L1 antibiotics Flashcards

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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

A

Quinolone

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
Q

5 ways antibiotics kill bacteria

A
  • 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
Q
  • Narrow spectrum
A

○ Effective against only a few specific bacteria
○ Eg. Flucloxacillin
§ Active against staph aureus and many streps
§ Gram positive antibiotic

27
Q

Broad spectrum antibiotic

A

○ Effective against a wide range of bacteria, from different groups
○ Eg. Augmentin
§ Aureus, streptococci, enterococci, many gram negative coliforms, haemophilus influenzae

28
Q
  • Empirical therapy used when
A

○ 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

29
Q

reasons to name for narrower spectrum

A

Broad spectrum therapy
○ Encourages bacterial resistance
○ Kills more normal flora
○ Poses greater risk of drug adverse effects

30
Q

MIC

A
  • The minimum inhibitory concentration (MIC)

○ The minimum concentration of an antibiotic that inhibits visible growth of bacteria in an in vitro test system

31
Q

MIC testing process

A

○ 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
Q

instead of doing a formal MIC, what is done instead

A
  • Routine susceptibility tests are done in simplified form, rather than doing a formal MIC in each case
33
Q

process of routine susceptibility test

A

○ 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

34
Q

MIC < 0.12

A

highly susceptible

35
Q

MIC < 0.05

A

relatively resistant

36
Q

MIC < 4.00

A

resistant

37
Q

MIC > 4.00

A

highly resistant

38
Q

Mechanisms of resistance to antibiotics

A

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
Q

Active removal of an antibiotic from a cell

A
  • Efflux pumps

Bacteria have many different types of energy driven mechanisms to remove substances from the cell

40
Q

Inhibition of antibiotic entry to target site

A
  • 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
Q
  1. Production of enzymes which modify or destroy antibiotics
A

§ 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

42
Q
  • Antibiotics resistant to beta lactamase
A

§ Penicillins that can resist
□ Methicillin, flucloxacillin
§ Cephalosporins that can resist
□ cephalexin and others

43
Q

Normal transpeptidase gene

A

§ Normal gene called pbpB encodes PBP2

44
Q

mutated transpeptidase gene

A

§ Mutated gene called mecA encodes PBP2a

45
Q

MRSA

A

methicilin resistant staph aureus

46
Q
  • Route of antibiotic administration
A
  • Oral - PO
    - Parenteral - IV or IM
    - Rectal - PR