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Macrolides, Aminoglycosides, Polyene & polypeptide antibiotics.pptx

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Macrolides, Aminoglycosides, Polyene & polypeptide antibiotics.pptx

  1. 1. Macrolides, Aminoglycosides, Polyene & polypeptide antibiotics
  2. 2. Contents  Macrolide  Mechanism & Resistance Pharmacokinetic Therapeutic uses, adverse effect and drug interaction Aminoglycoside Mechanism & Resistance Pharmacokinetic Therapeutic uses, adverse effect and drug interaction Polyene and polypeptide
  3. 3. Resistance
  4. 4. • Streptococcus pneumoniae, strepto. Pyrogenes • Staphylococci Gram positive cocci • N. gonorrhoea • Moraxella catarrhalis Gram negative cocci • Bacillus anthracis, Corynebacterium diphtheriae • Clostridium tetani Gram positive bacilli • Legionella pneumophila, Bordetella pertussis • H. pylori Gram negative bacilli • Mycobacterium leprae • M. avium intracellulare Acid fast bacilli Peptostreptococcus, Actinibacilus, Pasteurella, B. fragilis, MRSA
  5. 5. • Moraxella catarrhalis • Less potent- Bordetella pertussis Roxithromycin • Legionella pneumophila, H. influenzae • Chlamydia trochomatis, M leprae Clarithromycin • Moraxella catarrhalis, Chlamydia trochomatis • H. influenzae, M. pneumoniae Azithromycin • Toxoplasma gondii • Cryptosporidium Spiramycin
  6. 6. Pharmacokinetics erythromycin Absorption • Oral • Destroy by gastric acid Distribution • Tonsillar tissue • middle ear fluid • prostatic fluid • CSF Excretion • Bile • 5% Urine
  7. 7. Acid stable macrolides Roxithromycin Clarithromycin Azithromycin Spiramycin
  8. 8. Therapeutic uses- Erythromycin FIRST CHOICE OF DRUG 1) Atypical pneumonia 2) Pneumonia 3) Whooping cough SECOND CHOICE OF DRUG 1) Campylobacter gastroenteritis 2) Chancroid 3) Chlamydial conjunctivitis
  9. 9.  Non- Chemotherapeutic uses  Anti-inflammatory Rheumatoid arthritis, cystic fibrosis, asthma
  10. 10. Clarithromycin • Lung disease Mycobacterium avium complex • Pneumonia, epiglottis • Meningitis H. influenzae • Toxoplasma Toxoplasma gondii • Leprosy Mycoplasma leprae
  11. 11. Azithromycin H. influenzae Moraxella catarrhalis Legionella Pneumonia epiglottis Meningitis Otitis media COPD Acute bacterial rhinosinusitis lung infection Pontiac fever
  12. 12.  Spiramycin – Toxoplasma gondii  Adverse Effect Cholestatic hepatitis  Epigastric pain  Ototoxicity  Tinnitus
  13. 13. Drug interactions Erythromycin Clarithromycin Theophylline, Carbamazepine, warfarin Macrolide Digoxin
  14. 14. Aminoglycoside
  15. 15. How Cidal action is achieved Ans- Defective proteins incorporated in cell membrane. Due to secondary changes in the integrity of bacterial cell membrane. (Increase permeability for ions, amino acids, proteins- Leading to leaking of these out side) Bonus of incorporation of defective protein in cell membrane More entry of antibiotic occurs in to the cell. Further increasing affectivity Death Of Bacteria
  16. 16. Resistance 1. Inactivation through enzymes 2. Mutation / deletion of porin channels 3. Alteration of the receptor protein on 30s ribosome
  17. 17.  Aminoglycoside exhibit Concentration Dependent Killing  Aminoglycoside also posses post-antibiotic effect
  18. 18. Pharmacokinetics  Oral drugs Highly polar, basic drugs Poor oral bioavailability  Excreted in faeces IV Kidney Urinary tract infection Dose for a case of renal = insufficiency
  19. 19. Antibacterial spectrum Gram negative aerobic bacilli • E.coli • Klebsiella • Shigella • Proteus Gram positive cocci • Staph. aureus • Streptococcus viridans Gram positive bacilli, gram negative cocci, anaerobes
  20. 20. Streptomycin 1. Plague 2. Tularemia 3. Brucellosis - -Subacute bacterial endocarditis 1 g/day IM + Tetracycline
  21. 21. Gentamicin  Combination with other antibiotics • Septicaemia • Sepsis • Fever Ampicillin • Pelvic infection Metronidazole • Subacute Bacterial Endocarditis (SABE) Benzathine penicillin G • UTI Ampicillin/ ceftriaxone
  22. 22. Gentamycin Sisomicin Greater efficacy against Pseudomonas Beta- haemolytic streptococci Tobramycin Proteus, pseudomonas acinetobacter Netilmicin Resistant to aminoglycoside inactivating enzyme Proteus, pseudomonas, klebsiella, E.coli, Staph. aureus
  23. 23.  Kanamycin Arbekacin  Stable in presence of aminoglycoside inactivating enzyme Effective against gram positive and gram negative bacteria  MRSA, P.aeruginosa, E.coli, K. Peumoniae, Enterobacter cloacae Serratia marcescens  proteus mirabilis, proteus rattegiri proteus vulgaris morganelloa morganii
  24. 24. Amikacin: resistant to enzyme inactivation, used in combination with antitubercular drugs Neomycin With bacitracin- prevent infection in wound and cuts 1. As preoperative intestinal antiseptic  framycetin  skin infection, burns  ophthalmic infection
  25. 25. Adverse Effects 1. Nephrotoxicity 2. Ototoxicity 3. Neuromuscular blockage
  26. 26. Polyene & polypeptide antibiotics
  27. 27.  Polymyxin-B  Colistin / Polymyxin-E
  28. 28. Cationic detergent displace calcium and magnesium from membrane Disrupt bacterial cell membrane osmotic integrity Leakage of contents Cell death
  29. 29.  Polymyxin-B sulfate used primarily topically Used in treatment of skin, ear and eye infection  Colistin sulfate- GIT infection  Colistimethane sodium- Respiratory infection Effective against Gram negative bacilli Except Proteus, serratia, Bacteroides fragalis
  30. 30. Adverse effect Nephrotoxicity  Bronchoconstriction

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