Merck Manual

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Tigecycline

By

Brian J. Werth

, PharmD, University of Washington School of Pharmacy

Last full review/revision May 2020| Content last modified May 2020
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NOTE: This is the Professional Version. CONSUMERS: Click here for the Consumer Version

Tigecycline, a derivative of the tetracycline minocycline, is the first available glycylcycline antibiotic. Tigecycline inhibits protein synthesis by binding to the 30S ribosomal subunit. It is bacteriostatic.

Pharmacokinetics

Tigecycline is given IV. Tigecycline has a large volume of distribution (> 12 L/kg), penetrating well into bone, lung, liver, and kidney tissues. However, because of its extensive distribution into tissue, blood levels are low, so tigecycline is probably not a good choice for patients with bacteremia especially those with intravascular sources of infection.

Most of the drug is excreted in bile and feces.

Indications

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 species, Morganella morganii, or Proteus species.

Tigecycline is indicated for

However, a recent meta-analysis showed that patients treated with tigecycline (particularly those treated for ventilator-associated pneumonia) had a higher mortality than those given other antibiotics, resulting in a black box warning from the U.S. Food and Drug Administration. In general, tigecycline should be reserved for infections with multidrug-resistant (MDR) organisms when other treatment options are more toxic or less effective. Because of its parenteral activity against C. difficile, tigecycline may be a useful antibiotic when a patient requires concurrent treatment of an MDR infection and a C. difficile infection.

Contraindications

Tigecycline is contraindicated in patients who have had an allergic reaction to it and in children < 8 years.

Use During Pregnancy and Breastfeeding

Tigecycline, like tetracyclines, can affect fetal bones and teeth. If a pregnant woman takes it during the 2nd or 3rd trimester, it may cause permanent discoloration of the fetus's teeth.

Whether tigecycline enters breast milk and is safe to use during breastfeeding is unknown; however, it has limited oral bioavailability.

Adverse Effects

Adverse effects of tigecycline include

  • Nausea, vomiting, and diarrhea

  • Photosensitivity

  • Hepatotoxicity

Nausea and vomiting are common. Increases in serum amylase, total bilirubin concentration, prothrombin time, 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).

Dosing Considerations

Dose is adjusted in patients with hepatic dysfunction but not in those with renal dysfunction.

Serum levels of warfarin may increase, but international normalized ratio does not appear to increase.

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NOTE: This is the Professional Version. CONSUMERS: Click here for the Consumer Version
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