ANTIBIOTICS

INHIBITING CELL WALL

SYNTHESIS AND
PROTEIN SYNTHESISSUBMITTED BY-
FARHEEN KHAN
Roll No.- 19MBSOO7
MSc Biosciences 1st year
 INDEX

Introduction
Spectrum of antimicrobial activity
Type of action
Mechanism of action
 INTRODUCTION

• Antibiotics are defined as chemical substances or compounds

produced by various microorganisms or produced synthetically
which in low concentrations destroy, kill or inhibit the growth of
living organisms .
• There is an increasing urgency to find new antibiotics to
address the growing problem of antibiotic resistance, a
phenomenon in which formerly effective medication have less &
less imapact on bacteria .
SPECTRUM OF ANTIMICROBIAL ACTIVITY
 Narrow spectrum antibiotics :
Acts against single or limited group of bacteria. For e.g. Penicillin
affects gram positive bacteria but a very few gram negative
bacteria.
 Broad spectrum antibiotics :
Drugs affecting wide variety of microbial species (can cause
superinfection). e.g. Tetracycline and Chloramphenicol .
Spectrum of Antimicrobial Activity
TYPE OF ACTION
 Bacteriocidal : They kill
microbes directly .
 Bacteriostatic : They
prevent microbes from
growing. The host own’s
defenses such as
phagocytosis and antibody
production that usually
destroy microorganisms .
 MECHANISM OF ACTION OF ANTIBACTERIAL DRUGS

• Inhibition of cell wall synthesis

• Inhibition of protein synthesis
• Inhibition of nucleic acid
synthesis
• Inhibition of metabolic pathways
• Interference with cell membrane
integrity
 Inhibition of Cell Wall Synthesis
• Penicillin – The term penicillin refers to a group of over 50 chemically related antibiotics having a
common core structure containing a β-lactam ring called the nucleus. Penicillins prevent the cross-
linking of the peptidoglycans, which interferes with the final stages of the synthesis
of the cell walls, primarily of gram-positive bacteria .

∆ Natural Penicillin
Penicillin G – Effective against gram positive bacteria, requires injection
Penicillin V – Effective against gram positive bacteria, oral administration

∆ Semisynthetic Penicillin
Oxacillin – Narrow spectrum, resistant to penicillinase
Ampicillin – Broad spectrum
Amoxicilliin – Broad spectrum, combined with inhibitor of penicillinase i.e potassium clavulanate
(Clavulanic acid)

• Carbapenems
Imipenem and Cilastin – Very broad spectrum, cilastin has no antimicrobial activity but prevents
imipenem from being degraded in the kidneys
• Monobactems
Aztreonam – effective against gram negative bacteria including Pseudomonas species

• Cephalosporins
Cephalothin –1st generation of cephalosporins,activity resembles those of
penicillin,requires injection
Ceftaroline – 5th generation cephalosporins,activity against MRSA

• Polypeptide antibiotics
Bacitracin – Effective against gram positive bacteria,topical application
Vancomycin – the last line of antibiotic defense for treatment of Staphylococcus aureus
infections that are resistant to other antibiotics and this has led to appearance of vancomycin
resistant enterococci (VRE) pathogens which is considered medical emergency

• Antimycobacterial
Isomiazid (INH) – inhibit synthesis of mycolic acids which are components of cell wall
of Mycobacterium species
Ethambutol – Inhibits incorporation of mycolic acid into the cell wall of mycobacterium
species .
 Inhibition of Protein Synthesis

• Nitrofurantoin – Used to treat urinary bladder infections

• Chloramphenicol – Broad spectrum, potentially toxic as it can cause aplastic anemia
• Aminoglycosides
Streptomycin – Used as an alternative drug in treatment of Tuberculosis
Neomycin – Topical use
Gentamicin – Useful against Pseudomonas infections
• Tetracyclines
Tetracycline, oxytetracycline, chlortetracycline – effective against rickettsias &
Chlamydias
• Glycylcyclines
Tigecyclin – effective against MRSA and multi drug resistant strains of
Acinetobacter
baumanii
• Macrolides
Erythromycin – alternative drug to penicillin
Azithromycin & Clarithromycin – broad spectrum , semisynthetic
Telithromycin – new generation of semisynthetic macrolides

• Streptogramins
Dalfopristin and Quinupristin (Synercid) – alternative for treating vancomycin
resistant gram positive bacteria

• Oxazolidinones
Linezolid – mainly to combat MRSA

• Pleuromutilins – effective against gram positive

Retapamulin – limited to topical use only
 Inhibition of Nucleus Synthesis

A no. of antibiotics interfere with the process of DNA replication and

transcription in microorganisms. These drugs block bacterial topoisomerase
or DNA polymerase
• Rifamycin – inhibit synthesis of mRNA , used against Mycobacteria in
treatment of Tuberculosis & Leprosy
• Quinolones & Fluoroquinolones
Nalidixic Acid – Selectively inhibit DNA gyrase needed for DNA replication
Ciproflaxin
Gemifloxacin & moxifloxacin – Used to treat urinary tract infections
 Inhibition of Essential Metabolites

Blocking a cells ability to synthesize essential metabolites is

another mode of drug action .
• Sulfonamides (sulpha drug) – similar to folic acid precursor
called PABA (para-aminobenzoic acid) , allowing to bind with
enzyme for PABA and block folic acid production
Sulfamethoxazole & Trimethoprim – It is an example of drug
synergism the combination has broader spectrum of action and
reduces emrgence of resistant strains .
 Interference with Cell Membrane Integrity

Ceratin antibiotics bring changes in permeability of plasma membrane that results in

loss of important metabolites and some of the polypeptide antibiotic disrupt both inner
and outer membranes of gram -ve bacteria.
The synthesis of plasma membrane requires synthesis of fatty acids as building blocks
• Lipopeptides
Daptomycin – effective against gram positive bacteriaproduced by streptomycetes
approved for certain skin infection
Polymyxin B – effective against gram negative bacteriaused in topical treatment
PolymyxinE – treatment of antibiotic resistance ventilator associated pneumonia by
gram negative bacteria