Antibacterials 2 Flashcards

1
Q

what two antibacterials target the cell envelope

A

beta-lactams and glycopeptides

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2
Q

what do beta-lactams consist of

A

beta lactam ring

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3
Q

what do beta-lactams compete with

A

d-ala d-alanine

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4
Q

what does the serine in b-lactams cause

A

breaking down of d-ala d-ala

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5
Q

what does b-lactam bind to and what does it cause

A

to the active site so transpeptidation cannot occur

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6
Q

After b-lactam is bound to the active site so transpeptidation cannot occur what does this result in

A

cross-links cannot form resulting in a weak cell wall and lysing of the cell

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7
Q

What are the three types of beta-lactam

A

penicilin (penicillin G), cephlasporins and carbapenems

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8
Q

What are carbapenems used for

A

last port of call for gram negative that are multidrug resistant

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9
Q

what is penicillin G used to treat

A

pneumonia, syphillis and gonorrhea

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10
Q

three glycopeptides

A

Vancomycin, Polymyxins B and E, daptomycin

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11
Q

what is the prime mode of action of vancomycin

A

transglycoylation

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12
Q

what does vancomycin bind to

A

d-ala d-ala

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13
Q

is vancomycin active against gram negative

A

no

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14
Q

why might vancomycin be used

A

if the patient cannot have b-lactam because of resistance or hypersensitivity

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15
Q

what is vancomycin used to treat

A

serious MRSA and other gram positives

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16
Q

adverse side effects of vancomycin (5)

A
'Red man'
Histamine release
Ototoxic 
Neutropenia
Thrombocytopenia
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17
Q

are polymyxins active for gram positives

A

no

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18
Q

what do polymyxins interact with

A

liposaccharide leaflet of -VE, penetrating outer membrane

19
Q

what are polymyxins used to treat

A

cystic fibrosis, decontamination of gut and burns infections

20
Q

toxicity of polymyxins

A

potential neurotoxicity and nephro due to accumulation on kidneys

21
Q

how does daptomycin work

A

by interaction with membrane via acyl chain integration , causing integration, aggregation and membrane depolarisation causing leakagr and cell death

22
Q

are daptomycins used for gram negative

A

no

23
Q

what are daptomycins used to treat

A

soft tissue infections

24
Q

what two drugs target nucleic acids and nucleic acid biosynthesis

A

Sulfa drugs and trimethoprim

25
Q

how do drugs that target nucleic acids and their biosynthesis work

A

inhibiting dihydropteroate synthase ( DHPS)

26
Q

how do sulfa drugs work

A

they are structural analogues of the substrates for DHPS

27
Q

what are the substrates for DHPS

A

p-aminobenzoic acid

28
Q

what happens when sulfa binds to DHPS

A

forms a dead end complex and therefore no tetrahydrofolate

29
Q

what is trimethoprim formed of

A

2 pyridimes joined together

30
Q

how does trimethoprim work

A

inhibiting dihydrofolic reductase catalysing the reduction of dihydrofolic acid to tetrahydrofolic acid

31
Q

what are both sulfa and trimethoprim used to treat

A

short term respiratory, urinary and digestive tract infections

32
Q

what are sulfa and trimethoprim used to treat in HIV patients

A

pneumonia

33
Q

what two drugs are involved in targeting the synthesis of DNA-pre-existing DNA

A

Quinolones and fluoroquinolones

34
Q

what do all quinolones and fluoroquinolones drugs end in

A

-floaxacin

35
Q

how do quinolones and fluoroqunolones work (2 things)

A
  1. they interfere with enzymes responsible for bacterial topology
  2. they catalyse ATP dependant DNA double strand breakages
36
Q

what two enzymes do quinolones and fluoroquinolones target

A

DNA gyrase and DNA topoisomerase IV

37
Q

how do nitroheterocyclic drugs work

A

targeting obligate anaerobes to cause DNA damage

38
Q

two examples of nitroheterocyclic drugs

A

Metronidazole and Tinidazole

39
Q

are nitroheterocyclic bacteriostatic or cidal

A

cidal

40
Q

what drug works by targeting RNA synthetase

A

Rifamycin

41
Q

how does Rifamycin stop rNA synthetase

A

blocks RNA exit channel, RNA knocks into rifamycin and spontaneously dissociates

42
Q

is rifamycin bacteriostatic or cidal

A

cidal

43
Q

what is rifamycin used to treat

A

TB, leprosy, penicillin resistant s.pneumoniae