Antimicrobials Flashcards

1
Q

overall, what are the 3 main types of antibacterial antibiotics?

A
  1. bacterial cell wall synthesis inhibitors
  2. bacterial protein synthesis inhibitors
  3. nucleic acid synthesis inhibitor
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2
Q

what are bacterial cell wall synthesis inhibitors usually used for?

A

those bacteria that are gram-stainable; cocci and rods

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3
Q

what are the 2 classes of bacterial cell wall inhibitors?

A
  1. beta lactams (penicillin, special penicillin, cephalosporins, carbapenem and monobactams)
  2. glycopeptide (vancomycin)
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4
Q

what is the general MOA of bacterial cell wall inhibitors?

A

binds to enzyme transpeptidase and prevents cross linking = weakened cell wall = lyse

*only works in actively dividing bacteria

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5
Q

what is the general side effect of bacterial cell wall inhibitors?

A

TOXICITY TO ALL:

  1. hepatotoxicity and neurotoxicity
  2. some extent of renal toxicity too

OTHERS:

  1. c-diff associated colitis
  2. SJS, Toxic epidermal necrosis
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6
Q

how is strep pneumo resistance conferred?

A

mutations to penicillin-binding receptors = not susceptible to beta lactams anymore

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7
Q

how is staph resistance conferred?

A

activation of mecA gene = production of beta lactamases = not susceptible to beta lactams anymore

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8
Q

what are examples of penicillin?

A
  1. benzylpenicillin
  2. cloxacillin
  3. amoxicillin
  4. piperacillin
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9
Q

what does benzylpenicillin target?

A
  1. gram pos and neg cocci
  2. some gram pos rods
  3. spiral bacteria: treponema pallidum

NOTE: usually for streps

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10
Q

what does cloxacillin target?

A

for MRSA

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11
Q

what does amoxicillin target?

A

same as benzylpenicillin (gram pos and neg cocci + gram pos rods)

additional: gram neg rod (listeria)

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12
Q

what does piperacillin target?

A

pseudomonas aeruginosa (who usually can also be targeted by the same tx for E. coli)

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13
Q

what are the examples of special penicillins?

A

co-amoxiclav (amoxicillin + clavulanate)

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14
Q

what does coamoxiclav target?

A

generally: gram neg and pos bacteria

but more so for bacteria causing LRTI and UTI
e.g. burkholderia pseudomallei, E. coli

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15
Q

what are the examples of cephalosporins?

A

1st/2nd gen

3rd gen: ceftriaxone, ceftazidime, cefixime

4th gen: cefepime

5th gen: ceftaroline

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16
Q

what does ceftriaxone target?

A

generally:

  1. gram pos and neg cocci
  2. gram pos and neg rods
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17
Q

what does cefapime target?

A

same as 3rd gen but extra coverage of pseudomonas

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18
Q

what does ceftaroline target?

A

widest coverage, including MRSA

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19
Q

what are the examples of carbapenems?

A

imipenem

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20
Q

what does imipenem target?

A

essentially same as the above but is only used in really really serious infections

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21
Q

what are the examples of monobactams?

A

aztreonam

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22
Q

what does aztreonam target?

A

alternative for penicillin allergic patients

but only targets gram neg cocci and rods

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23
Q

what are the examples of glycopeptides?

A

vancomycin

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24
Q

what does vancomycin target?

A

mostly gram positive cocci and rods

especially for MRSA and CDAC

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25
Q

note about vancomycin upon first administration

A

may cause red man syndrome

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26
Q

moving on from bacterial cell wall synthesis inhibitors, let’s talk about bacterial protein synthesis inhibitors - what are the diff classes of them?

A

30S inhibitors:
Tetracyclines
Aminoglycosides
Glycylcycline

50S inhibitors:
Macrolides
Clindamycin
Linezolid

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27
Q

what is the general MOA of protein synthesis inhibitors?

A

inhibits 30S/50S units of ribosomes and prevent binding of tRNA

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28
Q

what are the general side effects of protein synthesis inhibitors?

A

TOXICITY:

  1. hepatotoxicity
  2. phytotoxicity for TA
  3. ototoxicity for G + MCL

OTHERS:

  • rare to have SJS or other hypersensitivity reactions
  • macrolides have many DDI’s
  • tetracyclines not used in young and pregnant
29
Q

what are the examples of tetracyclines?

A

tetracycline and doxycycline

30
Q

what does tetracycline and doxycycline target?

A

broad spectrum gram neg and pos bacterial (e.g. burkholderia pseudomallei - DCCC)

but more for intracellular obligate parasites (rickettsia)

31
Q

what are the examples of aminoglycosides?

A

gentamicin
streptomycin
tobramycin

32
Q

what do aminoglycosides target?

A

gram neg aerobic rods (e.g. listeria, corynebacterium, bacillus)

but honestly is not very commonly used

33
Q

important! what are the 6 NO’s of aminoglycosides?

A
  1. NO protein synthesis
  2. only for gram Negative Organisms
  3. administered Not Orally (by IV instead)
  4. NO pregnancy
  5. NO csf penetration
  6. Nephrotoxicity and Ototoxicity
34
Q

what are the examples of gylcylcyclines?

A

tigecycline

35
Q

what does tigecycline target?

A

MRSA (but we usually use vancomycin for this)

36
Q

what are the examples of macrolides?

A

erythromycin
clarithromycin
azithromycin

37
Q

what does erythromycin target?

A

alternative to penicillin for patients allergic to penicillin (similar to aztreonam)

used specifically for campylobacter jejuni

38
Q

what does clarithromycin target?

A

same as erythromycin but has additional bacterial targets

used specifically for h. pylori

39
Q

what does azithromycin target?

A

same as erythromycin but more specific to gram neg bacterial related to respiratory infections

40
Q

what does clindamycin target?

A

anaerobic bacteria + gram pos cocci

not very commonly used

41
Q

what does linezolid target?

A

all the resistant gram positive bacteria e.g. MRSA, penicillin-resistant strep, cephalosporin-resistant enterococcus

42
Q

moving on from cell wall synthesis and protein synthesis inhibitors, let’s talk about nucleic acid inhibitors - what are the different classes?

A
  1. fluoroquinolones
  2. folic acid inhibitor
  3. urinary antiseptic
43
Q

what is an example of fluoroquinolone and its MOA?

A

ciprofloxacin/levofloxacin/moxifloxacin

inhibits dna gyrase in gram negs and topoisomerase 4 in gram pos = no making of supercoils

44
Q

what is the side effects of fluoroquinolones?

A

TOXICITY:
1. phytotoxicity

OTHERS:

  • GI and CNS disturbance
  • cannot be used in pregnant and young
  • peripheral neuropathy
45
Q

what does ciprofloxacin target?

A

mostly enterobacteriaceae and pseudomonads

46
Q

what does levofloxacin and moxifloxacin target?

A

known as respiratory quinolones

used as second line therapy for TB

47
Q

what are examples of folic acid synthesis inhibitors?

A

cotrimox, sulfonamides, trimethoprim

48
Q

what is the MOA of folic acid synthesis inhibitors?

A

binds to enzyme that synthesises folate acid = no purine or pyramiding synthesis

49
Q

what are the general side effects of folic acid synthesis inhibitors?

A

TOXICITY:
1. nephrotoxicity

OTHERS:
- cannot give to G6PD deficiency people as it would include hemotopoietic disturbances

50
Q

what does sulfonamide target?

A

enterobacteriaceae

51
Q

what does trimethoprim target?

A

same as sulphonamide but stronger

52
Q

what is cotrimox? (aka bactrim)

A

combination of trimethoprim and sulfamethoxazole

53
Q

what does cotrimox target?

A

UTI-causing bacteria, respiratory tract bacteria and pneumocystis jiroveci

54
Q

what are examples of urinary antiseptics?

A

nitrofurantoin

55
Q

what is the MOA of urinary antiseptics?

A

blocks enzymes involved in protein synthesis and DNA

56
Q

what are the general side effects of urinary antiseptics?

A

TOXICITY:
1. pulmonary toxicity in elderly and babies < 1 month

OTHERS:

  • CNS and GI disturbances
  • haemolytic anemia in G6PD deficient patients (like folic acid synthesis inhibitor)
57
Q

what does nitrofurantoin target?

A

only E. coli

58
Q

moving on from anti-bacterials, let’s talk about anti-fungals - what are the 3 most important anti-fungals?

A
  1. amphotericin B
  2. 5-flucytosine
  3. azoles
  4. nystatin
59
Q

what is the general MOA of anti-fungals?

A

similar to cell wall synthesis inhibitors; in which it binds to ergosterol in plasma membrane of fungal cells to form pores = lysis

60
Q

what are the general side effects of anti-fungals?

A

TOXICITY:
1. nephrotoxicity

OTHERS:
- hematopoeitic dysfunctions (like folic acid inhibitors and urinary antiseptics)

61
Q

out of the 4 important anti-fungals, which target systemic infections?

A

the first 3 - amphotericin b, 5-flucytosine and azoles

62
Q

what is amphotericin b used for?

A

used to treat candida, histoplasma, aspergillus and cryptococcus

63
Q

what is 5-flucytosine used for?

A

used in combination with amphotericin b

why? because it has high risk of resistance if used as monotherapy

64
Q

what are azoles used for?

A

same as amphotericin b

65
Q

can azoles be used easily with other drugs?

A

no as it has many DDI’s (like macrolides)

66
Q

lastly, let’s talk about anti-protozoal drugs - what is the most important type?

A

metronidazole

67
Q

what are the general side effects of anti-protozoal?

A

TOXICITY:
1. neurotoxicity

OTHERS:

  • bitter metallic taste
  • GI discomfort
68
Q

what is metronidazole used for?

A
  • giardia/entamoeba

- and also c. diff

69
Q

what anti-bacterials are safe to use in pregnancy?

A
  1. beta lactams (cell wall synthesis)
  2. macrolides (50S protein synthesis)
  3. clindamycin (50S protein synthesis)