

Generation IV

Clinical uses

A

(All Cefepime)

  • S. pneumoniae*
  • P. aeruginosa*
  • Klebsiella*
60
Q

Cephalosporins

Adverse Reactions and Toxicity

A

Well tolerated

Do not give to patients with history of immeidate sensitivity to Penicillin

Can intensify oral anticoags

61
Q

Carbapenems

MOA

A

Interact with penicillin binding porteins responsible for elongation

B-lactamase resistance

62
Q

Carbapenems

Pharmacokinetics

A

Parenteral

Tissue penetrant, including CSF

imipenem- renal metabolism and excretion

Meropenem and ertapenem not ensitive to renal dipeptidase

63
Q

Carbapenems

Clinical Uses

A

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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