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Overview of Macrolides by Mind Map: Overview of Macrolides
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Overview of Macrolides

General information


large macrocyclic lactone ring to which deoxy sugars are attached

fist macrolide was erythromycin

semi-synthetic derivatives (commonly used)




Ketolides are active against some macrolide-resistant strains

semi-synthetic derivatives

example: telithromycin

Mechanism of action

bacteriostatic (inhibit protein synthesis)

binds irreversibly to 50 S ribosomes

same or close to binding site of chloramphenicol (so they antagonize each other)

Antimicrobial spectrum

gm+, and to lesser extend gm- cocci. gm- bacilli are resistant


clarithromycin is superior especially with strept. pygenes and strept. pneumoniae

cocci, streptococci, staphylococci











absorbed from upper small intestines (enteric coated tablet)

food delay absorption but reduce side effects

plasma protein binding affinity 70-80%

5-20% of serum concentration crosses placenta

50% in milk


rapidly absorbed from GI

reduced bioavailability due to first pass metabolism, metabolized in the liver to 14 hydroxy clarithromycin (active form)

tissue concentration > serum co.

plasma protein binding affinity 40-70%

elimination half life 3-7 hours, and 5-9 hours for the active form


rapid and widely distributed (except brain and CSF)

plasma protein binding 50%

12% eliminated unchanged in urine

elimination half life is 40-68 hours due to extensive distribution

Therapeutic uses

Respiratory tract infections

erythromycin, upper and lower reps. tract infection, strept. pyogenes, strept. pneumoniae, mycoplasma pneumonia, whooping cough (B. pertussis)

clarithromycin and azithromycin, mild to moderate community acquired pneumonia

Skin and soft tissue infections

alternative agents, strept. pyogenes, staph. aureus


Erythromycin 250mg

Campylobacter infections

gastroenteritis, erythromycin 250-500mg

Helicobacter pylori infection

peptic ulcer is treated by combination of, clarithromycin 500mg, omeprazole 20mg, amoxicillin 1gm

Mycobacterial infections

clarithromycin or azithromycin

treating M. avium in AIDS patients

pulmonary disease in non HIV patients

Prophylactic uses

erythromycin, alternative for patients allergic to penicillin, prophylaxis of rheumatic fever

clarithromycin or azithromycin, alternatives for prevention of bacterial endocarditis for patients doing dental procedures

Adverse effects

Erythromycin causes heptotoxicity and epigastric distress

clarithromycin and azithromycin have the same side effects but at lower rate

Erythromycin and clarithromycin causes ventricular techycardia

allergenic reactions may occur

ototoxicity after IV erythromycin (deafness)

Drug interactions

Erythromycin and clarithromycin inhibit CYP3A4, thus increase the effect of these drugs, carbamzepine, corticosteroids, cyclosporine, digoxin, theophylline, valproate, warfarin