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ANTIBIOTICS:

ANTIBIOTICS:. By: Prof Avijit Mazumder. Objectives:. What are antibiotics? What are the various classes and their mode of action? Why is resistance developing to antibiotics? Is this a problem? What role can the pharmaceutical scientists play in regard to this problem?. Penicillins.

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ANTIBIOTICS:

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  1. ANTIBIOTICS: By: Prof Avijit Mazumder DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  2. Objectives: What are antibiotics? What are the various classes and their mode of action? Why is resistance developing to antibiotics? Is this a problem? What role can the pharmaceutical scientists play in regard to this problem? DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  3. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  4. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  5. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  6. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  7. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  8. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  9. Penicillins • First antibiotic to be used in 1941 • Originally isolated from Pc notatum Low toxicity • Effective derivatives created from manipulating drug’s basic molecular structure • Kills bacteria by preventing them from forming the rigid cell wall • Because human cells do not have cell walls, they are not affected DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  10. MODE OF ACTION: NAM NAG NAM NAG L-Ala L-Ala D-Glu D-Glu L-Lys L-Lys GLY 5 D-Ala D-Ala D-Ala DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI D-Ala D-Ala

  11. Drug List Penicillins • amoxicillin (Amoxil, Trimox) • amoxicillin-clavulanate (Augmentin) • ampicillin (Principen) • ampicillin-sulbactam (Unasyn) • carbenicillin (Geocillin) DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  12. Drug List Penicillins • dicloxacillin • oxacillin • penicillin G (various) • penicillin V (Veetids) • piperacillin DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  13. Drug List Penicillins • piperacillin-tazobactam (Zosyn) • ticarcillin (Ticar) • ticarcillin-clavulanate (Timentin) DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  14. Therapeutic Uses of Penicillins • Beta-hemolytic streptococcus • Meningitis • Otitis media • Pneumonia • Respiratory infections • Tooth and gum infections • Venereal diseases (syphilis and gonorrhea) • Endocarditis due to streptococci DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  15. Penicillins’ Side Effects • Diarrhea • Allergies in 7% to 10% of population DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  16. Penicillins’ Dispensing Issues • Take on an empty stomach • Food slows absorption • Acids in fruit juices or colas could deactivate the drug DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  17. Penicillin Resistance • Penicillinase-resistant penicillins work against gram-positive aerobes • Extended-spectrum penicillins are more resistant to gram-negative bacteria • Penicillin combinations improve effect DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

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  19. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

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  23. Classification of newer penicillins • Acid Resistant Penicillins: Phenoxymethyl Pc. • Penicillinase resistant Penicillins: Methicillin, Cloxacillin • Extended Spectrum Penicillins: Ampicillin, Mezlocillin, Ticarcillin, Piperacillin • Β lactamase inhibitors: Clavulanic acid Salbactum DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  24. BETA LACTAMASE INHIBITORS • Clavulanic acid : Obtained from Streptomyces clavuligerus, it has a beta lactum ring but no antibacterial activity. • Addition of clavulanic acid reestablishes the activity of amoxicillin against beta lactamase producing acid resistant S.aureus, E.coli, Proteus, Salmonella that are not responsive to amoxicillin alone. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  25. Cephalosporins • Have a mechanism of action similar to penicillins • A person allergic to penicillin, about 10% chance of being allergic DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  26. Cephalosporins Alert the Pharmacist if a patient allergic to penicillins is receiving a cephalosporin prescription. Warning! DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  27. Cephalosporins • First-generation • Similar to penicillinase-resistant penicillins with greater gram-negative coverage • Used for • community-acquired infections • mild to moderate infections DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  28. Cephalosporins • Second-generation • Increased activity, especially against Haemophilus influenzae • Used for Respiratory infections • UTIs DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  29. Cephalosporins • Third-generation • Active against a wide spectrum of gram-negative organisms • Long half-life, so once-a-day dosing for some • Used for • Ambulatory patients • Children DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  30. Cephalosporins • Fourth-generation • Active against a wide spectrum of gram-negative organisms • Long half-life, so once-a-day dosing for some. • Highly resistant to beta lactamases and so widely used against hospital acquired serious infections • Eg: Cefepime DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

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  32. Cephalosporins Side Effects • Share side effects of penicillin • Few may initiate unique toxic reactions • Lower frequency of toxicity than many other antibiotics DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  33. Cephalosporins All of the cephalosporins look alike when written in the generic form. Watch for dosing and indications for use. Warning! DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  34. Drug List Cephalosporins • cefaclor (Ceclor) • cefadroxil (Duricef) • cefazolin (Ancef) • cefdinir (Omnicef) • cefditoren (Spectracef) • cefepime (Maxipime) DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  35. Drug List Cephalosporins • cefotaxime (Claforan) • cefotetan (Cefotan) • cefoxitin (Mefoxin) • cefpodoxime (Vantin) • cefprozil (Cefzil) • ceftazidime (Fortaz) • ceftibuten (Cedax) DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  36. Drug List Cephalosporins • ceftizoxime (Cefizox) • ceftriaxone (Rocephin) • cefuroxime (Ceftin, Zinacef) • cephalexin (Keflex) • cephradine (Velosef) DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  37. USES OF CEPHALOSPORINS • Alternative to Pc G particularly in allergic patients • Respiratory tract infections caused by gram negetive spp • Penicillinase resistant staphylococal infection • Septicaemias caused by gram negetive organism: aminoglycosides+ cephalosporins • Surgical prophylaxis: First generation cephalosporins eg cefazolin(im) is employed in all surgery. • Meningitis: Pyogenic meningitis require bactericidal activity in CSF pref with Ab at sev times higher conc than MBC • Hospital acquired infection DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

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  41. Aminoglycosides • Treat serious infections • Inhibits bacterial protein synthesis by binding to ribosomal subunits DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  42. Aminoglycosides • Less frequent dosing may help reduce toxicity • Less drug accumulates in the kidney and ear • Simplified drug monitoring • Levels should be checked prior to administration of second dose to confirm drug elimination DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  43. Aminoglycosides’ Side Effects • Nephrotoxicity, destructive to kidney • Ototoxicity • Permanent deafness • Equilibrium problems DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  44. Drug List Aminoglycosides • amikacin • gentamicin (Garamycin, Genoptic) • kanamycin (Kantrex) • neomycin (Myciguent, Neo-Fradin) • streptomycin (none) • tobramycin (Nebcin) DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  45. Tetracyclines • Broad-spectrum bacteriostatic antibiotics • Inhibit protein synthesis in bacteria by binding to ribosomes • Suppress the infection and require phagocytes to complete the eradication of the bacteria DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  46. Therapeutic Uses of Tetracyclines • Acne • Chronic bronchitis Pneumoniae infection • Rickettsia infection • Chlamydia infection • Traveler’s diarrhea DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  47. Tetracyclines’ Side Effects • Gastrointestinal upset with nausea and vomiting DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  48. Tetracyclines’ Dispensing Issues • Avoid antacids to avoid chelation with minerals • Photosensitization • To be avoided by pregnant women and children • Expired drugs are dangerous DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  49. Drug List Tetracyclines • doxycycline (Vibramycin) • minocycline (Minocin) • tetracycline (Sumycin) DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

  50. DR AVIJIT MAZUMDER, SPTM,NMIMS UNIVERSITY, MUMBAI

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