Antibiotic

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Antibiotic
2

• Antibiotics-
• Are chemicals work only on bacteria .
• Bactericidal Kill bacteria
• Bacteriostatic Inhibits the growth of bacteria.
  
• Narrow- spectrum antibiotics- act only on gmve
  or gm-ve .
• Broad spectrum antibiotics act on both
  gmve gm-ve bacteria.

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• ????? ??? Antibiotic ???? ??????? ?? ?????? ???
  ???? ??? Fungus ?? ??????? Actinomycete
• ???? ?????? ?????? ??? ????? ??? ?? ???
  ????????? ?????? ???? ????.
• ???? ??? ??????? ????? ???????? ??? ???????
  (Semi-synthetic) ??? Clarithromycin ? Ampicillin
  ????????? ??????? (Synthetic) ??? Ciprofloxacin ?
  ???? ??? Fluoroquinolones

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• Antibiotic against life(The life of pathogens
• Antiagainst BiosisLife

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• ?? ?? ????? ??? Antimicrobial ? Antibiotic?
• ?????- (Antimicrobial)-
• ???? ??? ??????? (non-microbial in origin)
• ??? ?????? ?? ??? Antibiotic
• ???? ??????? ??????? ?????? ?????? ???? ????
  ?????? ??? Mic (Minimum Inhibitory Concentration)
  ?????? ?????? ???? ????? ?? ??? ?? ???????????
• Mic few mg/ml

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• ??? ??????? ??? Antimicrobial ????? ???????
  ??????????????
• Mic 100 mg/ml
• ???? ??? Antimicrobial Metronidazole ???????
  ??????
• ??? ??? Anti-Infective ??????? ??? ???????
  ?????? ?????? ????? ?????????? ?????
  Anti-Infective
• ??????? ????? ???? Antimicrobial ????
• (antibiotics,antifungal,and antiprasitic dmgs)

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????? ?????? ???????? ??????? History Of
Antibiotic Discovery
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• Alexander Fleming microbiologist ?? ?????????-
  ??? ?????? S.aureus ???? ?? ????? ??????? ????
  ??? ??? plates ???? ??????? ???? ?? ??? ????? ??
  penicillium notatum
• ????? ?? ????????? ?? ???? ?????? ?? ??? ?????
  ????? ?????? ???.

9

• ??????? Fleming ?? ??? ????? ???? ???? ????? ????
  ????????? . ????? ????? ????? ?????????1. ??
  ??????F ?? ???????? ????????? ?????? ??? ?? ?????
  ??? ??? S.aureus ???? ??? ??? 1928.
• ??? ?????? ??? ???????? ??? ???? ???? ????? ?????
  ???? ?? ??? ????? ???? ???? ???? ?????? ???? ??
  ?????? ???? ???? ????? ???? ???? ???? ????????
  ???? ????? ???????.

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• ?? ??? 1943 ?????????
• Penicillium chrysogenum ????? ????
  
• Penicillin II
• Penicilline G
• Benzylepenicillin American
  penicilline

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• ??? ??? ?????????? ?? penicillin II ????
  pnicillin I ?? ??? ??????? ????????? ????????.
  ???????? ??? ??? ?????? ?????? ???????. ????
  ????? ???? ??? ?????? ???? ?? ????? ????? ?????
  ?????? ??? ??????? ?????? ???? ???? ?? P.I ????
  40 ??? ?????? ???? ???? ?? P.II ???? ???? ???.
• ?? ????? 650 ????? ???? ?? P.II ??? 1943? ?? ???
  ???? ????? ??? ??????? ?? ????? P.I ????? 400
  ????? ???? ?? ???? ?? ????? ????
• ???? ??? ??????? ???? Penicillin G ?? ????????
  ?????? ??? Penicillin I ????? ?? ???? ???????
  ???.

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• ??????
• ?? ?????? ????? Pencillinum notatum ?????
  pencillin G ??? ????????? ???????? ??? ???? ????
  ??? ?? ???? ?????? ????? (Cornsteep) ??? ??????
  ?? ??? Corn.
• ?? ????? ??? Phenoxymethypenicillin ??? ?? ????
  ?? penicillin V ?? ????? ?????????? ????????
  ??????? ??????
• Sterptomycin 1944
• Chloramphenicol 1947
• Tetracycline 1948

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• Semi-synthetic penicillins 1958
• Cephalosporins 1960
• Fluoroquinolones 1980

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• ????? ???????? ???????(Classification of
  antibiotics)-
• ????? ??? ??? ??????? ???? ???-
• ?????? ????? ???? ??? ?????????? (Bacteriostatic)
  ????? ????-
• Teracycline.
• Chloramphenicol.
• Erythromycin.
• Spectinomycin.
• Florfenicol.
• ?????? ????? ???? ?????? ????????? Bactericidal
  ????? ????-
• Gentamycin.
• Bacitracin.
• Colistin.
• Penicllins.
• Amoxycillin.
• Cephalosporins.
• Neomycin.

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• ?????? ??? ??? ?? ???? ?????? ???? ???-
• ?????? ????? ?????? ?????? (Narrow-spectrum) -
• Benzyl Penicillin Or Penicillin
• Streptomycin.
• Temosillin.
• Polymxin B
• 2. ?????? ????? ????? ?????? (Broad-spectrum)-
• Ampicillin
• Amoxycillin
• Gentamycin
• Chloramphenicol
• Cephalosporins
• Tetracycline

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• ?????? ??? ???? ????? ??? ?????? ????????? ????
  ???-
• ?????? ????? ???? ????? ???? ??????(Inhibits Cell
  Wall Synthesis)-
• Penicillin
• Cephalosporins
• Bacitracin
• 2. ?????? ????? ???? ????? ?????? ??????(Inhibits
  Protein Synthesis)-
• Chloramphenicol.
• Tetracycline
• Gentamycin.
• Neomycin.
• Erythromycin.
• Streptomycin.
• Tylosin.

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• 3. ?????? ????? ???? ?? ?????? ???? ??????(Cell
  memberane) -
• ???-
• Polymxin B
• 4. ?????? ????? ???? ?? ???? ????? ???????
  ??????? ?? ?????? ???-
• Quinolone (Flumeqine)
• Rifampin (Disrupts RNA Synthesis)

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• ?????? ??????? ????????? ?????? ???-
• Beta-Lactam-antibiotics
• Aminoglycosides Aminocyclitol
• Tetracyclines
• Macrolides
• Polypeptides
• Miscellaneous

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• ??????????????(B-lactams)-
• ????? ?????
• Penicillins
• Cephalosporins
• Carbapenems
• Monobactams

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• ???????????????-
• ????? ????? ????? ?? ??????????
• Natural penicillins e.g penicillin G
• Aminopenicillins e.g amoxycillin Ampicillin-
  Hetacillin
• Penicillinase resistant penicillins e.g
• Cloxacillin
• Dicloxacillin
• Methicillin
• Naficillin
• Oxacillin

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• D. Extended spectrum pemicillins
• mega - spectrum
• e.g
• Ticarcillin
• Carbenicillin
• Mezlocillin
• Piperacillin

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• ???? ???????? ????? ?? ?? ??????? ??????????
  ????? ????? ????? ?? ???? ????????? ????????
  ??????????? ??? ???? ?????? ????? ?? ?????????
  ????? ?????? ??? ???? ?? ?? ????????? ????? ???
  ??? ???????? ?? ??? ????? ?? ?????????.
• ??? ????? ??? ???????? ???????????
  (Carbenicillin).
• ????? ????????? ????????? ??? ?????? ????????
  ???? ????????.??????? ????? ?? ????? ?????????
  ????????. ????? ?? ???? ??? ???????? ???????
  ?????????? ??????? ???? ??? ???????(????????)
  ?????? ?????? ?????? ??????????? ????? ?? ????
  ????? ?? ????? ???.

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• ?????????? ????? ?? ???? ????? ????????.
• ?????????? ????? ?? ??? ???????? ??????? ?????
  ??????? ???? ?????? ???????? ??? ??? ?? ?????????
  ??? ?????? ???????? ??? ???????? ???????? ???????
  ???? ?????? ???????? ??????? ??? ????? ????????
  ????? ?????? ?? ???????.
• ?????????? ??? ?? ???? ?????? ??? ???????? ??????
  ?? ???????? ??? ????????? ?? ??? ???????? ???
  ??????? ??????

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• ???????? ?????? (Benzylpenicillin)-
• ??? ???????? ?????? ?? ???????? ?????? ?????????
  ?? ???? ??????? ??? ?? ???????? ??????? ????????
  ????? ?? ??? ????? ????? ?? ?????? ?????
  ?????(??? ???? ???????? ?? ???? ?????? ????)
• ????????? ?????? ?? ?????? ????? ?? ??? ????????
  ?????? ????? ???? ??? ??????? ?? ??????? ?????.
• ???????? ?????? ???? ??? ?? ???????? ????? ??????
  ???
• Staphylococci.
• Streptococci
• Clostiridia.

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• ??? ?????? ?????? ??
• Leptospira
• Erysiplothrix
• Listeria
• ???? ?? ???? ???????? ????? ?????? ????? ???
  ?????? ??? ?????? Neisseria ? Pasteurella ????
  ??? Haemophilus ??? ?????? ?????? ??????.
• ?????? ??????? ??????? ???????? ?????? ???? 24-48
  ????
• ?? ???? ???????? ?????? ????? ???? ????? ?????
  ???? ?????? ?????? ?????? ?????? ???????? ?????
  ???? ?????? ?? ????? ?? ????????? ??????? ????
  ????? ?? ????? ???????.

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• ???? ???????? ?????? ?? ????? ????? ????? ????
  ??????? ?????? ??????? ??????? ???????? ??
  ???????? ???????. ????? ??????? ?????? ?????? ???
  ??? ????.
• ???? ????? ??? ???? ???????? ?????? ?? ?????
  ?????? ????? ???? ?????? ?? ???? ??????? ???????
  ??? (Probencid) ??? ??? ?????? ??? ???? ????????
  ???? ????? ???????? ???????? ???? ???? ??????
  ???? ?????.

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• ?? ?? ???????? ?????? (Procainepenicillin)?
• ???????? ?? ??? ??????? ???? ???? ????? 40 ???
  ???????? ?????? ????? ?????? ???? ?? ???? ???????
  ????.
• Benzathinepenicillin-
• ??? ????? ?? ???????? ???? ??????? ???? ???????
  ?? ???? ????? ???? 6 ???? ????? ?? ?????? ??????
  ??????? ???????? ?? ???? 72 ???? ??? ??? ????
• ???? ?????? ?? ???? ??????? ? Dihydrostreptomycin
• Penethamate-
• ???? ????? ???? ?????? ????? ?????? ??????.

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• Phenoxymethylpenicillin-
• ?? ??? ?????? ???????? ?????? ??????? ?? ???????
  ????????? ?????????? ???????? ?????? ??? ?? ???
  ???? ?? ????? ??????? ?????? ???? ????? ??????
  ?????? ?????????? ????? ???? ?????.
• ?????? ??????? ???? ???? ?? Aminopenicillins
  (semi-ynthetic)
• ????? ??? ???????? ????? ?? ?????????? ???????
  ?????????? ???????.
• ???? ??????? ????? ????? ?? ?????????? ?????
  ?????? ??? Salmonella E.coli- proteus Mirabilis
  ?????? ??? ????? ?? Bacteroides- Pseudomonas
  fragilis

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• ??? ??? ????? ?? ??? Penicillinase-producting
  staphylococcuss (SPP)
• ?? ??? ????? ??? ???????? ??? Amoxycillin-Ampicill
  in

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• Ampicillin-
• ????? ???????? ?????? ????????? ????? ????? ????
  ???? ????? ?? ??? ?????????? ??????? ????????
  ????? ????. ??????? ???? ???? ?????????? ?????
  ??? ???? ????????? ?? ???? ??????? ???? ????
  ?????? ??????? ????????? ???????? ??????????.
• ????? ?? ???? ???? ?????? ??? ???? ?? ???? ?????.
  
• ?????? ????????? ?? ?????????? ????? ????? ??????
  ?????? ???? ?? ???????????? ????????????????
  ????? ????? ?? ???? ???????? ??????? ????? ?????
  ?? ??????????.
• ????????? ????? ?????? ?????????? ????? ???? ??
  ??? ??????? ???? ???? ??? ??????? ???
• Olivanic acid- Clavulanic acid - Sulbactam

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• ?? ???? ?????? ???? ???? ??????? ??? ?? ????
  ?????? ???????.
• ????? ?????? ?????? ??????? ??????? ?????? ?????
  ?? ????? ?? ??????? ?????.
• Ampicillin Prodrugs-
• ???? ????????? ????? ???? ????? ???? ?? ???
  Prodrug ??? ???? ??????? ?? ????? ?????? ???
  ???????. ????? ????? ???? ??? Prodrug ???
  ??????? ????? ???????.
• ??????
• ?????? 4-12 ???/ ??? ????? 1-2 ??? ??????
• ?????? ?????? 4-20???/ ??? ????? 1-2 ???
  ??????

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• Amoxycillin-
• ?? ???? ???? ???? ??? Ampicillin ???? ????? ???
  ????? ???? ?? ????????? ???? ????? ????? ????
  ?????.
• ???? ????? ??? ???????? ?????? (70-92) ????
  ????? ????? ?????? ?? ??????. ??? ?????? ?????
  ????? ?? ?? ????? ?????? ??? ??????? ?????.
• ?????? ?????????? ???? ???? ?? Penicillinase-resis
  tant penicillin-
• ??? ???????? ????? ?? ???? ????? ???
  Penicillinase- producing staphylococcus ????
  ????? ?????????? ???????? ???????? ??????.
• ???? ?????? ?? ??? ????????? ????? ?????? ?????
  ??? ?????? ?? ????? ?????????? ??????.

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• ????? ?????? ??? ????????-
• Oxacillin
• Cloxacillin
• Dicloxacillin
• Naficillin
• ???? ????? ??? ???????? ??? ?????????? ???? ?????
  ????? ???????? ? ???? ???????? ??????? ??????????
  ????? ??? ????????? ????? ????? ?????? ?????
  ?????? ???? ?? ?????? ?????? ????????? ?
• ???? ??? ??????? ????? ??? ??? ??????????
  ??????? ????? ???? ??? ?????? ????????? ??????
  ???? ??????? ?? ???????

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• ?????? ???????????????? (Cephalosporins)-
• ???? ??? ????? ????? ??? ??? ?????? ?? ??????????
  ??????? ????? ????. ????? ??? ?????? ??????
  ??????????????.
• ????? ????? (First Generation)-
• ??? ??? ????? ??? ?????-
• Cefadroxil.
• Cefazolin.
• Cephalexi n.
• Cephalothin.
• Cephapirin.
• Cephradine

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• ????? ????? ??? ????? ???? ???? ???? ??
  ?????????? ??????
• Staphylococci spp
• Streptococci spp
• E.coli
• Proteusmirabilis
• Klebsiella spp
• ???? ???? ????? ??? ????? ?????? ???
  Aminopenicillins ???? ???? ??? ????? ??? ????? ??
  ???????????????? ????? ????? ?? ???????? ?? ???
  Staphylocci spp. ????? ??? ????? ??? ????? ????
  ?? ?????? ?? ????????? ????? ??????.

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• ????? ??? ????? ??? ??? ?????? ?? ?????????
  ?????????? ??? ??? ??????? ?? ?????????-
• Pseudomonas spp.
• Enterococcus spp.
• Enterobacter spp.
• Other proteus.
• Serratia

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• ????? ????? ?????? (Second Generation)
• ??? ??? ????? ??? ?????-
• Cafaclor.
• Cefamandole.
• Cefonicid.
• Ceforanide.
• Cefotetan.
• Cefoxitin.
• Cefprozil.
• Cefuroxime
• Loracarbef.
• Cefmetazole.

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• ????? ??? ????? ??? ?????? ?? ?? ???????? ????
  ???? ????? ????? ????? ????? .
• ????? ??? ????? ???????? Cefaclor ????? ????????
  ????????? ????? ??????.
• ?????? ??? ????? ?????? ?? ??? ????? ?????????
  ???? ???? ?????? ?????? ????? ????? ??? ???
  ??????? ?? Enterobacter, E.coli, Klebsiella,
  Proteus
• ????? ??????? ??????? ?? ??? ???????? ??? ??????
  ????????? ??????????
• Cefoxitin.
• Cefotetan.
• Cefmefazole
• Cefamandole.
• ???? ??? ??????? ?????? ?????? ?????????????? ??
  Cefuroxime

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• ????? ????? ?????? (Third Generation)
• ??? ??? ????? ??? ?????-
• Cefixime
• Cefoperazone
• Cefotaxime
• Cefpodoxime
• Ceftazidime
• Ceftiofur
• Ceftizoxime
• Ceftriaxone (Ceftriaxame)
• Moxalactam

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• ????? ??? ????? ?? ???? ??????????????? ?????? ??
  ?????????? ??????? ????? ???? ???? ????????
  ??????? ? ?????? ????? ??? ????? ???? ??????
  ?????? ?????? ??????????????.
• ????? ????? ??? ????? ???? ???????????????? ??
  ?????????? ????? ?????? ??????? ?????? ?? ???
  Staphylacocci.
• ?? ????? ????????? ??????? ?????? ???????? ??????
  ????? ????? ??????? ?????? ?????? ?????? ?????
  ??????.
• ???? ????? ??? ????? ??? ?????? ?? ???
  pseudomonas spp.
• ???? Cefotaxime ?? ?????? ???? ?? ?????????
  ??????????.
• ?????? ??? ?????? ??? ????? ??? ????? ??? ??
  ?????? ?? ?????????? ????? ??????.
• ??? ???? Ceftizoxime ?? ?????? ?? ??????????
  ?????????? ???? ?? ?? ????? ??? ?????.

41

• ??????? ?? ????? ????? ???? ?????? ?? ???? ????
  ?? ????? ??????? ??
• Cephradine Cephalexin Cefadroxil
• ??? ??????? ???????? ????????? ?? ???? ?????
  ???
• Cephalothin Na Cefazolin Na Cephapirin Na
  Cephradine
• ???? ??? Cephapirin Na ?????? ?? ???? ????? ??
  ????? ??????? ?????? ????? Cephapirin Benzathine
  ?????? ?? ???? ????? ?? ????? ??????? ??????.
• ?? ????? ?????? ????? Cefuroxime and Cefaclor
  ??????? ????????? ?? ???? ????.
• ?? ??? ??????? ?? ??? ????? ???? ?????? ?? ????
  ?????
• Cefotetan Cefoxitin
• ????????? ???? ???????? ??? ??????? ????? ?????
  ?????? ?? ????? ??????? ???? ???? ???????
  ???????.

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• ????? ????? ?????? ????? ??? ???????? ?????????
  ??????? ??? ?? ????? ????? ??? ?????? ????
  ??????? ??? ?? ???? ????? ?? ??? ???? Cefixime
  ???? ?????? ?? ???? ????.
• ???? ???? ??? ?? ??????????????? ??? ????? ????
  ???? ?????? ????????? ??????? ?????? ??? ???? ???
  ???? ???????? ??? ??????? ????? ?? ???? ?????? ??
  ???? ?????.
• ?????? ??????????????? ???? ???? ?? ???? ???????
  ?????? ??????? ???? ????? ???????? ??? ????
  ?????? ?????? ?? ??????? ????? ?????? ???????
  ????? ????? ????? ?? ???? ?????? ????? ???? ?????
  ?????? ???????.

43

• Beta-Lactamase Inhibitors
• Clavulanic acid
• Sulbactam(Penicillanic acid)
• ??? ????? ???? ??? ?????????? ???? ??????? ??????
  ?? ????? ?????? ???????????? ?? ???? ????? ???
  ??????? ?? ????? ????? ????????????? ???? ????
  ??? ????? ??? ??????.
• ?????? ?? ???? ???????? ????? ?? ??????????? ????
  ?????????? ?? ?????????? ????? 14.

44

• ????? ??? ??????? ?? ????????? ?????? ??? ?????
  ????????????????-
• Methicillin resistant staphylococcus spp
• Enterococcis spp
• ???????????????? ?? ???? ??? ???? ?? ????? ????
  ?? ?????????????????? (Incompatibility)

45

• ?????? Carbapenems
• ?????? ?????? ??????? ?? ????? ??????? ?? ???
  ???????? ?? Imipenem.
• ?? ?????? ??? ???????? ???? ?????? ??????
  ??????(Renal Toxicity) ???? ?? ?????? ??
  CIlastatin ??? ??? ??????? ??? ??? Cilastatin
  ????? (Renal Enzyme Inhibitor) ????? ??? ??????
  Imipenem-Cilastatin ?? ??????? ??????? ??
  ????????? ????? ?????? ???????? ??????????? ???
  ???? ???????????

45
46

• ?????? Monobactam-
• ??? ????? ??? ???????? Aztreonam.
• ????? ??? ?????? ???? ???? ?? ????????? ?????
  ?????? ??? ???? ??????????? ???? ??????? ??
  ????????? ????? ?????? ???? ???? ??????.
• ????? ??? ?????? ????? ?? ?????? ?????? ?????
  ????????????.

46