Penicillin is one of the foremost important antibiotic in the world. It is used against the gram positive bacteria. But the resistance mechanism has been developed by them. But researchers are taking step to synthesis such synthetic penicillin for multipurpose use.
2. PENICILLINS
• Beta- lactam antibiotics
• Derivatives of 6- aminopenicillanic acid
• Alteration of the side group resulted in
cpds with :
• Broader spectrum of activity
• Resistance to penicillinase
• Stability in acid PH
• Most widely effective antibiotics
• Least toxic drugs known
3. Antibiotics are antimicrobial agents
produced naturally by other
microbes (usually fungi or
bacteria).
The first antibiotic was discovered
in 1896 by Ernest Duchesne and
"rediscovered" byAlexander
Flemming in 1928 from the
filamentous fungus Penicilium
notatum.
4. • The antibiotic substance, named penicillin,
was not purified until the 1940s (by Florey and
Chain), just in time to be used at the end of the
second world war.
• Penicillin was the first important commercial
product produced by an aerobic, submerged
fermentation
5. Production of penicillin
• To be able to identify useful products
from microorganisms
• To be able to identify the microorganisms
used and the main stages in the
production of penicillin.
• To be able to describe how Downstream
processing is carried out to extract and
purify the end-product of fermentation.
6. Downstream Processing
• Products in a fermentor are impure and dilute,
so need to be purified by downstream
processing.
• This usually involves filtration to separate the
microbial cells from the liquid medium,
followed by chemical purification and
concentration of the product
• Downstream processing can account for 50%
of the cost of a process
7. Cont.
• Downstream processing is relatively easy since
penicillin is secreted into the medium (to kill
other cells), so there is no need to break open
the fungal cells.
• However, the product needs to be very pure,
since it being used as a therapeutic medical
drug, so it is dissolved and then precipitated as
a potassium salt to separate it from other
substances in the medium.
8. MECHANISM OF ACTION
They act by inhibition of bacterial cell wall
synthesis
Thus exposing the osmotically less stable membrane
This cause lysis of bacterial cell wall
These agents are bactericidal
Active against multiplying and not resting bacteria
Inactive against mycobacteria, protozoa, fungi and
viruses
9.
10. Uses
H. Influenza infections ( otitis media, sinusitis,
chronic bronchitis, pneumonia, bacterial meningitis ).
M.catarrhalis
E. Coli infections ( Urinary & biliary infections ).
Samonella infections ( typhoid fever )
Shigella infections ( ampicillin )
Gonococcal infections ( alternative for penicillin in
the treatment of gonorrhea )
Prophlaxis of infective endocarditis
Disadvantages
Amoxicillin & ampicillin alone are readily destroyed
by Staph. Penicillinase.
11. 1.Hypersensitivity reactions ( occur in 1-10% of pts;
fatality occur in 0.002%)
( immediate, accelerated & late allergic rxns)
Urticarial rash
Fever
Bronchspasm
Serum sickness
Exfoliative dermatitis
Stevens- Johnson syndrome
Anaphylaxis
2. Super infections
3. Diarrhoea
4. May cause convulsions after high doses by i.v or in
renal failure