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Tigecycline !

An IV glycylcycline that escapes the usual tetracycline resistance. Kept for complicated infections because of a boxed warning on mortality.

Updated 2026-11-01

  • Class: Tetracyclines
  • Target: Bacterial ribosome, 30S subunit (16S rRNA, A site)
  • ATC code: J01AA12

The figure shows tigecycline bound to the Escherichia coli 70S ribosome.

Target in 3D: Bacterial ribosome, 30S subunit (16S rRNA, A site). PDB structure 5J91 (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Tigecycline, a minocycline derivative, binds the 30S subunit more tightly than older tetracyclines and blocks aminoacyl-tRNA from the A site. It is little affected by the two main tetracycline resistance mechanisms, efflux pumps and ribosomal protection, nor by β-lactamases.

  1. Given IV and spreads widely into tissues
  2. Binds the 30S subunit tightly
  3. Aminoacyl-tRNA is blocked from the A site
  4. Even resistant bacteria stop growing

Pharmacokinetics

Distribution
Large volume of distribution, with low blood levels.
Elimination
Mainly bile, as unchanged drug and metabolites; kidney excretion is minor.

Indications

Adverse effects

Common

  • Nausea and vomiting, usually in the first days
  • Diarrhoea
  • Raised liver enzymes

Contraindications

  • Allergy to tigecycline or its excipients

Key interactions

Warfarin
Prothrombin time is checked.

What is monitored

  • Liver tests and coagulation, including fibrinogen, at baseline and during treatment
  • Abdominal pain (pancreatitis)
  • Clinical response

Administration and safety

  • IV infusion only
  • Reconstituted and diluted as the product describes; the solution is checked for colour and particles

Nursing care

  • Give antiemetics as ordered and watch fluid balance
  • Watch for bleeding or bruising
  • Report severe abdominal pain

Pregnancy and breastfeeding

Can cause fetal harm; like other tetracyclines it is avoided in the second half of pregnancy.

Test yourself

Think of the answer, then tap the question to see it.

Which resistance mechanisms does tigecycline largely escape?

Tetracycline efflux pumps and ribosomal protection proteins.

What is its boxed warning?

An increase in all-cause mortality compared with other antibiotics.

Which pneumonia is tigecycline not used for?

Hospital-acquired and ventilator-associated pneumonia.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - TIGECYCLINE injection, powder, lyophilized, for solution (DailyMed (U.S. National Library of Medicine), 2026); Tigecycline Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Structure of the Wild-type 70S E coli ribosome bound to Tigecycline (RCSB Protein Data Bank, 2026).

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Representative model, for educational purposes only.