Tigecycline, a derivative of the tetracycline minocycline, is the first available glycylcycline. Tigecycline inhibits protein synthesis by binding to the 30S ribosomal subunit. It is bacteriostatic.
Tigecycline is given IV. Tigecycline has a large volume of distribution (> 12 L/kg), penetrating well into bone, lung, liver, and kidney tissues. A half-life of 36 h should provide for once/day dosing. Most of the drug is excreted in bile and feces.
Tigecycline is effective against many resistant bacteria, including those with resistance to tetracyclines. Tigecycline is active against
It is not effective against Pseudomonas aeruginosa, Providencia sp, Morganella morganii, or Proteus sp.
Tigecycline is indicated for complicated skin and soft-tissue infections and complicated intra-abdominal infections, but the drug shows promise for other infections as well. Clinically, tigecycline is used mainly for the following:
Tigecycline is contraindicated in patients who have had an allergic reaction to it and in children ≤ 8 yr.
Use During Pregnancy and Breastfeeding
Tigecycline is in pregnancy category D (there is evidence of human risk, but clinical benefits may outweigh risk); it, like tetracyclines, can affect fetal bones and teeth.
Whether tigecycline enters breast milk and is safe to use during breastfeeding is unknown.
Adverse effects include
Nausea and vomiting are common. Increases in serum amylase, total bilirubin concentration, PT, and transaminases can occur in patients treated with tigecycline. Isolated cases of significant hepatic dysfunction and hepatic failure have been reported in patients being treated with tigecycline. Many of tigecycline's adverse effects are similar to those of tetracyclines (eg, photosensitivity).
Dose is adjusted in patients with hepatic dysfunction but not in those with renal dysfunction. Serum levels of warfarin may increase, but INR does not appear to increase.
Last full review/revision July 2009 by Matthew E. Levison, MD