Macrolides.pdf
- 1. Prof. Shaikh Abusufiyan Assistant Professor, AIKTC-School of Pharmacy, New Panvel-410206 Antibiotics: Macrolide Pharma Learning Forever
- 2. At the end of this e-learning session you are able to… A. Discuss Mechanism of action of Macrolide B. Give classification and Explain pharmacology of Macrolide. Copyright @shaikhabusufiyan2021
- 3. Macrolide • The term 'macrolide' a many membered lactone ring to which one or more deoxy sugars are attached. • Erythromycin --> the first member discovered in the 1950. • The two most important macrolides are clarithromycin and azithromycin.
- 4. MOA • The macrolides inhibit bacterial protein synthesis by inhibiting translocation. • Their action may be bactericidal or bacteriostatic the effect depending on the concentration and on the type of microorganism.
- 5. • The drugs bind to the 50S subunit of the bacterial ribosome • The binding site is the same as that of Chloramphenicol and Clindamycin they could compete, if given concurrently.
- 6. Antimicrobial spectrum • Very similar to that of penicillin • Safe and effective alternative for penicillin- sensitive patients. • It is effective against • Gram-positive bacteria and spirochaetes • But not against most Gram-negative organisms
- 7. Resistance • Resistance can occur and results from a plasmid-controlled alteration of the binding site for erythromycin on the bacterial ribosome.
- 8. Azithromycin • It is less active against Gram-positive bacteria than erythromycin • It is considerably more effective against H. influenzae and may be more active against Legionella. • It has excellent action against Toxoplasma gondii, killing the cysts.
- 9. Clarithromycin • It is as active, against H. influenzae as erythromycin. • But its metabolite has twice activity against H. influenzae as erythromycin. • It may be useful in leprosy and against Helicobacter pylori.
- 10. Pharmacokinetic aspects: • The macrolides are administered orally • Azithromycin and Clarithromycin are more acid stable than erythromycin. • Erythromycin can also be given parenterally.
- 11. Pharmacokinetic aspects......... • Do not cross the blood-brain barrier • It has poor penetration into synovial fluid • Macrolides are concentrated within phagocytes • Azithromycin concentrations in phagocyte lysosomes can be 40 times higher than in the blood can enhance phagocyte killing of bacteria.
- 12. Plasma Half life: • Erythromycin - about 90 minutes • Clarithromycin - three times longer then erythromycin • Azithromycin - 8-16 times longer then erythromycin
- 13. Unwanted effect • Gastrointestinal disturbances with erythromycin • Hypersensitivity reactions such as: • skin rashes • and fever • Transient hearing disturbances • Cholestatic jaundice--> rarely, with treatment longer than 2 weeks. • Opportunistic infections of the gastrointestinal tract or vagina.
- 14. Reference: • H.P Rang. M M Dale, J.M Ritter, R.J Flower, G Henderson. Pharmacology, Seventh Edition. Elsevier Churchill Livengston Publication. Page no:631-632
- 15. 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.