INTRODUCTION TO

CHEMOTHERAPY AND
ANTIBACTERIAL AGENTS
Prepared by :- Hitesh Chandpa
(M. Pharm, pharmacology)
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DEFINITION

• Chemotherapy is the use of drugs to treat the diseases caused

by microorganisms, parasites and tumour cells without affecting
the host.
• These drugs are known as Chemotherapeutic agents.
• Paul Ehrlich – Father of Modern Chemotherapy

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GOAL OF CHEMOTHERAPY

• Goal of chemotherapy is to study and use the drugs of selective

toxicity to pathogenic microorganism or tumour cells and have
less or no effect on host or healthy cells.

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ANTI-MICROBIAL AGENTS (ANTIBIOTICS)

• These are the substances derived from microorganisms or

synthesized in labs to kill or suppress the growth of other
microorganisms,
e.g. Penicillin discovered by Alexander Fleming from
Penicillium rubens (Moulds)
• Anti-microbial agents includes Antibacterial, Antifungal,
Antiprotozoal and Antiviral drugs. 4
BACTERIA

• Bacteria are most divers and abundant group of organism on earth

as it is found in sea water, soil, animal’s GIT, hot springs and even
beneath the Earth’s crust.
• Mainly divided in two types on the bases of structure of cell wall
1) Gram positive e.g. Staphylococcus Aureus
2) Gram negative e.g. Escherichia coli
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ANTIBACTERIAL DRUGS

• Mainly two types of antibacterial drugs

1)Bacteriostatic
e.g. Erythromycin, Chloramphenicol
2) Bacteriocidal
e.g. Penicilin, Streptomycin

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POTENTIAL TARGETS FOR ANTIBACTERIAL
DRUGS
• The biochemical reactions that are potential targets for
antibacterial drugs:

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POTENTIAL TARGETS FOR ANTIBACTERIAL
DRUGS

• Class I reaction
i) Glucose utilization pathways
e.g. Embden–Meyerhof pathway and the tricarboxylic acid cycle
ii) Energy sources
e.g. Glucose, amino acids, lactate

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POTENTIAL TARGETS FOR ANTIBACTERIAL
DRUGS

• Class II reaction
1) Folate biosynthesis – e.g. Sulfonamides
2) Pyrimidine and purine analogues

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POTENTIAL TARGETS FOR ANTIBACTERIAL
DRUGS
• Class III reaction
1) Synthesis of peptidoglycans
a) Prevention of addition of terminal alanine – e.g. Cycloserine
b) Inhibition of the release of the building block unit – e.g.
Vancomycin
c) Interference to the regeneration of the lipid carrier – e.g.
Bacitracin
d) Inhibition of transpeptidation – e.g. Penicillins, Cephalosporins 10
POTENTIAL TARGETS FOR ANTIBACTERIAL
DRUGS

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POTENTIAL TARGETS FOR ANTIBACTERIAL
DRUGS
2) Protein Synthesis
a) Competition with tRNA for site A – e.g. Tetracyclines
(doxycycline)
b) Codon:Anticodon misreading – e.g. Aminoglycosides
(Gentamycin)
c) Inhibition of transpeptidation – e.g. Chloramphenicol
d) Premature termination of peptide chain – e.g. Puromycin
e) Inhibition of translocation – e.g. erythromycin 12
POTENTIAL TARGETS FOR ANTIBACTERIAL
DRUGS
3) Nucleic acid synthesis
a) DNA gyrase – e.g. fluoroquinolones (ciprofloxacin)
b) Alteration of the base-pairing properties of the template – e.g.
acridines (proflavine and acriflavine)
c) Inhibition of either DNA or RNA polymerase – e.g. rifamycin,
rifampicin
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REFERENCES

• Rang and Dale’s Pharmacology, 7th Edition, Chapter 49.

• Essential of Medical Pharmacology by K D Tripathi, 7th Edition,
section 12, Page no 688 – 849

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