Macrolides

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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