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Pharmacology > Antimicrobial Therapy 3 > Flashcards

Antimicrobial Therapy 3 Flashcards

1
Q

Which antibiotics act on 30S Ribosomal Subunit?

A
  1. Tetracyclines

2. Aminoglycosides

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2
Q

What is the MOA for Tetracyclines?

A

Inhibit bacterial protein synthesis by binding to 30S ribosome; Causes misreading of genetic code

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3
Q

What are the Pharmacokinetics of Tetracyclines?

A
  1. Bacteriostatic
  2. Broad Spectrum
  3. Requires Active and passive transport to cross cell wall
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4
Q

When do you not use Tetracyclines?

A

Don’t use in pregnancy and when breastfeeding; Chelates with calcium inhibits bone and teeth formation in fetus. Avoid until eruption of permanent teeth

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5
Q

What are the mechanisms of resistance for Tetracyclines?

A
  1. Enzymatic inactivation
  2. Impaired influx by protein pump
  3. Proteins protecting binding site Tet(M) mutation
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6
Q

What are the side effects of Tetracycline?

A
  1. NVD
  2. Photosensitivity
  3. Teeth discoloration
  4. Bone deformities
  5. Liver toxicity
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7
Q

Discuss Tigecycline

A

Withstands resistance that affects other tetracyclines.

  1. Broad spectrum
  2. Great tissue penetration
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8
Q

What is the MOA for Aminoglycosides?

A

Used for Aerobic Gram-

  1. Inteferes with initiations complex
  2. Induces misreading of mRNA
  3. Breaks up polymers into nonfunctional monomers
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9
Q

What are the pharmacokinetics of Aminoglycosides?

A
  1. Bactericidal
  2. Concentration depedent killing
  3. Small Volume of distribution; cant cross BBB
  4. Post antibiotic effect
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10
Q

What are the mechanisms of resistance for Aminoglycosides?

A
  1. Enzymatic inactivation
  2. Impaired entry into cell
  3. Ribosome mutation
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11
Q

How do aminoglycosides get into bacterial cell?

A
  1. Passive diffusion across Gram- OM

2. Active transport across CM via oxygen dependent process

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12
Q

What are the side effects of Aminoglycosides?

A
  1. Neuromuscular blockade
  2. Ototoxicity
  3. Nephrotoxicity
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13
Q

Which drugs act on the 50s Ribosomal subunit?

A
  1. Macrolides
  2. Clindamycin
  3. Streptogramins
  4. Oxazolidinones
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14
Q

What is the MOA of Macrolides?

A

Binds to 50S ribosome by blocking transpeptidation and translocation reaction.

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15
Q

What are the pharmacokinetics of Macrolides?

A
  1. Bacteriostatic

2. Good distribution

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16
Q

What is the resistance of Macrolides?

A
  1. Reduced permeability
  2. Esterases hydrolyze macrolides
  3. Production of methylase that modifies ribosome.
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17
Q

What are the side effects of Macrolides?

A
  1. Abdominal pain
  2. Cholestatic hepatitis
  3. Prolonged Qtc interval
  4. Skin rash
18
Q

Discuss Fidaxomicin

A
  1. Used for C. difficile diarrhea
  2. Bacteriocidal
  3. Large MW
19
Q

What is the MOA of Clindamycin?

A

Inhibits translocation reactions on 50s ribosomes

20
Q

What are the pharmacokinetics of Clindamycin?

A
  1. Bacteriostatic
  2. Good distribution
  3. Treats abscesses
21
Q

What are the side effects of Clindamycin?

A
  1. Skin rash
  2. Nausea
  3. Diarrhea
22
Q

What is the MOA for Streptogramins?

A

Dalfopristin- Causes conformational change in ribosome preventing peptide chain formation.
Quinupristin: Blocks elongation of peptide; Binds 50s

23
Q

What are the pharmacokinetics of Streptogramins?

A
  1. Bactericidal
  2. Inhibits Cyp450
  3. Synergistic combination
24
Q

What are the side effects of Streptogramins?

A
  1. Thrombocytopenia
  2. Hyperbilirubinemia
  3. Arthralgia-Myalgia Syndrome
25
Q

What is the MOA for Oxazolidinones?

A

Linezolid: Binds 23s ribosome subunit preventing formation of ribosome complex
Tedizolid: Binds P site of 50s subunit of bacterial ribosome; Prevents protein synthesis

26
Q

Are Oxazolidinones Bacteriostatic?

A

YES

27
Q

What are the side effects of Oxazolidinones?

A
  1. Thrombocytopenia
  2. Neutropenia
  3. Serotonin Syndrome
28
Q

What is the MOA of Fluroquinolones?

A

Inhibit bacterial topoisomerases

29
Q

What are the pharamcokinetics of Fluroquinolones?

A
  1. Bactericidal
  2. Time and concentration dependent killing
  3. Renally cleared except Moxifloxacin
30
Q

Which drugs inhibit DNA replication?

A

Fluoroquinolones, Metronidazole, and Rifampin

31
Q

What are the mechanisms of resistance of Fluoroquinolones?

A
  1. Altered target sites
  2. Altered Cell wall permeability
  3. Active efflux pump
32
Q

What are the side effects of Fluoroquinolones?

A
  1. Photosensitivity
  2. QT prolongation
  3. May damage cartilage; Avoid in pregnancy
33
Q

What is the MOA for Metronidazole?

A

Disrupts DNA and inhibits nucleic acid synthesis in anaerobic bacteria

34
Q

What are the pharmacokinetics of Metronidazole?

A
  1. Bactericidal

2. Good for anaerobic infections

35
Q

What are the side effects of Metronidazole?

A
  1. Dry mouth
  2. Pancreatitis
  3. Nausea
36
Q

What is the MOA of Rifampin?

A

Binds beta-subunit of DNA-dependent RNA polymerase; Inhibits RNA synthesis (No effect on elongation)

37
Q

What are the pharmacokinetics of Rifampin?

A
  1. Bactericidal
  2. Good bioavailibility
  3. CYP450 inducer
38
Q

What is the resistance to Rifampin?

A

Point mutation to beta subunit of RNA polymerase

39
Q

What are the side effects of Rifampin?

A
  1. Orange body fluid
  2. Rash
  3. Thrombocytopenia
  4. Cholestatic jaundice
40
Q

What is the MOA of Nitrofurantoin?

A

Interferes with metabolism, protein and cell wall synthesis

41
Q

What are the side effects of Nitrofurantoin?

A
  1. Nausea
  2. Vomiting
  3. Neuropathies and hemolytic anemia in G6PD deficiency.

Pharmacology (25 decks)

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