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Microbe pharmacology > Drugs > Flashcards

Drugs Flashcards

1
Q

Reversed

Penicillin G, Penicillin V

(Drug Class, spectrum width?)

A

Narrow Spectrum, Penicillinase-sensitive Penicillins

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1
Q

Aminoglycosides

(Route?)

A
  • IV/IM
  • poor oral absorption
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1
Q

Tetracycline

(Excretion?)

A
  • Primary: renal excretion > 60%
  • Remainder: fecal excretion
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1
Q

Tetracyclines

(Spectrum, resistance, uses?)

A
  • Broad Spectrum: (However, many Gram (+)/(-) organisms are now resistant).
  • Good Choice for CA-MRSA (Community associated MRSA)
  • Works for Atypicals: Chlamydia spp., Mycoplasma spp., Rickettsia spp., & Spirochetes.
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2
Q

Reversed

Protein Synthesis Inhibitor of 50S subunit

Bacteriostatic

inhibits translocation of the bacterial ribosome along the mRNA

(Drug(s)?)

A

Clindamycin or Macrolides

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3
Q

Erythromycin

(Metabolism, does per day?)

A
  • Metabolized by liver with a short half-life.
  • Thus, typically taken four times per day (QID)
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4
Q

Aminoglycosides

(Distribution?)

A

Distribution is limited to the extracellular fluid (**ECF) **due to the polarity of these drugs

  • Distribute well in synovial, peritoneal, ascitic and pleural fluids.
  • High concentrations are obtained in renal tissue especially in renal cortex.
  • Penetration of these drugs is poor in eye and central nervous system

http://campus.usal.es/~galenica/clinpkin/Aminoglycosides.htm

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5
Q

Reversed

Amoxicillin, Ampicillin

(Drug Class, spectrum width?)

A

Extended Spectrum, Penicillinase-sensitive Penicillins

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5
Q

Aminoglycosides

(Tissue Accumulation?)

A
  • Kidney, especially renal cortex.
  • Inner ear
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6
Q

Fluoroquinolones

(Adverse Reactions?)

[Give 3-5]

A
  • Generally well tolerated, some GI upset.
  • C. difficile Superinfections possible.
  • Pediatric: potential for arthralgias, not 1st choice.
  • Rare: CNS disorders
  • Rare: Increased QT interval of heart rhythm
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7
Q

Reversed

Vancomycin, Bacitracin

(Drug Class?)

A

Glycopeptides

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8
Q

Penicillinase-resistant Penicillins

(Examples)

A

Dicloxacillin, Oxacillin, Methicillin, Nafcillin

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9
Q

Metronidazole

(Route?)

A

Good Oral Bioavailability

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9
Q

These Drugs require O2 for uptake.

Therefore, they are ineffective against anaerobes.

(Drug class, examples?)

A

Aminoglycosides

  • Gentamicin
  • Neomycin
  • Amikacin
  • Tobramycin
  • Streptomycin

Mnemonic: “Mean GNATS cannot kill anaerobes”

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10
Q

Reversed

Azithromycin, Erythromycin, Clarithromycin

(Drug Class)

A

Macrolides

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10
Q

Moxifloxacin

(Spectrum, uses?)

A

Respiratory FQ due to activity against Streptococcus pneumoniae.

Broad Spectrum: Gram (+), (-) & atypical coverage

Effective against some anaerobes and atypicals compared to earlier generation FQs.

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11
Q

What would you use to treat Anaerobic Bacteria below the diaphragm?

A

Metronidazole

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12
Q

What would you use to treat:

  • the 1st episode Clostridium difficile, C. perfringens, Bacteroides fragilis.
  • ** **OR to treat Protozoa (trichomoniasis, amebiasis, giardiasis)?
A

Metronidazole

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13
Q

What would you use to treat these conditions?

  • bacterial vaginosis,
  • pelvic inflammatory disease,
  • pseudomenbranous colitis
A

Metronidazole

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14
Q

What would you use to treat Anaerobic Bacteria below the diaphragm?

1st episode Clostridium difficile, C. perfringens, Bacteroides fragilis.

*** **or *Protozoa?

trichomoniasis, amebiasis, giardiasis

Also: bacterial vaginosis, pelvic inflammatory disease, pseudomenbranous colitis

A

Metronidazole

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14
Q

Macrolides

(Routes?)

A
  • Good oral bioavailability
  • IV also Common
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15
Q

Clindamycin

(Tissue accumulation?)

A

Penetrates into bone

  • Particularly effective against Staphylococcus aureus in bone and joint infections. (osteomyelitis [OM] and septic arthritis).
  • note: S. aureus is the most common bacterial cause of OM except for patients with sickle cell disease where Salmonella spp. is twice as likely.

​http://en.wikipedia.org/wiki/Osteomyelitis

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16
Q

Metronidazole

(Spectrum, Uses [3-8], diseases [3]?)

A

Narrow spectrum: Anaerobic Bacteria

  • 1st episode of mild to moderate:
    • Clostridium difficile, C. perfringens, Bacteroides fragilis.​
  • **Protozoa: **
    • trichomoniasis, amebiasis, giardiasis
  • Diesases:
    • Bacterial vaginosis, pelvic inflammatory disease (PID), pseudomenbranous colitis
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17
Q

Nitrofurantoin

(Adverse Reactions, how to minimize them?)

A

GI side effects

Macrocrystalline [more slowly absorbed] forms better tolerated.

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17
Q

Reversed

A partially reduced form of the drug inhibits nucleic acid synthesis by disrupting the DNA of anaerobic microbial cells.

Bactericidal

A

Metronidazole

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18
Q

Clindamycin or Macrolides

(MOA, bacteriostatic or bactericidal?)

A

Protein Synthesis Inhibitor of 50S subunit

Bacteriostatic

inhibits translocation of the bacterial ribosome along the mRNA

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19
Q

Macrolides

(Adverse Reactions [2]?)

A
  • **DDI **(drug-drug interactions) due to inhibition of CYP450. Azithromycin does not inhibit CYP450.
  • GI disturbances
    • n/v/d (nausea, vomiting, diarrhea)

Note: Erythromycin causes more GI upset than Clarithromycin or Azithromycin.

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20
Q

Aminoglycosides

(Examples?)

A

Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, (GNATS)

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20
Q

Clindamycin

(Oxygen tolerance + location, Spectrum, Uses [3], ?)

A

Anaerobes above the diaphragm.

  • Narrow spectrum:
    • Gram (+) cocci (including CA-MRSA)
      • Anaerobes (NOT Clostridium difficile)
      • **Acne **(topical route to treat Propionibacterium acnes)
  • Note: In treatment of Gram (+) cocci Clindamycin is used as a PCN alternative.
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20
Q

Macrolides

(MOA, Bacteriostaic or Bactericidal?)

A
  • Protein Synthesis Inhibitor of 50S subunit
  • Bacteriostatic

Blocks translocation of the bacterial ribosome along the mRNA by binding to the 23S rRNA of the 50S subunit.

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21
Q

Nitrofurantoin

(Spectrum/Uses?)

A

Extended spectrum

UTIs

especially for TMP-SMZ resistant Escherichia coli

Also, G(+) cocci: Staphylococcus spp., Streptococcus spp, Enterococcus spp.

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22
Q

4th Generation [Fluoro]quinolone

(Example, meaning?)

A

Moxifloxacin

A Respiratory FQ - G(+), some anaerobe, atypical coverage added.

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23
Q

Metronidazole

(Adverse Reactions?)

A

Disulfiram [Antabuse®]-like reaction

(severe flushing, tachycardia, hypotension, vomiting)

nausea

headache

GI distress

Candidal Superinfection (occasional)

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24
Q

Tetracyclines

(MOA, Bacteriostatic or Bactericidal?)

A
  • **Binds to 30S subunit **in the A-site and prevents attachment of incoming aminoacyl-tRNAs (tRNAs bound to their respective amino acids).
  • Protein synthesis Inhibition
  • Bacteriostatic
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25
Q

2nd Generation Fluoroquinolone

(Drug?)

A

Ciprofloxacin

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26
Q

Minocycline

(Excretion?)

A
  • Primary: biliary excretion.
  • Remaining excretion: urine
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27
Q

Glycopeptides

(Examples?)

A

Vancomycin, Bacitracin

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27
Q

Fluoroquinolones

(Routes?)

A

Good **oral **bioavailability, IV

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27
Q

2nd Generation [Fluoro]quinolone

(Example?)

A

Ciprofloxacin

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28
Q

Fluoroquinolones

(Spectrum?)

A

Extended Spectrum: 2nd & 3rd generations.

Broad Spectrum: 4th generation

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28
Q

Clindamycin

(Elimination?)

A

Primary elimination: hepatobiliary

Secondary elimination: renal

Hepatic metabolism

http://sepia.unil.ch/pharmacology/index.php?id=57

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29
Q

Aminoglycosides

(Special Requirements?)

A

These Drugs require O2 for uptake.

Therefore, they are ineffective against anaerobes.

Mnemonic: “Mean GNATS cannot kill anaerobes”

30
Q

Extended Spectrum, Penicillinase-sensitive Penicillins

(Examples?)

A

Amoxicillin, Ampicillin

32
Q

Cephalosporins 2nd Generation

(Examples?)

A

Cefaclor, Cefuroxime, Cefoxitin

34
Q

Reversed

Cefaclor, Cefuroxime, Cefoxitin

(Drug class, which generation?)

A

Cephalosporins 2nd Generation

34
Q

Macrolides

(Toxicities?)

A

Toxicities:

  • *M** - Motility issues in GI tract
  • *A** - Arrhythmia from prolonged QT
  • *C** - [acute] Cholestatic hepatitis
  • *R** - Rash
  • *O** - eOsinophilia

I - Increase serum concentration of Theophyllines and oral anticoagulants

35
Q

Clarithromycin

(Metabolism, does per day?)

A
  • Metabolized by liver to active metabolite.
  • Typically taken twice daily (BID).
  • Primary excretion: renal (20-40% unchanged)
36
Q

Tetracylines

(Resistance Mechanisms?)

A

in progress

37
Q

Reversed

Imipenem, Meropenem, Doripenem, Ertapenem

(Drug class, MOA, spectrum, Clinical significance?)

A
  • Class: Carbapenems
  • MOA: ß-lactam antibiotics - inhibits cross linking of peptidoglycan (stage 3)
  • spectrum: Broad
  • Clinical significance: antibiotics of last resort for certain bacterial infections
38
Q

Fluoroquinolones Generations 1 &2

(MOA, Bacteriostatic or Bactericidal?)

A
  • Inhibits DNA gyrase (a type IIA topoisomerase) which leads to DNA fragmentation.
  • Bactericidal
39
Q

Moxifloxacin

(Excretion?)

A

Primarily Hepatic excretion

(20% renal)

41
Q

Nitrofurantoin

(MOA, bacteriostatic or bactericidal?)

A

Damages Bacterial DNA

Bactericidal

Drug is reduced intracellularly by nitrofuran reductase to multiple highly reactive intermediates.

Bacterial cells activate Nitrofurantoin more rapidly than mammalian cells

42
Q

Ciprofloxacin

(Spectrum, uses?)

A

UTIs, Pseudomonas spp.

Extended Spectrum:

  • Excellent Gram (-) coverage.
  • atypicals (Chlamydia, Mycoplasma)
44
Q

Ciprofloxacin

(Excretion?)

A

Primary excretion: Renal

45
Q

Cephalosporins 3rd Generation

(Examples?)

A

Cefdinir, Ceftriaxone, cefotaxime,

46
Q

Reversed

Piperacillin, Ticarcillin

(Drug Class, spectrum width?)

A

Antipseudomonals

Extended Spectrum

48
Q

Nitrofurantoin

(Excretion?)

A

Rapid excretion via kidneys

Thus, acts as a urinary antiseptic

49
Q

Narrow Spectrum, Penicillinase-sensitive Penicillins

(Examples?)

A

Penicillin G, Penicillin V

50
Q

Aminoglycosides

(Spectrum, oxygen tolerance, uses 2 e.g.s?)

A
  • Narrow spectrum: Gram (-) aerobes
    • ​Escherichria coli
    • Pseudomonas spp.
  • Presurgical bowel sterilization (Neomycin)
  • Tuberculosis (Streptomycin)
51
Q

Reversed

Dicloxacillin, Oxacillin, Methicillin, Nafcillin

(Drug class, spectrum width, effective against?)

A

Penicillinase-resistant Penicillins

Narrow Spectrum:

  • Gram (+) only
52
Q

Cephalosporins 1st Generation

(Examples?)

A

Cephalexin, Cefazolin

52
Q

Tetracyclines

(Examples?)

A

Doxycycline, Minocycline, Tetracycline

52
Q

Metronidazole

(MOA, bacteriostatic or bactericidal?)

A

A partially reduced form of the drug inhibits nucleic acid synthesis by disrupting the DNA of anaerobic microbial cells.

Bactericidal

53
Q

Fluoroquinolones

(Examples?)

A

Ciprofloxacin, Levofloxacin, Moxifloxacin, or any other drug ending in -oxacin

54
Q

These drugs (Drug class, examples?):

  • Inhibit protein synthesis at the 30S subunit.
  • Are bactericidal
  • Inhibit formation of the initiation complex
  • Cause misreading of the mRNA
  • And block translocation of the ribosome
A

Aminoglycosides

  • Gentamicin
  • Neomycin
  • Amikacin
  • Tobramycin
  • Streptomycin

Mnemonic: “Mean GNATS…” [mean sounds like amino]

55
Q

Reversed

Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, (GNATS)

(Drug class?)

A

Aminoglycosides

57
Q

Fluoroquinolones

(DDIs?)

A
  • Possible drug-drug interatctions (DDI) with Theophylline (an asthma/COPD drug).
  • Antacids reduce GI absorption of FQs.
58
Q

Aminoglycosides

(Adverse Reactions?)

A
  • Ototoxicity - Vestibular and Cochlear
  • **Nephrotoxic - **Increase in serum creatinine and BUN

Therefore, Routine monitoring of Cp levels is necessary.

http://campus.usal.es/~galenica/clinpkin/Aminoglycosides.htm

60
Q

Reversed

Doxycycline, Minocycline, Tetracycline

(Drug Class?)

A

Tetracyclines

62
Q

Metronidazole

(Metabolism?)

A

Hepatic

63
Q

Reversed

Cefdinir, Ceftriaxone, cefotaxime,

(Drug class, which generation?)

A

Cephalosporins 3rd Generation

64
Q

Carbapenems

(Examples?)

A

Imipenem, Meropenem, Doripenem, Ertapenem

65
Q

Aminoglycosides

(MOA, Bacteriostatic or Bactericidal?)

A
  • Protein synthesis inhibition at the 30S subunit.
  • Bactericidal
  • These drugs:
    • inhibit formation of the initiation complex
    • cause misreading of the mRNA
    • block translocation of the ribosome
67
Q

Levofloxacin

(Spectrum, uses?)

A

Respiratory, UTIs.

Extended Spectrum:

  • Excellent Gram (+) coverage, lesser Gram (-) coverage than Ciprofloxacin.

Respiratory FQ due to activity against Streptococcus pneumoniae.

69
Q

Reversed

Antabuse®-like reaction

nausea

headache

GI distress

Candidal Superinfection (occasional)

A

Metronidazole

70
Q

Moxifloxacin

(Drug class, generation?)

A

4th Generation Respiratory Fluoroquinolone (FQ)

71
Q

For these drugs, Distribution is limited to the extracellular fluid (ECF) due to their chemical polarity.

They:

  • Distribute well in synovial, peritoneal, ascitic and pleural fluids.
  • Accumulate in high concentrations in renal tissue especially in renal cortex.
  • penetrate poorly to eyes and central nervous system

(Drug class, examples?)

A

Aminoglycosides

  • Gentamicin
  • Neomycin
  • Amikicin
  • Tobramycin
  • Streptomycin

Mnemonic: “Mean GNATS cannot kill anaerobes”

73
Q

Levofloxacin

(Excretion?)

A

Primarily renal excretion

74
Q

Doxycycline

(Excretion?)

A
  • Primary: biliary excretion ≈ 60%
  • Remaining excretion: urine ≈ 40%
75
Q

1st Generation Quinolone

(Example?)

A

Nalidixic Acid

76
Q

Macrolides

(Spectrum, uses?)

A

Extended spectrum:

  • G(+) cocci/rods [as PCN substitute]
  • G(-) rods: Legionella spp., Bordetella spp.,
  • H. pylori.*
  • Atypicals: Mycoplasma, Chlamydia (Chlamydophila pneumoniae).
78
Q

4th Generation Respiratory Fluoroquinolone (FQ)

(Drug?)

A

Moxifloxacin

79
Q

Reversed

Ciprofloxacin, Levofloxacin, Moxifloxacin, or any other drug ending in -oxacin

(Drug class?)

A

Fluoroquinolones

80
Q

Clindamycin

(Routes?)

A
  • Good oral bioavailability
  • IV is also common
  • Topical for acne
81
Q

Tetracyclines

(Route and considerations?)

A
  • Good Oral Bioavailability
  • Avoid taking these medications with:
    • Diary (Ca2+)
    • Antacids (Ca2+ or Mg2+)
    • Iron containing preparations

Becasue divalent cations inhibit absorption in the GI tract

82
Q

Reversed

Cefepime

(Drug class, which generation?)

A

Cephalosporins 4th Generation

83
Q

Reversed

Cephalexin, Cefazolin

(Drug class, which generation?)

A

Cephalosporins 1st Generation

85
Q

3rd Generation [Fluoro]quinolone

(Example, meaning?)

A

Levofloxacin

A Respiratory FQ, G(+) coverage added

86
Q

Tetracyclines

(Adverse Reactions?)

A
  • Abnormal bone and tooth development
    • ​Avoid during pregnancy and children < 8 yo.
  • Fungal Superinfections
  • DDIs (drug drug interactions) with divalent cations in stomach.
  • n/v/d (nausea, vomiting, diarrhea)
88
Q

Ciprofloxacin

(Drug class, generation?)

A

2nd Generation Fluoroquinolone

89
Q

Reversed

Damages Bacterial DNA

Bactericidal

A

Nitrofurantoin, Metronidazole

90
Q

What drug would you choose to treat CA-MRSA? (Community associated Methicillin-resistant Staphylococcus aureus)

A

Clindamycin or Tetracyclines

92
Q

Levofloxacin

(Drug class, generation?)

A

3rd Generation respiratory Fluoroquinolone (FQ)

93
Q

Aminoglycosides

(Excretion?)

A

Renal Excretion

Primarily unchanged (not metabolized)

http://campus.usal.es/~galenica/clinpkin/Aminoglycosides.htm

94
Q

Fluoroquinolones Generations 3 & 4

(MOA, Bacteriostatic or Bactericidal?)

A
  • Inhibits topoisomerase IV (a type IIA topoisomerase) which leads to DNA fragmentation. The selectivity of topoisomerasse IV explains the Gram (+) coverage of later gen FQs.
  • Bactericidal
95
Q

Clindamycin

(Adverse reactions?)

A
  • Severe diarrhea
  • Pseudomembranous colitis (C. difficile colitis)
96
Q

Nitrofurantoin

(Route/Absorption?)

A

Route = Oral

Rapid and complete GI absorption

98
Q

Cephalosporins 4th Generation

(Example?)

A

Cefepime

99
Q

Clindamycin

(MOA, bacteriostatic or bactericidal?)

A
  • Blocks peptide transfer (translocation) at the 50S subunit, resulting in protein synthesis inhibition.
  • Bacteriostatic
100
Q

Azithromycin

(Metabolism, does per day?)

A
  • Metabolized by liver.
  • Typically taken once daily (QD) after a loading dose.
  • Primary excretion: Biliary
  • Remaining excretion: renal (4.5%)
101
Q

Macrolides

(Examples?)

A

Azithromycin, Erythromycin, Clarithromycin

102
Q

Macrolides

(Tissue Accumulation?)

A

Concentrates in the Lungs.

103
Q

Antipseudomonals

(Examples?)

A

Piperacillin, Ticarcillin

104
Q
  • These drugs have a **narrow spectrum limited to Gram (-) aerobes **(drug class?).
  • They are effective against:
    • ​Escherichria coli
    • Pseudomonas spp.
  • Common uses include:
    • Presurgical bowel sterilization (drug name?)
    • Tuberculosis (drug name?)
A
  • Aminoglycosides
  • Presurgical bowel sterilization (Neomycin)
  • Tuberculosis (Streptomycin)

Microbe pharmacology (5 decks)

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