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Macrolides

  1. Antibiotics with large rings
  2. Bacteristatic (except: H. Influenza)
  3. Protein synthesis inhibitors (50 S)
  4. Water soluble drugs
  5. Immunomodulatory/anti-inflmmatory
  6. All activate MOTILIN receptors
     
    i. Erythromycin is most potent

MAO

  1. Inhibit initiation of chain elongation

MOR

  1. Defective permeability

P/K

  1. Well absorbed
  2. Azithromycin-long acting; half life-50 hours
    1. Sequestrated in tissues
    2. Food reduces its absorption
    3. Has no antipseudomonal activity  
  3. Erythromycin-eliminated by bile
     
    i. Short acting; half life -1 hour  

P/D: Macrolides exhibit postantibiotic effects

Means, killing continues even when antibiotic is cleared from plasma or too low

Two types

  1. Concentration dependent
    1. Azithromycin
    2. Aminoglycosides
       
      Single large dose is more effective; less toxic than multiple small doses
  2. Time dependent
    1. Beta-lactam
    2. Fluoroquinolones
       
      So long, antibiotic conc. Remains above MIC; it will work

Uses

  1. Erythromycin
    1. Whooping cough            
    2. Bacillary angiomtosis            
    3. Compylobacter jijuni
    4. Diphtheria (prophylaxis)      
    5. Chancroid
  2. Clindamycin
     
    a. DOC
    1. Bacteroides fragilis
    2. Bacterial vaginosis in first triamester pregnancy
    3. Used in MDR malaria; babesiosis, phenumocystis
  3. Roxithromycin
     
    i. More active on respiratory pathogens, than erythromycin
  4. Azithromycin (DOC)
    1. Trochoma
    2. Legionella
    3. Short course antibiotic therapy
  • Absorption is reduced by food
  • No action against pseudomonas
  • NO DRUG INTERACTIONS
  1. Telithromycin
     
    i. Macrolide resistant bacteria

S/E

  1. MC-diarrhoea
  2. Cholestatic hepatitis
    1. Estolate salt
    2. More common in pregnancy
  3. Ototoxicity (erythromycin)
  4. Telthromycin
    1. Hepatitis
    2. QT interval prolongation
  5. Clindamycin
     
    i. Psedomembranous enterocolinitis  




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