Tetracyclines and Glycylcycline

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Anonymous
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45457
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Tetracyclines and Glycylcycline
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2010-10-27 12:56:19
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Tetracyclines Glycylcycline
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Tetracyclines and Glycylcycline
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  1. Mechanism of Action (Tetracyclines)
    Protein synthesis inhibitor
  2. Spectrum of Activity (Tetracyclines)
    • CA-MRSA
    • S. pneumoniae and othe Streptococci
    • Enterococcus - poor activity
    • H. Flu
    • M. catarrhalis
    • Moderate to poor against Enterobacteriacea
    • Used in combinations for H. pylori
    • DOC for Brucella spp. and Vibrio Cholerae
    • Excellent against spirochetes, Rickettsia, Chlamydia and Mycoplasma
  3. Mechanisms of Resistance (Tetracyclines)
    • Efflux (Do not affect doxycycline or minocycline)
    • Ribosomal Protection Proteins
  4. Bioavailability (Tetracyclines)
    • Tetracyline 60-80%
    • Doxycycline 90-100%
    • Minocycline 90-100%

    • Food and milk decrease absorption
    • Do not take with an antacid.
  5. Distribution (Tetracyclines)
    • Excellent tissue penetration
    • Lipophilicity: Tetra < Doxy < Mino

    CNS penetration follow lipophilicity

    Readily cross placenta and into breast milk
  6. Tetracycline
    • Bioavailability: 60-80%
    • Minimal hepatic metabolism
    • Eliminated 60% unchanged in urine, significatnt bile/fecal elimination
    • Half Life: approx. 6 hr
  7. Doxycycline
    • Bioavailability: 90-100%
    • Hepatic Metabolism: approx 50%
    • Elimination: 20-30% in urine, remainder in bile/feces
    • Half Life: 15-24 hrs
  8. Minocycline
    • Bioavailabity: 90-100%
    • Hepatic Metabolism: more than 50%
    • Elimination: Approx. 10% in urine, remainder in bile/feces
    • Half Life: 11-22 hrs
  9. Adverse Effects (Tetracyclines)
    • Gastrointestinal (worst with tetracycline)
    • Photosensitivity
    • Hepatitis (rare)
    • Hypersensitivity (uncommon)
    • Tooth discoloration
    • Antianabolic effects
  10. Precautions (Tetracyclines)
    • Should not be used in pregnant or breastfeeding women
    • Cause inhibtion of bone growth in fetus.
  11. Therapeutic Uses (Tetracyclines)
    • Rickettsial Infections
    • Lyme Disease
    • Acne (minocycline) - When systemic antibiotic is required
    • Acute exacerbations of chronic bronchitis
    • SIADH (Syndrome of Inappropriate Antidiuretic Hormone)
    • Prevention of Travelers Diarrhea (Doxycycline) - Not recommended
  12. Drug Interactions (Tetracyclines)
    • Antacids
    • Calcium supplements
    • Iron supplements

    These Chelate with tetracyclines
  13. Mechanism of Action (Tigecycline)
    Prevents protein synthesis by binding to 30S ribosomal subunit
  14. Spectrum of Activity (Tigecycline)
    • S. aureus (including MRSA)
    • Entercoccus spp.
    • S. pheumoniae
    • Enterobacteriaceae
    • Acinetobacter spp
    • Pseudomonas - poor activity
    • Good anaerobic coverage.
  15. Tigecycline
    • In quassi-class called gylcylcylcines
    • Derivative of minocycline
    • IV only
    • Biliary elimination
    • Half Life: 36 hrs
    • Usually dosed BID because more likely to vomit with once daily.
    • Good tissue penetration, with slow release from tissues.
  16. Therapeutic Uses (Tigecycline)
    • Complicated skin and skin structure infections
    • Intra-abdominal infections
  17. Adverse Reactions (Tigecycline)
    Nausea/vomiting (approx. 30%)

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