Antibiotics: Penicillin.pdf

At the end of this e-learning session you are able to…
A. Discuss history and Mechanism of action of Penicillin
B. Give classification and Explain pharmacology of Penicillin.

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1. Prof. Shaikh Abusufiyan
Assistant Professor,
AIKTC-School of Pharmacy,
New Panvel-410206
Antibiotics: Penicillin
Pharma Learning Forever

2. At the end of this e-learning session you are able to…
A.Discuss historyandMechanism
of action of Penicillin
B. Give classificationand Explain
pharmacology of Penicillin.
Copyright @shaikhabusufiyan2021

3. Story to tell:
PENICILLIN:
•In 1928, Alexander Fleming
•observed that a culture plate on which
staphylococci were being grown had become
contaminated with a mould of the genus Penicillium
•Bacterial growth in the vicinity of the mould had
been inhibited.
•isolated the mould in pure culture
•Demonstrated that it produced an antibacterial
substance, penicillin

4. FIRST clinical use of penicillin
•Itsremarkableantibacterialeffectsinhumanswere
demonstratedin1941.
•Asmallamountofpenicillin(extractedfromcrude
culturesinthelaboratories)
•Testedonapoliceman(staphylococcalandstreptococcal
septicaemiawithmultipleabscesses,andosteomyelitiswith
dischargingsinuses).

5. •He was in great pain and was desperately ill.
(Sulfonamideswere available but would have had
no effect in the presence of pus)
•IV injections of penicillinwere given every 3
hours.
•All the patient's urine was collected and each
day the excreted penicillin was extracted and
used again.

6. Result:
•After5days,thepatient'sconditionwasvastlyimproved
•histemperaturewasnormal
•hewaseatingwell
•resolutionoftheabscesses.
•notoxiceffectsofthedrug.
•Thenthesupplyofpenicillinranout
•Hisconditiongraduallydeteriorated
•Hediedamonthlater.

7. Story discussion

8. Mechanisms of action:
•All β-lactam antibiotics interfere with the
synthesis of the bacterial cell wall peptidoglycan.
1. attached to binding sites on bacteria (termed
penicillin-binding proteins)
inhibit the transpeptidation enzyme (cross-links the
peptide chains attached to the backbone of the
peptidoglycan).
Lysis of the bacterium.

9. 2.Semisyntheticpenicillin’s:by
addingdifferentside-chainstothe
penicillinnucleus(atR1).
2a. β-lactamase-
resistant penicillin's (e.g.
flucloxacillin)
2b. Broad-spectrum
penicillin's(e.g. Ampicillin,
amoxicillin)
2c. Extended-spectrum
penicillins(e.g.
carbenacillin, ticarcilin
Naturally occurring
“Benzylpenicillin”
CLASSIFICATION OF PENICILLINS

10. Classification:
1.Naturallyoccurringbenzylpenicillin
•Benzylpenicillinisactiveagainstawiderangeoforganisms
•Andisthedrugoffirstchoiceformanyinfections.
Drawbacks:
•Poorabsorptioninthegastrointestinaltract(itmustbegivenbyinjection)
•Anditissusceptibletobacterialβ-lactamases.

11. Pharmacokinetics
Routeofadministration:
-Oralroute:differentpenicillinareabsorbedto
differentdegreedependingontheiracidstability.
-ItcanbegivenbyIMorIVinjection
-Intrathecaladministration-->isinadvisable,
particularlywithbenzylpenicillinasitcancause
convulsion.

12. Distribution:
-Widely distributedinto body fluid
-Passing into
-Joint
-Pleural and pericardial cavity
-Saliva
-Milk
-Placenta
lDo not cross BBB-lipid insoluble

13. lElimination:
-Eliminated through urine
lShort plasma half lifeis potential problem in
clinical use of benzyl penicillin.

14. Q&A: Activity III
Q.1 Give mechanism of action of Penicillin?
Q.2 Who is the investigator of Penicillin?
Q.3 What is potential problem in clinical use of benzyl penicillin?
Copyright @shaikhabusufiyan2021

15. Clinical /Therapeutic Uses
•Bacterialmeningitis:Benzylpenicillin,highi.vdoses
•Boneandjointinfections:Flucloxacillin
•Skinandsofttissueinfections:benzylpenicillin,
flucloxacillin
•Animalbites:co-amoxiclav

16. •Pharyngitis: phenoxymethylpenicillin
•Otitis media: Amoxicillin
•Bronchitis: Amoxicillin
•Pneumonia: Amoxicillin
•UTI: Amoxicillin

17. •Gonorrhoea (Painful urinationand pain around the
urethra): Amoxicillin
•Syphilis (systemic infection cause by treponema
pallidum spirochetes): Procaine benzylpenicillin
•Endocarditis
•Serious infections with Pseudomonas aeruginosa:
•piperacillin.

18. Unwanted effects
•Penicillin'sarerelativelyfreefromdirecttoxiceffects.
•Themainunwantedeffectare
1.Hypersensitivityreactions
causedbythedegradationproductsofpenicillin
Combinewithhostprotein
becomeantigenic.

19. Symptoms:
•Skinrashesandfever
•Delayedtypeofserumsickness.
•Acuteanaphylacticshock.
2.Broad-spectrumpenicillingivenorally
alterthebacterialflorainthegut
Leadtogastrointestinaldisturbances.

20. Q&A: Activity II
Q.1 Name penicillin use for boneand jointinfection?
Q.2 Give few clinical uses of Amoxicillin
Q.3 What is main unwanted effect of penicillin?
Copyright @shaikhabusufiyan2021

21. Reference:
•H.PRang.MMDale,J.MRitter,R.JFlower,GHenderson.
Pharmacology,SeventhEdition.ElsevierChurchillLivengston
Publication.Pageno:625-626.
Copyright @shaikhabusufiyan2021

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