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Pharmacology Unit 6 > Antibiotics IV > Flashcards

Antibiotics IV Flashcards

1
Q

What are the 3 drug classes that inhibit bacterial nucleic acid synthesis?

A
  1. Fluoroquinolones
  2. Rifampin
  3. Metronizadole
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2
Q

What is the first generation FQ? Mechanism?

A

Ciprofloxacin; Inhibit DNA gyrase

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3
Q

What is the 2nd generation FQ? Mechanism?

A

Levofloxacin; Inhibit gyrase and bacterial topoisomerase IV

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4
Q

Why are FQs typically well-tolerated?

A

Humans don’t have DNA gyrase and therefore the drugs are well-tolerated

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5
Q

What additional spectrum is added in 2nd generation FQs?

A

Streptococcus pneumoniae

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6
Q

Adverse SEs of FQs

A
  • Allergy
  • Second Generation FQs may cause polymorphic ventricular tachycardia (Torsades de Pointes)
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7
Q

MOA of rifampin?

A

Inhibition of DNA-dependent RNA polymerase to stop the replication of RNA from the daughter DNA strand

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8
Q

Adverse SEs of Rifampin?

A
  • Allergy
  • Possible centrolobular hepatitis when used with isonazid
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9
Q

AB spectrum of rifampin?

A
  • Mycobacterium tuberculosis
  • Staphylococcus aureus
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10
Q

What is the MOA of Metronidazole?

A

Prodrug that is activated in an anaerobic environment to a drug that is toxic to nucleic acids

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11
Q

Adverse SE of Metronidazole?

A
  • Allergy
  • Inhibits aldehyde dehydrogenase to cause profound vasodilation and tachyarrhythmias due to the accumulation of acetyl aldehyde when metronidazole is taken with ethanol
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12
Q

What is the AB spectrum of metronidazole?

A
  • Anaerobic bacteria such as Clostridium difficile
  • Selected Protozoa (Entamoeba histolytica, Giardia lamblia)
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13
Q

What are the 30S ribosome inhibitors?

A
  1. Aminoglycosides (gentimicin, tobramycin)
  2. Tetracyclines (Doxycycline)
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14
Q

What are the 50S Ribosome inhibitors?

A
  1. Macrolides (azithromycin)
  2. Linezolid
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15
Q

What is the mechanism of gentamicin?

A

The aminoglycoside binds to the 30S ribosome which causes the transfer of the incorrect amino acyl transfer RNA and hence the wrong amino acid

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16
Q

To what bugs are aminoglycosides restricted? Why?

A

Aerobic or facultative aerobic Gram (-) rods; To enter cells, AGs must be uptaken by an oxygen dependent method

17
Q

What is important about the administration of AGs?

A

They have rapid lethality and superior prolonged AB effect on Gram (-) rods

18
Q

What is the spectrum of AGs?

A

Gram negative rods (Enterobacteriacaie) because of ESBL and Carbapenemase-producing strains of Enterobacter cloacae; Furthermore, FQs, 3rd gen cephs. and ES penicillins have promoted resistance

19
Q

What is an important consideration in AG administration in regards to SEs?

A

While AGs are nephrotoxic, they are only nephrotoxic when they accumulate in the kidney. Therefore, nephrotoxicity is not observed if use is < 48hrs

20
Q

When is AG (gentamicin) use most efficacious?

A

W/i first 12-24 hrs after exposure

21
Q

What is the MOA for Doxycycline?

A

Tetracycline that blocks the access of the tRNA anticodon to its codon

22
Q

What is the AB spectrum of tetracyclines?

A

Doxycycline is effective for intracellular pathogens (mycoplasma, chlamydia, legionella, rickettsia); Gram (+) organisms (S. pneumoniae, MRSA) in face of resistance to lactams

23
Q

Adverse SEs of doxycycline?

A
  • Allergy
  • Photosensitivity RXN
  • Not orally bioavailable when administered w/ di/tri-valent cations due to chelation
24
Q

MOA for azithromycin?

A

Macrolide that prevents the release and removal of the “naked” transfer RNA from the “A” site into the cytoplasm (inhibits transolcation by inhibiting translocase enzyme)

25
Q

Spectrum of Azithromycin?

A

Effective for intracellular pathogens (mycoplasma, chlamydia, legionella), H. influenzae, Gram (+) organisms [pneumococci, MRSA] that have lactam resistance

26
Q

Adverse SEs of Macrolides?

A
  • allergy
  • GI distress with oral administration
  • Potential of Torsades de pointes
27
Q

What is the most likely method of AB resistance for azithromycin or doxycycline?

A

Methylation of the target site or efflux pump

28
Q

MOA of Linezolid?

A

Inhibit transfer of the peptide chain from the “A” site to the P” site via the inhibition of the peptidyl transferase

29
Q

Spectrum of Linezolid?

A

Gram (+) organisms; It was primarily developed for infections of MRSA and VRSA

30
Q

Adverse Rxns to Linezolid?

A
  • Allergy
  • Agranulocytosis with prolonged use
31
Q

MOA of clindamycin?

A

Inhibit incorporation of new AA into growing peptide chain

32
Q

Clindamycin spectrum?

A

All anerobes except C. difficile, pneumococci and MRSA in face of lactam resistance

33
Q

Adverse effects of Clindamycin?

A
  • allergy
  • AB most closely associated with C. difficile colitis

Pharmacology Unit 6 (15 decks)

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