Antibiotics Flashcards

1
Q

Mechanism of Action
Penicillins

A

beta-lactam antibiotic
binds to penicillin binding proteins:

  1. Inhibit transpeptidase cell wall cross link
  2. Activation autolysin

weakens the cell wall
results in bacterial cell lysis

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2
Q

SE of Penicillins

A
  1. CNS toxicity (hallucinations, delusions, seizures)
    Renal dose adjustment required
  2. Anaphylaxis 7/100 people
  3. GI upset
  4. Blood dyscaria
  5. phlebitis if IV
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3
Q

Penicillins and pregnancy

A

safest antibiotic
PBPs only exist in bacteria

Safe in pregnancy, infancy, childhood, old age

Amoxicillin safe in breast feeding

First line treatment for pregnancy UTIs

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4
Q

Penicillin G and V Coverage

A

Gram positive bacteria

Anaerobic Spirochettes (Treponem pallidum - syphillus)

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5
Q

Penicillin is used to treat…

A

Meningitis - streptococcus pneumoniae

Group A strep infections (GAS)

Syphillus

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6
Q

MOA and SE of Cephalosporins

A

MOA:
beta-lactam antibiotic
weaken cell wall
bind PBP
*same as penicillins

  1. CNS toxicity (renal dose adjustment required)
  2. Disulfram reaction (acetaldehyde build up if you drink)
  3. C. diff infections (during and post)
  4. Bleeding (inhibits Vitamin K coagulation factor synthesis)
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7
Q

Which Cephalosporins cross the BBB

A

Third generation
- Cefixime, Cefotaxime, Ceftazidime, Ceftriaxone

Fourth Generation
- Cefepime

Fifth Generation (USA only)
- Ceftaroline

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8
Q

Which Cephalosporins cover pseudomonas infections?

A

Third generation (ceftazidime)

Fourth generation
(cefepime)

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9
Q

Which cephalosporins cover MRSA infections

A

Fifth generation
Ceftaroline

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10
Q

First generation Cephalosporins

A

Cephalexin
Cefazolin
Cefadroxil

*cross reactivity with penicillin 1%
contraindicated with penicillin anaphylaxis

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11
Q

Second generation cephalosporins

A

Cefaclor
cefuroxime
cefoxitin
cefprozil
cefotetan

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12
Q

Third generation cephalosporins

A

Cefotaxime
Ceftriaxone
ceftazidime
Cefixime

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13
Q

Fourth and fifth generation cephalosporins

A

Cefepime
ceftaroline

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14
Q

Penicillins

A

Penicillin G
Penicillin V
Cloxicillin
Amoxicillin/Clavulanate
Ampicillin/Sulbactam
Pipperacillin/tazobactam

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15
Q

Carbapenems MOA and route

A

beta-lactam antibiotic
bind to PBPs 1. transpeptidase inhibitor 2. autolysin disinhibitor

Imipenem
Meropenem
Ertapenem

*IV Only

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16
Q

Prescribing considerations and contraindications of carbapenems

A

IV only

gram positive, negative, pseudomonas infections - broad spectrum, empric

Do not give alone to treat pseudomonas to avoid resistance (prescribe with pipperacillin/tazobactam and/or aminoglycosides)

Contraindicated with VPA (seizures)

Renal dose adjustment

1% cross reactivity with penicillins

Super infections

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17
Q

Carbapenem SE

A

N/V/D
superinfections
hypersensitivity
cross reactivity with penicillins 1%
seizures with VPA

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18
Q

Mechanism of action carbapenems

A
  1. inhibition transpeptidase
  2. activation autolysin

Disrupt cell wall synthesis resulting in bacterial lysis

Only active against actively growing and dividing bacteria

Resistant against beta-lactamases - do not need to prescribe sulbactam, clavulanate, or tazobactam

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19
Q

Mechanism of action cephalosporins

A
  1. Inhibition transpeptidase
  2. Activation autolysin

Disrupt cell wall synthesis resulting in lysis of bacteria
*beta-lactam antibiotic
same as penicillins and carbapenems

3rd and 4th resistant against beta lactamases, BBB penetration, and pseudomonas coverage
5th generation MRSA coverage

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20
Q

Cephalosporins SE, and pregnancy

A

SE:
N/V/D, c.diff
disulfram reaction
neuerotoxicity
cross reaction with penicillins 1% first generaitons
bleeding risk

safe in pregnancy
safe in breastfeeding
3rd generations used to treat infants
dose reduction in kidney disease

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21
Q

Vancomycin

Mechanism of Action

A

Disrupts cell wall synthesis by binding to cell wall precursors - peptidoglycans

Results in cell lysis

Not absorbed systemically through PO administration - too big

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22
Q

Vancomycin

SE

A

Ototoxic - high pitch, low pitch, blance

Nephrotoxic - casts, proteinuria

Blood trough level (low trough)
TDM required
Monitor BUN, creatinine clearance

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23
Q

Pathophysiology of

C. Difficile

A

Antibiotics kill microbiome
Overgrowth of bad bacteria such as C. Diff

Toxin A and B produced and damage colon
Inflammation, pus, watery diarrhea

Gram positive, spore forming bacteria

First line treatment: Metronidazole IV and Vancomycin PO

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24
Q

Vancomycin and Pregnancy

A

PO vancomycin does not get absorbed systemically (too big, hydrophilic), safe in pregnancy and breast feeding

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25
Q

Vancomycin Coverage

A

Gram positive bacteria and MRSA

MRSA (gram positive cocci in clusters) - methicillin resistance, PBP different shape

C. difficile (gram positive bacilli)

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26
Q

Fosfomycin Coverage

A

Gram positive,
Gram negative,
Pseudomonas

*Cannot be used to treat pyelonephritis/renal infections (systemic) - too big to be absorbed

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27
Q

Fosfomycin mechanism of action

A

Prevents production of the building blocks of the cell wall peptidoglycan layer

Disrupts cell wall synthesis

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28
Q

Penicillin and Cephalosporin Drug interactions

A

Oral contraceptives

Probenicid (increases level)

Synergistic with aminoglycosides

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29
Q

Antibiotics that inhibit 50S Ribosome Subunit

A

Macrolides (Azithromycin, Erythromycin, Clarithromycin)

Licosamides (Clindamycin, linomycin)

Linezolid

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30
Q

Macrolide SE

A
  1. Prolonged QT interval
  2. Ototoxic
  3. Diarrhea (Motilin receptors) and metallic taste in mouth
  4. Elevated LFTs (biliary clearance)
  5. Renal dose adjustment needed
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31
Q

Macrolide Drug interactions

A

Inhibition CYP450

Synergistic with beta-lactam antibiotics

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32
Q

Macrolide coverage

A

Atypical infections (GERD, CAP, STIs)

Gram positive, gram negative (no pseudomonas coverage)

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33
Q

Erythromycin Drug Interactions

A

CYP3A4 metabolism

Cardiac death increases 6x when prescribed with CYP3A4 inhibitors
- CCB
- Azoles
- HIV protease inhibitors
- Anti-depressants

Inhibits CYP450 Enzyme, increasing level of
- warfarin
- theophylline
- carbamazepine

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34
Q

Macrolide mechanism of action

A

Inhibition 50S subunit on the ribosome

Bacteriostatic and bacteriocidal at higher concentrations

35
Q

Licosamide antibiotics and mechanism of action

A

Clindamycin
Linomycin

Bacteriostatic and bacteriocidal

Inhibit 50S ribosomal subunit

36
Q

Macrolides and Pregnancy

A

Safe in pregnancy however crosses the placenta

> 1 month of age

Do not breast feed

37
Q

Clindamycin SE

A
  1. QT Interval prolonged
  2. LFT elevation
  3. renal dose adjustment
    (similar to macrolide)
  4. C. diff infection (4 -6 weeks post, fatal)
  5. Rash/hypersensitivity/SJS*
38
Q

Clindamycin Coverage

A

MRSA
Gram positive
Anaerobes

Examples:
Gardenella Vaginalis
Clostridium
MRSA
Acne
Intra-abdominal infections and ulcers
Gangrene

39
Q

Clindamycin and Pregnancy

A

Safe in pregnancy

Avoid breast feeding - secreted in breast milk

40
Q

Drugs that CANNOT cross the BBB

A
  • 1st and 2nd generation cephalosporins
  • Clindamycin
  • Macrolides
  • Fluroquinolones
41
Q

Mechanism of Action Linezolid

A

Binds to the 23S portion of the 50S ribosomal subunit and stop s protein synthesis

bacteriostatic

42
Q

SE of linezolid

A

Myelosupression (monitor CBC weekly)

demyelination CNS

Hypertensive crisis

Serotonin Syndrome

43
Q

Linezolid coverage

A

gram positive organisms

MRSA

V

44
Q

Linezolid drug interactions

A

Do not prescribe with
- MAOI
- SSRI
- Sympatheticomimetics (methylphenidate, etc.)

45
Q

Aminoglycosides

A

Gentamycin
Tobramycin
Streptomycin
Neomycin
Amikacin
*end in mycin

46
Q

Aminoglycoside mechanism of action

A

bind to the 30S ribosomal subunit and

  1. prevent activation
  2. early termination of protein synthesis
  3. mis-reading of proteins, mutation

Bacteriostatic
Bacteriocidal - mutated proteins inserted into membrane and lysis results

47
Q

Aminioglycoside SE and contraindications

A

Neurotoxic

Nephrotoxic

Ototoxic (hearing, and balance)

Teratogenic (do not use if pregnant)

Do not breast feed *lacking data

48
Q

Aminoglycoside coverage

A

Pseudomonas
Gram negative bacteria

*no coverage for gram positive
*no coverage for anaerobes
* does not cross the BBB or GI (too positively charged)

IV form or IM form only

49
Q

Aminoglycoside drug interactions

A

Caution with
- Nephrotoxic drugs
- ototoxic drugs
- perforated ear drum D/C

Synergistic with
- beta-lactam antibiotics or vancomycin
- do not mix in the same IV bag *precipitates out

50
Q

Aminoglycoside monitoring

A

Peak and trough levels

*high trough is associated with high SE, want it as close to zero as possible

51
Q

Tetracyclines

A

Tetracycline
doxycycline
minocycline

52
Q

Tetracycline mechanism of action

A

Inhibits 30S ribosomal subunit

prevents synthesis of the protein / misread / early termination

53
Q

Tetracycline contraindications

A

Children < 8 years

Pregnancy

Post-Partum women

Breastfeeding

54
Q

Tetracycline SE

A

Deposition in bones (growth suppression)

Deposition in enamel (yellow/grey teeth) and hypoenamel

Hepatotoxic / Renal toxicity (higher in pregnant and post partum women)

GI upset

sunburn / photosensitivity

C. difficile infections

55
Q

Tetracycline drug interactions

A

Increase levels of digoxin and warfarin

Cations decrease absorption, do not take with food (1 hour before, 2 hours after)

56
Q

Tetracycline coverage

A

MRSA, Gram positive, some gram negative

*Used to treat peridontal, acne, and atypical infections (spotted fever, lyme disease, anthrax etc.)

57
Q

Nitrofurantoin drugs

A

Nitrofurantoin
Macrobid

58
Q

Nitrofurantoin Mechanism of Action

A

Binds to 30S ribosomal subunit and inhibits protein synthesis

Prodrug is activated by bacterial enzyme

59
Q

Nitrofurantoin Coverage

A

Gram positive, gram negative

*Pseudomonas is resistant

60
Q

Nitrofurantoin SE

A

Lungs
- inflammation lungs (dyspnea, infiltration) D/C
- Chronic lung fibrosis

Blood
- Agranulocytosis, thrombocytopenia, hemolytic anemia (newborn, G6PD deficiency)

NEUROTOXICITY
- demyelination of sensory and motor neurons
- chronic use

Heptatotoxicity

Birth defects
- Do not give in 38th week of pregnancy
- Do not breast feed

61
Q

Nitrofurantoin contraindications

A

Pregnancy 38 weeks
Breastfeeding
Children < 1 month
G6PD Deficiency

*hemolytic anemia

62
Q

Nitrofurantoin monitoring

A

CrCl > 50mL/min in order to reach the bladder

If < 50mL/min do not prescribe, it will not reach effective concentration

CBC

G6PD status

Lung function

63
Q

Fosfomycin dosing

A

Concentration dependent killing

one dosage, high concentration, with lots of water

64
Q

Fosfomycin monitoring

A

Requires CrCl > 50mL/min
*similar to Nitrofurantoin

65
Q

Fluroquinolone antibiotics

A

Ciprofloxacin
Moxifloxacin
Levofloxacin

66
Q

Fluroquinolone
Mechanism of Action

A

Inhibits DNA replication and cell division through 2 actions:

DNA topoisomerase inhibitor
- Cannot separate daughter strands during cell division

DNA gyrase inhibitor
- Supercoils DNA for replication (condenses DNA)

67
Q

Fluroquinolone SE and Contraindications

A

Contraindications
- Pregnancy
- Infants/children
- Myasthenia gravis
- Caution - greater than 60 years, glucocorticoid use, transplants, renal disease (increased risk of tendon rupture)

SE
- Prolonged QT interval
- Tendon rupture
- Sunburn / phototoxicity
- CNS toxicity - seizures
- C. Diff infections

68
Q

Fluroquinolone Coverage

A

Gram positive
Gram negative
Pseudomonas

*Neisseria gonorrhea is resistant

69
Q

Fluroquinolone drug interactions

A

Cations decrease absorption

increase warfarin, theophylline and carbamazepine (CYP450 inhibitor)

70
Q

Fluroquinolone monitoring

A

CrCl
high risk for CNS toxicity and tendon rupture if renal disease

71
Q

Metronidazole mechanism of action

A

Prodrug activated by bacterial enzyme

Generates ROS which damage DNA

Concentration dependent killing

72
Q

Metronidazole coverage

A

Anaerobes, protozoa

fusobacterium, gardenella vaginalis, trichomatis, C. difficile, etc.

73
Q

Metronidazole SE and education

A

VRE
Carcinogenic in mice
GI upset
hepatotoxic (metabolism)
Disulfram reaction (do not drink)

74
Q

Metronidazole contraindications

A
  • alcohol
  • caution in liver disease
75
Q

Metronidazole in pregnancy and breast feeding

A

Can take while pregnant
Will result in bitter tasting breast milk

76
Q

Sulfonamide SE

A

Rash

Phototoxicity

Hemolytic anemia (< 2 months, G6PD deficiency)

agranulocytosis, thrombocytopenia

kernicterus (displaces from bilirubin)

Renal toxicity - crystalizes

77
Q

Sulfonamide Education

A
  • do not breast feed (kernicterus, hemolytic anemia)
  • drink 8-10 glasses of water a day
78
Q

Sulfonamide drug interactions

A

Increases dose of
- hypoglycemics
- warfarin
- AEDs (phenytoin)

79
Q

Sulfonamide Contraindications

A
  • Sulfa allergy
  • Pregnancy first / third trimester
  • breast feedin
  • infants < 2 months old
  • G6PD deficiency
  • Caution in elderly - more likely to have TEN, SJS, and neutropenia
80
Q

Trimethoprim mechanism of action

A

inhibition of folate synthesis
unable to replicate DNA/RNA

81
Q

SE of Trimethoprim

A

Megaloblastic anemia (more common pregnant, alcoholics)

hyperkalemia (worsened by ACE inhibitors, ARBs, potassium sparing diuretics)

Do not give in first and third trimester (Neural tube risk)

82
Q

Trimethoprim contraindications

A
  • folate deficiency
  • pregnancy (first trimester - NTD)
  • lactation
83
Q

TMP/SMX monitoring

A
  • CBC and WBC differential
  • CrCl (reduce dose by 50% if CrCl < 30)
  • Potassium
  • Pregnancy stage
84
Q

TMP/SMX ratio

A

1:5