ANTIMICROBIAL DRUGS

HISTORY OF CHEMOTHERAPY
● PAUL EHRLICH
○ Credited to the efforts of modern chemotherapy
○ “MAGIC BULLET” that would selectively find and destroy pathogens but not harm the host
■ Chemotherapy – a term he coined
● ALEXANDER FLEMING 1982
○ He observed the growth of the bacterium staphylococcus aureus was inhibited in the area
surrounding the colony of a mold that had contaminated a Petri Plate
■ The mold was identified as
PENICILLIUM NOTATUM – isolated a
short time later was named as
PENICILLIN
■ Antibiosis – mechanism of inhibition
■ Antibiotic – a substance produced by
microorganism that in small amounts
inhibits another microorganisms
● HOWARD FLOREY AND ERNST CHAIN 1940
○ Scientist at oxford university
○ Succeeded in the first clinical trials of pinicillin
○ The original culture of P. notatum was not a
very efficient producer of the antibiotic
○ It was soon replaced by a more prolific strain
Penicillium chrysogenum
● Antibiotics
○ Are produced by species of streptomyces ,
filamentous bacteria that are commonly inhabit
soil
○ A few antibiotics are produced by endospore-forming bacteria such as BACILLUS , and
other are produced by molds , mostly of the genre PENICILLIUM and CEPHALOSPORIUM

ANTIBIOTIC DISCOVERY TODAY

★ Most antibiotics in use today were discovered by methods that required identifying and growing
colonies of antibiotic producing organisms, mostly by screening soil samples.
★ To find an antibiotic that is produced by only one soil or sea microbe in 10 million, though, is a
daunting task
○ About 1 in every 100 actinomycetes in soil produce streptomycin
○ About 1 in 250 produce tetracycline
★ It is comparatively easy to find or develop drugs that are effective against prokaryotic cells and that
do not affect the eukaryotic cells of humans
★ The problem is more difficult when the pathogen is a eukaryotic cell, such as a fungus, protozoan,
or helminth.
★ At the cellular level, these organisms resemble the human cell much more closely than a bacterial
cell does.
★ Viral infections are particularly difficult to treat because the pathogen is within the human host’s
cells and because the genetic information of the virus is directing the human cell to make viruses
rather than to synthesize normal cellular materials.
★ Narrow spectrum of microbial or a range of different microbial types the affect
○ example: Penicillin G → it affects the gram-positive but not as efficient to gram negative
bacteria
★ Antibiotics that affect a broad range of gram-positive or gram-negative bacteria are therefore called
broad-spectrum antibiotics.
 ★ Candida albicans – not sensitive to bacterial antibiotics
★ Superinfection – a term that is also applied to growth of a target pathogen that has developed
resistance to the antibiotic
★ Antimicrobial drugs are either
○ bactericidal : they kill microbes directly
○ Bacteriostatic : they prevent microbes from growing
■ The hosts own defenses such as phagocytosis and antibody production , usually
destroy the microorganism
Inhibiting Cell Wall Synthesis
● Penicillin
○ first antibiotic to be discovered and used
○ Is an example of an inhibitor of cell wall synthesis
○ It targets the synthesis process , only actively growing cells are affected by these antibiotics
● 87h
○ Cell wall of a bacterium consists of a macromolecular
○ Is only found in bacterial cell walls
○ Penicillin and certain other antibiotics prevent the synthesis of intact peptidoglycan