Antibiotics Flashcards

1
Q

penicillin MOA

A

Cell Wall Synthesis Inhibitor

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2
Q

penicillin adverse effects

A

nephrotoxicity, allergic interstitial nephritis, seizures (toxic levels due to renal dysfunction), diarrhea, C. difficile infection (with broader spectrum)

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3
Q

penicillin ___ killing, half life

A

Time-dependent killing; most effective against microorganisms rapidly growing + dividing
* Very short half-life <2 hrs; dosed multiple times/day

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4
Q

penicillin for special population

A

safe for infants and pregnancy
dose adjustment for renal dysfunction

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5
Q

penicillin has sensitivity to

A

cephalosporins

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6
Q

amoxicillin is __ spectrum

A

broad spectrum

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7
Q

cephalosporin MOA

A

Cell Wall Synthesis Inhibiton

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8
Q

adverse effects of cephalosporin

A

GI intolerance, seizures (high doses), interstitial nephritis, rare
blood dyscrasias,
***C. difficile infection

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9
Q

cephalosporin is ___ killing

A

Time-dependent killing; most effective against microorganisms rapidly growing + dividing

  • Renal elimination for all except ceftriaxone (liver) – adjust dose prn
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10
Q

CSF penetration of cephalosporin

A

1st + 2nd Gen: low CSF penetration – do not use for bacterial meningitis

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11
Q

special population for cephalosporin

A

Safe for use in infants/children (avoid ceftriaxone in neonates -> bilirubin displacement and kernicterus )
Crosses placenta + present in breastmilk Generally safe in pregnancy/breastfeeding
Adjust dose with renal dysfunction for older adults

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12
Q

CARBAPENEMS MOA

A

Cell Wall Synthesis Inhibitor

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13
Q

adverse effects of carbapenems

A

confusion, delirium, seizure, diarrhea, C. difficile infection anemia, ↑LFT’s

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14
Q

carbapenems ____ killing
_____ CSF

A

Time-dependent killing
* Post-antibiotic effect
* Penetrates CSF

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15
Q

Drug interactions of carbapenems

A

valproic acid (reduced effect -> seizures)

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16
Q

monitoring for carbapenems

A

renal/liver/hematologic function periodically

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17
Q

penicillin monitoring for

A

renal function with renal disease

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18
Q

cephalosporin monitoring for

A

c. diff symptoms

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19
Q

monobactams MOA

A

Cell Wall Synthesis Inhibitor

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20
Q

adverse effects of monobactams

A

thrombophlebitis at injection site, neutropenia + ↑lft’s in peds, C. difficile infection

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21
Q

monobactams are___ killing
____ CSF

A

Time-dependent killing
* Penetrates CSF

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22
Q

beta lactam antibiotics metabolism and elimination
except

A
  • Minimal hepatic metabolism
  • Renal elimination (adjust dose prn)
    except ceftriaxone (liver) – adjust dose prn
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23
Q

monobactams special population

A

Not recommended in pediatric CNS infections due to seizure risk
Crosses placenta + present in breastmilk Use only if safer alternative not available.
Adjust dose with renal dysfunction for older adults

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24
Q

__ generations of cephalosporin

A

There are 5 generations and as they proceed from the 1st to the 5th generation, there is more gram negative and anaerobic coverage, less resistance to beta lactamases and more CSF penetration.

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25
Q

vancomycine MOA

A

Cell Wall Synthesis Inhibitor

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26
Q

vancomycine is reserved for ___

A

Reserve for Gram (+) infections where B-lactams cannot be used

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27
Q

adverse effects of vancomycin

A

renal toxicity,
ototoxicity (tinnitus, hearing loss, vertigo/dizziness),
neurotoxicity, hypersensitivity/anaphylaxis,
C. difficile (IV use),
thrombocytopenia, neutropenia, pancytopenia, thrombophlebitis, infusion reaction with rapid administration (red man syndrome)

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28
Q

pharmacokinetics of vancomycin
____ killing
metabolism and elimination

A

Time-dependent killing
* Post-antibiotic effect
* No B-lactam ring
* Poor GI absorption; minimal hepatic metabolism
* Renal elimination (adjust dose prn)

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29
Q

special population for vancomycin

A

Caution in neonates/infants due to renal immaturity
Crosses placenta + present in breastmilk. Limited data. Use only if safer alternative not available.
Caution with older adults due to nephrotoxicity, ototoxicity, + neurotoxicity

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30
Q

Drug of choice for MRSA and C. difficile and severe infections

A

vancomycin

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31
Q

monitoring of vanco

A

renal function, serum drug levels, hydration

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32
Q

Oral formulation of vanco only indicated for

A

C. Diff

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33
Q

FOSFOMYCIN
MOA
___ killing
____ metabolism and elimination

A

Concentration-dependent killing
* Bactericidal in the urine
* Minimal hepatic metabolism
* Renal elimination (adjust dose prn)

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34
Q

FOSFOMYCIN indication

A

Only indicated for acute uncomplicated cystitis in females >18 yrs caused by E. coli or E. faecalis

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35
Q

fosfomycin should be taken

A

take without food
can cause dizzy and drowsy

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36
Q

Protein Synthesis Inhibitors
30s
antibiotics

A

Aminoglycosides
Tetracyclines

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37
Q

Protein Synthesis Inhibitors
50s
antibiotics

A

Macrolides
Lincosamides
Oxazolidinones

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38
Q

Aminoglycosides e.g.

A
  • gentamycin
  • tobramycin
  • neomycin
  • streptomycin
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39
Q

Aminoglycosides MOA

A

Binds bacterial 30S ribosomal subunit, causing production of abnormal protein synthesis + interruption of usual protein synthesis = cell death

40
Q

adverse effects of Aminoglycosides

A

nephrotoxicity, ototoxicity, neurotoxicity (neuromuscular blockade + respiratory paralysis

41
Q

drug interactions with Aminoglycosides

A

Drug Interactions: loop diuretics (↑ototoxicity), nephrotoxic drugs (i.e., NSAIDs, cephalosporins, vancomycin, cyclosporine, amphotericin B)

42
Q

drug monitoring Aminoglycosides

A

Monitoring: serum drug levels (peak levels high to kill bacteria, trough levels low to reduce oto/nephrotoxicity

43
Q

PK and PD of aminoglycosides
____ killing
_____ CNS penetration
elimination

A

Concentration-dependent killing
* Post-antibiotic effect
* Poor GI absorption + CNS penetration
* Renal elimination (adjust dose prn)
* Serum drug levels can vary widely between patients

44
Q

special population aminoglycosides

A

safe for children
not safe for pregnancy
caution for older adults with renal impairment

45
Q

TETRACYCLINES MOA

A

Binds bacterial 30S ribosomal subunits, causing cessation of usual protein synthesis to prevent bacterial growth + multiplication

46
Q

adverse effects of tetracycline

A

renal toxicity,
hepatoxicity
GI (esophageal irritation, n/v, diarrhea, abd pain),
C. difficile,
Teeth discolouration/enamel hypoplasia (binds to calcium in teeth), Photosensitivity

47
Q

PK/PD of tetracycline
____ killing
CNS penetration
elimination

A

Time-dependent killing
* Post-antibiotic effect
* Food may affect absorption (individual drug dependent)
* Poor CNS penetration
* Renal elimination (tetracycline) or hepatic elimination (doxycycline, minocycline)

48
Q

tetracycline can cause_____

A

esophageal irritation
take full glass of water and remain upright for 1-2 hours after

49
Q

special population consideration tetracycline

A

Avoid under 8 yrs: permanent teeth discolouration
Hepatotoxicity risk in pregnancy, crosses placenta -> staining of deciduous teeth of fetus, long bone growth suppression (reversible with discontinuation); use only if benefit >risks; avoid in breastfeeding
Dose adjustments prn with renal impairment

50
Q

examples of macrolides

A

erythromycin
* azithromycin
* clarithromycin

51
Q

MOA of macrolides

A

Binds bacterial 50S ribosomal subunits, causing blockage of new amino acids to the peptide chain to prevent bacterial growth + multiplication

52
Q

adverse effects of macrolides

A

sudden cardiac death from QT prolongation -> torsades de pointes (small risk with high drug concentrations), GI (epigastric pain, n/v, diarrhea), transient ↑ LFT’s

53
Q

contraindications of macrolides

A

hypersensitivity, congenital QT prolongation, antiarrhythmic drugs (class IA or III),
concurrent CYP3A4 inhibitors (i.e., Ca++ channel blockers,
Antifungals -> “azoles,” HIV protease inhibitors)

54
Q

PK/PD of macrolides
____killing
CNS penetration
metabolism and elimination

A
  • Time-dependent killing
  • Post-antibiotic effect
  • Food may affect absorption
  • Poor CNS penetration
  • Hepatic metabolization + elimination (toxicity rare): metabolism by CYP3A4 (isoenzyme of
    cytochrome P450)
55
Q

special population macrolides

A

Risk of infantile hypertrophic pyloric stenosis in neonates
Crosses placenta but no adverse fetal risks with erythromycin/azithromycin. Potential fetal adverse effects with clarithromycin. Low transfer to breastmilk, generally safe in breastfeeding
Potential for reversible ototoxicity (tinnitus, hearing loss) with large doses or renal/hepatic impairment

56
Q

LINCOSAMIDES e.g.

A

clindamycin

57
Q

MOA of lincosamides

A

Binds bacterial 50S ribosomal subunits, causing blockage of new amino acids to the peptide chain to prevent bacterial growth + multiplication

58
Q

PD/PK of lincosamides

A

Time-dependent killing
* Post-antibiotic effect
* No CNS penetration
* Hepatic metabolism + renal elimination (adjust dose prn hepatic dysfunction, no renal
dose adjustment required)
* Metabolism by CYP3A4 (isoenzyme of cytochrome P450) but not significant

59
Q

adverse effects with lincosamides

A

fatal C. Diff

60
Q

special population of lincosamides

A

Caution with severe hepatic impairment
Crosses placenta + present in breastmilk Generally safe in pregnancy + breastfeeding
Caution in older adults with renal or hepatic impairment

61
Q

OXAZOLIDINONES e.g.

A

linezolid
tedizolid

62
Q

MOA of oxazolinones

A

Binds bacterial 50S ribosomal subunits, causing blockage of new amino acids to the peptide chain to prevent bacterial growth + multiplication

63
Q

Drug interaction of oxazolinones

A

MAO inhibitors + sympathomimetic/vasopressive/dopaminergic drugs ->
hypertensive crisis, SSRIs/triptans/opiods -> ↑risk serotonin syndrome

64
Q

Reserve for treatment of MRSA and VRE to delay emergence of resistance

A

oxazolinones
e.g.
linezolid
tedizolid

65
Q

significant food interaction of

A

food/drinks high in tyramine, dopamine, tyrosine,
phenylalanine, tryptophan + caffeine -> hypertensive crisis or serotonin syndrome

66
Q

FLUOROQUINOLONES
e.g.

A

ciprofloxacin
* levofloxacin
* moxifloxacin

67
Q

FLUOROQUINOLONES MOA

A

Inhibits DNA gyrase + DNA topoisomerase IV enzymes to impair DNA replication + cell division = cell death

68
Q

contraindication of fluoroquinolones

A

myasthenia gravis -> neuromuscular blocking activity =death/respiratory failure

69
Q

adverse effects of fluoroquinolones

A

tendinopathy/tendon rupture (esp. Achilles)
QT prolongation
C. diff

70
Q

PK/PD of fluoroquinolones

A

Concentration-dependent killing
* Post-antibiotic effect
* Upper GI absorption
* CYP450 inhibition (Cipro)
* Minimal hepatic metabolism; renal elimination (adjust dose adjustments prn)

71
Q

special populations for fluoroquinolones

A

Avoid due to potential MSK toxicity (cartilage + joint damage)
Crosses placenta + present in breastmilk
Avoid (use only if safer alternative not available)
Caution in older adults due to risk altered mental status, psychosis, + vision disturbances

72
Q

NITROIMIDAZOLES e.g.

A

metronidazole

73
Q

MOA of NITROIMIDAZOLES

A

Enters bacteria through passive diffusion. Damages+breaks helical DNA structure, inhibiting DNA synthesis = cell death

74
Q

NITROIMIDAZOLES contraindications

A

Caution in CNS disease

75
Q

adverse effects of NITROIMIDAZOLES

A

potential carcinogen

76
Q

PK/PD of NITROIMIDAZOLES
______Killing
______ CNS penetration
metabolism and elimination

A

Concentration-dependent killing
* Post-antibiotic effect
* Good GI absorption with oral
* Penetrates CSF
* Extensive hepatic metabolism (adjust dose prn hepatic dysfunction)
* Renal elimination + small percentage fecal elimination (no dose adjustment required)

77
Q

what causes metalic taste and GI upset and should be taken with food?

A

NITROIMIDAZOLES
e.g. metronadazole

78
Q

NITROFURANTOIN e.g.

A

nitrofurantoin

79
Q

NITROFURANTOIN MOA

A

MOA: DNA/RNA Synthesis Inhibitor
Bacteriostatic (low concentrations) Bactericidal (therapeutic concentrations)

80
Q

contraindications for NITROFURANTOIN

A

G6PD deficiency, pregnancy, infants <1
month

81
Q

PK/PD of NITROFURANTOIN

A

Bactericidal in urine only at therapeutic concentrations
* Time-dependent killing
* Short post-antibiotic effect
* Good GI absorption
* Minimal hepatic metabolism; rapid renal elimination leading to high concentrations in urine

82
Q

special population for NITROFURANTOIN

A

Avoid in infants <1 month due to risk of hemolytic anemia
Potential teratogen. Contraindicated in 3rd trimester, during L+D, and breastfeeding in premature or <1 month of age infants due to risk of hemolytic anemia
Avoid in older adults with renal impairment

83
Q

it’s important to avoid ___ when taking NITROIMIDAZOLES

A

avoidance of alcohol during treatment and at least 72 hours following completion

84
Q

3 types of ABX DNA synthesis inhibitors

A

Fluoroquinolones
Nitroimidazoles
Nitrofurantoin

85
Q

Folic Acid Synthesis Inhibitors

A

Sulfonamides

86
Q

adverse effects of sulfonamides

A

photosensitivity, Stevens-Johnson syndrome, hemolytic anemia (with G6PD deficiency), megaloblastic anemia (with concurrent folate deficiency), renal damage,

87
Q

MOA of sulfonamides

A

Sulfonamides: Inhibits synthesis of tetrahydrofolate, causing inhibition of DNA, RNA, and protein synthesis to prevent bacterial growth + multiplication

88
Q

PK/PD of Folic Acid Synthesis Inhibitors

A

Time dependent killing
* Well absorbed orally
* Hepatic metabolism
* Renal elimination (adjust dose prn)

89
Q

special population for Folic Acid Synthesis Inhibitors

A

Avoid in infants <2 months due to kernicterus (potentially fatal)
Avoid in pregnancy: may cause birth defects (1st trimester) and kernicterus (near term)
Caution in breastfeeding: can cause kernicterus in breastfeeding infants <2 months
Caution in older adults due to more severe adverse effects (can be life-threatening)

90
Q

Cell Membrane Disruptor

A

daptomycin

91
Q

daptomycin MOA

A

Binds to cell membrane, causing rapid depolarization of membrane potential, disrupting vital intracellular processes (such as DNA, RNA + protein synthesis) = cell death

92
Q

adverse effects of daptomycin

A

DRESS (Drug Reaction with Eosinophilia + Systemic Symptoms), TIN (Tubulointerstitial nephritis), anaphylaxis, myopathy/↑CPK, peripheral neuropathy, GI upset, C. difficile

93
Q

drug interaction of daptomycin

A

statins

94
Q

“Last-resort” antibiotic

A

daptomycin

95
Q

Drug Interaction of sulfonamides

A

warfarin, phenytoin, sulfonylurea hypoglycemics (glipizide, glyburide) -> ↑ effect for all;
ACE inhibitors/ARBs -> hyperkalemia