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Macrolides
Macrolides
5
Pharmacology
Graduate
02/11/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
General Structure and Mechanims of Macrolides
Definition

Lactone ring +1 or more deoxy-sugars.

All are effective against MRSA, Moraxella Catarrhalis, H Influenza

Mostly static

 

Mechanism:

inhibits translocation from A to P site

release peptidyl tRNA from ribosome (premature)

block formation of initiation complex (cant get protein off the ground)

Term
Erythromycin
Definition
  • 1st drug effective against legionaires disease
  • Metabolites complex with cytochrome heme Fe & inhibit CYP3A4 (isozyme that metabolizes erythromycin)
  • Can prolong cardiac repolarization (Torsades de pointes) - be careful if used with another drug that inhibits CYP3A4
  • Increased risk of sudden death
  • Prokinetic - stimulates GI motility vs motilin receptors
Term
Azithromycin
Definition

concentrates intracellularly

 

Used for: community acquired pneumonia, legionaires disease, Mycobacterium avium complex

 

70hr 1/2-life. Does not inhibit P450 and is excreted unchanged in the bile

Term
Clarithromycin
Definition

for community acquired pneumoni and mycobacterium avium complex

Inhibits transcription of mRNA for proinflammatory cytokines (IL8, NFKB, AP1)

Can cause very low blood sugar

Inhibits CYP3A

Term
Telithromycin
Definition
  • a ketolide (macrolide derivative)
  • increased G+ activity
  • Same mechanism as macrolide but different domain (broader spectrum of activity)
  • Use - community acquired infections
  • Accumulates in pulmonary tissue, WBCs
  • Active vs beta-lacatams & macrolide resistant bacteria
  • Inhibits CYP3A4
  • Prolongs Q-T interval
  • BBW: dont use with myasthenia gravis
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