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spriomycin
Erythromycin
classification of macrolides
route of administration
MOA:
reversibly inhibit 50S subunit of bacterial ribosome
by “dual MOA”
Macrolide, Chloramphenicol, Clindamycin may competitively inhibit each other activity
Cidal/ Static:
Pharmacokinetics of Macrolides:
Absorption:
Erythromycin
Erythromycin is given as:
The best absorption is obtained with
absorption
Azithromycin, Roxithromycin ,Clarithromycin &Telithromycin
Distribution
Azithromycin > Clarithromycin → has unique pharmacokinetic properties
Azithromycin is taken up extensively in high amounts by “tissues”
unique properties of azithromycin permit once-daily dosing & shortening of the duration of treatment in many cases
how??
Metabolism & Excretion
Macrolides
Advantages of newer 2nd -Generation macrolides
Azithromycin
(Azithromycin has no effect on hepatic metabolizing enzyme)
Resistance is becoming increasingly common& occurs by one of several mechanisms
Efflux & methylase production are the most important resistance mechanisms in
Resistance Macrolides
- Complete cross-resistance between Erythromycin & the other Macrolides
Partial cross-resistance
Antibacterial spectrum of activity of Telithromycin,Clarithromycin & Azithromycin
Antibacterial spectrum of activity of Telithromycin,Clarithromycin & Azithromycin
Some/few Gram -ve organisms
Ketolides:
As Telithromycin orally
Telithromycin is active against many
Teilthromycin is limited by
antimicrobial spectrum of Teilthromycin
Therapeutic uses of Erythromycin
Therapeutic uses of Azithromycin
Therapeutic uses of Clarithromycin
Therapeutic uses of Macrolide
Older-generation (Erythromycin)
MLCDPSS
Mycoplasma pneumoniae
Legionnaire’s pneumonia
Chlamydia pneumoniae
: Macrolides in
Chlamydia pneumoniae
Tetracyclines in
Chlamydia pneumoniae
Diphtheria
Macrolide (Erythromycin) is very effective for eliminating the carrier state
Pertussis (Whooping cough) caused by
Bordetella pertussis
“alternative” in patient who are allergic to PenicillinG
Macrolides good for!!!
URTIs
TX of
H. influenza
TX of
M. catarehalis
Empiric Tx
Acute otitis media
Empiric Tx
CAP
Q- A 54- year-old man with no significant past medical history who presents with CAP of
mild-moderate severity. He is probably allergic to Penicillin
A 27-year-old pregnant patient with a history of pyelonephritis has developed a severe upper respiratory infection that appears to be due to a bacterial pathogen. The woman is hospitalized. Which Macrolide is to be selected for treatment!
Antimicrobial drugs that are eliminated via hepatic metabolism or biliary excretion include
pseudomembranous colitis has been
associated with the use of many agents including
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