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Antibiotics > Inhibitors of Bacterial Proteins Synthesis > Flashcards

Inhibitors of Bacterial Proteins Synthesis Flashcards

1
Q

Tetracyclins

A

Drugs:

  • Oral or IV tetracycline
  • Oral doxycycline
  • Oral demeclocycline
  • Oral or IV minocycline

Mechanism of action:

  • Inhibits bacterial protein synthesis by blocking incoming aminoacyl-tRNA from binding to the ribosome acceptor site.
  • Bacteriostatic

CNS penetration:
Poor

Route of elimination:

  • Renal elimination
  • Doxycycline: only GI elimination

Clinical use:

  • Atypical bacteria such as Borrelia, Mycoplasma, Rickettsia, Anaplasma, Ehrlichia, Chlamydia, Ureaplasma, Vibrio cholerae
  • Acne

Adverse effects:

  • Hepatotoxicity
  • Deposition in bones and teeth → discoloration of teeth and inhibition of bone growth in children
  • Damage to mucous membranes (e.g., esophagitis)
  • Photosensitivity: UV light is absorbed by the drug, which releases energy to the surrounding area and damages exposed areas
  • Degraded tetracyclines associated with Fanconi syndrome

Contraindications:

  • Children < 8 years
  • Pregnancy
  • Lactating women
  • Renal failure (except doxycycline)
  • Hepatic failure (relative contraindication)
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2
Q

Macrolides

A

Drugs:

  • Oral or IV erythromycin
  • Oral or IV azithromycin
  • Oral clarithromycin

Mechanism of action:

  • Inhibits bacterial protein synthesis by blocking translocation; bind to the 23S ribosomal RNA molecule of the 50S subunit
  • Bacteriostatic

CNS penetration:
- Poor

Route of elimination:
- Biliary

Clinical use:

  • Atypical pneumonia
  • Mycoplasma pneumonia
  • Legionella pneumophila
  • Chlamydophila pneumoniae
  • Upper respiratory infections
  • STIs caused by Chlamydia (including chancroid)
  • Gram-positive cocci
  • Bordetella pertussis
  • Neisseria
  • Erythromycin: gastroparesis (e.g., resulting from diabetes mellitus)
  • Azithromycin: treatment and prophylaxis of Mycobacterium avium complex infection

Adverse effects:

  • Increased intestinal motility → GI discomfort
  • QT-interval prolongation
  • Acute cholestatic hepatitis
  • Eosinophilia
  • Exanthem
  • CYP3A4 inhibition

Contraindications:

  • Pregnancy
  • Erythromycin is relatively contraindicated in hepatic failure.
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3
Q

Lincosamides

A

Drugs:
- Clindamycin

Mechanism of action:

  • Inhibits bacterial protein synthesis by binding the 50S subunit of the bacterial ribosome and inhibits peptide translocation
  • Bacteriostatic

CNS penetration:
- Poor

Route of elimination:
- Both renal and biliary

Clinical use:

  • Anaerobes (e.g., Clostridium, Bacteroides)
  • Aspiration pneumonia
  • Lung abscesses
  • Partially effective against gram-positive aerobes (MRSA)
  • Babesiosis

Adverse effects:

  • GI side effects
  • Pseudomembranous colitis
  • Fever
  • Cross-resistance with macrolides

Contraindications:

  • Pregnancy (relative contraindication)
  • Clindamycin is indicated for anaerobes above the diaphragm and metronidazole treats anaerobes below it!
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4
Q

Amphenicols

A

Amphenicols:
Drugs:
- Chloramphenicol

Mechanism of action:

  • Inhibits bacterial protein synthesis by blocking peptidyl transferase at the 50S subunit
  • Bacteriostatic

CNS penetration:
- Good

Route of elimination:
- Renal elimination

Clinical use:

  • Meningitis caused by H. influenzae, N. meningitidis, and/or S. pneumonia
  • Rickettsia (Rocky Mountain spotted fever)

Adverse effects:

  • Dose-dependent bone-marrow depression: anemia, leukopenia, thrombocytopenia
  • Aplastic anemia
  • Gray baby syndrome (in infants ): cyanosis, vomiting, flaccidity, hypothermia, shock

Contraindications:

  • Infancy
  • Last trimester of pregnancy
  • Hepatic failure (relative contraindication)
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5
Q

Oxazolidinones

A

Oxazolidinones:
Drugs:
- Linezolid

Mechanism of action:

  • Inhibition of bacterial protein synthesis by binding at the 50S subunit of the bacterial ribosome
  • Bacteriostatic
  • Additionally bactericidal only against streptococci

CNS penetration:
- Good

Route of elimination:
- Both biliary and renal elimination

Clinical use:
- Gram-positive resistant bacteria (VRE, MRSA)

Adverse effects:

  • Bone marrow suppression (especially thrombocytopenia)
  • Peripheral neuropathy
  • GI upset
  • Serotonin

Contraindications:
- Concurrent use with monoamine oxidase inhibitors (MAOI) and selective serotonin reuptake inhibitors (SSRIs)

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6
Q

Aminoglycosides

A 
Aminoglycosides: 
Drugs: 
- IM or IV gentamicin
- IV or IM amikacin
- IV or IM tobramycin
- IV or IM streptomycin
- Oral neomycin

Mechanism of action:

  • Inhibits bacterial protein synthesis by binding to the 30S subunit of the bacterial ribosome
  • Damage to the cell wall
  • Bactericidal
  • Synergistic effect when combined with beta-lactam antibiotics: Beta-lactams inhibit cell wall synthesis → facilitate entry of aminoglycoside drugs into the cytoplasm

CNS penetration:
- Poor

Route of elimination:
- Renal

Clinical use:

  • Severe gram-negative bacilli infections
  • Not effective against anaerobes
  • Neomycin, which is not absorbed systemically, is administered orally to prepare the gut for bowel surgery.
  • Streptomycin: Mycobacterium tuberculosis, M. avium-intracellulare

Adverse effects:

  • Nephrotoxicity
  • Ototoxicity and vestibulotoxicity (impaired hearing and balance)
  • Neuromuscular blockade

Contraindications:

  • Myasthenia gravis, botulism
  • Renal failure (relative contraindication)
  • Pregnancy (relative contraindication)
  • Streptomycin is absolutely contraindicated during pregnancy
  • Mechanism of antibiotics resistance: Secreted bacterial enzymes inactivate the antibiotics through acetylation, phosphorylation, or adenylation.

Mean GNATScaNNOT kill anaerobes. (AMINoglycosides; Gentamycin, Neomycin, Amikacin, Tobramycin, Streptomycin; Nephrotoxicity, Neuromuscular blockade, Ototoxicity, Teratogenic)

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7
Q

Glycylcyclins

A

Glycylcyclins:
Drugs:
- Tigecycline

Mechanism of action:

  • A glycylcycline that inhibits bacterial protein synthesis by blocking peptidyl transferase at the 30S subunit
  • Bacteriostatic

CNS penetration:
- Poor

Route of elimination:
- Mostly biliary

Clinical use:

  • Gram-positive aerobes
  • MRSA
  • Anaerobes
  • Partially effective against gram-negative aerobes
  • Atypical bacteria: Borrelia, Mycoplasma, Rickettsia, Chlamydia

Adverse effects:

  • Gastrointestinal side effects
  • Hepatotoxicity
  • Deposition in bones and teeth
  • Damage to mucous membranes (these antibiotics should be taken with a lot of water)
  • Photosensitivity

Contraindications:

  • Pregnancy
  • Hepatic failure (relative contraindication)
  • Should be used with caution for children < 8 years and lactating women
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8
Q

Nitrofurans

A

Nitrofurans:
Drugs:
- Nitrofurantoin

Mechanism of action:

  • Nonspecific binding to bacterial ribosomal proteins → impaired metabolism, impaired protein, DNA, and RNA synthesis
  • Bactericidal

Route of elimination:
- Mostly renal

Clinical use:
- Treatment of and/or prophylaxis against lower urinary tract infections (e.g., urethritis, cystitis)

Adverse effects:

  • Gastrointestinal side effects
  • Reversible peripheral neuropathy
  • Pulmonary fibrosis
  • Triggers hemolytic anemia in G6PD-deficient patients

Contraindications:

  • Renal injury
  • Lactating women
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Antibiotics (5 decks)

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