Antibiotics Flashcards

1
Q

What class of antibiotics does Clindamycin belong to?

A

Lincosamide (related to macrolide)

Clindamycin is related to the macrolide class of antibiotics.

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2
Q

What is the primary mechanism of action of Clindamycin?

A

Protein synthesis inhibitor

Clindamycin is known to limit exotoxin production.

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3
Q

How does Clindamycin affect outcomes in Toxic Shock caused by Strep pyogenes?

A

Improves outcomes

Clindamycin is effective in managing Toxic Shock related to Strep pyogenes.

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4
Q

Is Clindamycin well absorbed in the body?

A

Yes

Clindamycin is a good option for skin and soft tissue infections if the bacteria are susceptible.

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5
Q

In which pediatric conditions is Clindamycin increasingly supported for effectiveness?

A
  • Pneumonia
  • Empyema
  • Bone/joint MRSA infections

Literature supports Clindamycin’s use in these pediatric infections.

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6
Q

What type of resistance is associated with Clindamycin?

A

Resistance mediated by the same gene as erythromycin

This resistance occurs via target site modification of the ribosomal binding site.

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7
Q

What risk is associated with erythromycin-resistant bacteria?

A

Inducible clindamycin resistance

If a bacteria is erythromycin-resistant, there is a risk of developing inducible resistance to clindamycin.

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8
Q

Fill in the blank: Clindamycin is known to limit _______ production.

A

exotoxin

Clindamycin’s inhibition of exotoxin production helps in treating certain infections.

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9
Q

True or False: Clindamycin is ineffective against severe S. aureus infections.

A

False

Clindamycin has a similar effect in severe S. aureus infections.

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10
Q

What types of infections is Doxycycline not recommended for?

A

Complicated or serious infections

Doxycycline should not be used for endovascular infections.

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11
Q

What are the common side effects of Doxycycline?

A
  • Photosensitivity
  • Oesophageal irritation
  • Enamel stain

Enamel staining is more pronounced when comparing tetracycline to doxycycline.

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12
Q

Beta-lactam antibiotics

A

Penicillins, Cephalosporins, Carbapenems, Monobactams

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13
Q

Mechanism of action of beta lactam antibiotics

A

Interfere with cell wall synthesis

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14
Q

Glycopeptide antibiotic

A

Vancomycin

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15
Q

Mechanism of action of Vancomycin

A

Interfere with cell wall synthesis, binds to D-Alanyl-D-Alanine and prevents cross linking

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16
Q

Antibiotics that interfere with nucleic acid synthesis

A

Sulfonamides, Trimethoprim, Quinolones, Rifampicin

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17
Q

Antibiotics target folate synthesis

A

Sulfonamides, Trimethoprim

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18
Q

Antibiotics target DNA gyrase

A

QuinolonesA

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19
Q

Antibiotic target RNA polymerase

A

Rifampicin

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20
Q

Antibiotics targeting protein synthesis

A

Tetracylines, Aminoglycosides, Macrolides, Clindamycin, Linezolid, Chloramphenicol

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21
Q

Antibiotics targeting 30s subunit ribosome

A

Tetracylines, aminoglycosides

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22
Q

Antibiotics targeting 50s subunit ribosome

A

Macrolides, Clindamycin, Linezolid, Chloramphenicol

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23
Q

Antibiotics that depend on CMax

A

Aminoglycosides, fluoroquinolones

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24
Q

Antibiotics that depend on AUC/MIC

A

Vancomycin, Azithromycin, Fluoroquinolones, Aminoglycosides, LinezolidA

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25
Q

Antibiotics that depend on T >MIC (dosing interval)

A

Beta lactams, Clindamycin, Vancomycin, Macrolides

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26
Q

Antibiotics with >90% bioavailability

A

Clindamycin, Doxycycline, Linezolid, Metronidazole, Rifampin, Fluconazole, Voriconazole

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27
Q

Antibiotics with 80- 90% bioavailability

A

Amoxicillin, Cephalexin, Ciprofloxacin, Cotrimoxazole

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28
Q

Antibiotics with 60 - 80% bioavailability

A

Penicillin VK, Valganciclovir

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29
Q

Antibiotics with <60% bioavailability

A

Cefuroxime, Augmentin, Azithromycin, Aciclovir, Fosfomycin, Clarithromycin

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30
Q

Antibiotics with low oral bioavailability due to low intestinal permeability

A

Amikacin, Gentamicin, Ceftazadime, Vancomycin

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31
Q

Beta lactam antibiotic side effects

A

Hypersensitivity, neurotoxicity and reduced seizure threshold at higher doses, GI upset, LFT derangement

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32
Q

Glycopeptide side effects (Vancomycin)

A

Red Man Syndrome (fast infusion rate), nephrotoxicity

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33
Q

Aminoglycoside side effects

A

Ototoxicity, nephrotoxicity

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34
Q

Macrolide side effects

A

QTc prolongation, CYP3A4 enzyme inhibition

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35
Q

Fluoroquinolone side effects e.g. Ciprofloxacin

A

Tendinopathy, neurotoxicity and seizure threshold, QTC prolongation

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36
Q

Tetracycline side effects

A

Enamel staining, oesophageal irritation, photosensitivity

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37
Q

Antifolate (Cotrim)

A

Rash (including SJS), Cytopenia

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38
Q

Chloramphenicol side effect

A

Grey baby syndrme, aplastic anaemia

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39
Q

Clindamycin s/e

A

GI upset, rash

40
Q

Metronidazole s/e

A

Peripheral neuropathy

41
Q

Nitrofurantoin s/e

A

Peripheral neuropathy, hepatotoxic (long term), pulmonary fibrosis (long term), haemolytic anaemia in neonates

42
Q

Daptomycin s/e

A

Myopathy, Rhabdomyolysis, Eosinophillic Pneumonia

43
Q

Antbiotics that disrupt bacterial cell membrane

A

Daptomycin, Polymixin B

44
Q

Penicillin mechanism of action

A

Bind to PBPs and inhibit completion of peptidoglycans and bacteral cell wall lysis

45
Q

Penicillinase resistant penicillins

A

Methicillin, Flucloxacillin (treat staph + strep, don’t treat enterococci)

46
Q

Aminopenicillins

A

Amoxicillin (has amino group that give it some gram negative cover)

47
Q

Natural penicillins

A

Penicillin G (Strep, Enterococci, Listeria, Neisseria, Syphillis)

48
Q

Acyl Ureidopenicillins

A

Piperacillin (extended gram negative cover, including Pseudomonas)

49
Q

Beta lactam/Beta lactamase inhibitor antibiotics (overcome acquired resistance mechanism of enzymatic modification)

A

Augmentin (Amox/Clavulanic Acid) and Tazocin (Piperacillin/Tazobactam)

50
Q

Benefit of beta-lactam/beta lactamase inhibitor antibiotics

A

Better activity against gram negative bacilli, MSSA, Beta-lactam producing anaerobes. Tazoscin is also antipseudomonal

51
Q

Cephalosporins mechanism of action

A

Same as penicillins (bind to PBPs, but differing affinity) and cause cell wall lysis. NO activity against enterococci and reduced activity against listeria. Resistant to beta lactamases produced by Staph Aureus

52
Q

1st generation Cephalosporins

A

Cephazolin, Cephalexin (MSSA, Strep cover)

53
Q

2nd generation Cephalosporins

A

Cefuroxime, Cefaclor (better Gram negative, specifically against H. Influenzae)

54
Q

3rd generation Cephalosporins

A

Ceftriaxone, Cefotaxime, Ceftazadime (good gram negative and broad spectrum gram positive), good CNS penetration

55
Q

What bacteria enzymes inactivate 3rd generation cephalosporins

A

ESBL and AmpC

56
Q

Why can Ceftriaxone be once daily dosed?

A

Highly protein bound

57
Q

Which 3rd generation cephalosporin has anti-pseudomonal activity?

A

Ceftazadime

58
Q

4th generation cephalosporins

A

Cefepime, Ceftaroline

59
Q

Cefepime coverage

A

Antipseudomonal, AmpC resistant

60
Q

Ceftaroline coverage

A

Anti MRSA and resistant pnuemonocci, able to bind to PBP2a

61
Q

Carbapenem antibiotics

A

Meropenem, Ertapenem, Imipenem

62
Q

Carbapenem coverage

A

Gram positive, Gram negative including ESBL+, Pseudomonas (except Ertapenem). Not MRSA or VREi

63
Q

Side effect of Carbapenem

A

Neurotoxicity, lowers seizure threshold (especially Imipenem)

64
Q

Types of antibiotic resistance

A

Intrinsic, Acquired and Adaptive/Inducible

65
Q

Example of intrinsic antibiotic resistance

A

Vancomycin and Penicillins don’t work for Gram negatives as cannot penetrate LPS layer, Cephalosporins don’t work for Enterococci due to low affinity for enterococcal PBP

66
Q

Example of acquired antibiotic resistance

A

Usually chromosome or plasmid mediated (MRSA = Chromosome, ESBL = Plasmid)

67
Q

Example of adaptive/inducible resistance

A

Upregulates in presence of stressors e.g. ESCAPM versus beta lactams, Pseudomonas efflux pumps or porin channels versus everything

68
Q

Four main mechanisms of antibiotic resistance

A

Enzymatic inactivation of antibiotic e.g. beta-lactamase
Alteration of antimicrobial binding side
Active efflux
Alterations in membrane permeability

69
Q

Choice of antibiotic for enterococcus faecalis

A

Penicillin or Amoxicillin

70
Q

Choice of antibiotic for Enterococcus faecium

A

Vancomycin

71
Q

Streptococcus Pneumoniae resistance mechanism

A

Decreased affinity of PBP. Enzyme gene alteration, leading to decreased affinity of penicillin to penicillin binding proteins (2b alterations give low level resistance, 2x alterations give high level resistance)

72
Q

Streptococcus Pneumoniae choice of antibiotic

A

Penicillin (provided not meningitis), aiming MIC ) of 0.06 to 2
Cephalosporin (Ceftriaxone, Cefotaxime) if meningitis for CNS penetration, wouldn’t rationalise to Penicillin unless MIC <0.06. Vancomycin added as potential for altered PBPs within pneumococcus

73
Q

Strep Pneumoniae treatment if resistant to cephalosporins and penicillins

A

Vancomycin, add Rifampicin. Consider Linezolid or Moxifloxacin

74
Q

Haemophillus Influenzae mechanism of antibiotic resistance

A

Enzymatic deactivation (beta-lactamase positive e.g. Amox resistant and Augmentin susceptible)
Alteration of PBP (BLNAR- beta lactamase negative antibiotic resistance, treat with Cephalosporin or Cotrimoxazole)

75
Q

Staphyloccous Aureus resistance mechanisms

A

90% produce enzyme (beta-lactamase/penicillinase) that inactivates penicillins

76
Q

How do anti-staph penicillins work

A

Different side chain which reduces access of b-lactamase enzyme

77
Q

Flucloxacillin adverse effects

A

Allergy, Bone marrow suppression at thigh doses, hepatotoxicity (including cholestatic liver failure), interstitial nephritis

78
Q

What disease states is Vancomycin best for and why?

A

Hydrophillic drug therefore good for bacteraemia and endocarditis but poor tissue penetration

79
Q

MRSA mechanisms of antibiotic resistance

A

Altered receptor binding or replacement of target site. Altered PBP2a (acquired genetic element unlike intrinsic set PBP1-4), which is encoded by the mec gene therefore penicillin can’t bind. Lab can test for mecA gene by PCR s rapid MRSA diagnostics

80
Q

Antibiotics which MRSA is resistant to

A

All penicillins and cephalosporins

81
Q

MRSA therapy options

A

Clindamycin, Vancomycin, Cotrimoxazole, Erythromycin Doxycline, (Gentamicin, Rifampicin, Fusidic Acid). Linezolid, Daptomycin, Ceftaroline

82
Q

What is the D zone test?

A

Inducible macrolide-lacosamide resistance. Modification of target RRNA of Staph Aureus on ERM gene. Erythromycin are strongest inducers of these gene but lincosamides are also weak inducers. Therefore if S.Aureus resistance to erythromycin on this test, there is a risk of inducible clindamycin resistance

83
Q

What type of infection should Co-trimoxazole not be used for?

A

Endovascular

84
Q

What does Co-trimoxazole cover?

A

MRSA, Gram positives and negatives, unusual infections (PJP, Toxoplasma, Stenotrophomonas)

85
Q

Linezolid class of antibiotic

A

Oxazolidinone

86
Q

Linezolid coverage

A

Gram positive action including MRSA and penicillin resistant S. Pnuemoniae, For serious VRE and MRSA organisms

87
Q

Linezolid mechanism of action

A

Targets protein synthesis at early stage (?alternative to Clindamycin for STSS)

88
Q

Side effects of Linezolid

A

Optic neuritis and peripheral neuropathy with >4 weeks therapy, thrombocytopenia

89
Q

Anti-toxin production options in STSS

A

Clindamycin, Linezolid, IVIg

90
Q

Gram negative organism mechanisms of resistance

A

ESBLs and AMPc

91
Q

What antibiotic are ESBL organisms sensitive and resistant to?

A

Sensitive: Carbapenems +/- Amikacin. Nitrofurantoin for lower UTI, Fosfomycin
Resistant: Penicillins, Cephalosporins, Monobactam

92
Q

Risk factors for ESBL organism

A

Travel, prolonged hospitalisation, multiple courses of antibiotics, indwelling catheters, malignancy, GI tract disease

93
Q

What organisms are ESBL found on

A

E. Coli, Klebsiella Pneumoniae, Klebsiella Oxytoca

94
Q

What is AMPc

A

Cephalosporinase, inducible resistance to penicillins, cephalosporins and gram negative acting penicillins (Tazoscin)

95
Q

What organisms produced AMPc

A

ESCAPM organisms. Enterobacter species, Citrobacter freundii, Serratia Marcescens, Proteus species, Providencia species, Morganella morganii

96
Q

Oral antibiotics are non-inferior in

A

BJI without bacteremia, pneumonia, SSTI

97
Q

MERINO trial finding

A

Tazoscin is not as effective as Meropenem for treatment of ESBL gram negative organisms