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ANTIBIOTICS
AND THEIR MODE OF
ACTION
1
By
Akhtar Ali
Staff Nurse EICU
2020
Objectives
2
 After the completion of the session the learner
will be able to
 Define antibiotics.
 Understand the structure and function of bacterial
cell.
 Recall some common terminologies.
 Discuss the criteria for selecting an antimicrobial
agent.
continue…
3
 Know the antibiotic spectra.
 Classify antibiotics according to there mode of
actions.
 Define the term pharmacokinetics and
Pharmacodynamics.
Structure of Bacteria
4
Some common terminologies
5
 Antibiotics.
Agent that kill or static the growth of microorganism
without harming the host cell.
 DNA (Deoxyribo Nucleic Acid).
Material which helps in cell division and
transmit the genetical characteristics in the
offspring.
 Cell wall
The outer protective covering of the cell.
Continue….
6
 Bactericidal.
Agents that kill the bacteria.
 Bacteriostatic.
Agents that inhibit the growth or multiplication
of bacteria.
(Mycek JM. Et al.2004)
Continue…………..
7
 Beta lactam Ring
 Beta-lactamase or penicillinase
An enzyme produce by the bacteria which
destroy the beta lactam ring in the chemical
structure of the beta lactam antibiotics.
(Mycek JM. Et al.2004)
Selection of antimicrobial Agent
8
 Empirical therapy prior to organism
identification.
 Identification and sensitivity of the organism.
 The effect on the site of infection.
 Status of the patient.(immune system, Renal and hepatic
dysfunction, poor perfusion, pregnancy, Lactation, Age)
 Safety of the agent.
 Cost of therapy.
(Katzung .GB 2007)
Antibiotic spectra
9
 Narrow spectrum
Agent acting only on a single or limited group of
microorganism
e.g. Isoniazid is active only against
mycobacterium
 Extended spectrum
Antibiotics that are effective against gram positive
organism and also against significant number of
gram negative bacteria
e.g.ampiciilin act against gram positive and some
gram negative bacteria.
Broad spectrum
10
 Drugs such as tetracycline and
chloramphenicol affect a wide variety
of microbial species are referred to as
broad spectrum antibiotics.
(Danish.IM 2000)
Classification of Antimicrobials
11
 Antibacterial
 Antiviral
 Antifungal
 Antiamoebic
 Antimalarial
 Antiprotozoal
(Mycek JM. Et al.2004)
Antibacterial classification
12
Antibacterial classification is based on the mode of
action there are four major classification
A. Cell wall synthesis inhibitor.
B. Metabolism inhibitor.
C. DNA synthesis inhibitor.
D. Protein synthesis
inhibitor.
(Mycek JM. Et al.2004)
Monobactum
Beta lactam
antibiotics
Cephalosporins
Other antibiotics
Penicillins
2nd
generation
Beta lactamase
antibiotics
Inhibitors of cell
wall synthesis
Carbapenums
3rd
generation
1st
generation
4th
generation
Vancomycin
Bacitracin
Imipenum
Meropenum
Aztreonem
Ampicillin
Amoxicilli
n
Piperacilli
n
Methicillin
Oxacillin
Cloxacillin
Cephradine
Cephalexin
Cefadroxil
Cefaclor
Cefuraxime
Cefamandole
Cefoxitin
Cefotaxime
Ceftrixone
Cefoperezone
Ceftazidme
Cefixime
Cefipime
Clavulanic acid
Sulbactum
Tazobactum
13
(Mycek JM. Et al.2004)
A. Cell wall synthesis inhibitor.
14
 Antibiotics that inhibit the formation of cell wall
of bacteria no cell wall no bacteria. They are
further divided in to six groups
1) Penicillin group.
2) Cephalosporin.
3) Carbapenum group. (Beta-lactam
antibiotics)
4) Monobactum.
5) Combination.
6) Others.
1.Penicillin group
15
 Most widely effective antibiotics and are
among the least toxic drugs the major adverse
reaction is hypersensitivity.
Some common penicillin
16
 Ampicillin
 Amoxicillin
 Piperacillin
 Methiciilin
 Oxacillin
 Cloxaciilin
Cephalosporins
17
 Cephalosporins are beta lactam antibiotic that
are closely related both structurally and
functionally to the penicillin.
 Mode of action of Cephalosporins is same as
that of penicillin but they are more resistant to
beta lactamase than penicillins.
(Mycek JM. Et al.2004)
Classification of cephalosporin
18
First generation cephalosporins:
 Display good activity against gram positive organism but
have some activity against gram negative e.g. proteus E
.Coli and klebsilla.
 No effect on pseudomonas.
 Resistant to beta lactamase of staphylococci.
 Indication
 Gram positive infection and UTI.
 Some common first generation cephalosporin.
 Cephradine(velosef) oral,inj
 Cephalexin(Ceporex ,keflex) oral , inj
 Cefadroxil monohydrate(oral).
Second generation
cephalosporins
19
 More effective against gram negative less effective
against gram positive as compare to first
generation.e.gE.Coli,klebsella enterobactur, proteus,
 Indication
 skin or soft tissue infections ,urinary tract infections (UTIs) ,strep throat ,ear infections
,pneumonia
 sinus infections ,meningitis, gonorrhea
 Examples
• Cefaclor
• Cefuraxime
• Cefamandole
Third generation
cephalosporins
20
 Mainly effective against gram negative organisms there
activity against gram positive is very less as compared to first
and second generations.
 Indication
 Serious infections caused by gram negative infection
 Meningitis
 Gonorrhea
 As an empirical therapy of sepsis of unknown origin.
Examples
 Cefotaxime
 Ceftrixone
 Cefoperezon
 Ceftazidme
 Cefixime
Fourth generation
Cephalosporin
21
 It is similar to third generation but is more
resistant to beta lactamase.
 Indication
 Good activity against pseudomonas, S.aureus, S.
pnumoniae and H.influinza.
 Cefipime (Cefstar) Inj.
 Only one antibiotic in fourth generation
3.Carbapenum group
22
 Are synthetic beta lactam antibiotics
 Imipenum and Meropenum are currently
available antibiotics.
 These drugs play a role in empiric therapy
since it is active against pencilliniase
producing gram positive and gram negative
organism, anaerobes and pseudomonas
aerogenosia
4.Monobactum
23
 Cell wall synthesis inhibitor
 Aztreonam is the only available
antibiotic
 Less commonly use
5.Combination
24
 These are the combinations of beta-lactam
and Beta-lactamase inhibitor.
 Beta lactam inhibits the cell wall while the beta
lactamase inhibitor inhibits the enzyme beta
lactamase which destroy the beta lactam ring
thus inhibit the function of beta-lactam.
 Some Common Combinations
 Amoxicillin+Clavulanic acid= Co-Amoxiclav
 Piperacillin+Tazobactum=Tazocin
 Cefoperezone+salbactam=Sulzon
(Mycek JM. Et al.2004)
6.Others
25
 A . Vancomycin
Become increasingly important due to
its effectiveness against multiple drug
resistant organism such as MRSA .
 B . Bacitracin
Active against wide variety of gram
positive organism.
(Mycek JM. Et al.2004)
Monobactum
Beta lactam
antibiotics
Cephalosporins
Other antibiotics
Penicillins
2nd
generation
Beta lactamase
antibiotics
Inhibitors of cell
wall synthesis
Carbapenums
3rd
generation
1st
generation
4th
generation
Vancomycin
Bacitracin
Imipenum
Meropenum
Aztreonam
Ampicillin
Amoxicilli
n
Piperacilli
n
Methiciilin
Oxacillin
Cloxaciilin
Cephradine
Cephalexin
Cefadroxil
Cefaclor
Cefuraxime
Cefamandole
Cefoxitin
Cefotaxime
Ceftrixone
Cefoperezone
Ceftazidme
Cefixime
Cefipime
Clavulanic acid
Sulbactum
Tazobactum
26
B.Metabolism Inhibitors
27
 Trimethropin
 Sulfonamides
 Mode of action
 Folic acid is essential for the formation of bacterial DNA .DNA helps
in cell division
 These antibiotics inhibits the formation of folic acid
 In the absence of folic acid cell cannot grow or divide
 Indication
 Sulfonamides alone are less commonly used there
combination with Trimethropin called Cotrimaxole are
more commonly used.
 Silver Sulfa diazineis used to prevent infection in Burn
Wounds.
(Katzung .GB 2007)
C.DNA synthesis Inhibitors
28
 Mode of action
 Block bacterial DNA synthesis by inhibiting bacterial
(DNA gyrase),an enzyme involved in DNA
replication. They are rapidly bactericidal.
 All fluroquinolones are DNA synthesis
inhibitors.
 Ciprofloxacin
 Ofloxacin
 Norfloxacin
 Levofloxacin
(Katzung .GB 2007)
D. Protein synthesis inhibitors
29
 30 subunits binders
 50 subunits binders
30 sub units of
protein
50 sub units of
protein
30 subunits binders
30
1. Tetracycline.
E.g. Doxycycline
2. Amino glycosides.
 Amikacin sulphate
 Tobramycin sulphate
 Gentamycin
 Streptomycin.
 Neomycin
Inhibit protein synthesis in bacteria exert
inhibitory effects at the ribosome bind specially to
30s ribosomal subunit ,this binding results in the
blocking of the link of transfer RNA to messenger
RNA essential for the transmission of accurate
coding of new protein structure.
50 sub units of
protein
30 sub units of
protein
50 sub units binders
31
1.Chloramphenicol
2.Macrolides
 Erythromycin
 Clarythromycin
 Azithromycin
3. Oxazolidones
Linezolid
 Inhibit protein synthesis in bacteria exert inhibitory
effects at the ribosome bind specially to 50s
ribosomal subunit ,this binding results in the
blocking of the link of transfer RNA to messenger
RNA essential for the transmission of accurate
coding of new protein structure.
Mechanism of Action:
1. Inhibition of Cell Wall
Synthesis
2. Disruption of DNA
synthesis.
3. Inhibition of Protein
Synthesis
4. Interference with Metabolic
Processes
32
Pharmacokinetics
33
How the Body acts on a drug
 Absorption
 Distribution
 Metabolism
 Elimination
(Mycek JM. Et al.2004)
Absorption
34
 The movement of drug From the site
of administration to the systemic
circulation.
 For Oral=First pass effect(liver)
 For I/v = Zero pass effect
 Bioavailability
 Concentration of drug in systemic circulation that
is available for action
Distribution
35
 There are many compartments in the body
where drug is distributed.
 Brain
 Lungs
 Liver
 Heart
 kidneys
Metabolism
36
Prodrug (inactive) Active Drug
Liver Action
Metabolize Inactive(liver)
Active Water soluble
Elimination
Elimination
37
 Kidneys
 Liver
 Lungs
 Skin
 Eyes
 saliva
Pharmacodynamics
38
How the drugs act on the body.
 Indication
 Contraindication
 Adverse effect
 Toxic effect
 Drug receptor interaction
 Tolerance
 Potency
(Mycek JM. Et al.2004)
References
39
 Mycek JM,Harvey AR,Champe CP(2009) illustrated
pharmacology 6th edition. Lippincott William and Wilkins.
 Katzung GB (2007) Basic and clinical pharmacology 10th
edition. McGraw hill and companies.
 Danish IM (2000) Short text book of clinical pharmacology 3rd
edition. Danish3939 medical publisher.
 Larch AM (2006) Focus on Nursing Pharmacology, 3rd
Edition. Lippincott Williams & Wilkins
 Rang et al (2003) Pharmacology, 5th Edition. Churchill
Livingstone
 Lilley et al (2005) Pharmacology and the Nursing Process, 4th
Edition. Mosby
 Dorland's pocket medical dictionary 27th edition.
40
41

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Antibiotics MOA 2020.pptx

  • 1. ANTIBIOTICS AND THEIR MODE OF ACTION 1 By Akhtar Ali Staff Nurse EICU 2020
  • 2. Objectives 2  After the completion of the session the learner will be able to  Define antibiotics.  Understand the structure and function of bacterial cell.  Recall some common terminologies.  Discuss the criteria for selecting an antimicrobial agent.
  • 3. continue… 3  Know the antibiotic spectra.  Classify antibiotics according to there mode of actions.  Define the term pharmacokinetics and Pharmacodynamics.
  • 5. Some common terminologies 5  Antibiotics. Agent that kill or static the growth of microorganism without harming the host cell.  DNA (Deoxyribo Nucleic Acid). Material which helps in cell division and transmit the genetical characteristics in the offspring.  Cell wall The outer protective covering of the cell.
  • 6. Continue…. 6  Bactericidal. Agents that kill the bacteria.  Bacteriostatic. Agents that inhibit the growth or multiplication of bacteria. (Mycek JM. Et al.2004)
  • 7. Continue………….. 7  Beta lactam Ring  Beta-lactamase or penicillinase An enzyme produce by the bacteria which destroy the beta lactam ring in the chemical structure of the beta lactam antibiotics. (Mycek JM. Et al.2004)
  • 8. Selection of antimicrobial Agent 8  Empirical therapy prior to organism identification.  Identification and sensitivity of the organism.  The effect on the site of infection.  Status of the patient.(immune system, Renal and hepatic dysfunction, poor perfusion, pregnancy, Lactation, Age)  Safety of the agent.  Cost of therapy. (Katzung .GB 2007)
  • 9. Antibiotic spectra 9  Narrow spectrum Agent acting only on a single or limited group of microorganism e.g. Isoniazid is active only against mycobacterium  Extended spectrum Antibiotics that are effective against gram positive organism and also against significant number of gram negative bacteria e.g.ampiciilin act against gram positive and some gram negative bacteria.
  • 10. Broad spectrum 10  Drugs such as tetracycline and chloramphenicol affect a wide variety of microbial species are referred to as broad spectrum antibiotics. (Danish.IM 2000)
  • 11. Classification of Antimicrobials 11  Antibacterial  Antiviral  Antifungal  Antiamoebic  Antimalarial  Antiprotozoal (Mycek JM. Et al.2004)
  • 12. Antibacterial classification 12 Antibacterial classification is based on the mode of action there are four major classification A. Cell wall synthesis inhibitor. B. Metabolism inhibitor. C. DNA synthesis inhibitor. D. Protein synthesis inhibitor. (Mycek JM. Et al.2004)
  • 13. Monobactum Beta lactam antibiotics Cephalosporins Other antibiotics Penicillins 2nd generation Beta lactamase antibiotics Inhibitors of cell wall synthesis Carbapenums 3rd generation 1st generation 4th generation Vancomycin Bacitracin Imipenum Meropenum Aztreonem Ampicillin Amoxicilli n Piperacilli n Methicillin Oxacillin Cloxacillin Cephradine Cephalexin Cefadroxil Cefaclor Cefuraxime Cefamandole Cefoxitin Cefotaxime Ceftrixone Cefoperezone Ceftazidme Cefixime Cefipime Clavulanic acid Sulbactum Tazobactum 13 (Mycek JM. Et al.2004)
  • 14. A. Cell wall synthesis inhibitor. 14  Antibiotics that inhibit the formation of cell wall of bacteria no cell wall no bacteria. They are further divided in to six groups 1) Penicillin group. 2) Cephalosporin. 3) Carbapenum group. (Beta-lactam antibiotics) 4) Monobactum. 5) Combination. 6) Others.
  • 15. 1.Penicillin group 15  Most widely effective antibiotics and are among the least toxic drugs the major adverse reaction is hypersensitivity.
  • 16. Some common penicillin 16  Ampicillin  Amoxicillin  Piperacillin  Methiciilin  Oxacillin  Cloxaciilin
  • 17. Cephalosporins 17  Cephalosporins are beta lactam antibiotic that are closely related both structurally and functionally to the penicillin.  Mode of action of Cephalosporins is same as that of penicillin but they are more resistant to beta lactamase than penicillins. (Mycek JM. Et al.2004)
  • 18. Classification of cephalosporin 18 First generation cephalosporins:  Display good activity against gram positive organism but have some activity against gram negative e.g. proteus E .Coli and klebsilla.  No effect on pseudomonas.  Resistant to beta lactamase of staphylococci.  Indication  Gram positive infection and UTI.  Some common first generation cephalosporin.  Cephradine(velosef) oral,inj  Cephalexin(Ceporex ,keflex) oral , inj  Cefadroxil monohydrate(oral).
  • 19. Second generation cephalosporins 19  More effective against gram negative less effective against gram positive as compare to first generation.e.gE.Coli,klebsella enterobactur, proteus,  Indication  skin or soft tissue infections ,urinary tract infections (UTIs) ,strep throat ,ear infections ,pneumonia  sinus infections ,meningitis, gonorrhea  Examples • Cefaclor • Cefuraxime • Cefamandole
  • 20. Third generation cephalosporins 20  Mainly effective against gram negative organisms there activity against gram positive is very less as compared to first and second generations.  Indication  Serious infections caused by gram negative infection  Meningitis  Gonorrhea  As an empirical therapy of sepsis of unknown origin. Examples  Cefotaxime  Ceftrixone  Cefoperezon  Ceftazidme  Cefixime
  • 21. Fourth generation Cephalosporin 21  It is similar to third generation but is more resistant to beta lactamase.  Indication  Good activity against pseudomonas, S.aureus, S. pnumoniae and H.influinza.  Cefipime (Cefstar) Inj.  Only one antibiotic in fourth generation
  • 22. 3.Carbapenum group 22  Are synthetic beta lactam antibiotics  Imipenum and Meropenum are currently available antibiotics.  These drugs play a role in empiric therapy since it is active against pencilliniase producing gram positive and gram negative organism, anaerobes and pseudomonas aerogenosia
  • 23. 4.Monobactum 23  Cell wall synthesis inhibitor  Aztreonam is the only available antibiotic  Less commonly use
  • 24. 5.Combination 24  These are the combinations of beta-lactam and Beta-lactamase inhibitor.  Beta lactam inhibits the cell wall while the beta lactamase inhibitor inhibits the enzyme beta lactamase which destroy the beta lactam ring thus inhibit the function of beta-lactam.  Some Common Combinations  Amoxicillin+Clavulanic acid= Co-Amoxiclav  Piperacillin+Tazobactum=Tazocin  Cefoperezone+salbactam=Sulzon (Mycek JM. Et al.2004)
  • 25. 6.Others 25  A . Vancomycin Become increasingly important due to its effectiveness against multiple drug resistant organism such as MRSA .  B . Bacitracin Active against wide variety of gram positive organism. (Mycek JM. Et al.2004)
  • 26. Monobactum Beta lactam antibiotics Cephalosporins Other antibiotics Penicillins 2nd generation Beta lactamase antibiotics Inhibitors of cell wall synthesis Carbapenums 3rd generation 1st generation 4th generation Vancomycin Bacitracin Imipenum Meropenum Aztreonam Ampicillin Amoxicilli n Piperacilli n Methiciilin Oxacillin Cloxaciilin Cephradine Cephalexin Cefadroxil Cefaclor Cefuraxime Cefamandole Cefoxitin Cefotaxime Ceftrixone Cefoperezone Ceftazidme Cefixime Cefipime Clavulanic acid Sulbactum Tazobactum 26
  • 27. B.Metabolism Inhibitors 27  Trimethropin  Sulfonamides  Mode of action  Folic acid is essential for the formation of bacterial DNA .DNA helps in cell division  These antibiotics inhibits the formation of folic acid  In the absence of folic acid cell cannot grow or divide  Indication  Sulfonamides alone are less commonly used there combination with Trimethropin called Cotrimaxole are more commonly used.  Silver Sulfa diazineis used to prevent infection in Burn Wounds. (Katzung .GB 2007)
  • 28. C.DNA synthesis Inhibitors 28  Mode of action  Block bacterial DNA synthesis by inhibiting bacterial (DNA gyrase),an enzyme involved in DNA replication. They are rapidly bactericidal.  All fluroquinolones are DNA synthesis inhibitors.  Ciprofloxacin  Ofloxacin  Norfloxacin  Levofloxacin (Katzung .GB 2007)
  • 29. D. Protein synthesis inhibitors 29  30 subunits binders  50 subunits binders 30 sub units of protein 50 sub units of protein
  • 30. 30 subunits binders 30 1. Tetracycline. E.g. Doxycycline 2. Amino glycosides.  Amikacin sulphate  Tobramycin sulphate  Gentamycin  Streptomycin.  Neomycin Inhibit protein synthesis in bacteria exert inhibitory effects at the ribosome bind specially to 30s ribosomal subunit ,this binding results in the blocking of the link of transfer RNA to messenger RNA essential for the transmission of accurate coding of new protein structure. 50 sub units of protein 30 sub units of protein
  • 31. 50 sub units binders 31 1.Chloramphenicol 2.Macrolides  Erythromycin  Clarythromycin  Azithromycin 3. Oxazolidones Linezolid  Inhibit protein synthesis in bacteria exert inhibitory effects at the ribosome bind specially to 50s ribosomal subunit ,this binding results in the blocking of the link of transfer RNA to messenger RNA essential for the transmission of accurate coding of new protein structure.
  • 32. Mechanism of Action: 1. Inhibition of Cell Wall Synthesis 2. Disruption of DNA synthesis. 3. Inhibition of Protein Synthesis 4. Interference with Metabolic Processes 32
  • 33. Pharmacokinetics 33 How the Body acts on a drug  Absorption  Distribution  Metabolism  Elimination (Mycek JM. Et al.2004)
  • 34. Absorption 34  The movement of drug From the site of administration to the systemic circulation.  For Oral=First pass effect(liver)  For I/v = Zero pass effect  Bioavailability  Concentration of drug in systemic circulation that is available for action
  • 35. Distribution 35  There are many compartments in the body where drug is distributed.  Brain  Lungs  Liver  Heart  kidneys
  • 36. Metabolism 36 Prodrug (inactive) Active Drug Liver Action Metabolize Inactive(liver) Active Water soluble Elimination
  • 37. Elimination 37  Kidneys  Liver  Lungs  Skin  Eyes  saliva
  • 38. Pharmacodynamics 38 How the drugs act on the body.  Indication  Contraindication  Adverse effect  Toxic effect  Drug receptor interaction  Tolerance  Potency (Mycek JM. Et al.2004)
  • 39. References 39  Mycek JM,Harvey AR,Champe CP(2009) illustrated pharmacology 6th edition. Lippincott William and Wilkins.  Katzung GB (2007) Basic and clinical pharmacology 10th edition. McGraw hill and companies.  Danish IM (2000) Short text book of clinical pharmacology 3rd edition. Danish3939 medical publisher.  Larch AM (2006) Focus on Nursing Pharmacology, 3rd Edition. Lippincott Williams & Wilkins  Rang et al (2003) Pharmacology, 5th Edition. Churchill Livingstone  Lilley et al (2005) Pharmacology and the Nursing Process, 4th Edition. Mosby  Dorland's pocket medical dictionary 27th edition.
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