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Antibiotics

From Prof. Dr. Hussien Khairy
          Lectures
             By
     Mohamad Alasmar
Oral                             The Prototype
Penicillin V                     Crystalline Penicillin
Long Acting                       ● Benzyle Penicillin
                                  ● Penicillin G
Benzathine Penicillin            Reversed Spectrum
 ● 2-4 weeks
 ● Ttt of lymphoedema
                                 Selexid
Broad Spectrum                   In UTI
                                 AntiPsodomonal
Amoxicillin +clavulanic Acid =
Augmentin                        Carbinicllin
Ampicillin +Sulbactam =          Ticaracillin +clavulanic Acid =
Unasyn                           Timentin
Anti Beta Lactamase
                                 Pipracillin
Flucxacillin
Flucluxacillin
Spectrum                       Side Effects

    G +ve      Spirocheats
                               Very Safe
                                ● So used in long term Prophylaxis
                                ● Allergy
  Anaerobs        NOT
                                ● Enceph;opathy
                  G –ve         ● Electrolytes load
                ● E Coli       Route
                ● Shigella
                ● Salmonella   Parentral
                ● Psodomona
                  s
                               Excretion
Mechanism of Action            Kidney
Cell Wall                      By Tubular Secretion

Cidal
First Generation
                   Second Generation
Cephradine
                   Mefoxine
Velosef ®          Effective against anaerobes

Third Generation
                   Forth Generation
Cefoprazone        Maxipime®
Cefobid®
Cefotoxime
Meningitis

Ceftriaxone
Rocephen®
Long half life
Side Effects
Spectrum
                              Safe
    G –ve          G+ve        ● Allergy may present
                              Share Pinicillins in allergy in 10% of
     Some against anaerobes   cases
                               ● Hypoprothrombinaemia
            Mefoxine          Route
                              Oral • Parentral
                              1st • 2nd • 3rd • 4th
Mechanism of Action
                               1. Resist beta lactamase
Cell wall                      2. Parenteral
                               3. G –ve effective
Cidal                          4. Broader spectrum
Like Pinicillins              Excretion
                              Kidney
                              By Tubular Secretion
Imipenim +                      Aztreonam
Cilastitin                      Azactam ®
Enzyme Inhibitor                ● Very narrow spectrum
Inhibit distruction by Kidney   ● G –ve onle
                                ● Parentral
= Tienam ®
 ● The broadest spectrum ever
 ● Parentral
Clavulanic Acid
+ Amoxicillin •
Augmantin
+Ticaracillin •
Tementin

Sulbactam
+ Cephoperazon •
Sulperazon
+Ampicillin •
Unasyn

Tazobactam
Erythromycin
 ● Like Pinicillin              Azithromycin
 ● Used in Pinicillin Allergy
 ● Bowel Preparation            Zithromax ®
                                Long Half life
                                1 tablet daily
                                Used in chest infection
Clarythromycin                  Haemophilus influenza
AntiHelicobacter pylori
Spectrum                       Side Effects

                    NOT G-ve   GIT upsets
   G +ve
    Anaerobes                  Route
  ● Bowel Preparation          Oral
  ● Like Pinicillin


                               Excretion
Mechanism of Action
                               Biliary
Ptn Synthesis
                               Hepatic
Static •Cidal
According to the dose
Garamycin
                     ● Very potent
Tobramycin           ● Very toxic
                     ● Very cheep
Nebcin ®
The safest          Streptomycin
                    In TB
Amikacin
Amikin ®            Kanamycin
                     ● Very toxic
Broadest Spectrum
                     ● Very old


                    Neomycin
                     ● Bowel Preparation with
                       Metronidazol
Side Effects
Spectrum
                               Nephrotoxic
                       G +ve
   G –ve                       Ototoxicity
                               Neurotoxcity
      NOT effective against
          anaerobes            Route
                               Parentral
                               Not absorbed by bowel
Mechanism of Action
Ptn Synthesis                  Excretion

Cidal                          Kidney
Should enter the cell          By GF
Needs energy = O2              Not by excretion
So can not act on anaerobes    So lower the dose in cases with renal
                               impairment
Ceprofloxacin         Levofloxacin
Drug of Choice in
 ● Entric Infection
                      Tavanic ®
 ● UTI                ● Pneumococci
 ● Prostatitis        ● G +ve


Ofloxacin
Tarvid ®
 ● UTI
 ● Typhoid
Spectrum                        Side Effects

                       G +ve
                                Safe
   G –ve                        Musculoskeletal Side Effects
   ● UTI                         ● Young Age • Arthropathy
   ● Enteric                     ● Old Age • Tendonitis
     Infection                  Not recommended in young age
 Better than                    Route
 AminoGlycosid
 Because its less
                                Oral & Parentral
 side efects
Mechanism of Action
                                Excretion
DNA Synthesis
                                Kidney
Gyrase Inhibitor                By GF
Topoisimerase Inhibitor
Relax supercoils of DNA to be
duplicated
Spectrum
Side Effects
AntiBiotic Associated
colitis =
Psudomembranous
colitis
By Cl. Difficil         Route
ttt
   ● Vencomycin         Parentral
   ● Metronidazol
Mechanism of Action     Excretion
Ptn Synthesis           Kidney
Route                       Spectrum
Oral                        ●Amebiasis
IV expensive
Suppositories               ●Trichomonas
Excretion                   ●Giardia
Kidney                      ●Anaerobs
Side Effects
                            ●Hilicobacter
Metallic taste
Neurotoxic                   pylori
Nausea
Alcohol • Disulfuram like
Route
                      MRSA
Oral                  Methicillin resistent staph. Aureus
                      Produced By Fluxacillin &
Mechanism of Action   Flucluxacillin
Cell Wall Synthesis   Pseudomembranous
                      colitis
                      Produced By Clindamycin
                      Cl. Difficile
                      Endocarditis
● Metronidazole
● Penicillins
● Erythromycin
● Tienam
● Clindamycin
● Mefoxine

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Antibiotics -simplified-

  • 1. Antibiotics From Prof. Dr. Hussien Khairy Lectures By Mohamad Alasmar
  • 2. Oral The Prototype Penicillin V Crystalline Penicillin Long Acting ● Benzyle Penicillin ● Penicillin G Benzathine Penicillin Reversed Spectrum ● 2-4 weeks ● Ttt of lymphoedema Selexid Broad Spectrum In UTI AntiPsodomonal Amoxicillin +clavulanic Acid = Augmentin Carbinicllin Ampicillin +Sulbactam = Ticaracillin +clavulanic Acid = Unasyn Timentin Anti Beta Lactamase Pipracillin Flucxacillin Flucluxacillin
  • 3. Spectrum Side Effects G +ve Spirocheats Very Safe ● So used in long term Prophylaxis ● Allergy Anaerobs NOT ● Enceph;opathy G –ve ● Electrolytes load ● E Coli Route ● Shigella ● Salmonella Parentral ● Psodomona s Excretion Mechanism of Action Kidney Cell Wall By Tubular Secretion Cidal
  • 4. First Generation Second Generation Cephradine Mefoxine Velosef ® Effective against anaerobes Third Generation Forth Generation Cefoprazone Maxipime® Cefobid® Cefotoxime Meningitis Ceftriaxone Rocephen® Long half life
  • 5. Side Effects Spectrum Safe G –ve G+ve ● Allergy may present Share Pinicillins in allergy in 10% of Some against anaerobes cases ● Hypoprothrombinaemia Mefoxine Route Oral • Parentral 1st • 2nd • 3rd • 4th Mechanism of Action 1. Resist beta lactamase Cell wall 2. Parenteral 3. G –ve effective Cidal 4. Broader spectrum Like Pinicillins Excretion Kidney By Tubular Secretion
  • 6. Imipenim + Aztreonam Cilastitin Azactam ® Enzyme Inhibitor ● Very narrow spectrum Inhibit distruction by Kidney ● G –ve onle ● Parentral = Tienam ® ● The broadest spectrum ever ● Parentral
  • 7. Clavulanic Acid + Amoxicillin • Augmantin +Ticaracillin • Tementin Sulbactam + Cephoperazon • Sulperazon +Ampicillin • Unasyn Tazobactam
  • 8. Erythromycin ● Like Pinicillin Azithromycin ● Used in Pinicillin Allergy ● Bowel Preparation Zithromax ® Long Half life 1 tablet daily Used in chest infection Clarythromycin Haemophilus influenza AntiHelicobacter pylori
  • 9. Spectrum Side Effects NOT G-ve GIT upsets G +ve Anaerobes Route ● Bowel Preparation Oral ● Like Pinicillin Excretion Mechanism of Action Biliary Ptn Synthesis Hepatic Static •Cidal According to the dose
  • 10. Garamycin ● Very potent Tobramycin ● Very toxic ● Very cheep Nebcin ® The safest Streptomycin In TB Amikacin Amikin ® Kanamycin ● Very toxic Broadest Spectrum ● Very old Neomycin ● Bowel Preparation with Metronidazol
  • 11. Side Effects Spectrum Nephrotoxic G +ve G –ve Ototoxicity Neurotoxcity NOT effective against anaerobes Route Parentral Not absorbed by bowel Mechanism of Action Ptn Synthesis Excretion Cidal Kidney Should enter the cell By GF Needs energy = O2 Not by excretion So can not act on anaerobes So lower the dose in cases with renal impairment
  • 12. Ceprofloxacin Levofloxacin Drug of Choice in ● Entric Infection Tavanic ® ● UTI ● Pneumococci ● Prostatitis ● G +ve Ofloxacin Tarvid ® ● UTI ● Typhoid
  • 13. Spectrum Side Effects G +ve Safe G –ve Musculoskeletal Side Effects ● UTI ● Young Age • Arthropathy ● Enteric ● Old Age • Tendonitis Infection Not recommended in young age Better than Route AminoGlycosid Because its less Oral & Parentral side efects Mechanism of Action Excretion DNA Synthesis Kidney Gyrase Inhibitor By GF Topoisimerase Inhibitor Relax supercoils of DNA to be duplicated
  • 14. Spectrum Side Effects AntiBiotic Associated colitis = Psudomembranous colitis By Cl. Difficil Route ttt ● Vencomycin Parentral ● Metronidazol Mechanism of Action Excretion Ptn Synthesis Kidney
  • 15. Route Spectrum Oral ●Amebiasis IV expensive Suppositories ●Trichomonas Excretion ●Giardia Kidney ●Anaerobs Side Effects ●Hilicobacter Metallic taste Neurotoxic pylori Nausea Alcohol • Disulfuram like
  • 16. Route MRSA Oral Methicillin resistent staph. Aureus Produced By Fluxacillin & Mechanism of Action Flucluxacillin Cell Wall Synthesis Pseudomembranous colitis Produced By Clindamycin Cl. Difficile Endocarditis
  • 17. ● Metronidazole ● Penicillins ● Erythromycin ● Tienam ● Clindamycin ● Mefoxine