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Antibiotics > Inhibitors of Protein Synthesis > Flashcards

Inhibitors of Protein Synthesis Flashcards

0
Q

Gentamicin

A
  • Aminoglycoside
  • MOA: bactericidal; binds 30S subunit
    1. Inhibit formation of initiation complex
    2. Causes misreading of mRNA
    3. Requires O2 for uptake: useless w/ anaerobes
  • Use: Severe gram - rods
    1. synergistic w/ beta lactams
  • Toxicity: Nephrotoxicity (esp w/ cephalosporins)
    1. Ototoxicity esp with loop diuretics
    2. Teratogen
  • Resistance: transferase enzymes that inactivate drug by acetylation, phosphorylation, or adenylation
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1
Q

Specificity of Protein Synthesis Inhibitors

A
  • Targets smaller bacterial ribosome
  • Bacterial ribosome: 70S made up of 50S and 30S
  • Human ribosome (80S) Unaffected
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2
Q

Neomycin

A
  • Aminoglycoside
  • MOA: bactericidal; binds 30S subunit
    1. Inhibit formation of initiation complex
    2. Causes misreading of mRNA
    3. Requires O2 for uptake: useless w/ anaerobes
  • Use: Severe gram - rods
    1. synergistic w/ beta lactams
    2. Used in bowel surgery
  • Toxicity: Nephrotoxicity (esp w/ cephalosporins)
    1. Ototoxicity esp with loop diuretics
    2. Teratogen
  • Resistance: transferase enzymes that inactivate drug by acetylation, phosphorylation, or adenylation
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3
Q

Amikacin

A
  • Aminoglycoside
  • MOA: bactericidal; binds 30S subunit
    1. Inhibit formation of initiation complex
    2. Causes misreading of mRNA
    3. Requires O2 for uptake: useless w/ anaerobes
  • Use: Severe gram - rods
    1. synergistic w/ beta lactams
  • Toxicity: Nephrotoxicity (esp w/ cephalosporins)
    1. Ototoxicity esp with loop diuretics
    2. Teratogen
  • Resistance: transferase enzymes that inactivate drug by acetylation, phosphorylation, or adenylation
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4
Q

Tobramycin

A
  • Aminoglycoside
  • MOA: bactericidal; binds 30S subunit
    1. Inhibit formation of initiation complex
    2. Causes misreading of mRNA
    3. Requires O2 for uptake: useless w/ anaerobes
  • Use: Severe gram - rods
    1. synergistic w/ beta lactams
  • Toxicity: Nephrotoxicity (esp w/ cephalosporins)
    1. Ototoxicity esp with loop diuretics
    2. Teratogen
  • Resistance: transferase enzymes that inactivate drug by acetylation, phosphorylation, or adenylation
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5
Q

Streptomycin

A
  • Aminoglycoside
  • MOA: bactericidal; binds 30S subunit
    1. Inhibit formation of initiation complex
    2. Causes misreading of mRNA
    3. Requires O2 for uptake: useless w/ anaerobes
  • Use: Severe gram - rods
    1. synergistic w/ beta lactams
  • Toxicity: Nephrotoxicity (esp w/ cephalosporins)
    1. Ototoxicity esp with loop diuretics
    2. Teratogen
  • Resistance: transferase enzymes that inactivate drug by acetylation, phosphorylation, or adenylation
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6
Q

Tetracycline

A
  • Tetracyclines are bacteriostatic by binding 30S subunit
  • MOA: Bind 30S and prevent attachment of aminoacyl tRNA
    1. Limited CNS penetration
    2. NO milk/antacids b/c divalent cations inhibit absorption
  • Use: Borrelia burgdorferi, M. pneumonia
    1. Accumulate intracellularly: effective for Rickettsia & Chlamydia
  • Toxicity:
    1. GI distress
    2. Discoloration of teeth and inhibited bone growth in children
    3. Photosensitivity
    4. Contraindicated in pregnancy
  • Resistance: decreased uptake into cells or increased efflux
    1. Plasmid-encoded transport pumps
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7
Q

Doxycycline

A
  • Tetracyclines are bacteriostatic by binding 30S subunit
  • MOA: Bind 30S and prevent attachment of aminoacyl tRNA
    1. Limited CNS penetration
    2. NO milk/antacids b/c divalent cations inhibit absorption
    3. Eliminated fecally, so can use in renal failure patients
  • Use: Borrelia burgdorferi, M. pneumonia
    1. Accumulate intracellularly: effective for Rickettsia & Chlamydia
  • Toxicity:
    1. GI distress
    2. Discoloration of teeth and inhibited bone growth in children
    3. Photosensitivity
    4. Contraindicated in pregnancy
  • Resistance: decreased uptake into cells or increased efflux
    1. Plasmid-encoded transport pumps
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8
Q

Demeclocycline

A
  • Tetracyclines are bacteriostatic by binding 30S subunit
  • MOA: Bind 30S and prevent attachment of aminoacyl tRNA
    1. Limited CNS penetration
    2. NO milk/antacids b/c divalent cations inhibit absorption
  • Use: Borrelia burgdorferi, M. pneumonia
    1. Accumulate intracellularly: effective for Rickettsia & Chlamydia
    2. ADH antagonist-diuretic in SIADH
  • Toxicity:
    1. GI distress
    2. Discoloration of teeth and inhibited bone growth in children
    3. Photosensitivity
    4. Contraindicated in pregnancy
  • Resistance: decreased uptake into cells or increased efflux
    1. Plasmid-encoded transport pumps
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9
Q

Minocycline

A
  • Tetracyclines are bacteriostatic by binding 30S subunit
  • MOA: Bind 30S and prevent attachment of aminoacyl tRNA
    1. Limited CNS penetration
    2. NO milk/antacids b/c divalent cations inhibit absorption
  • Use: Borrelia burgdorferi, M. pneumonia
    1. Accumulate intracellularly: effective for Rickettsia & Chlamydia
  • Toxicity:
    1. GI distress
    2. Discoloration of teeth and inhibited bone growth in children
    3. Photosensitivity
    4. Contraindicated in pregnancy
  • Resistance: decreased uptake into cells or increased efflux
    1. Plasmid-encoded transport pumps
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10
Q

Erythromycin

A
  • Macrolide
  • MOA: inhibits protein synth by blocking translocation “macroslide”
    1. Binds 23S rRNA on 50S subunit
    2. Bacteriostatic
  • Use:
    1. Atypical Pneumonias: mycoplasma, chlamydia, legionella
    2. URI
    3. STDs
    4. gram + cocci (strep if allergic to penicillin
    5. Neisseria
  • Toxicity:
    1. Prolonged QT interval
    2. GI discomfort (most common cause of noncompliance)
    3. Acute cholestatic hepatitis
    4. eosinophilia
    5. Skin rashes
  • Drug interactions: increases serum concentrations of theophyllines and oral anticoagulants
  • Resistance: methylation of 23S rRNA binding site
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11
Q

Azithromycin

A
  • Macrolide
  • MOA: inhibits protein synth by blocking translocation “macroslide”
    1. Binds 23S rRNA on 50S subunit
    2. Bacteriostatic
  • Use:
    1. Atypical Pneumonias: mycoplasma, chlamydia, legionella
    2. URI
    3. STDs
    4. gram + cocci (strep if allergic to penicillin
    5. Neisseria
  • Toxicity:
    1. Prolonged QT interval
    2. GI discomfort (most common cause of noncompliance)
    3. Acute cholestatic hepatitis
    4. eosinophilia
    5. Skin rashes
  • Drug interactions: increases serum concentrations of theophyllines and oral anticoagulants
  • Resistance: methylation of 23S rRNA binding site
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12
Q

Clarithromycin

A
  • Macrolide
  • MOA: inhibits protein synth by blocking translocation “macroslide”
    1. Binds 23S rRNA on 50S subunit
    2. Bacteriostatic
  • Use:
    1. Atypical Pneumonias: mycoplasma, chlamydia, legionella
    2. URI
    3. STDs
    4. gram + cocci (strep if allergic to penicillin
    5. Neisseria
  • Toxicity:
    1. Prolonged QT interval
    2. GI discomfort (most common cause of noncompliance)
    3. Acute cholestatic hepatitis
    4. eosinophilia
    5. Skin rashes
  • Drug interactions: increases serum concentrations of theophyllines and oral anticoagulants
  • Resistance: methylation of 23S rRNA binding site
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13
Q

Chloramphenicol

A
  • MOA: bacteriostatic; blocks bond formation at 50S
  • Use: Meinigitis (H. influenzae, N. meningitidis, S. pneumoniae)
    1. Conservative use due to side effects
  • Toxicity:
    1. Dose dependent anemia
    2. Aplastic anemia
    3. Gray baby syndrome (no UDP-glucuronyl transferase)
  • Resistance: Plasmid encoded acetyltransferase inactivates drug
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14
Q

Clindamycin

A
  • MOA: Bacteriostatic
    1. Blocks peptide bond formation at 50S subunit
  • Use: Anaerobic infections in aspiration pneumonia or lung abscess
    1. Includes Bacteriodes fragilis and clostridium perfringins
  • Toxicity: Pseudomebraneous colitis from C. diff overgrowth, fever, diarrhea
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Antibiotics (9 decks)

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