1 ATB Cell Wall Inhibitors, Naim Kittana

Antimicrobial agents
Faculty of Medicine & Health Sciences

An-Najah National University 1
Selection of anti-microbial agents
• Empiric therapy:
– In critically ill patients: meningitis
– Treat with antimicrobial agent that is

usually effective in a such situation.
 If a culture to be done: sample should be

obtained before antibiotic
2
Selection of anti-microbial agents
 Prophylaxis therapy:
– Directed against the most likely organism
 Examples of situations:
• Pretreatment of a sore throat: rheumatic heart disease
• Before dental extraction
3
Spectra of antimicrobial agents
• Narrow-spectrum
– Affect a single pathogen or limited group of pathogens
– Ex: Vancomycin: only against gram positive bacteria
• Extended-spectrum
– Effective for gram-pos & a significant number of gram-neg
– Ex: ampicillin
4
Spectra of antimicrobial agents
• Broad spectrum
– Affect a wide variety of microbial species
– Ex: Tetracycline & chloramphenicol
– Can affect the normal flora & induce super infection (clostridum difficile:
pseudomembranous colitis)
5
Types of antimicrobial agents
• Bacteriostatic: Antibiotics that inhibit the proliferation of bacteria
• Bactericidal: Antibiotics that kill the bacteria
6
Resistance to antimicrobial agents
 Inherited
 Ex: gram-neg resistance to Vancomycin
 Acquired
 Genetic alterations
 Decreased accumulation
 Enzymatic inactivation
7
Classification of antimicrobial agents
• According to the mechanism of drug action:

– Inhibits bacterial cell wall biosynthesis
– Inhibits bacterial protein synthesis
– Inhibits bacterial metabolism
– Inhibits bacterial nucleic acid synthesis
8
Inhibitors of bacterial cell wall biosynthesis
• Penicillins
• Cephalosporins
• Carbapenemes
• Others: Colistin and Vancomycin
9
Beta-lactam ring
10
Inhibitors of bacterial cell wall biosynthesis
Penicillins
– Mechanism of action:
• Inhibit bacterial cell wall synthesis, reduce integrity
• This results in loss of rigidity and a susceptibility to rupture
– Bactericidal drugs
– The major cause of resistance is the production of beta-lactamases

(penicillinases)
11
Synthetic penicillins
 Ampicillin & Amoxicillin
– Useful for infections caused by G+ve bacteria (e.g. Streptococcus &

Enterococcus) and some G-ve (e.g. Haemophilus influenzae)
– Inactivated by β-lactamases
• Amoxicillin+ Clavulanic acid (β-lactamase inhibitor)
 Anti-pseudomonas agents: Piperacillin

Have good activity against Pseudomonas aeruginosa
12
Common Adverse effects Penicillins
• Hypersensitivity reactions:
• Nearly 5-10% of the patients
• All types of reactions, from a simple rash to anaphylaxis
• Can be observed within 2 minutes or up to 3 days following
administration
• Diarrhea due to superinfection (colitis)
13
Cephalosporins
• Structure and mechanism of action
– Cephalosporins have a β-lactam ring
– Have the same mechanisms of action as penicillins
– Cephalosporins are sensitive to β-lactamase and cephalosporinase
– Each newer generation of cephalosporins is increasingly resistant to

penicillinases and wider antibacterial spectrum
14
Cephalosporins’ Generations
– First: Cephalexin
– Second: Cefuroxime
– Third: Ceftriaxone
– Fourth: Cefepime
• These agents have good activity against some gram-positive organisms

(streptococci) & many gram-negative organisms (e.g. E. coil)
15
General clinical uses of cephalosporins
• Used primarily in the management of infections of

 urinary tract
 respiratory tract
 bone, and soft-tissue
• Also used prophylactically in various surgical procedures
16
Main adverse effects of Cephalosporins
• Cephalosporins most commonly cause hypersensitivity reactions (2–5%);

5%–10% of penicillin-sensitive persons are also hypersensitive to
cephalosporins.
• May cause superinfection with gram-positive organisms or fungi
17
Carbapenemes
• Carbapenems include:
 Meropenem (Meronem®)
• Relatively resistant to Beta-lactamases
• Demonstrate no cross-resistance with other antibiotics
Most common adverse effects:

• Nausea, vomiting, diarrhea
• Skin rashes
• Seizures: at higher doses
18
Other inhibitors of bacterial cell wall biosynthesis
19
Colistin
• Cationic detergent that damages bacterial cytoplasmic membrane, causing

cell death
• Multi-drug resistant gram-neg. infections
• Adverse effects:
 Neurotoxicity
 Nephrotoxicity
 Acute respiratory failure and paralysis (inhalation route)
 Dizziness
20
Vancomycin
• Active against infections caused by gram-positive organisms including

methicillin-resistant Staphylococcus aureus (MRSA)
• Side effects:
– fever, chills and flushing
– Rapid infusion of vancomycin may cause anaphylactoid reactions and “red

neck” syndrome (flushing caused by release of histamine)
– Rarely, ototoxicity with permanent auditory impairment, and nephrotoxicity
21

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Antimicrobial agents

Faculty of Medicine & Health Sciences

– Treat with antimicrobial agent that is

 If a culture to be done: sample should be

• Bacteriostatic: Antibiotics that inhibit the proliferation of bacteria

• Bactericidal: Antibiotics that kill the bacteria

• According to the mechanism of drug action:

• This results in loss of rigidity and a susceptibility to rupture

– The major cause of resistance is the production of beta-lactamases

 Ampicillin & Amoxicillin

– Useful for infections caused by G+ve bacteria (e.g. Streptococcus &

 Anti-pseudomonas agents: Piperacillin

• Diarrhea due to superinfection (colitis)

• Structure and mechanism of action

– Cephalosporins have a β-lactam ring

– Have the same mechanisms of action as penicillins

– Cephalosporins are sensitive to β-lactamase and cephalosporinase

– Each newer generation of cephalosporins is increasingly resistant to

• These agents have good activity against some gram-positive organisms

• Used primarily in the management of infections of

• Also used prophylactically in various surgical procedures

• Cephalosporins most commonly cause hypersensitivity reactions (2–5%);

• May cause superinfection with gram-positive organisms or fungi

• Relatively resistant to Beta-lactamases

• Demonstrate no cross-resistance with other antibiotics

Most common adverse effects:

• Cationic detergent that damages bacterial cytoplasmic membrane, causing

• Multi-drug resistant gram-neg. infections

• Active against infections caused by gram-positive organisms including

– fever, chills and flushing

– Rapid infusion of vancomycin may cause anaphylactoid reactions and “red

– Rarely, ototoxicity with permanent auditory impairment, and nephrotoxicity

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