Macrolides - The Veterinary Site

Macrolides


Macrolides and Ketolides 
(by MAAZ AHMED SIDDIQUI)

Macrolides
Ketolides
FDA Approved
Non-FDA Approved

1)      Erythromycin
§  It can be used in patients allergic to Penicillin
2)      Clarithromycin
§  It is methylated erythromycin
§  Its spectrum is similar to Erythromycin
3)      Azithromycin
4)      Telithromycin
5)      Roxithromycin
1)      Spiramycin
§  It is Europe approved
2)      Midecamycin
3)      Tylosin
§  Approved for animal use
4)      Solithromycin
5)      Josamycin

1)      Telithromycin
2)      Ansamycin
3)      Cethromycin
4)      Oleandomycin
5)      Carbomycin
6)      Tilmicosin

Macrolides contain macrocyclic lactone ring or structure attached to one or more deoxyribose sugars. These are drug of choice for lower and upper respiratory infections. Macrolides are bacteriostatic in low concentration while bactericidal in high concentration.
Mode of Action
These bind reversibly to 50S ribosomal subunit and inhibit the translocation (mRNA => Protein) step in the protein synthesis.
Resistance
There are 3 basic reasons for resistance development against tetracyclines:
1)      Less influx, more efflux
·         There is less uptake of macrolides by bacteria
2)      Less affinity for 50S ribosomal subunit to attach with macrolides and ketolides
3)      Plasma associated enzymes i.e. erythromycin esterase are produced which cause inactivation of macrolides especially Erythromycin and Clarithromycin
Why Macrolides should be our choice??
Macrolides should be choice due to their high concentration at infection site rather than blood because these conjugate with cytosolic proteins of macrophages, neutrophils and fibroblasts. As these immune cells reach the infection site in high proportion and release their cytosolic proteins conjugated with macrolides after dying in the battle with pathogens, the macrolides will also be released.
þ  Always consider drug interactions of macrolides with other drugs i.e. Cimetidine
Adverse effects of Macrolides & Ketolides
®  Cholestatic jaundice
®  Epigastric disturbance
®  Ototoxicity

þ  Don’t administer in renal and hepatic compromised patients


Macrolides Macrolides Reviewed by Maaz ahmed siddiqui on 09 May Rating: 5

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