Application of Antibiotics: Chloramphenicol and Tetracycline

Application of Antibiotics:
Chloramphenicol and Tetracycline

1
GUIDED BY:- SUBMITTED BY:-

MR.NITIN SAHAI AMIT SHARMA
REG. NO:-1120070036
B.PHARMACY
7TH SEM.
Introduction to Antibiotics
2
Antibiotics are agents that are "selectively" toxic

for bacteria (either killing them that is bactericidal
or inhibiting their growth that is bacteriostatic)
without harm to the patient and can thus be
ingested.
Antibiotics work most efficiently in conjunction
with an active immune system to kill infecting
bacteria in the host
Hugo and Russell’s,Pharmaceutical Microbiology BY Stephen. P. Denyer, Norman A Hodges, Sean P Gorman, seventh edition,
Page no.153-186
History
3
For more than 2,500 years, people have treated certain
skin infections with moulds that form antibiotics.
At that time, the French chemist Louis Pasteur
discovered that bacteria spread infectious diseases.
Robert Koch, a German bacteriologist, developed
methods of isolating and growing various kinds of
bacteria.
In 1928 Alexander Fleming observed that a mould of the
genus Penicillium produced a substance that destroyed
bacteria. He called it as Penicillin.
http://en.wikipedia.org/wiki/Antibiotic
Classification
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 β-Lactam antibiotics- Eg. Penicillin

 Tetracycline group- Eg. Tetracycline
 Rifamycins- Eg. Rifampicin
 Aminoglycoside-aminocyclitol antibiotics- Eg. Gentamicin
 Macrolides- Eg. spiramycin
 Lincosamides- Eg. Lincomycin
 Streptogramins- Eg. Pristinamycin
 Polypeptide antibiotics- Eg. Capreomycin
 Glycopeptide antibiotics- Eg. Vancomycin
 Miscellaneous antibacterial antibiotics- Eg. Chloramphenicol
 Antifungal antibiotics- Eg. Griseofulvin
 Synthetic antimicrobial agents- Eg. Sulphonamides
Hugo and Russell’s,Pharmaceutical Microbiology BY Stephen. P. Denyer, Norman A Hodges, Sean P Gorman, seventh edition,
Page no.153-186
Chloramphenicol
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Originally produced from a Streptomyces,

chloramphenicol has since been totally synthesized.
It has a broad spectrum of activity, but exerts a
bacteristatic effect. It has antirickettsial activity and
is inhibitory to the larger viruses.
The highly water-soluble. Chloramphenicol sodium
succinate is used in the parenteral formulation, and
acts as a pro-drug. A semisynthetic derivative of
chloramphenicol thiamphenicol, is claimed to be less
toxic than chloramphenicol.
Chloramphenicol,Meeting of the NTP Board of Scientific Counselors Prepared by:Technology Planning and Management
Corporation Canterbury Hall, Suite 310 4815 Emperor Blvd Durham, NC 27703, page no.1-3
Mode of action
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Chloramphenicol is bacteriostatic (that is, it stops

bacterial growth).
It is a protein synthesis inhibitor, inhibiting
peptidyl transferase activity of the bacterial
ribosome, binding to A2451 and A2452 residues in
the 23S rRNA of the 50S ribosomal subunit,
preventing peptide bond formation.
Chloramphenicol,Meeting of the NTP Board of Scientific Counselors Prepared by:Technology Planning and Management
Corporation Canterbury Hall, Suite 310 4815 Emperor Blvd Durham, NC 27703, page no.1-3
Uses
7
Chloramphenicol may be used as a second-line

agent in the treatment of tetracycline-resistant
cholera.
It is also useful in the treatment of brain abscesses
due to mixed organisms or when the causative
organism is not known.
Tripathi; K.D ; Essentials of pharmacology; sixth edition 2008 ; Jaypee publishers ; page no. 717 and Hugo and
Russell’s,Pharmaceutical Microbiology BY Stephen. P. Denyer, Norman A Hodges, seventh edition, Page no-156-186
Adverse effects
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Aplastic anemia
Leukemia
Gray baby syndrome
Bone marrow suppression
Tripathi; K.D ; Essentials of pharmacology; sixth edition 2008 ; Jaypee publishers ; page no. 717
Introduction ofTetracycline
Antibiotics
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A family of antibiotics that inhibit protein synthesis

by preventingthe attachment of aminoacyl-tRNA to
the ribosomal acceptor(A) site.
Broad-spectrum agents- active against a wide range
of gram-positive and gram-negative bacteria,
atypical organisms such as chlamydiae,
mycoplasmas, and rickettsiae, and protozoan
parasites.
Microbiology and molecular biology reviews Vol. 65, June 2001, page no. 232–260
DISCOVERY AND DEVELOPMENT OF
THE TETRACYCLINES
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Chlortetracycline and oxytetracycline, both discovered

in the late 1940s, were the first members of the
tetracycline group to be described.
These molecules were products of Streptomyces
aureofaciens and S. rimosus, respectively. Other
tetracyclines were identified later, either as naturally
occurring molecules, e.g., tetracycline from S.
aureofaciens, S.rimosus, and S. viridofaciens and
demethylchlortetracycline from S. aureofaciens, or as
products of semisynthetic apapproaches, e.g.,
methacycline, doxycycline, and minocycline.
Mode of Action
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Protein synthesis inhibitors

Inhibits the binding of aminoacyl-tRNA to the
mRNA-ribosome complex by binding to the 30S
ribosomal subunit in the mRNA translation complex.
Tetracyclines also have been found to inhibit matrix
metalloproteinases
Resistance
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Develops slowly in a graded manner. Usually the

tetracycline concentrating mechanism becomes less
efficient or the bacteria acquire capacity to pump it
out.
Another mechanism is plasmid mediated synthesis
of a protection protein which protects the ribosomal
binding from tetracycline.
Tripathi, K.D; Essentials of pharmacology; Sixth edition; Jaypee publishers; Page no. 710-713
Adverse effects
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Irritative effects
Dose related toxicity:-
1. Liver damage
2. Kidney damage
3. Phototoxicity
4. Teeth and bones
Uses
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Tetracycline are the first choice of drug for –

1. Venereal diseases : Endocervicitis ,
lymphogranuloma, granuloma.
2. Atypical pneumonia
3. Cholera
Broad spectrum antibiotics, they should be
employed only for those infection for which a more
selective and less toxic antimicrobial agent is not
available
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Application of Antibiotics:

Chloramphenicol and Tetracycline

GUIDED BY:- SUBMITTED BY:-

Antibiotics are agents that are "selectively" toxic

 β-Lactam antibiotics- Eg. Penicillin

Originally produced from a Streptomyces,

Chloramphenicol is bacteriostatic (that is, it stops

Chloramphenicol may be used as a second-line

A family of antibiotics that inhibit protein synthesis

Chlortetracycline and oxytetracycline, both discovered

Protein synthesis inhibitors

Develops slowly in a graded manner. Usually the

Tetracycline are the first choice of drug for –

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