Protein Synthesis Inhibitors Flashcards
Macrolides MOA
Inhibition of protein synthesis, binds 50S ribosomal subunit, selective toxicity - no binding to mamillian ribosome. Bacteriostatic
Macrolide Examples
Erythromycin
Clarithromycin
Azithromycin
Macrolide distribution
Wide, except for CNS. Crosses placenta
Erythromycin Metabolism/excretion
Liver, excreted in bile. Avoid in liver disease.
Excreted in breast milk - check infants for thrush
Clarithromycin metabolism/excretion
Renally eliminated, may require adjustment
Excreted in breast milk - check infants for thrush
Macrolide uses, gram + cocci
alternative in penicillin allergic patients
Streptococci (phayngitis), pneumococci (pneumonia)
Macrolide uses, gram - cocci
Moraxella catarrhalis (otitis media, community acquired pneumonia)
Macrolide uses, gram - bacilli
H. influenzae –> upper respiratory infections, bronchitis
Azithromycin and Clarithromycin are the best
Macrolide uses, atypicals
Chlmydia (trachoma, community acquired pneumonia, urethritis) -- Azithromycin Mycoplasma pneumoniae (community-acquired pneumonia)
Azythromycin Metabolism
NOT metabolized, high tissue penetration
Excreted in breast milk, check infant for thrush
Macrolide drug interactions
Erythromycin and clarithromycin are inhibitors of cytochrome p450
Macrolide heart ADR
prolongs the QT interval – caution with other QT-prolonging drugs
Tetracycline MOA
Inhibition of bacterial protein synthesis, binds 30S ribosome, selective toxicity due to human cell ability to efflux the drug. Bacteriostatic
Tetracycline Examples
Doxycycline
Minocycline
Tetracycline Absorption
Give on an empty stomach, impaired by milk products