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Beta lactam antibiotics
β LACTAM ANTIBIOTICS
Have a β-lactam ring in their structure
•Penicillins
•Cephalosporins
•Carbapenems
•Monobactams
all are bactericidal
PENICILLINS
Mechanism of Action
• Bind to penicillin binding proteins on the cytoplasmic
membrane and Inhibit the enzyme transpeptidase that is
essential for the bacterial cell wall rigidity.
• This results in the formation of bacteria with weak cell wall
& undergo lysis.
Mechanism of Resistance:
• Beta lactamase (penicillinase) enzyme produced by the
bacteria inactivate penicillins (most common cause)
PENICILLINS
A. Narrow Spectrum Penicillins
Penicillinase sensitive (Natural Penicillins)
• Benzyl penicillin (Penicillin-G )
• Benzathine penicillin
• Penicillin V (oral)
Penicillinase Resistant (Antistaphylococcal penicillins)
• Methicillin
• Nafcillin
• Cloxacillin
B. Extended Spectrum Penicillins
Penicillinase sensitive
 Aminopenicillins
• Ampicillin,
• Amoxycillin,
 Antipseudomonial penicillins
• Ticarcillin
• Pipercillin
ANTIMICROBIAL SPECTRUM & USES
BENZYLPENICLLIN (Penicillin G):
• Infections caused by Streptococcus pyogenes
(pharyngitis, otitis media, oral infections) Streptococcus
pneumoniae (pneumonia)
• Enterococcus ( bacterial endocarditis) –synergistic when
combined with gentamicin
• Actinomycetes israelii ( Actinomycosis) Bacillus anthracis
(Anthrax)
• Clostridium tetani, (tetanus) Cl. Perfringes ( Gas
gangrene), Bacteroides oropharyngeal strains, Treponema
pallidum (syphillis)
BENZATHINE PENICILLIN
• Prophylaxis against reinfection with β haemolytic
streptococcal pharyngitis (Rheumatic fever)
PENICILLIN V
• Used in Oropharyngeal infections
CLOXACILLIN, NAFCILLIN (Antistaphylococcal )
• Used in Staphylococcal infections like
osteomyelitis, septicaemia, endocarditis
• Dental uses : Endodontic
infections, Periodontitis, Gingivitis, Odontogenic
infections, Periodontal abscess, Acute necrotizing ulcerative
gingivitis.
EXTENDED SPECTRUM PENICILLINS
AMOXYCILLIN & AMPICILLIN
• Amoxycillin is better absorbed orally and food does not interfere
with its absorption.
• Diarrhea & rash is more common with ampicillin and rare with
amoxycillin
• Ampicillin ( four times daily) Amoxicillin ( thrice daily)
• Their antibacterial activity is enhanced if used in combination with
beta lactamase inhibitors
USES
• H influenzae (pneumonia, otitis media, sinusitis)
• E. coli (UTI)
• Enterococcal infections
• Oropharyngeal infections
• Helicobacter pyroli eradication in peptic ulcer.
Antipseudomonal penicillins
• TICARCILLIN & PIPERACILLIN
• Pseudomonal infections it is combined with Clavulanic acid
Adverse effects of Penicillins
Hypersensitivity reaction
• Mild urticarial skin rash to a serious anaphylactic shock (
severe hypotension, bronchospasm & laryngeal edema)
Maculopapular rash - Ampicillin
Diarrhea , pseudomembranous colitis- Ampicillin
Interstitial Nephritis : Methicillin
BETA LACTAMASE INHIBITORS
• β lactamase inhibitors are drugs that inhibit β-lactamases -
enzymes produced by bacteria that inactivate the β-lactam
antibiotics.
• Drugs are Clavulanic acid, Sulbactam
• Clavulanic acid is combined with Amoxycillin
• Sulbactam is combined with Ampicillin
Uses:
• Effective against β lactamase producing bacteria eg Strep.
Pneumoniae , H influenzae (otitis media, sinusitis, orofacial
infections)
• Neisseria gonorrhoeae (gonorrhoea)
• Anaerobes ( Intra abdominal abscess)
CEPHALOSPORINS
I Generation – Active against Gm+ve,(staphylo & streptococci)
but a moderate effect on Gm-ve bacteria ( klebsiella & E coli) .
• Cephalexin, Cefadroxil
II Generation- Resistant to beta-lactamase, active against almost
all Gm-ve bacilli—
• Cefaclor , Cefprozil
III Generation- More active than either of two generations against
certain Gm-ve bacteria-
• Ceftibuten and Cefixime
IV Generation - More resistant to some beta-lactamase
producing species.
• Cefepime
Therapeutic uses of Cephalosporins
I Generation Cephalosporins :
• Infections caused by G +ve cocci such as, Staphyl aureus,
strepto pneumoniae, strepto pyogenes, Anaerobic streptococci.
II Generation Cephalosporins:
• Strepto pneumoniae, strepto pyogenes, Neisseria gonorrhoeae,
E coli, H influenzae, Klebsiella pneumoniae. Infections caused
by anaerobes Bacteroides fragilis & H influenza
III Generation Cephalosporins :
• Neiseria gonorrhoeae, E coli, Salmonella, H influenzae,
Proteus & Pseudomonas aeruginosa, penicillin resistant
pneumococci
Adverse effects of Cephalosporins
• Hypersensitivity reactions – Less compared to Penicillins
• Superinfection:
• Pseudomembranous enterocolitis
• Diarrhoea
• Hypoprothrombinemia (Bleeding)
Carbapenems
Imipenem &Meropenem
• Effective against Gm+ve, Gm-ve including
pseudomonas, anaerobes & β lactamase producing
organisms.
Uses
• Mixed aerobic & anaerobic infections
• Penicillin resistant pneumococci
• Enterobacter infections
• Pseudomonal infections
Adv effects
• Vomiting, diarrhoea, Seizures
Monobactams
Eg: Aztreonam
• Resistant to β-lactamases & active against pseudomonas
• No activity against G+ve or anaerobes.
• Uses:
• Patients allergic to penicillins
• Pseudomonal and other Gm-ve infections .

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6 beta lactum drugs dental

  • 2. β LACTAM ANTIBIOTICS Have a β-lactam ring in their structure •Penicillins •Cephalosporins •Carbapenems •Monobactams all are bactericidal
  • 3. PENICILLINS Mechanism of Action • Bind to penicillin binding proteins on the cytoplasmic membrane and Inhibit the enzyme transpeptidase that is essential for the bacterial cell wall rigidity. • This results in the formation of bacteria with weak cell wall & undergo lysis. Mechanism of Resistance: • Beta lactamase (penicillinase) enzyme produced by the bacteria inactivate penicillins (most common cause)
  • 4. PENICILLINS A. Narrow Spectrum Penicillins Penicillinase sensitive (Natural Penicillins) • Benzyl penicillin (Penicillin-G ) • Benzathine penicillin • Penicillin V (oral) Penicillinase Resistant (Antistaphylococcal penicillins) • Methicillin • Nafcillin • Cloxacillin B. Extended Spectrum Penicillins Penicillinase sensitive  Aminopenicillins • Ampicillin, • Amoxycillin,  Antipseudomonial penicillins • Ticarcillin • Pipercillin
  • 5. ANTIMICROBIAL SPECTRUM & USES BENZYLPENICLLIN (Penicillin G): • Infections caused by Streptococcus pyogenes (pharyngitis, otitis media, oral infections) Streptococcus pneumoniae (pneumonia) • Enterococcus ( bacterial endocarditis) –synergistic when combined with gentamicin • Actinomycetes israelii ( Actinomycosis) Bacillus anthracis (Anthrax) • Clostridium tetani, (tetanus) Cl. Perfringes ( Gas gangrene), Bacteroides oropharyngeal strains, Treponema pallidum (syphillis)
  • 6. BENZATHINE PENICILLIN • Prophylaxis against reinfection with β haemolytic streptococcal pharyngitis (Rheumatic fever) PENICILLIN V • Used in Oropharyngeal infections CLOXACILLIN, NAFCILLIN (Antistaphylococcal ) • Used in Staphylococcal infections like osteomyelitis, septicaemia, endocarditis • Dental uses : Endodontic infections, Periodontitis, Gingivitis, Odontogenic infections, Periodontal abscess, Acute necrotizing ulcerative gingivitis.
  • 7. EXTENDED SPECTRUM PENICILLINS AMOXYCILLIN & AMPICILLIN • Amoxycillin is better absorbed orally and food does not interfere with its absorption. • Diarrhea & rash is more common with ampicillin and rare with amoxycillin • Ampicillin ( four times daily) Amoxicillin ( thrice daily) • Their antibacterial activity is enhanced if used in combination with beta lactamase inhibitors USES • H influenzae (pneumonia, otitis media, sinusitis) • E. coli (UTI) • Enterococcal infections • Oropharyngeal infections • Helicobacter pyroli eradication in peptic ulcer.
  • 8. Antipseudomonal penicillins • TICARCILLIN & PIPERACILLIN • Pseudomonal infections it is combined with Clavulanic acid Adverse effects of Penicillins Hypersensitivity reaction • Mild urticarial skin rash to a serious anaphylactic shock ( severe hypotension, bronchospasm & laryngeal edema) Maculopapular rash - Ampicillin Diarrhea , pseudomembranous colitis- Ampicillin Interstitial Nephritis : Methicillin
  • 9. BETA LACTAMASE INHIBITORS • β lactamase inhibitors are drugs that inhibit β-lactamases - enzymes produced by bacteria that inactivate the β-lactam antibiotics. • Drugs are Clavulanic acid, Sulbactam • Clavulanic acid is combined with Amoxycillin • Sulbactam is combined with Ampicillin Uses: • Effective against β lactamase producing bacteria eg Strep. Pneumoniae , H influenzae (otitis media, sinusitis, orofacial infections) • Neisseria gonorrhoeae (gonorrhoea) • Anaerobes ( Intra abdominal abscess)
  • 10. CEPHALOSPORINS I Generation – Active against Gm+ve,(staphylo & streptococci) but a moderate effect on Gm-ve bacteria ( klebsiella & E coli) . • Cephalexin, Cefadroxil II Generation- Resistant to beta-lactamase, active against almost all Gm-ve bacilli— • Cefaclor , Cefprozil III Generation- More active than either of two generations against certain Gm-ve bacteria- • Ceftibuten and Cefixime IV Generation - More resistant to some beta-lactamase producing species. • Cefepime
  • 11. Therapeutic uses of Cephalosporins I Generation Cephalosporins : • Infections caused by G +ve cocci such as, Staphyl aureus, strepto pneumoniae, strepto pyogenes, Anaerobic streptococci. II Generation Cephalosporins: • Strepto pneumoniae, strepto pyogenes, Neisseria gonorrhoeae, E coli, H influenzae, Klebsiella pneumoniae. Infections caused by anaerobes Bacteroides fragilis & H influenza III Generation Cephalosporins : • Neiseria gonorrhoeae, E coli, Salmonella, H influenzae, Proteus & Pseudomonas aeruginosa, penicillin resistant pneumococci
  • 12. Adverse effects of Cephalosporins • Hypersensitivity reactions – Less compared to Penicillins • Superinfection: • Pseudomembranous enterocolitis • Diarrhoea • Hypoprothrombinemia (Bleeding)
  • 13. Carbapenems Imipenem &Meropenem • Effective against Gm+ve, Gm-ve including pseudomonas, anaerobes & β lactamase producing organisms. Uses • Mixed aerobic & anaerobic infections • Penicillin resistant pneumococci • Enterobacter infections • Pseudomonal infections Adv effects • Vomiting, diarrhoea, Seizures
  • 14. Monobactams Eg: Aztreonam • Resistant to β-lactamases & active against pseudomonas • No activity against G+ve or anaerobes. • Uses: • Patients allergic to penicillins • Pseudomonal and other Gm-ve infections .