Merck Manual

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Brian J. Werth

, PharmD, University of Washington School of Pharmacy

Reviewed/Revised May 2022

Tigecycline, a derivative of the tetracycline minocycline, is the first available glycylcycline antibiotic Overview of Antibacterial Drugs Antibacterial drugs are derived from bacteria or molds or are synthesized de novo. Technically, “antibiotic” refers only to antimicrobials derived from bacteria or molds but is often (including... read more Overview of Antibacterial Drugs . 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. 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. No dosing adjustment is required in patients who have renal insufficiency.

Indications for Tigecycline

Tigecycline is effective against many resistant bacteria, including those with resistance to tetracyclines. Tigecycline has in vitro activity against the following:

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 Hospital-Acquired Pneumonia Hospital-acquired pneumonia (HAP) develops at least 48 hours after hospital admission. The most common pathogens are gram-negative bacilli and Staphylococcus aureus; antibiotic-resistant... read more ) 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 to Tigecycline

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

Tigecycline has a black box warning because it increases the risk of mortality and so should be reserved for situations where there are no suitable alternatives.

Use During Pregnancy and Breastfeeding

Tigecycline, like tetracyclines Use During Pregnancy and Breastfeeding Tetracyclines are bacteriostatic antibiotics that bind to the 30S subunit of the ribosome, thus inhibiting bacterial protein synthesis. Specific tetracyclines are Doxycycline Eravacycline (IV... read more Use During Pregnancy and Breastfeeding , 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 of Tigecycline

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 Adverse Effects Tetracyclines are bacteriostatic antibiotics that bind to the 30S subunit of the ribosome, thus inhibiting bacterial protein synthesis. Specific tetracyclines are Doxycycline Eravacycline (IV... read more Adverse Effects (eg, photosensitivity).

Dosing Considerations for Tigecycline

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.

Drugs Mentioned In This Article

Drug Name Select Trade
Emtet-500, Panmycin, Sumycin
Amzeeq, Arestin, Dynacin, Minocin, minolira, Myrac, Solodyn, Ximino, Zilxi
FIRVANQ, Vancocin, Vancocin Powder, VANCOSOL
Coumadin, Jantoven
NOTE: This is the Professional Version. CONSUMERS: View Consumer Version
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