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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
# Reversed A partially reduced form of the drug inhibits nucleic acid synthesis by **disrupting the DNA of anaerobic microbial cells.** ## Footnote **Bactericidal**
Metronidazole
18
Clindamycin or Macrolides (MOA, bacteriostatic or bactericidal?)
**Protein Synthesis Inhibitor of 50S subunit** **Bacteriostatic** inhibits translocation of the bacterial ribosome along the mRNA
19
Macrolides ## Footnote (Adverse Reactions [**2**]?)
* **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.
20
Aminoglycosides | (Examples?)
Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, (GNATS)
20
Clindamycin ## Footnote (Oxygen tolerance + location, Spectrum, Uses [**3**], ?)
**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.
20
Macrolides ## Footnote (MOA, Bacteriostaic or Bactericidal?)
* **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.
21
Nitrofurantoin | (Spectrum/Uses?)
**Extended** spectrum **UTIs** especially for TMP-SMZ resistant *Escherichia coli* Also, G(+) cocci: *Staphylococcus spp., Streptococcus spp, Enterococcus spp.*
22
4th Generation [Fluoro]quinolone | (Example, meaning?)
Moxifloxacin ## Footnote **A Respiratory FQ - G(+), some anaerobe, atypical coverage added.**
23
Metronidazole | (Adverse Reactions?)
**Disulfiram [Antabuse®]-like reaction** ## Footnote (severe flushing, tachycardia, hypotension, vomiting) nausea headache GI distress Candidal Superinfection (occasional)
24
Tetracyclines ## Footnote (MOA, Bacteriostatic or Bactericidal?)
* **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**
25
2nd Generation Fluoroquinolone | (Drug?)
Ciprofloxacin
26
Minocycline ## Footnote (Excretion?)
* **Primary: biliary excretion.** * Remaining excretion: urine
27
Glycopeptides | (Examples?)
**Vancomycin**, Bacitracin
27
Fluoroquinolones | (Routes?)
Good **oral **bioavailability, **IV**
27
2nd Generation [Fluoro]quinolone | (Example?)
Ciprofloxacin
28
Fluoroquinolones | (Spectrum?)
**Extended** Spectrum: 2nd & 3rd generations. **Broad** Spectrum: 4th generation
28
Clindamycin ## Footnote (Elimination?)
**Primary elimination: hepatobiliary** ## Footnote Secondary elimination: renal Hepatic metabolism [http://sepia.unil.ch/pharmacology/index.php?id=57](http://sepia.unil.ch/pharmacology/index.php?id=57)
29
Aminoglycosides ## Footnote (Special Requirements?)
**These Drugs require O2 for uptake.** Therefore, they are ineffective against anaerobes. Mnemonic: "Mean GNATS cannot kill anaerobes"
30
Extended Spectrum, Penicillinase-sensitive Penicillins (Examples?)
**Amoxicillin**, Ampicillin
32
Cephalosporins 2nd Generation | (Examples?)
**Cefaclor**, Cefuroxime, Cefoxitin
34
# Reversed **Cefaclor**, Cefuroxime, Cefoxitin | (Drug class, which generation?)
Cephalosporins 2nd Generation
34
Macrolides ## Footnote (Toxicities?)
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
Clarithromycin ## Footnote (Metabolism, does per day?)
* **Metabolized by liver to active metabolite.** * Typically taken twice daily **(BID)**. * **Primary excretion: renal** (20-40% unchanged)
36
Tetracylines ## Footnote (Resistance Mechanisms?)
in progress
37
# Reversed Imipenem, Meropenem, Doripenem, Ertapenem (Drug class, MOA, spectrum, Clinical significance?)
* 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
Fluoroquinolones Generations 1 &2 | (MOA, Bacteriostatic or Bactericidal?)
* **Inhibits DNA gyrase** (a type IIA topoisomerase) which leads to DNA fragmentation. * **Bactericidal**
39
Moxifloxacin | (Excretion?)
Primarily Hepatic excretion | (20% renal)
41
Nitrofurantoin | (MOA, bacteriostatic or bactericidal?)
**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
Ciprofloxacin | (Spectrum, uses?)
**UTIs, *Pseudomonas spp.*** **Extended Spectrum:** * Excellent **Gram (-)** coverage. * **atypicals (*Chlamydia*, *Mycoplasma***)
44
Ciprofloxacin | (Excretion?)
Primary excretion: **Renal**
45
Cephalosporins 3rd Generation | (Examples?)
**Cefdinir, Ceftriaxone,** cefotaxime,
46
# Reversed **Piperacillin**, Ticarcillin | (Drug Class, spectrum width?)
**Antipseudomonals** **Extended** Spectrum
48
Nitrofurantoin | (Excretion?)
Rapid excretion via kidneys Thus, acts as a **urinary antiseptic**
49
Narrow Spectrum, Penicillinase-sensitive Penicillins (Examples?)
**Penicillin G, Penicillin V**
50
Aminoglycosides ## Footnote (Spectrum, oxygen tolerance, uses 2 e.g.s?)
* **Narrow spectrum**: Gram (-) **aerobes** * ***​Escherichria coli*** * ***Pseudomonas spp.*** * Presurgical bowel sterilization (Neomycin) * Tuberculosis (Streptomycin)
51
# Reversed **Dicloxacillin**, Oxacillin, Methicillin, Nafcillin (Drug class, spectrum width, effective against?)
**Penicillinase-resistant Penicillins** **Narrow** Spectrum: * **Gram (+) only**
52
Cephalosporins 1st Generation | (Examples?)
**Cephalexin**, Cefazolin
52
Tetracyclines | (Examples?)
**Doxycycline, Minocycline**, Tetracycline
52
Metronidazole | (MOA, bacteriostatic or bactericidal?)
A partially reduced form of the drug inhibits nucleic acid synthesis by **disrupting the DNA of anaerobic microbial cells.** ## Footnote **Bactericidal**
53
Fluoroquinolones | (Examples?)
**Ciprofloxacin, Levofloxacin, Moxifloxacin**, or any other drug ending in -oxacin
54
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
**Aminoglycosides** * **G**entamicin * **N**eomycin * **A**mikacin * **T**obramycin * **S**treptomycin Mnemonic: "Mean GNATS..." [mean sounds like amino]
55
# Reversed Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, (GNATS) (Drug class?)
Aminoglycosides
57
Fluoroquinolones | (DDIs?)
* Possible drug-drug interatctions (DDI) with **Theophylline** (an asthma/COPD drug). * **Antacids reduce GI absorption** of FQs.
58
Aminoglycosides ## Footnote (Adverse Reactions?)
* **Ototoxicity** - Vestibular and Cochlear * **Nephrotoxic - **Increase in serum creatinine and BUN ## Footnote Therefore, **Routine monitoring of Cp** levels is necessary. [http://campus.usal.es/~galenica/clinpkin/Aminoglycosides.htm](http://campus.usal.es/~galenica/clinpkin/Aminoglycosides.htm)
60
# Reversed Doxycycline, Minocycline, Tetracycline | (Drug Class?)
Tetracyclines
62
Metronidazole | (Metabolism?)
Hepatic
63
# Reversed **Cefdinir, Ceftriaxone,** cefotaxime, | (Drug class, which generation?)
Cephalosporins 3rd Generation
64
Carbapenems | (Examples?)
Imipenem, Meropenem, Doripenem, Ertapenem
65
Aminoglycosides | (MOA, Bacteriostatic or Bactericidal?)
* **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
Levofloxacin | (Spectrum, uses?)
**Respiratory, UTIs.** **Extended Spectrum:** * **Excellent Gram (+) coverage**, lesser Gram (-) coverage than Ciprofloxacin. **Respiratory FQ** due to activity against *Streptococcus pneumoniae.*
69
# Reversed **Antabuse®-like reaction** nausea headache GI distress Candidal Superinfection (occasional)
Metronidazole
70
Moxifloxacin | (Drug class, generation?)
4th Generation **Respiratory** Fluoroquinolone (FQ)
71
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?)
**Aminoglycosides** * **G**entamicin * **N**eomycin * **A**mikicin * **T**obramycin * **S**treptomycin Mnemonic: "Mean GNATS cannot kill anaerobes"
73
Levofloxacin | (Excretion?)
Primarily renal excretion
74
Doxycycline ## Footnote (Excretion?)
* **Primary**: **biliary excretion** ≈ 60% * Remaining excretion: urine ≈ 40%
75
1st Generation Quinolone | (Example?)
Nalidixic Acid
76
Macrolides ## Footnote (Spectrum, uses?)
**Extended spectrum:** * **G(+) cocci/rods** [as PCN substitute] * **G(-) rods**: *Legionella spp.*, *Bordetella spp.*, * H. pylori.* * **Atypicals**: ***Mycoplasma***, ***Chlamydia*** (*Chlamydophila pneumoniae)*.
78
4th Generation Respiratory Fluoroquinolone (FQ) (Drug?)
Moxifloxacin
79
# Reversed **Ciprofloxacin, Levofloxacin, Moxifloxacin**, or any other drug ending in -oxacin (Drug class?)
Fluoroquinolones
80
Clindamycin ## Footnote (Routes?)
* Good **oral** bioavailability * **IV** is also common * Topical for acne
81
Tetracyclines ## Footnote (Route and considerations?)
* **Good Oral Bioavailability** * Avoid taking these medications with: * Diary (Ca2+) * Antacids (Ca2+ or Mg2+) * Iron containing preparations ## Footnote Becasue **divalent cations inhibit absorption** in the GI tract
82
# Reversed Cefepime | (Drug class, which generation?)
Cephalosporins 4th Generation
83
# Reversed **Cephalexin**, Cefazolin | (Drug class, which generation?)
Cephalosporins 1st Generation
85
3rd Generation [Fluoro]quinolone | (Example, meaning?)
Levofloxacin ## Footnote **A Respiratory FQ, G(+) coverage added**
86
Tetracyclines ## Footnote (Adverse Reactions?)
* **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
Ciprofloxacin | (Drug class, generation?)
2nd Generation Fluoroquinolone
89
# Reversed **Damages Bacterial DNA** **Bactericidal**
Nitrofurantoin, Metronidazole
90
What drug would you choose to treat CA-MRSA? (Community associated Methicillin-resistant *Staphylococcus aureus*)
Clindamycin or Tetracyclines
92
Levofloxacin | (Drug class, generation?)
3rd Generation **respiratory** Fluoroquinolone (FQ)
93
Aminoglycosides ## Footnote (Excretion?)
**Renal Excretion** ## Footnote Primarily unchanged (not metabolized) [http://campus.usal.es/~galenica/clinpkin/Aminoglycosides.htm](http://campus.usal.es/~galenica/clinpkin/Aminoglycosides.htm)
94
Fluoroquinolones Generations 3 & 4 | (MOA, Bacteriostatic or Bactericidal?)
* **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
Clindamycin ## Footnote (Adverse reactions?)
* **Severe diarrhea** * **Pseudomembranous colitis** (*C. difficile* colitis)
96
Nitrofurantoin | (Route/Absorption?)
Route = Oral Rapid and complete GI absorption
98
Cephalosporins 4th Generation | (Example?)
Cefepime
99
Clindamycin ## Footnote (MOA, bacteriostatic or bactericidal?)
* Blocks peptide transfer (translocation) at the **50S subunit**, resulting in **protein synthesis inhibition.** * **Bacteriostatic**
100
Azithromycin ## Footnote (Metabolism, does per day?)
* **Metabolized by liver.** * Typically taken once daily **(QD)** after a loading dose. * **Primary excretion: Biliary** * Remaining excretion: renal (4.5%)
101
Macrolides | (Examples?)
**Azithromycin**, Erythromycin, Clarithromycin
102
Macrolides ## Footnote (Tissue Accumulation?)
Concentrates in the **Lungs.**
103
Antipseudomonals | (Examples?)
**Piperacillin**, Ticarcillin
104
* 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?)
* **Aminoglycosides** * Presurgical bowel sterilization (Neomycin) * Tuberculosis (Streptomycin)

Microbe pharmacology (5 decks)

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