Get information about the pharmacology of antibiotics,their classification and mechanism of action.

1. ANTIBIOTICS

2. ANTIBIOTICS — are chemical compounds of biologic origin
that exert selective damaging or subversive effect on microorganisms.
There are antibiotics with Antibacterial, Antifungal and Antitumor actions .
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3. I. Inhibitors of cell wall synthesisI. Inhibitors of cell wall synthesis::
1.1. β-Lactam antibioticsβ-Lactam antibiotics:: 2. Others2. Others::
PenicillinsPenicillins PolypeptidesPolypeptides
CephalosporinsCephalosporins GlycopeptidesGlycopeptides
CarbapenemsCarbapenems
MonobactamsMonobactams
II. Producing disturbance in cell wall permeability:II. Producing disturbance in cell wall permeability:
Polypeptides (Polymyxins)Polypeptides (Polymyxins)
III Protein synthesis inhibitorsIII Protein synthesis inhibitors::
MacrolidesMacrolides ChloramfenicolChloramfenicol
TetracyclinesTetracyclines LincosamidesLincosamides
AminoglicosidesAminoglicosides
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5. 1. Narrow spectrum:1. Narrow spectrum:
 Gr(+) bacteria:Gr(+) bacteria: ●● Gr(-) bacteria:Gr(-) bacteria:
BenzylpenicillinsBenzylpenicillins PolymyxinsPolymyxins
OxacillinOxacillin
ErythromycinErythromycin
2. Broad Spectrum:2. Broad Spectrum:
TetracyclinesTetracyclines
AminoglycosidesAminoglycosides
Semi-synthetic Penicillins of Broad-spectrumSemi-synthetic Penicillins of Broad-spectrum
CarbapenemsCarbapenems
CephalosporinsCephalosporins
Levomycetin (Levomycetin (ChloramphenicolChloramphenicol))
RifampicinRifampicin 55

6. PENICILLINSPENICILLINS
I.I. Biosynthetical PenicillinsBiosynthetical Penicillins:: Narrow SpectrumNarrow Spectrum Gr(+)Gr(+)
A. For parenteral introductionA. For parenteral introduction::
Short actingShort acting (3-4 hs)(3-4 hs)::
Benzylpenicillin-NatriumBenzylpenicillin-Natrium
Benzylpenicillin-KaliumBenzylpenicillin-Kalium
Long actingLong acting::
Benzylpenicillin-NovocainBenzylpenicillin-Novocain (12 hs)(12 hs)
Bicillin-1Bicillin-1 (once a week)(once a week)
Bicillin-5Bicillin-5 (once a month)(once a month)
B. For enteral introduction:B. For enteral introduction:
PhenoxymethylpenicillinPhenoxymethylpenicillin (4-6 hs)(4-6 hs)
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7. II. Semisynthetic PenicillinsII. Semisynthetic Penicillins::
A. ForA. For parenteralparenteral andand enteralenteral introduction (introduction (acid-resistantacid-resistant):):
1.1. Penicillinase-resistant:Penicillinase-resistant: 2. Extended spectrum2. Extended spectrum::
OxacillinOxacillin •• AMINOPENICILLINS:AMINOPENICILLINS:
CloxacillinCloxacillin AmoxicillinAmoxicillin
FlucloxacillinFlucloxacillin AmpicillinAmpicillin
MethicillinMethicillin BacampicillinBacampicillin
B. ForB. For parenteralparenteral introductionintroduction::
BroadBroad spectrumspectrum includingincluding
blue pus bacilliblue pus bacilli Pseudomonas aeruginosaPseudomonas aeruginosa::
•• Carboxy penicillinsCarboxy penicillins:: •• UreidopenicillinsUreidopenicillins::
Carbenicillin disodiumCarbenicillin disodium PiperacillinPiperacillin
TicarcillinTicarcillin AzlocillinAzlocillin
MezlocillinMezlocillin
C. For enteral introductionC. For enteral introduction (acid-resistant):(acid-resistant):
Carbenicillin-indanylCarbenicillin-indanyl
Carbenicillin phenylCarbenicillin phenyl
CarfecillinCarfecillin 77

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11. CLINICAL USE of PENICILLINSCLINICAL USE of PENICILLINS
Bacterial MeningitisBacterial Meningitis:: BenzylpenicillinBenzylpenicillin, high doses IV, high doses IV
Bone and Joint InfectionsBone and Joint Infections
(eg with(eg with Staphylococcus aureusStaphylococcus aureus)):: FlucloxacillinFlucloxacillin
Skin and Soft Tissue InfectionsSkin and Soft Tissue Infections
(eg with(eg with Streptococcus pyogenesStreptococcus pyogenes oror S. aureusS. aureus))::
Benzylpenicillin, FlucloxacillinBenzylpenicillin, Flucloxacillin
animal bitesanimal bites:: CoamoxiclavCoamoxiclav
PharyngitisPharyngitis ((S.pyogenesS.pyogenes) -) - PhenoximethylpenicillinPhenoximethylpenicillin
BronchitisBronchitis (mixed infections common) and(mixed infections common) and PneumoniaPneumonia::
AmoxicillinAmoxicillin
GonorrheaGonorrhea:: AmoxicillinAmoxicillin (plus(plus ProbenecidProbenecid))
SyphylisSyphylis:: Procain BenzylpenicillinProcain Benzylpenicillin
EndocarditisEndocarditis (eg with(eg with Streptococcus viridansStreptococcus viridans oror
Enterococcus faecalisEnterococcus faecalis))
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12. Benzylpenicillin-natriumBenzylpenicillin-natrium (vial 500,000 and 1,000,000 UA) -(vial 500,000 and 1,000,000 UA) -
biosynthetical penicillin of narrow spectrum (biosynthetical penicillin of narrow spectrum (GramGram+).+).
It is the drug of choice for infections caused by:It is the drug of choice for infections caused by:
Streptococci, Meningococci, Enterococci,Streptococci, Meningococci, Enterococci,
Penicillin-Susceptible Pneumococci,Penicillin-Susceptible Pneumococci,
non-beta-lactamase-producing Staphylococci,non-beta-lactamase-producing Staphylococci,
Treponema PallidumTreponema Pallidum and many otherand many other SpirochetesSpirochetes,,
Bacillus Antracis, Clostridium SpeciesBacillus Antracis, Clostridium Species,,
ActinomycesActinomyces and other Gr (+) rods,and other Gr (+) rods,
Non-beta-lactamase-producingNon-beta-lactamase-producing Anaerobic organismsAnaerobic organisms
Depending upon the organism, the site, and the severity ofDepending upon the organism, the site, and the severity of
infection, effective doses range betweeninfection, effective doses range between 44 andand 24 mln24 mln UnitsUnits
per day administered IV inper day administered IV in 4-64-6 divided doses.divided doses.
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13. Bicillin-5Bicillin-5 ––
1 part of1 part of benzylpenicillin-Novocainebenzylpenicillin-Novocaine (300,000 UA)(300,000 UA)
4 parts of4 parts of Biccilin-1Biccilin-1 (1,200,000 UA)(1,200,000 UA)
The drug is used as suspension onlyThe drug is used as suspension only IM once 4 weeksIM once 4 weeks
The drug provides high concentrations in the plasmaThe drug provides high concentrations in the plasma
for long period of time (ad 4 weeks).for long period of time (ad 4 weeks).
Infections byInfections by Streptococci, Pneumococci,Streptococci, Pneumococci,
StaphylococciStaphylococci etc.etc.
Bicillin-5 is especially useful for permanentBicillin-5 is especially useful for permanent
(whole-year) prophylaxis of rheumatism relapses.(whole-year) prophylaxis of rheumatism relapses.
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14. AmoxicillinAmoxicillin (tab and caps 250 and 500 mg)(tab and caps 250 and 500 mg)
semisyntheticsemisynthetic bactericidal antibiotic ofbactericidal antibiotic of broad-spectrumbroad-spectrum actionaction
(Gr+ and some Gr(-).(Gr+ and some Gr(-).
The drug adheres to bacterialThe drug adheres to bacterial penicillin-bindingpenicillin-binding proteins, thusproteins, thus
inhibiting bacterial cell synthesis.inhibiting bacterial cell synthesis.
Systemic InfectionsSystemic Infections
Urinary or Respiratory Tract InfectionsUrinary or Respiratory Tract Infections
oral prophylaxis oforal prophylaxis of Bacterial EndocarditisBacterial Endocarditis..
Uncomplicated GonorrheaUncomplicated Gonorrhea (3 g PO as a single dose)(3 g PO as a single dose)
Ulcer of the stomach and duodenumUlcer of the stomach and duodenum associating withassociating with
Helicobacter pyloriHelicobacter pylori infection in combination with base agentsinfection in combination with base agents
(inhibiting secretion and antacids).(inhibiting secretion and antacids).
AdultsAdults:: usually 500 mg (in severe cases 1 g) PO q 8 hours.usually 500 mg (in severe cases 1 g) PO q 8 hours.
Unwanted reactions:Unwanted reactions: Hypersensitivity Reactions, Seizures,Hypersensitivity Reactions, Seizures,
Agranulocytosis, Hemolytic Anemia, Thrombocytopenia,Agranulocytosis, Hemolytic Anemia, Thrombocytopenia,
Eosinophilia, Leukopenia, Interstitial Nephritis, Nephropathy,Eosinophilia, Leukopenia, Interstitial Nephritis, Nephropathy,
EnterocolitisEnterocolitis
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15. CEPHALOSPORINSCEPHALOSPORINS
I GenerationI Generation::
Parenteral cephalosporinsParenteral cephalosporins:: Cefazolin, CefalotinCefazolin, Cefalotin
Enteral (PO) cephalosporinsEnteral (PO) cephalosporins:: CephalexinCephalexin
II GenerationII Generation::
Parenteral cephalosporinsParenteral cephalosporins:: Cefuroxim, CefamandoleCefuroxim, Cefamandole
Enteral cephalosporinsEnteral cephalosporins:: CefaclorCefaclor
III GenerationIII Generation::
Parenteral cephalosporinsParenteral cephalosporins::
Ceftriaxone, Cefotaxime, CeftazidimeCeftriaxone, Cefotaxime, Ceftazidime
Enteral cephalosporinsEnteral cephalosporins:: CefiximCefixim
IV GenerationIV Generation::
Parenteral cephalosporinsParenteral cephalosporins:: Cefepime, CefpiromeCefepime, Cefpirome 1515

16. CeftriaxoneCeftriaxone (vial 0.5 and 1.0) –(vial 0.5 and 1.0) –
a 3d-generation cephalosporin, acts bactericidally bya 3d-generation cephalosporin, acts bactericidally by
adhering to bacterial penicillin-binding proteins, inhibitingadhering to bacterial penicillin-binding proteins, inhibiting
cell wall synthesis.cell wall synthesis.
Ceftriaxon (Ceftriaxon (as a single 250 mg IM) andas a single 250 mg IM) and CefiximCefixim (as a single(as a single
400 mg PO) are 1st line drugs for treatment of400 mg PO) are 1st line drugs for treatment of GonorrheaGonorrhea
IndicationsIndications:: Bacteremia, septicemia, respiratory, bone, joint,Bacteremia, septicemia, respiratory, bone, joint,
urinary, gynecologic, intra-abdominal, and skin infectionsurinary, gynecologic, intra-abdominal, and skin infections
from susceptible organismsfrom susceptible organisms;;
Gonorrhea, gonococcal meningitis, Syphilis,Gonorrhea, gonococcal meningitis, Syphilis,
Lyme disease, Endocarditis.Lyme disease, Endocarditis.
3d-generation cephalosporins3d-generation cephalosporins influence on hemostaticinfluence on hemostatic
properties since they possessproperties since they possess coumarin-like actioncoumarin-like action, may, may
induce bleeding disorders by decreasing level of plasmainduce bleeding disorders by decreasing level of plasma
coagulation factors (II, VII, IX, X)coagulation factors (II, VII, IX, X);; inducinginducing
hypoprothrombinemia. Administration ofhypoprothrombinemia. Administration of Vitamin KVitamin K, 10 mg, 10 mg
twice weekly, can prevent this.twice weekly, can prevent this.
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22. AzithromycinAzithromycin ((SumamedSumamed) tab. 0.5, caps 0.25 g) tab. 0.5, caps 0.25 g
Binds to theBinds to the 50S50S subunit of ribosomes,subunit of ribosomes,
blocking Protein Synthesis.blocking Protein Synthesis.
Active against respiratory infections due toActive against respiratory infections due to
Haemophilus influenzaeHaemophilus influenzae andand Moraxella catarrhalisMoraxella catarrhalis..
Has excellent action againstHas excellent action against Toxoplasma gondiiToxoplasma gondii
It is now preferred therapy forIt is now preferred therapy for
urethritis caused byurethritis caused by Chlamidia TrachomatisChlamidia Trachomatis..
Penetrates into most tissues (except cerebrospinal fluid)Penetrates into most tissues (except cerebrospinal fluid)
withwith TissueTissue >>>> Plasma ConcentrationPlasma Concentration by 10- 100-folds.by 10- 100-folds.
Community-acquiredCommunity-acquired PneumoniaPneumonia can be treated withcan be treated with
AzithromycinAzithromycin given asgiven as 500 mg500 mg loading dose, followed byloading dose, followed by
aa 250 mg250 mg singly daily dose for the next 4 days.singly daily dose for the next 4 days.
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27. Pseudomembranous ColitisPseudomembranous Colitis ––
thethe most serious potentially fatal adverse effectmost serious potentially fatal adverse effect
ofof ClindamycinClindamycin andand LincomycinLincomycin
Caused by overgrowth ofCaused by overgrowth of ClostridiumClostridium difficiledifficile
((superinfection developmentsuperinfection development)) which elaborateswhich elaborates
necrotizing toxinsnecrotizing toxins ..
The patient develops profuse, watery diarrhea,The patient develops profuse, watery diarrhea,
fever, abdominal pain, leukocytosis.fever, abdominal pain, leukocytosis.
C. difficileC. difficile infection is confirmed.infection is confirmed.
Treatment: Oral administration ofTreatment: Oral administration of MetronidazoleMetronidazole
oror VancomycinVancomycin is effectiveis effective
in controlling this serious problem.in controlling this serious problem.
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28. Thank You for Listening!Thank You for Listening!
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