Tigecyclines

Question 1

What is the MOA of tigecyclines?

Answer 1

Shares same binding site as tetracyclines. Time and concentration dependent effects. Exhibits post-antibiotic effect. Bacteriostatic.

Question 2

What are the pharmacokinetics?

Answer 2

A - only available as parenteral product
D - excellent tissue and intracellular penetration PPB is 68%
M - Glucuronidation. Amide Hydrolysis
E - 36 hours <15% is excreted in urine as unchanged drug.

Question 3

What is the spectrum of activity?

Answer 3

MRSA, MSSA, Strep. Pneumoniae, Vancomycin sensitive enterococcus faecali, Vancomycin resistant E.faecium, Listeria sp.

Question 4

What are gaps in the spectrum?

Answer 4

P.aeruginosa, proteus sp.

Question 5

What are some of its clinical uses?

Answer 5

Complicated infections (skin and soft tissue infections)
MDR infections, Activity against most gram- pathogens

Question 6

What are some adverse effects?

Answer 6

Nausea, Vomiting, Diarrhoea

Question 7

What is a warning for tigecyclines?

Answer 7

Increase in mortality and treatment failure. Reserve when no suitable alternatives.