Tigecycline

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics

Brand Names

Europe

Austria: Tygacil; Belgium: Tygacil; Bulgaria: Tygacil; Cyprus: Tygacil; Czech Republic: Tygacil; Denmark: Tygacil; Estonia: Tygacil; Finland: Tygacil; France: Tygacil; Germany: Tygacil; Greece: Tygacil; Hungary: Tygacil; Ireland: Tygacil; Italy: Tygacil; Latvia: Tygacil; Lithuania: Tygacil; Netherlands: Tygacil; Poland: Tygacil; Portugal: Tygacil; Romania: Tygacil; Slovakia: Tygacil; Slovenia: Tygacil; Spain: Tygacil; Sweden: Tygacil; UK: Tygacil.

North America

Canada: Tygacil; USA: Tygacil.

Latin America

Argentina: Tygacil; Brazil: Tygacil; Mexico: Tygacil.

Drug combinations

Chemistry

Tigecycline: C~29~H~39~N~5~O~8~. Mw: 585.65. (1) 2-Naphthacenecarboxamide, 4,7-bis(dimethylamino)-9-[[[(1,1-dimethylethyl)amino]acetyl]amino]-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-, (4S,4aS,5aR,12aS)-; (2)(4S,4aS,5aR,12aS)-9-[2-(tert-butylamino)acetamido]-4,7-bis(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide. CAS-220620-09-7 (2002).

Pharmacologic Category

Antibacterials; Tetracyclines; Glycylcyclines. (ATC-Code: J01AA12).

Mechanism of action

Binds to 30S ribosomal subunit of susceptible bacteria, inhibiting protein synthesis.

Therapeutic use

Treatment of complicated skin and skin structure infections caused by susceptible organisms, including methicillin-resistant Staphylococcus aureus and vancomycin-sensitive Enterococcus faecalis. Treatment of complicated intra-abdominal infections.

Pregnancy and lactiation implications

Adverse effects observed in animals. Potential for permanent tooth discoloration. Frequently causes nausea and vomiting and therefore may not be ideal for use in pregnancy-related nausea. Excretion in breast milk unknown (use with caution in nursing women).

Unlabeled use

Contraindications

Hypersensitivity to tigecycline or any component of the formulation.

Warnings and precautions

May cause life-threatening anaphylaxis/anaphylactoid reactions. Due to structural similarity with tetracyclines, use with caution in prior hypersensitivity and/or severe adverse reactions associated with tetracycline use. May be associated with antianabolic effects observed with tetracycline class (including increased BUN, azotemia, acidosis, and hyperphosphatemia). Abnormal liver function tests (total bilirubin, prothrombin time, transaminases) reported. Isolated cases of significant hepatic dysfunction and hepatic failure occurred. Adverse hepatic effects may occur after drug discontinuation. May be associated with pancreatitis, photosensitivity, and with pseudotumor cerebri due to structural similarities with tetracyclines. Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis. Use with caution in hepatic impairment. Not indicated for treatment of pneumonia. Demonstrated inferior efficacy, including lower cure rates and increased mortality, in subgroup of patients with ventilator-associated pneumonia. Use with caution if using as monotherapy for intestinal perforation. Permanent discoloration of teeth may occur if used during tooth development (fetal stage through children up to 8 years of age).

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