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BETA
LACTAM
ANTIBIOTICS
Antibiotic
An antibiotic is an agent that either kills or
inhibits the growth of a micro organism.
Tetracyclines
Spectinomycins
Sulphonamides
Macrolides
Chloramphenicol
Trimethoprim
Penicillins
Cephalosporins
Monobactams
Carbapenems
Fluoroquinolones
Glycopeptides
CLASSIFICATION OF
ANTIBIOTICS
(Based on mode of action)
BACTERIOSTATIC
ANTIBIOTICS
BACTERICIDAL
ANTIBIOTICS
CLASSIFICATION OF
ANTIBIOTICS
(Based on structural similarities)
Beta Lactams
Penicillins
Cephalosporins
Monobactams
Carbapenems
Fluoroquinolones
Macrolides
Tetracyclines
Aminoglycosides
Antibiotics: Mode of action
Inhibitors of DNA synthesis
Inhibitors of bacterial protein synthesis
Inhibitors of bacterial cell wall synthesis
Interference with metabolism
Impairment of nucleic acids
Bacterial cell structure
Gram positive more susceptible than gram negative
 Peptidoglycan layer is composed of alternating units of N-acetyl
glucosamine(NAGA) and N-acetyl muramic acid(NAMA)
 NAGA and NAMA are crosslinked by a class of transpeptidases
known as penicillin binding proteins (PBPs)
 Interfering with this cross linking disrupts the cell wall synthesis.
 POINT TO REMEMBER :
Beta Lactam antibiotics
• Contains a beta lactam ring in their molecular structure.
• Nitrogen is attached to the beta carbon relative to the carbonyl ring and
hence the name.
Classification of beta lactam antibiotics
 Penicillins
 Cephalosporins
 Carbapenems
 Monobactams
 B lactamase inhibitors
Mechanism of action
 The beta lactam antibiotics bind to Penicillin Binding
proteins(PBPs). ( transpeptidase , other enzymes and related
proteins )
 PBPs are unable to crosslink peptidoglycan chains.
 Bacteria is unable to synthesize a stable cell wall.
 Hence, the bacteria is lysed.
Penicillins
 Sir Alexander Fleming discovered penicillin from penicillium
notatum
 Now obtained from Penicillium chrysogenum for therapeutic
use
Classification of penicillins
A)NATURAL
1. Regular - Penicillin G (Benzyl penicillin)
2. Repository – Procaine penicillin
Benzathine penicillin
B) SEMISYNTHETIC
1. Acid resistant – Penicillin V
2. Penicillinase resistant – cloxacillin, methicillin, dicloxacillin, nafcillin
3. Aminopenicillins – ampicillin, bacampicillin, amoxicillin
4. Antipseudomonal –
i) Carboxypenicillins – carbenicillin, ticarcillin
ii) Ureidopenicillins – mezlocillin, piperacillin
3 & 4 are EXTENDED SPECTRUM PENICILLINS
Natural penicillins
 Penicillin G (Benzyl penicillin), Procaine penicillin, Benzathine penicillin
 Acid labile – given parenterally (IM/IV)
Uses
 Pneumococcal infections
 Streptococcal infections
 Meningococcal infections
 Staphylococcal infections
 Syphilis
 Diphtheria
 Actinomycosis
 Tetanus & gas gangrene
 Prophylaxis uses : Rheumatic fever, Gonorrhoea, Syphilis
Adverse effects
 Hypersensitivity – skin rash, urticaria, pruritus, bronchospasm, fever,
anaphylaxis
 hence intradermal skin injection test dose is a must before administration.
 Other than the rare event of anaphylaxis penicillins are one of the safest
antibiotics
 Local pain at injection site
 CNS : confusion,convulsions,coma
 Suprainfections
ANAPHYLATIC SHOCK TREATMENT
 DRUG OF CHOICE : )
 dose : 0.2 - 0.5 ml of 1: 1000 solution S.C ( if mild )
 50 - 100 ug of 1: 10,000 solution I.V ( if severe )
 corticosteroid : hydrocortisone
 others : antihistaminic , iv fluids , oxygen therapy , dopamine.
Semisynthetic penicillins
1.Acid resistant – Penicillin V
Use : Streptococcal pharyngitis, sinusitis and trench mouth.
2.Penicillinase resistant – cloxacillin, methicillin, oxacillin, nafcillin
Use : Staphylococcal infections ,treatment of human bites .
Aminopenicillins – ampicillin, bacampicillin, amoxicillin
Use :
1. Respiratory tract infections- bronchitis, sinusitis, otitis media
2. Urinary tract infections
3. Meningitis
4. Typhoid
5. Septicaemia
6. Bacillary dysentery
7. Bacillary endocarditis
Amoxicillin vs Ampicillin
 Amoxicillin is better absorbed orally
 Food does not interfere with its absorption
 Attains high blood levels after oral administration
 Diarrhoea is rare
 Longer acting than ampicillin (given thrice daily)
 Does not reduce the effectiveness of oral contraceptives.
Antipseudomonal penicillins
i) Carboxypenicillins – carbenicillin, ticarcillin
ii) Ureidopenicillins – azlocillin, mezlocillin, piperacillin
Use:
Pseudomonas, Klebsiella, Proteus infections
Adverse effects: Carbenicillin causes edema and CCF, bleeding
Beta lactamase inhibitors
 Beta lactamases are enzymes produced by bacteria which open up
the beta lactam ring and inactivates the beta lactam antibiotics.
 Beta lactamase inhibitors bind to and inactivates beta lactamases
thereby preventing destruction of beta lactam antibiotics.
 Clavulanic acid
 Sulbactam
 Tazobactam
Combinations
 Clavulanic acid + amoxicillin – oral/IV
 Clavulanic acid + ticarcillin – IV
 Sulbactam + ampicillin – IV
 Tazobactam + piperacillin – IV
Use:
Cellulitis, diabetic foot, skin & soft tissue infections, respiratory &
genitourinary infections, mixed aerobic-anaerobic & nosocomial
infections
Cephalosporins
 Semisynthetic antibiotics
 Wider spectrum of activity
 Mechanism of action similar to penicillins i.e. inhibits bacterial
cell wall synthesis
 Bactericidal
Classification
 First generation - effective against gram positive organisms
 Second generation - more active against gram negative
organisms
 Third generation - effective against gram negative organisms
and anaerobes
 Fourth generation - gram positive and gram negative
organisms
 Fifth generation – MRSA and gram negative organisms
 first and second generation cephalosporins are used as
substitutes to penicillins in those who have mild allergic reaction to
penicillin
 NOT IN THOSE WITH SEVERE REACTIONS LIKE
ANAPHYLAXIS/ ANGIOEDEMA .
 Used as a first line empirical therapy along with aminoglycosides
in treatment of bacteremia / septicemia.
 Cefoxitin , cefotetan ( both 2 nd generation )are used in anaerobic
infections.
CEFTRIAXONE : THIRD GENERATION
 ITS a third generation cephalosporin
 highly resistant to beta lactamases.
 good activity against gram positive and negative organisms,
moderate against psuedomonas .
 has the longest half life amongst beta lactam antibioitics ( 8 hrs )
 enters csf when meninges are inflammed , hence used in treatment
of meningitis .
 other uses : complicated UTI ,abdominal sepsis, chancroid
FOURTH GENERATION
 Similar to third generation but more resistant to beta
lactamases .
 active against enterobacteriacea ( gram negative ) and
psuedomonas resistant to group 3
 examples cefepime , cefpirome
 given parenterally .
Uses
 Gram negative infections- urinary, respiratory and soft tissue
infections
 Surgical prophylaxis
 Gonorrhoea
 Meningitis
 Mixed aerobic-anaerobic infections
 Typhoid
 Nosocomial infections
Adverse effects
 Hypersensitivity reactions-skin rash, fever, serum sickness,
anaphylaxis
 Nephrotoxicity
 Diarrhoea
 Bleeding
 Low WBC count
 Pain at injection site
Carbapenems :
imipenem, meropenem, ertapenem, doripenem, faropenem
 Spectrum : gram positive, gram negative and anaerobic
organisms.
 Mechanism of action: inhibits bacterial cell wall synthesis
 Uses : UTI, respiratory, skin, bone, soft tissue, intra abdominal
and gynecological infections
 only FAROPENEM IS ORALLY ACTIVE , hence can be given
orally . rest are given IV parenterally.
IMIPENEM
 BACTERICIDAL
 broad spectrum beta lactam antibiotic
 effective against gram positive , enterobacteriacea , psuedomonas
, anaerobes ( like clostridia difficile).
 rapidly hydrolysed by enzyme dehydropeptidase in renal tubules.
 hence combined with cilastin that reversibly blocks this enzyme
and protects imipenem .
 not absorbed from GIT , given parenterally .
Monobactam:
aztreonam
 Single beta lactam ring
 Effective against gram negative organisms but not against gram
positive and anaerobes.
 spectrum similar to aminoglycosides,hence used as a reserve drug in
treating gram -ve infections in those whom aminoglycosides are
contraindicated .
 MoA : inhibits bacterial cell wall synthesis ( bactericidal )
 Given parenterally
 Uses : nosocomial pseudomonas infections and other gram negative
infections
ANTIPSEUDOMONAL ANTIBIOTICS
Pneumonic : BLAQ Pseudomonas
 Beta Lactam antibiotics :
 Penicillins : i) Carboxypenicillins – carbenicillin, ticarcillin
ii) Ureidopenicillins – azlocillin, mezlocillin, piperacillin
 Cephalosporins : Ceftazidime, cefoperazone, cefepime, cefpirome
 Carbapenem : imipenem, meropenem, doripenem
 Monobactam : aztreonam
 Aminoglycosides
 Quinolones
 Polypeptides
THANK YOU

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Beta lactam nursing AHS.pptx

  • 2. Antibiotic An antibiotic is an agent that either kills or inhibits the growth of a micro organism.
  • 4. CLASSIFICATION OF ANTIBIOTICS (Based on structural similarities) Beta Lactams Penicillins Cephalosporins Monobactams Carbapenems Fluoroquinolones Macrolides Tetracyclines Aminoglycosides
  • 5. Antibiotics: Mode of action Inhibitors of DNA synthesis Inhibitors of bacterial protein synthesis Inhibitors of bacterial cell wall synthesis Interference with metabolism Impairment of nucleic acids
  • 6. Bacterial cell structure Gram positive more susceptible than gram negative
  • 7.  Peptidoglycan layer is composed of alternating units of N-acetyl glucosamine(NAGA) and N-acetyl muramic acid(NAMA)  NAGA and NAMA are crosslinked by a class of transpeptidases known as penicillin binding proteins (PBPs)  Interfering with this cross linking disrupts the cell wall synthesis.  POINT TO REMEMBER :
  • 8. Beta Lactam antibiotics • Contains a beta lactam ring in their molecular structure. • Nitrogen is attached to the beta carbon relative to the carbonyl ring and hence the name.
  • 9. Classification of beta lactam antibiotics  Penicillins  Cephalosporins  Carbapenems  Monobactams  B lactamase inhibitors
  • 10. Mechanism of action  The beta lactam antibiotics bind to Penicillin Binding proteins(PBPs). ( transpeptidase , other enzymes and related proteins )  PBPs are unable to crosslink peptidoglycan chains.  Bacteria is unable to synthesize a stable cell wall.  Hence, the bacteria is lysed.
  • 11. Penicillins  Sir Alexander Fleming discovered penicillin from penicillium notatum  Now obtained from Penicillium chrysogenum for therapeutic use
  • 12. Classification of penicillins A)NATURAL 1. Regular - Penicillin G (Benzyl penicillin) 2. Repository – Procaine penicillin Benzathine penicillin B) SEMISYNTHETIC 1. Acid resistant – Penicillin V 2. Penicillinase resistant – cloxacillin, methicillin, dicloxacillin, nafcillin 3. Aminopenicillins – ampicillin, bacampicillin, amoxicillin 4. Antipseudomonal – i) Carboxypenicillins – carbenicillin, ticarcillin ii) Ureidopenicillins – mezlocillin, piperacillin 3 & 4 are EXTENDED SPECTRUM PENICILLINS
  • 13. Natural penicillins  Penicillin G (Benzyl penicillin), Procaine penicillin, Benzathine penicillin  Acid labile – given parenterally (IM/IV)
  • 14. Uses  Pneumococcal infections  Streptococcal infections  Meningococcal infections  Staphylococcal infections  Syphilis  Diphtheria  Actinomycosis  Tetanus & gas gangrene  Prophylaxis uses : Rheumatic fever, Gonorrhoea, Syphilis
  • 15. Adverse effects  Hypersensitivity – skin rash, urticaria, pruritus, bronchospasm, fever, anaphylaxis  hence intradermal skin injection test dose is a must before administration.  Other than the rare event of anaphylaxis penicillins are one of the safest antibiotics  Local pain at injection site  CNS : confusion,convulsions,coma  Suprainfections
  • 16. ANAPHYLATIC SHOCK TREATMENT  DRUG OF CHOICE : )  dose : 0.2 - 0.5 ml of 1: 1000 solution S.C ( if mild )  50 - 100 ug of 1: 10,000 solution I.V ( if severe )  corticosteroid : hydrocortisone  others : antihistaminic , iv fluids , oxygen therapy , dopamine.
  • 17. Semisynthetic penicillins 1.Acid resistant – Penicillin V Use : Streptococcal pharyngitis, sinusitis and trench mouth. 2.Penicillinase resistant – cloxacillin, methicillin, oxacillin, nafcillin Use : Staphylococcal infections ,treatment of human bites .
  • 18. Aminopenicillins – ampicillin, bacampicillin, amoxicillin Use : 1. Respiratory tract infections- bronchitis, sinusitis, otitis media 2. Urinary tract infections 3. Meningitis 4. Typhoid 5. Septicaemia 6. Bacillary dysentery 7. Bacillary endocarditis
  • 19. Amoxicillin vs Ampicillin  Amoxicillin is better absorbed orally  Food does not interfere with its absorption  Attains high blood levels after oral administration  Diarrhoea is rare  Longer acting than ampicillin (given thrice daily)  Does not reduce the effectiveness of oral contraceptives.
  • 20. Antipseudomonal penicillins i) Carboxypenicillins – carbenicillin, ticarcillin ii) Ureidopenicillins – azlocillin, mezlocillin, piperacillin Use: Pseudomonas, Klebsiella, Proteus infections Adverse effects: Carbenicillin causes edema and CCF, bleeding
  • 21. Beta lactamase inhibitors  Beta lactamases are enzymes produced by bacteria which open up the beta lactam ring and inactivates the beta lactam antibiotics.  Beta lactamase inhibitors bind to and inactivates beta lactamases thereby preventing destruction of beta lactam antibiotics.  Clavulanic acid  Sulbactam  Tazobactam
  • 22. Combinations  Clavulanic acid + amoxicillin – oral/IV  Clavulanic acid + ticarcillin – IV  Sulbactam + ampicillin – IV  Tazobactam + piperacillin – IV Use: Cellulitis, diabetic foot, skin & soft tissue infections, respiratory & genitourinary infections, mixed aerobic-anaerobic & nosocomial infections
  • 23. Cephalosporins  Semisynthetic antibiotics  Wider spectrum of activity  Mechanism of action similar to penicillins i.e. inhibits bacterial cell wall synthesis  Bactericidal
  • 24. Classification  First generation - effective against gram positive organisms  Second generation - more active against gram negative organisms  Third generation - effective against gram negative organisms and anaerobes  Fourth generation - gram positive and gram negative organisms  Fifth generation – MRSA and gram negative organisms
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  • 27.  first and second generation cephalosporins are used as substitutes to penicillins in those who have mild allergic reaction to penicillin  NOT IN THOSE WITH SEVERE REACTIONS LIKE ANAPHYLAXIS/ ANGIOEDEMA .  Used as a first line empirical therapy along with aminoglycosides in treatment of bacteremia / septicemia.  Cefoxitin , cefotetan ( both 2 nd generation )are used in anaerobic infections.
  • 28. CEFTRIAXONE : THIRD GENERATION  ITS a third generation cephalosporin  highly resistant to beta lactamases.  good activity against gram positive and negative organisms, moderate against psuedomonas .  has the longest half life amongst beta lactam antibioitics ( 8 hrs )  enters csf when meninges are inflammed , hence used in treatment of meningitis .  other uses : complicated UTI ,abdominal sepsis, chancroid
  • 29. FOURTH GENERATION  Similar to third generation but more resistant to beta lactamases .  active against enterobacteriacea ( gram negative ) and psuedomonas resistant to group 3  examples cefepime , cefpirome  given parenterally .
  • 30. Uses  Gram negative infections- urinary, respiratory and soft tissue infections  Surgical prophylaxis  Gonorrhoea  Meningitis  Mixed aerobic-anaerobic infections  Typhoid  Nosocomial infections
  • 31. Adverse effects  Hypersensitivity reactions-skin rash, fever, serum sickness, anaphylaxis  Nephrotoxicity  Diarrhoea  Bleeding  Low WBC count  Pain at injection site
  • 32. Carbapenems : imipenem, meropenem, ertapenem, doripenem, faropenem  Spectrum : gram positive, gram negative and anaerobic organisms.  Mechanism of action: inhibits bacterial cell wall synthesis  Uses : UTI, respiratory, skin, bone, soft tissue, intra abdominal and gynecological infections  only FAROPENEM IS ORALLY ACTIVE , hence can be given orally . rest are given IV parenterally.
  • 33. IMIPENEM  BACTERICIDAL  broad spectrum beta lactam antibiotic  effective against gram positive , enterobacteriacea , psuedomonas , anaerobes ( like clostridia difficile).  rapidly hydrolysed by enzyme dehydropeptidase in renal tubules.  hence combined with cilastin that reversibly blocks this enzyme and protects imipenem .  not absorbed from GIT , given parenterally .
  • 34. Monobactam: aztreonam  Single beta lactam ring  Effective against gram negative organisms but not against gram positive and anaerobes.  spectrum similar to aminoglycosides,hence used as a reserve drug in treating gram -ve infections in those whom aminoglycosides are contraindicated .  MoA : inhibits bacterial cell wall synthesis ( bactericidal )  Given parenterally  Uses : nosocomial pseudomonas infections and other gram negative infections
  • 35. ANTIPSEUDOMONAL ANTIBIOTICS Pneumonic : BLAQ Pseudomonas  Beta Lactam antibiotics :  Penicillins : i) Carboxypenicillins – carbenicillin, ticarcillin ii) Ureidopenicillins – azlocillin, mezlocillin, piperacillin  Cephalosporins : Ceftazidime, cefoperazone, cefepime, cefpirome  Carbapenem : imipenem, meropenem, doripenem  Monobactam : aztreonam  Aminoglycosides  Quinolones  Polypeptides