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Tetracyclines and Chloramphenicol (broad spectrum antibiotics)
Source-  Soil actinomycetes Chlortetracycline-  introduced in 1948 Divided into three groups:  Group I-  Tetracycline Chlortetracycline Oxytetracycline  Group II- Demeclocycline Methacycline Lymecycline
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2.  Most gram positive bacilli-  Clostridia, Listeria &  Corynebacteria  are inhibited but not  Mycobacteria .  3.  Sensitive gram negative bacilli-  H.ducreyi,V .cholerae, Yersinia pestis etc. 4. Spirochetes 5. Rickettsiae  and  Chlamydiae   are highly sensitive 6.  Entamoeba histolytica  and  plasmodia -  at high concentration
[object Object],[object Object],[object Object]
Group I Tetracycline(T) Oxytetracycline (oxyT) Group II Demeclocycline (Deme) Group III Doxycycline(Doxy) Minocycline(Mino) Source T- semisynthetic OxyT-  S.rimosus S.aureofaciens Doxy- semisynthetic Mino- semisynthetic  Potency Low Intermediate High Intestinal  absorption T- intermediate OxyT- intermediate intermediate Complete, no interference by food Plasma protein binding OxyT- Low T- intermediate High High Elimination Rapid renal excretion Partial metabolism, Slower renal excretion Doxy- faeces Mino- urine and bile Plasma 6-10 hrs 16-18 hrs 18-24 hrs Dosage 250-500 mg QID or TDS 300-600 mg BD 200 mg initially, 100-200 mg OD
Group I Tetracycline(T) Oxytetracycline (oxyT) Group II Demeclocycline (Deme) Group III Doxycycline(Doxy) Minocycline(Mino) Alteration of intestinal flora Marked Moderate Least Incidence of diarrhoea High Intermediate Low Phototoxicity Low Highest Low Specific toxicity OxyT-less tooth discolouration More phototoxic Doxy-low renal toxicity
[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
CHLORAMPHENICOL Source-  Streptomyces venezuelae  in 1947 Mechanism of action- inhibits bacterial protein synthesis By interferring with transfer of elongating peptide chain  to the newly attached aminoacyl-tRNA at the ribosome-mRNA complex. It binds to 50S ribosome Probably by acting as peptide analogue, it prevents formation of peptide bonds
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Tetracyclines

  • 1. Tetracyclines and Chloramphenicol (broad spectrum antibiotics)
  • 2. Source- Soil actinomycetes Chlortetracycline- introduced in 1948 Divided into three groups: Group I- Tetracycline Chlortetracycline Oxytetracycline Group II- Demeclocycline Methacycline Lymecycline
  • 3.
  • 4.
  • 5. 2. Most gram positive bacilli- Clostridia, Listeria & Corynebacteria are inhibited but not Mycobacteria . 3. Sensitive gram negative bacilli- H.ducreyi,V .cholerae, Yersinia pestis etc. 4. Spirochetes 5. Rickettsiae and Chlamydiae are highly sensitive 6. Entamoeba histolytica and plasmodia - at high concentration
  • 6.
  • 7. Group I Tetracycline(T) Oxytetracycline (oxyT) Group II Demeclocycline (Deme) Group III Doxycycline(Doxy) Minocycline(Mino) Source T- semisynthetic OxyT- S.rimosus S.aureofaciens Doxy- semisynthetic Mino- semisynthetic Potency Low Intermediate High Intestinal absorption T- intermediate OxyT- intermediate intermediate Complete, no interference by food Plasma protein binding OxyT- Low T- intermediate High High Elimination Rapid renal excretion Partial metabolism, Slower renal excretion Doxy- faeces Mino- urine and bile Plasma 6-10 hrs 16-18 hrs 18-24 hrs Dosage 250-500 mg QID or TDS 300-600 mg BD 200 mg initially, 100-200 mg OD
  • 8. Group I Tetracycline(T) Oxytetracycline (oxyT) Group II Demeclocycline (Deme) Group III Doxycycline(Doxy) Minocycline(Mino) Alteration of intestinal flora Marked Moderate Least Incidence of diarrhoea High Intermediate Low Phototoxicity Low Highest Low Specific toxicity OxyT-less tooth discolouration More phototoxic Doxy-low renal toxicity
  • 9.
  • 10.
  • 11.
  • 12. CHLORAMPHENICOL Source- Streptomyces venezuelae in 1947 Mechanism of action- inhibits bacterial protein synthesis By interferring with transfer of elongating peptide chain to the newly attached aminoacyl-tRNA at the ribosome-mRNA complex. It binds to 50S ribosome Probably by acting as peptide analogue, it prevents formation of peptide bonds
  • 13.
  • 14.