MP321 week 2 Flashcards
where do drug molecules come from
bacteria, plants, fungi, animals, inorganic (lab)
why would you use a broth micro dilution assay
cheap, reproducible and robust giving accurate results
define cytotoxicity assay
assay test to measure the ability of cytotoxic compounds to cause cell damage or cell death
what do antibacterial drugs do
kill or inhibit the growth of microbes at low concentrations
what is B-lactam mode of action
stop bacterial cell wall being formed, because human (host) cells do not have cell walls it does not affect the host
do antibiotics kill or inhibit growth of bacteria
kill only
name one difference between gram positive and gram negative bacteria
gram negative have a much thinner cell wall than gram positive thus making them more vulnerable
explain how enzymes are used to make the bacterial cell wall more rigid
enzymes called transpeptidases or penicillin binding proteins link 2 strands of sugars together forming a bridge that is more rigid
what is called peptidoglycan
the bacterial cell wall, this is because it is made of peptides and sugars
name the 4 classes of B-lactams
penicillin
cephalosporin
carbapenem
monobactam
describe the structure of a penicillin type B-lactam
cyclic amide is fused to 5 membered ring with sulphur atom inside
describe the structure of a cephalosporin type B-lactam
cyclic amide is fused to a 6 membered ring with sulphur atom inside
describe the structure of a carbapenem type B-lactam
cyclic amide is fused to 5 membered ring with sulphur atom on the side (NOT inside ring)
describe the structure of a monobactam type B-lactam
there is no ring attached to the cyclic amide
how to spot if the B-lactam has lost antibacterial properties
if there is no longer the N, C double bond O square functional group
in which kind of medium are B-lactams the most degradable
acidic medium- ie stomach
why can some B-lactams not be administered orally
they are very degradable in acidic medium- ie stomach and so have lost their antibacterial properties by the time they reach the bloodstream
describe the mode of action of B-lactams
inhibit cell wall synthesis of bacteria
B-lactam mimic natural substrate for bacteria
when B-lactam bind to bacterial enzyme this is irreversible and so the bacteria cannot bind with real substrate
because the bacteria then do not have a rigid cell wall to protect them they go into cell lysis and die
why are B-lactams highly reactive
they have a cyclic amide which unlike normal amides are not planer therefore the movement of electrons make B-lactam unstable and very reactive
define narrow spectrum
these target a specific class of bacteria, normally only working on gram positive
define broad spectrum
normally work on both gram positive and gram negative but not always on antipseudomonal
what are antipsudomonal penicillins
antimicrobial agents, which are used to treat pseudomonal infections- gram negative
name one penicillin that does not work on gram negative bacteria
benzylpenicillin
how to bacteria try to protect themselves against B-lactams
produce a chemical called B-lactamase which inactivates B-lactams
how do we try to combat B-lactams instability in acidic medium
attach an electronegative group to minimise neighbouring group attack on the B-lactam carbonyl
Which one is true?
1. Benzylpenicillin can be given orally
2. Amoxicillin and piperacillin are both effective against pseudomonas
3. Cefuroxime is B-lactamase resistant
4. Cefaclor cannot be taken orally
3
how is phenoxymethyl penicillin administered
orally
what is the most appropriate antibiotic to treat strep
phenoxymethyl penicillin
what kind of bacteria is flucloxacillin used to treat
gram positive
what kind of B-lactam must be administered with another antibiotic
B-lactamase inhibitors like tazobactam and clavulanic acid
name 2 antibiotic that work on gram positive and gram negative but not pseudomonas
amoxicillin and ampicillin
name 2 antibiotics that are active against pseudomonas
ticarcillin
piperacillin
name 4 antibiotics active against gram positive
cefalexin
cefradine
cefadroxil
cefaclor
what are cefotaxime, cefriaxone, cefixime and cefpodoxime all effective on
gram negative
B-lactamase resistant
name 2 cephalosporins that can be given orally
cefalexin and cefaclor
name 4 parenteral administration routes
Subcutaneous (under the skin)
Intramuscular (in a muscle)
Intravenous (in a vein)
Intrathecal (around the spinal cord)
which of the following is true
1- The peptidoglycan in Gram-positive bacteria is thicker than the one in Gram-negative bacteria
2- Ticarcillin is a cephalosporin with antipseudomonal activity
3- Amoxicillin is active against Pseudomonas aeruginosa
4- Flucloxacillin is degraded by beta-lactamases
A beta-lactamase inhibitor can only be given parenterally
1
name the 4 main structural classes of antifungals
polyenes
azoles
echinocandins
allylamines
name the main functional group in polyenes
alkene groups
name the main functional groups in imidazoles
ring with 2 nitrogens- called imidazole group
this is basic (can accept hydrogen)
the nitrogen that is attached to amide accepts hydrogen, the other nitrogen is making the ring aromatic
name the main functional group in triazoles
ring with 3 nitrogens (tri=3)