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PR3124 CA1 > Lecture 1- beta lactam and glycopeptides > Flashcards

Lecture 1- beta lactam and glycopeptides Flashcards

1
Q

beta lactams MOA

A

interfere with synthesis of bacterial cell wall peptidoglycan
act by binding to active site of enzyme transpeptidase (catalyse cross linking of terminal peptide components) –> weakening of cell wall–> build up of intracellular osmotic pressure–> lysis

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2
Q

types of beta lactam (4)

A
  1. penicillin
  2. cephalosporins/ cephamycins
  3. carbapenems
  4. monobactams
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3
Q

types of penicillin (4)

A
  1. natural penicillin
  2. penicillinase resistant penicillins
  3. aminopenicillins (broad spectrum) + BL inhibitors
  4. anti pseudomonal penicillins (extended spectrum) + BL inhibitors
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4
Q

which types of penicillin are susceptible to beta-lactamase?

A

all, thats why they need a beta-lactamase inhibitor as add on

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5
Q

what are the names of natural penicillins (s)

A

penicillin G, pen V

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6
Q

ROA of penicillin G

A

IV, IM

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7
Q

ROA of penicillin v

A

oral coz have better absorption

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8
Q

indication of natural penicillins

A
  1. against beta lactamse -ve strains of gram +ve and -ve microbes
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9
Q

how is natural penicillin excreted?

A

renal, unchanged in urine

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10
Q

why is natural penicillin not effective against S. Aureus?

A

S. Aureus produces penicillinases– therefore need to use penicillinase resistant penicillin

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11
Q

name of penicillinase- resistant penicillins? (3)

A

cloxacillin, oxacillin, flucloxacillin

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12
Q

indication for penicillinase resistant penicillins

A

potent inhibitors of most penicillase producing staphylococci

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13
Q

what are penicillinase resistant penicillins INEFFECTIVE agaisnt? (2)

A

gram neg org and MO susceptible to penicillin G, only covers MSSA, not MRSA

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14
Q

how is penicillinase resistant penicillin excreted?

A

renal clearance

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15
Q

why does penicillinase resistant penicillin have narrow spectrum of action

A

bulky side group- cannot pass through porins on gram neg org

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16
Q

ROA of penicillinase resistant penicillins?

A

IV, IM, oral

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17
Q

names of aminopenicillins (2)

A

ampicillin, amoxicillin

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18
Q

what orgs does aminipenicillins cover? gram-___

A

gram pos and neg

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19
Q

ROA of ampicillin?

A

oral, IV

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20
Q

ROA of amoxicillin

A

oral, better absorption thatn ampicillin

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21
Q

indication of aminopenicillins (3)

A
  1. treat beta lactamase neg strains of gram neg/pos and anaerobic MO
  2. in resp inficetions against S. pneumoniae (+) and H. influenzae (-)
  3. amo: against e coli
  4. ampi (IV): in bacterial meningitis
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22
Q

what does aminopenicillin NOT cover?

A

pseudomonas and klebsiella

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23
Q

is it susceptible to beta lactamse production?

A

yes

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24
Q

name of anti pseudomonal penicillin (1)

A

piperacillin

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25
Q

ROA of piperacillin?

A

IV

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26
Q

what is piperacillin given with?

A

in combi with beta lactam inhibitors eg. clabulanic acid

27
Q

indication of piperacillin

A
  • greater activity then other penicillins against gram -VE bacteria esp. psesudomonas and proteus app. and klebsiella
  • used to treat severe infections caused by GRAM NEG
  • incrased anaerobic coverage
28
Q

what kind of bac does it cover? (gram __)/ aerobic/anaero

A

both pos and neg

and anaerobic

29
Q

penetration into CSF of piperacillin?

A

penetrates fairly well

30
Q

excretion of piperacillin?

A

renal. need dose adjustment if hv renal dysfunction

31
Q

what is piperacillin susceptible to

A

to inactivation by bacterial beta lactamase– therfore give as combi with beta lac inhibitor

32
Q

what are beta lactamase inhibitors?

A
  • have week anti-bac properties
33
Q

how do beta lactamase inhibitors work? MOA

A

inactivate serine beta lactamases (enzymes that hydrolyse and inactivate beta lactam ring)
- strong affinity for beta lactamases–> can bind and inactivate or bind irreversibly –> protect other beta lactam antibiotics from being targeted by beta lactamses

34
Q

3 names of beta lactamase inhibitors

A 
clavulate amoxicillin (augmentin)
sulbactam ampicillin
tazobactam piperacillin (zosyn)
35
Q

how are beta lactamase inhibitors cleared

A

renal , excreted unchnaged in urine, dose adjustment needed with renal impairment

36
Q

MOA of clavulanic acid

A

suicide inhibitor. covalently binds to beta lactamase and restructures it–> permanently inactivating it

37
Q

MOA of sulbactam and tazobactam

A

bind irreversibly to beta lactamase at its active site, protects other beta lactamase antibiotics from beta lactamase catalysis

38
Q

adverse reactions to penicillins (3)

A 
allergy/ hypersensitivity- 3 types
- immediate onset- 2 to 30 mins
- accelerated onset
- late onset - days to weeks
hepatotoxicity
neurotoxicity
CDAD
39
Q

how many generations of cephalosporins are there?

A

5

40
Q

examples of first gen cephalosporins (2) and their specturm

A
  • cefazolin, cephalexin

- active against gram pos eg. streptococci, staphylococcus aureus

41
Q

ROA for first gen cephalosporins

A

oral

42
Q

example of 2nd gen cephalosporins (1) + specturm

A

cefuroxime

  • against E.coli, klebsiella, proteus
  • not as active against gram pos
  • better coverage agaisnt gram -ve and those producing beta lactamases
43
Q

examples of 3rd gen cephalosporins (2) and spectrum

A
  • ceftriaxone , ceftazidime
  • activity against s.aureus, streptococcus pneumoniae, enterobacteriaceae…
  • can cover pseudomonas
44
Q

example of 4th gen cephalosporins (1)

A
  • cefepime

- same as 3rd gen but more resistant to beta lactamases and pseudomonas

45
Q

example of 5th gen cephalosporins (2)

A
  • ceftaroline, ceftobiprole

- can cover MRSA

46
Q

adverse reaction to cephalosporins (3)

A
  • hypersentivity- freq of cross allergy between cephalosporins and penicillins low chance but dont giev tgt
  • GIT eg. diarrhea, CDAD
  • thrombophlebitis (can minimise risk by giving diluted form and rotating infusion site)
47
Q

wat is the indication for carbapenem?

A

first line for extended spectrum beta lactamse producing bacteria
good coverage agaisnt gram neg and anaerobic spp

48
Q

exampels of carbapenem (3)

A

imipenem and cilastatin
meropenem
ertapenem

49
Q

ROA of carbapenem

A

IV

50
Q

carbapenem adverse effects

A

GIT sx eg. nausea, vomitting
rashed
neurotoxicity (seizures) at high blood conc
cross hypersen with penicillin

51
Q

example of monobactam (1)

A

aztreonam

52
Q

spectrum of activity of aztreonam

A
  • only against gram NEG

- useful against beta lactamase producing gram neg bacteria

53
Q

aztreonam indication (3)

A
  • UTI caused by enterobacteriaceae
  • lower resp tract infection eg. pneumonia, bronchitis
  • septicemia and intra abdominal infections
54
Q

ROA of aztreonam

A

IV/IM- poor bioavail

55
Q

excretion of aztreonam?

A

renal clearance, need dose adjustment if renal impair

56
Q

aztreonam adverse rxn

A

generally well tolerated

- skin rahs

57
Q

types of glycopeptides (1)

A

vancomycin

58
Q

Spectrum of vancomycin

A

gram POS due to large mol size- cannot penetrate gram neg

59
Q

ROA of vancomycin

A

IV and oral (only for CDAD)

poor bioavail

60
Q

how is vancomycin excreted

A

renal clearance, dose adjust

61
Q

vancomycin MOA

A

bind with high affinity to D-ala-d-ala terminus of NAM compoenent of peptidoglycan and interferes with transglycosylation of cell wall–> inhibit cell wall synthesis

62
Q

spectru of activity of vancomycin

A

broad spectrum of gram POS

- MRSA and MSSA

63
Q

what is resistant to vancomycin

A

all gram neg bacilli and mycobacteria and resistant to

64
Q

adverse rxn of vancomycin

A
  • thrombophlebitis with fever, chills
  • red neck
  • nephrotixicity and ototoxicity

PR3124 CA1 (5 decks)

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