Antibiotics Flashcards

1
Q

What is selective toxicity?

A

Where compounds harm the pathogen but not the host

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2
Q

Define antimicrobial

A

Any substance active against microbes

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3
Q

Define antibiotic

A

Naturally occurring product active against bacteria

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4
Q

Define broad spectrum

A

Kills most germs gram positive and negative or anaerobes

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5
Q

Define narrow spectrum

A

Kills narrow range of microbes

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6
Q

Define bactericidal

A

Actively kills bacteria

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7
Q

Define bacteriostatic

A

Prevents bacteria multiplying

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8
Q

What does an antibiotic’s role of being bactericidal or bacteriostatic depend on?

A
  • microorganism number (if lots of bacteria less likely to be bactericidal)
  • antibiotic concentration (if low may not be sufficient to kill so not cidal)
  • is immune system compromised as affects antibiotic efficacy
  • infection site penetration capability
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9
Q

Bactericidal agent examples

A

Penicillin
Beta lactams
Aminoglycosides

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10
Q

Bacteriostatic agent examples

A

Tetracyclines
Chloramphenicol
Azithromycin

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11
Q

What are synergistic antibiotics?

A

Combined activity is greater than sum of individual activities

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12
Q

Example of synergistic antibiotics

A

Beta lactams

Aminoglycoside

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13
Q

antagonistic antibiotics define

A

Activity of 1 drug is compromised by other

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14
Q

Example of antagonistic antibiotics

A

Tetracycline and chloramphenicol with beta lactam or aminoglycoside
2 beta lactams together (penicillin and flucloxacillin in staph)

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15
Q

What is the significance of a therapeutic index?

A

Narrower index means more likely to be toxic

= toxic/therapeutic

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16
Q

Example of an antibiotic with a high therapeutic index

A

Beta lactam

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17
Q

Example of an antibiotic with a low therapeutic index

A

Aminoglycosides

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18
Q

What do beta lactams and glycopeptides do?

A

Inhibit cell wall synthesis

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19
Q

What do quinolones do?

A

Inhibit DNA gyrase

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20
Q

What does trimethoprim and sulfonamides do?

A

Inhibit folic acid metabolism

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21
Q

What do polymixins do?

A

Destroy cytoplasmic membrane structure

22
Q

What does rifampicin do?

A

Inhibits DNA directed RNA polymerase

23
Q

What do macrolides, clindamycin and chloramphenicol do?

A

Inhibit protein synthesis

50S inhibitors

24
Q

What do aminoglycosides and tetracyclines do?

A

Inhibit protein synthesis

30S inhibitors

25
Examples of antibiotics against gram positive bacteria
``` Penicillins against strep, staph, listeria Fusidic acid Macrolides against strep Clindamycin - strep Glycopeptides against strep and staph Oxazolidinones - strep and staph Daptomycin - strep and staph ```
26
Examples of antibiotics against gram negative bacteria?
``` Polymixin Trimethoprim Aminoglycosides - also against strep and staph which are gram positive Monobactams Temocillin ```
27
Examples of broad spectrum antibiotics
``` Beta Lactams (Carbapenems Amoxicillin Piperacillin Cephalosporins) ``` Chloramphenicol - also positive, negative, anaerobes Tetracycline - also positives, negative, anaerobes
28
What is the bacterial cell wall like?
- peptidoglycan | - not contained in eukaryote cell wall
29
What do penicillins do? Use, dose, admin, side effects
- inhibit cell wall synthesis - gram positive - oral and IV - 4-6 times a day dose - penetrate most tissues inc. meninges - side effect allergy IgE mediated anaphylaxis, - pregnancy safe - for streptococcal and meningococcal disease - produces beta lactamase and alters protein binding protein to bacteria - resistance to many staphylococcus and S. penumoniae, worldwide gonococcal - rash with allopurinol
30
Amoxicillin
- inhibits cell wall synth - gram positive and negative - oral and IV - 3 x a day - penetrates most - penicillin allergy, fever, neutropenia, mononucleosis - pregnancy safe - resistance staphylococci and pneumoniae, worldwide gonococcal - for streptococcal drug choice if not sore throat, listeria - produces beta lactamase and PBP - rash with allopurinol
31
Flucloxacillin
- inhibits cell wall synth - gram positive - oral and IV - 4 x a day - penetrates most - penicillin allergy, rash, leukopenia - pregnancy - same resistance as pen - S. aureus drug of choice except MRSA - alters PBP
32
Co-amoiclav
- amoxicillin and clavulanic acid - inhibits cell wall synth and beta lactamase inhibitor - gram +, -, anaerobes - oral and IV - 3 x a day - penetrates most - liver injury - MRSA resistance to it - for polymicrobial infections - alters PBP, impermeability, efflux
33
Piptazobactam
- piperacillin and tazobactam - inhibits cell wall and beta lactamase inhibitor - gram +, -, anaerobes - IV - 3-4 x day - penetrates most - pen allergy, neutropenia, hypernatremia - MRSA resistant - for polymicrobial inf. - PBPs, efflux, impermeability - interacts with methotrexate
34
Cefuroxime
- cell wall - +, -, pseudomonas - IV - 3 x day - penetrates most - allergy, C. difficile - pregnancy and children - MRSA res. - for pneumonia, intra ab serious and UTIs - PBP, efflux, impermeability, beta lactamases
35
Ceftriaxone
``` - cell wall +, -, not pseudomonas - IV - 1/2 a day - penetrates most and inflamed meninges - allergy, C. difficile - MRSA resistant - for meningitis and pneumonia - PBPs, efflux, imp. ```
36
Ceftazidime
- cell wall - + and -, pseudomonas - IV 3 x day - penetrates most and inflamed meninges - allergy, C. difficile - MRSA resistant - for UTIs, inta ab, not for community acquired infection - PBPs, efflux, beta lactamase, impermeability
37
Carbapenems
- cell wall, beta lactamase inhibits - +, -, anaerobes, pseudomonas - IV - 3 x day - penetrates most inc. inflamed mininges - allergy, rash, seizures - MRSA resistant - for polymicrobial inf. - PBP, efflux, imp
38
Glycopeptides - vancomycin
- cell wall - +, anaerobes - IV - 1/2 x day - poor penetration into CSF - nephrotoxic - VRE resistant - for problem gram positive infections - alters binding site
39
Which agents inhibit protein synthesis?
``` Aminoglycosides Tetracyclines Chloramphenicol Macrolides (erythromycin, clarithromycin) Clindamycin Fusidic acid ```
40
Aminoglycosides - gentamicin, amikacin
- acts on 30S ribosome - gram +, -, pseudomonas - IV - 1 a day - water soluble, poor lung and CNS penetration - nephrotoxicity and ototoxicity - gram - org resistant some - use for serious systemic sepsis - efflux, imp - nephrotoic with vancomycin, colistin
41
Macrolides - erythromycin, azithromycin, clrithromycin
- acts on 50S ribosome - bacteriostatic - gram + - oral and IV - 1/2 x day - excellent IC penetration - children - QT prolong, inhibits P450, otitis media, pharyngitis, legionnairs - staph and strep resistance - for atypical agents, pen allergy and STIs - mutates binding site
42
Which drugs affect nucleic acid metabolism
- quinolones - rifampicin -metronidazole (nucleic metabolism similar in bacteria to mammals so selective toxicity is often poor except with these)
43
Quinolones
- inhibits DNA gyrase - +, staph not strep, -, pseudomonal - oral and IV - 2 x a day - meninges and most penetrate - not pregnant - lowers seizure threshold, tendon rupture - high resistance rates - UTI, intra abdom, - not for pneumonia - efflux and imperm
44
Examples of antifolates
Sulphonamides (inhibits dihydropteroate synthase) | Trimethoprim (inhibits dihydrofolate reductase which is in human cells to but is much more active on bacterial enzyme)
45
Role of dihydrofolate reductase
Dihydrofolate to tetrahydrofolate | - trimethoprim targets
46
Role of dihydropteroate synthase
Forms dihydropteroate from first molecules | Targeted by sulphonamide
47
Examples of membrane disorganising agents
Amphotericin (antifungal agent) Colistin (polymyxin) Daptomycin
48
Qualities of an ideal antibiotic
- selectively toxicity - reach and concentrate target organ - reach good levels in body fluids infected - minimally toxic - does not select resistance - inexpensive
49
Antibiotic misuse
Widely prescribed - often when conditions did not require them - agricultural use (dose cattle to increase yield, battery farming to control infection)
50
Antimicrobial resistance problems
``` UTIs RTIs Neisseria gonorrhea M. TB DIarrhoeal disease Penicillin resistance MDR Salmonella H. Influenzae Growing hospital resistant infections (methicillin resistant S. aureus, enterococci) Need in emergency department ```