Macrolides.pdf

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.

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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 classificationand Explain
pharmacology of Macrolide.
Copyright @shaikhabusufiyan2021

3. Macrolide
•Theterm'macrolide'
amanymemberedlactoneringtowhichoneormore
deoxysugarsareattached.
•Erythromycin-->thefirstmemberdiscoveredinthe
1950.
•Thetwomostimportantmacrolidesareclarithromycin
andazithromycin.

4. MOA
•Themacrolidesinhibitbacterialproteinsynthesisbyinhibitingtranslocation.
•Theiractionmaybebactericidalor
bacteriostatic
theeffectdependingontheconcentration
andonthetypeofmicroorganism.

5. •Thedrugsbindtothe50Ssubunitofthe
bacterialribosome
•Thebindingsiteisthesameasthatof
ChloramphenicolandClindamycin
theycouldcompete,ifgivenconcurrently.

6. Antimicrobial spectrum
•Very similar to that of penicillin
•Safe and effective alternativefor penicillin-
sensitive patients.
•It is effective against
•Gram-positive bacteria and spirochaetes
•But not against most Gram-negative organisms

7. Resistance
•Resistancecanoccurandresultsfrom
aplasmid-controlledalterationofthebindingsitefor
erythromycinonthebacterialribosome.

8. Azithromycin
•ItislessactiveagainstGram-positivebacteriathan
erythromycin
•ItisconsiderablymoreeffectiveagainstH.influenzae
andmaybemoreactiveagainstLegionella.
•IthasexcellentactionagainstToxoplasmagondii,
killingthecysts.

9. Clarithromycin
•Itisasactive,againstH.influenzaeas
erythromycin.
•ButitsmetabolitehastwiceactivityagainstH.
influenzaeaserythromycin.
•Itmaybeusefulinleprosyandagainst
Helicobacterpylori.

10. Pharmacokinetic aspects:
•Themacrolidesareadministeredorally
•AzithromycinandClarithromycinaremore
acidstablethanerythromycin.
•Erythromycincan also be given
parenterally.

11. Pharmacokinetic aspects.........
•Donotcrosstheblood-brainbarrier
•Ithaspoorpenetrationintosynovialfluid
•Macrolidesareconcentratedwithinphagocytes
•Azithromycinconcentrationsinphagocytelysosomes
canbe40timeshigherthanintheblood
canenhancephagocytekillingofbacteria.

12. PlasmaHalflife:
•Erythromycin -about 90 minutes
•Clarithromycin -three times longer then
erythromycin
•Azithromycin -8-16 times longer then
erythromycin

13. Unwanted effect
•Gastrointestinal disturbanceswith 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.PRang.MMDale,J.MRitter,R.JFlower,GHenderson.
Pharmacology,SeventhEdition.ElsevierChurchillLivengston
Publication.Pageno:631-632

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Copyright @ Presentation
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•Thepresentationisforeducationpurposeonly,don’tusethesameforanylegal
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16. Copyright @shaikhabusufiyan2021