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Macrolides - Coggle Diagram
Macrolides
Activity/Use
Erythromycin
Similar to Pencillin
Use if patient has a Penicillin allergy
Gram + bacteria
Spirochaetes
Mycoplasma pneuomoniae
Legionella
Pneumonia
Legionairre's disease
Sometimes used in paediatrics for whooping cough
Azithromycin
H. influenzae
More active
Atypical organisms
Chlamydia trachomatis
Mycoplasma
Legionella
Pneumonia
Legionairre's disease
Toxoplasmosis gondii
Borrelia burgdorferi
Lyme disease
Clarithromycin
H. influenzae
Streptococcus pneumoniae
Mycobacterium avium intracellulare
Leprosy
H. pylori
Triple therapy
Borrelia burgdorferi
Pneumonia
Skin/soft tissue infection
Corynebacterium
Diptheria
Bordetella pertussis
Whooping cough
Campylobacter
Diarrhea
Side Effects
GIT disturbances
Nausea
Vomiting
Diarrhea
Prolonged QT interval
Need to do baseline/routine ECGs
Hypersensitivity reactions
Rash
Fever
Opportunistic infections of GIT + vagina
Cholestatic jaundice
Mechanism of Action
Binds to 50s subunit of bacteria ribosomes
Inhibits translocation
Prevents protein production by bacteria
Competes with Chloramphenicol
Structure
Multiple lactone rings with deoxy sugars attached
Bactericidal/bacteriostatic depending on concentration + type of organism
ADME
Administration
Oral
IV
Erythromycin
Phlebitis
Distribution
Most tissues
Crosses placenta
Does not cross...
BBB
Synovial fluid
Excretion/Metabolism
Liver metabolism (CYP450)
Erythromycin
Clarithromycin
Active metabolite inhibits P450 system
Azithromycin (less so)
Excreted in bile
Resistance
Plasmid-controlled alteration of binding site and activation of efflux pump
Examples
Erythromycin
Clarithromycin
First line oral agent for atypical pneumonia
Azithromycin