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

Lecture 1- beta lactam and glycopeptides Flashcards

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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
ROA of piperacillin?
IV
26
what is piperacillin given with?
in combi with beta lactam inhibitors eg. clabulanic acid
27
indication of piperacillin
- 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
what kind of bac does it cover? (gram __)/ aerobic/anaero
both pos and neg | and anaerobic
29
penetration into CSF of piperacillin?
penetrates fairly well
30
excretion of piperacillin?
renal. need dose adjustment if hv renal dysfunction
31
what is piperacillin susceptible to
to inactivation by bacterial beta lactamase-- therfore give as combi with beta lac inhibitor
32
what are beta lactamase inhibitors?
- have week anti-bac properties
33
how do beta lactamase inhibitors work? MOA
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
3 names of beta lactamase inhibitors
``` clavulate amoxicillin (augmentin) sulbactam ampicillin tazobactam piperacillin (zosyn) ```
35
how are beta lactamase inhibitors cleared
renal , excreted unchnaged in urine, dose adjustment needed with renal impairment
36
MOA of clavulanic acid
suicide inhibitor. covalently binds to beta lactamase and restructures it--> permanently inactivating it
37
MOA of sulbactam and tazobactam
bind irreversibly to beta lactamase at its active site, protects other beta lactamase antibiotics from beta lactamase catalysis
38
adverse reactions to penicillins (3)
``` allergy/ hypersensitivity- 3 types - immediate onset- 2 to 30 mins - accelerated onset - late onset - days to weeks hepatotoxicity neurotoxicity CDAD ```
39
how many generations of cephalosporins are there?
5
40
examples of first gen cephalosporins (2) and their specturm
- cefazolin, cephalexin | - active against gram pos eg. streptococci, staphylococcus aureus
41
ROA for first gen cephalosporins
oral
42
example of 2nd gen cephalosporins (1) + specturm
cefuroxime - against E.coli, klebsiella, proteus - not as active against gram pos - better coverage agaisnt gram -ve and those producing beta lactamases
43
examples of 3rd gen cephalosporins (2) and spectrum
- ceftriaxone , ceftazidime - activity against s.aureus, streptococcus pneumoniae, enterobacteriaceae... - can cover pseudomonas
44
example of 4th gen cephalosporins (1)
- cefepime | - same as 3rd gen but more resistant to beta lactamases and pseudomonas
45
example of 5th gen cephalosporins (2)
- ceftaroline, ceftobiprole | - can cover MRSA
46
adverse reaction to cephalosporins (3)
- 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
wat is the indication for carbapenem?
first line for extended spectrum beta lactamse producing bacteria good coverage agaisnt gram neg and anaerobic spp
48
exampels of carbapenem (3)
imipenem and cilastatin meropenem ertapenem
49
ROA of carbapenem
IV
50
carbapenem adverse effects
GIT sx eg. nausea, vomitting rashed neurotoxicity (seizures) at high blood conc cross hypersen with penicillin
51
example of monobactam (1)
aztreonam
52
spectrum of activity of aztreonam
- only against gram NEG | - useful against beta lactamase producing gram neg bacteria
53
aztreonam indication (3)
- UTI caused by enterobacteriaceae - lower resp tract infection eg. pneumonia, bronchitis - septicemia and intra abdominal infections
54
ROA of aztreonam
IV/IM- poor bioavail
55
excretion of aztreonam?
renal clearance, need dose adjustment if renal impair
56
aztreonam adverse rxn
generally well tolerated | - skin rahs
57
types of glycopeptides (1)
vancomycin
58
Spectrum of vancomycin
gram POS due to large mol size- cannot penetrate gram neg
59
ROA of vancomycin
IV and oral (only for CDAD) | poor bioavail
60
how is vancomycin excreted
renal clearance, dose adjust
61
vancomycin MOA
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
spectru of activity of vancomycin
broad spectrum of gram POS | - MRSA and MSSA
63
what is resistant to vancomycin
all gram neg bacilli and mycobacteria and resistant to
64
adverse rxn of vancomycin
- thrombophlebitis with fever, chills - red neck - nephrotixicity and ototoxicity

PR3124 CA1 (5 decks)

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