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Infection and Immunity 2- Lecture 9
Macrolides and Ketolides
14
Medical
Professional
04/29/2013

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Cards

Term
Describe the structure of macrolide antibiotics
Definition
14 or 15 member lactone ring
Term
Erythromycin is a ___ with activity against ___
Definition

a (14 member) macrolide

 

against S. aureus, Strep., Atypical pneumonias: Mycoplasma, Chalmydia, Legionella, URIs, STDs

Term

Clarithromycin is a ___ with activity against ___

 

It's better than Erythromycin in treating ___ (3)

Definition

a macrolide

 

same as erythromycin + better for chlamydia, MSSA, strep

 

also against H. influenza and other stuff

Term

Azithromycin is a ___

+

Is less effective than erythromycin at treating ___ and ___

+

Is better at treating ___

Definition

Less effective at S. aureus and Strep.

 

Better at H. influenza

Term
Describe the MOA of Macrolides
Definition
Inhibit protein synthesis by binding to the 23S ribosomal subunit of bacteria (inhibits tRNA translocation)
Term

- Name the resistance gene for bacteria that allows them to modify their 23S rRNA and avoid macrolides

- Name 2 pathogens that may have this gene

Definition

23S rRNA modification (is called MLSB phenotype)

 

Resistance gene is called "erm"

 

Staph. and Strep. may have it

Term

Name 3 pathogens that may have a gene to pump out macrolide and are thereby resistant.

What is the name of this gene?

Definition

S. pyogenes, S. pneumoniae, Group C strep

 

"mef" gene, M phenotype

Term

Erythromycin

- how excreted

- where it concentrates

Definition

excreted in bile

 

concentrates in neutrophils and macrophages

Term

Clarithromycin

- % bioavailability

- how excreted

- where it concentrates

Definition

50%

excreted in bile OR by kidneys

concentrates in neutrophils (more than erythromycin)

Term
Which macrolide DOESN"T interact with P-450?
Definition
Azithromycin
Term
Compare Azithromycin to the other macrolides in terms of dispersion and elimination.
Definition

Higher tissue penetration

huge concentration in phagocytes

hepatic elimination

no drug interactions

Term
3 possible adverse effects of erythromycin
Definition

GI upset, diarrhea

QT prolongation (when in IV form)

Pyloric stenosis

Term
8 pathogens that are major indications for macrolide treament
Definition
Mycoplasma pneumonia
Legionellosis
Diphtheria
Pertussis
Chlamydia, neonatal and STD
Campylobacter gastroenteritis
Mycobacterium avium complex
Helicobacter
Term
What is a ketolide?
Definition
A new type of macrolide that's more acid stable and works better (+ less resistance to it)
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