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Antibiotics: Penicillin.pdf
- 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 history and Mechanism of action of Penicillin B. Give classification and 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 • Its remarkable antibacterial effects in humans were demonstrated in 1941. • A small amount of penicillin (extracted from crude cultures in the laboratories) • Tested on a policeman (staphylococcal and streptococcal septicaemia with multiple abscesses, and osteomyelitis with discharging sinuses).
- 5. • He was in great pain and was desperately ill. (Sulfonamides were available but would have had no effect in the presence of pus) • IV injections of penicillin were given every 3 hours. • All the patient's urine was collected and each day the excreted penicillin was extracted and used again.
- 6. Result: • After 5 days, the patient's condition was vastly improved • his temperature was normal • he was eating well • resolution of the abscesses. • no toxic effects of the drug. • Then the supply of penicillin ran out • His condition gradually deteriorated • He died a month later.
- 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.Semisynthetic penicillin’s: by adding different side-chains to the penicillin nucleus (at R1). 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. Naturally occurring benzylpenicillin • Benzylpenicillin is active against a wide range of organisms • And is the drug of first choice for many infections. Drawbacks: • Poor absorption in the gastrointestinal tract (it must be given by injection) • And it is susceptible to bacterial β-lactamases.
- 11. Pharmacokinetics Route of administration: - Oral route: different penicillin are absorbed to different degree depending on their acid stability. -It can be given by IM or IV injection - Intrathecal administration --> is inadvisable, particularly with benzylpenicillin as it can cause convulsion.
- 12. Distribution: - Widely distributed into body fluid - Passing into - Joint - Pleural and pericardial cavity - Saliva - Milk - Placenta l Do not cross BBB- lipid insoluble
- 13. l Elimination: - Eliminated through urine l Short plasma half life is 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 • Bacterial meningitis : Benzylpenicillin, high i.v doses • Bone and joint infections : Flucloxacillin • Skin and soft tissue infections: benzylpenicillin, flucloxacillin • Animal bites: co-amoxiclav
- 16. • Pharyngitis : phenoxymethylpenicillin • Otitis media : Amoxicillin • Bronchitis : Amoxicillin • Pneumonia: Amoxicillin • UTI : Amoxicillin
- 17. • Gonorrhoea (Painful urination and 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's are relatively free from direct toxic effects. • The main unwanted effect are 1. Hypersensitivity reactions caused by the degradation products of penicillin Combine with host protein become antigenic.
- 19. Symptoms: • Skin rashes and fever • Delayed type of serum sickness. • Acute anaphylactic shock. 2. Broad-spectrum penicillin given orally alter the bacterial flora in the gut Lead to gastrointestinal disturbances.
- 20. Q&A: Activity II Q.1 Name penicillin use for bone and joint infection? Q.2 Give few clinical uses of Amoxicillin Q.3 What is main unwanted effect of penicillin? Copyright @shaikhabusufiyan2021
- 21. Reference: • H.P Rang. M M Dale, J.M Ritter, R.J Flower, G Henderson. Pharmacology, Seventh Edition. Elsevier Churchill Livengston Publication. Page no:625-626. Copyright @shaikhabusufiyan2021
- 22. Disclaimer (Images) • The images used in this presentation are found from different sources all over the Internet, and are assumed to be in public domain and are displayed under the fair use principle for education purpose. Copyright @ Presentation • The said presentation is copyright under Copyright @shaikhabusufiyan2021 • The presentation is for education purpose only, don’t use the same for any legal perspective.