L1 antibiotics Flashcards

1
Q

anti infective drugs

A
Anti-infective drugs - antimicrobials 
		○ Antibacterials 
		○ Antivirals 
		○ Antifungals 
		○ Antiprotozoals 
		○ Antihelminths
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2
Q
  • Antibiotic
A

○ A chemical produces by a microorganism that kills or inhibits ither microorganisms
○ Synthetic or semisynthetic antimicrobials are not strictly antibiotics by definitions

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3
Q

In common clinical usage and antibiotic is

A

§ Agent active against bacteria
§ Natural, synthetic or semisynthetic
§ Done not include antiseptics or disinfectants

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4
Q

most antibiotics are from

A

○ Most antibiotics are products of bacteria or fungi that live in the soil

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5
Q

microbes that produce antibiotics

A

○ Microbes make these compounds in order to kill or inhibit other microbes that are competing for nutrients
○ The microbes which produce these compounds have also developed mechanisms to prevent themselves being killed by them (ie. Resistance mechanisms)

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6
Q

semisynthetic antibiotic

A

emisynthetic antibiotic

§ Based on a natural antibiotic scaffold with chemical modifications

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7
Q

synthetic antibiotic

A

○ Synthetic

§ Not common

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8
Q

4 beta lactams

A
  • Penicillins
    Cephalosporins
    Monobactams
    Carbapenems
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9
Q

what does transpeptidase do

A

joins together peptidoglycan precursors onto the growing cell wall

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10
Q

3 steps for the transpeptidase to join the peptidoglycan precursors to the cell wall

A

□ Breaks off one of the d alanines
□ Joins the pentapeptide onto the growing chain
□ Joins the sugars

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11
Q

how do beta lactam antibiotics work

A

B-lactam antibiotics work by binding to transpeptidase and stops it from working

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12
Q

another word for transpeptidase

A

Transpeptidase and called penicillin binding proteins PBPs

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13
Q
  • Glycopeptide antibiotics work by
A

○ work by binding the d ala d ala end of the peptidoglycan precursor
○ As the enzyme cant remove the d ala, the transglycosylase activity of the transpeptidase activity cant proceed
○ If peptidoglycan cant be strengthened and cross linked, cell wall is weakened and bacterial cell bursts under osmotic pressure

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14
Q

rifamycins work by

A

§ Inhibits the enzyme that produce mRNA

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15
Q

○ Macrolides, clindamycin, streptogramins, oxazolidinones work by

A

binds s to 50S part of the ribosome and inhibit protein elogation

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16
Q

○ Aminoglycosides work by

A

§ Binds to 30S part of the ribosomes and cause misreading of the code

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17
Q

○ Tetrecyclines, tigecycline work by

A

§ Block binding of tRNA to 30S part of the ribosome

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18
Q

2 antibiotics acting on folate synthesis

A
  • Sulfonamides and trimethoprim
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19
Q

antibiotics acting on folate synthesis work by

A

○ Prevent manufacture of DNA and RNA precursors

20
Q

Co trimoxazole

A

trimethoprim + suphamethoxazole

21
Q

1 Antibiotic acting on DNA replication and function

22
Q

Quinolone works by

A

inhibits action of enzymes necessary for DNA replication

23
Q

1 antibiotic acting on cell membrane

A

daptomycin

24
Q
  • Daptomycin works by
A

○ Has a lipophilic tail
○ Inserts itself into the phospholipid bilayer of the membrane and causes the membrane to depolarise which causes death of the bacterial cell

25
5 ways antibiotics kill bacteria
- work on production/maintenance of the cell wall - work on protein production - work on folate synthesis - work on DNA replication and function - work on cell membrane
26
- Narrow spectrum
○ Effective against only a few specific bacteria ○ Eg. Flucloxacillin § Active against staph aureus and many streps § Gram positive antibiotic
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Broad spectrum antibiotic
○ Effective against a wide range of bacteria, from different groups ○ Eg. Augmentin § Aureus, streptococci, enterococci, many gram negative coliforms, haemophilus influenzae
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- Empirical therapy used when
○ Specimens are not collected for lab investigation ○ While waiting for results of lab investigations - Empirical therapy generally broader spectrum than directed therapy - May switch from empirical to directed therapy
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reasons to name for narrower spectrum
Broad spectrum therapy ○ Encourages bacterial resistance ○ Kills more normal flora ○ Poses greater risk of drug adverse effects
30
MIC
- The minimum inhibitory concentration (MIC) | ○ The minimum concentration of an antibiotic that inhibits visible growth of bacteria in an in vitro test system
31
MIC testing process
○ A series of test tubes containing § Broth culture medium § Decreasing amounts of antibiotic being testes § An inoculum of the bacterium being tested (same inoculum into each tube) ○ The tubes are incubated overnight to allow bacterial growth ○ MIC - concentration at which the antibiotic first works
32
instead of doing a formal MIC, what is done instead
- Routine susceptibility tests are done in simplified form, rather than doing a formal MIC in each case
33
process of routine susceptibility test
○ Lawn inoculum of bacterium being tested - Even layer of bacteria ○ 'paper discs impregnated with a range of antibiotics ○ Incubated overnight and observed once the lawn has grown
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MIC < 0.12
highly susceptible
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MIC < 0.05
relatively resistant
36
MIC < 4.00
resistant
37
MIC > 4.00
highly resistant
38
Mechanisms of resistance to antibiotics
Active removal of an antibiotic from a cell Inhibition of antibiotic entry to target site Production of enzymes which modify or destroy antibiotics Alteration of the antibiotic's target site so it can no longer bind
39
Active removal of an antibiotic from a cell
- Efflux pumps | Bacteria have many different types of energy driven mechanisms to remove substances from the cell
40
Inhibition of antibiotic entry to target site
- Porin channels - Water filled channels which control the entry of aqueous molecules into the cell - Mutates into a kind of porin channel that doesn’t let the antibiotic in - Eg. Pseudomonas aeruginosa § Mutation confers resistance to imipenem
41
3. Production of enzymes which modify or destroy antibiotics
§ B-lactamases □ A large family of enzymes which break the B lactam ring of the antibiotic □ More than 1000 described □ Different affinities for different beta lactam antibiotics □ Penicillinases, cephalosporinases, carbapenemases
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- Antibiotics resistant to beta lactamase
§ Penicillins that can resist □ Methicillin, flucloxacillin § Cephalosporins that can resist □ cephalexin and others
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Normal transpeptidase gene
§ Normal gene called pbpB encodes PBP2
44
mutated transpeptidase gene
§ Mutated gene called mecA encodes PBP2a
45
MRSA
methicilin resistant staph aureus
46
- Route of antibiotic administration
- Oral - PO - Parenteral - IV or IM - Rectal - PR