antivirals and antimicrobial

Question 1

what is glutathione?

Answer 1

an endogenous antioxide

also used in drug metabolism to conjugate polar groups

Question 2

what happens if there is too much drug to detox?

Answer 2

glutathione used up – build up NAPQI – toxic – liver kills you – jaundice

Question 3

how do you develop antiviral and antimicrobial drugs?

Answer 3

look at the life cycle, how does it get into the cell, how is it processing itself and how is it released - find a way to block

Question 4

what is HIV viral attachment and entry blocked by?

Answer 4

enfuvirtide and maraviroc

Question 5

what is HIV penetration blocked by?

Answer 5

interferon alpha - HBV, HCV

Question 6

which drug stops the influenza virus from being released?

Answer 6

neuraminidase inhibitors

Question 7

what does acyclovir do?

Answer 7

blocks nucleic acid synthesis

Question 8

what is acyclovir

Answer 8

a guanosine analogue

Question 9

what makes the virus more susceptible to acyclovir than the host?

Answer 9

Herpesvirus-encoded thymidine kinase encoded in the viral genome phosphorylates acyclovir 100 fold faster than the host cell enzyme does

Question 10

what converts the monophosphate to do/triphosphate forms

Answer 10

host kinases

Question 11

what does acyclovir triphosphate do? (AcTP)

Answer 11

outcompetes deoxyguanosine triphosphate as the substrate for DNA polymerase infections - then incorporated into viral DNA - premature DNA chain termination

Question 12

what is the structural difference between acyclovir and guanosine

Answer 12

acyclovir has just an O where guanosine has a rind

Question 13

what are the 7 stages of the HIV virus life cycle?

Answer 13

• binding/attachment
• fusion
• reverse transcription
• integration
• replication
• assembly
• budding

Question 14

where in the life cycle does maraviroc target

Answer 14

the binding

Question 15

where in the life cycle does enfurivirtide target

Answer 15

fusion

Question 16

how does Nevirapine target HIV virus?

Answer 16

it is a non-nucleotide reverse transcriptase inhibitor

Question 17

how does AZT target HIV virus?

Answer 17

nucleotide reverse transcriptase inhibitor

Question 18

where in the life cycle does dolutegravir target

Answer 18

integration into the host DNA

Question 19

where in the life cycle does amprenavir target

Answer 19

it is a protease inhibitor

-the protease acts to break up the long protein chain that form the immature virus

Question 20

what is are the main components of bacterial cell membrane?

Answer 20

ergosteroids, mycolic acids

Question 21

what do ahminoglycosides names end

Answer 21

-mycin

kanamycin,vancomycin

Question 22

what do aminoglycocide and B lactase target

Answer 22

cell wall synthesis

Question 23

inhibitors of bacterial metabolism

Answer 23

sulphonamides and trimethoprim

Question 24

inhibitors of cell wall synthesis bacteria

Answer 24

ahminoglycosides (vancomycin…), B lactams

Question 25

which antimicrobials inhibit protein synthesis

Answer 25

tetracyclines, aminoglycosides, macrolides and chloramphenicol

Question 26

Rifamycin

Answer 26

nhibits prokaryotic DNA transcription into mRNA by inhibiting DNA-dependent RNA polymerase by binding its beta-subunit.

Question 27

Neomycin

Answer 27

prevents ribosome assembly by binding to the prokaryotic 30S ribosomal subunit.

Question 28

Tetracyclines

Answer 28

block the A site on the ribosome, preventing the binding of aminoacyl tRNAs.

Question 29

Chloramphenicol

Answer 29

blocks the peptidyl transfer step of elongation on the 50S ribosomal subunit in both bacteria and mitochondria

Question 30

Macrolides

Answer 30

as well as inhibiting ribosomal translocation[8] and other potential mechanisms) bind to the 50s ribosomal subunits, inhibiting peptidyl transfer

Question 31

fluroquinolones

Answer 31

inhibition of nucleic acid function or synthesis

Question 32

what has resulted in the resistance to fluroquinolones/

Answer 32

alteration in the target enzyme - DNA gyrase

Question 33

how do Blactams enter gram negative bacteria?

Answer 33

through porin channels

Question 34

how are enterobacter largely resistant to cephalosporins?

Answer 34

B lactamases (also may have altered channels through which now cannot pass through)

Question 35

what has stopped tetracyclines being effective against gynecologic infections

Answer 35

plasmid mediated protein that promoted efflux of drug

Question 36

B lactamases (penicillinases) do what

Answer 36

destroy the B lactic ring

Question 37

methicillin binding site responsible for what ?

Answer 37

methicillin resistance in staph aureus

Question 38

what shape is the B lactic ring/

Answer 38

square

Question 39

what does clavulanic acid do?

Answer 39

inhibits many B lactamases by binding to the B lactamase - protecting other B lactase from the enzyme

Question 40

which B lactcams are B lactase resistant?

Answer 40

monobactam and carbapenem nucleus