Tigecycline

Intravenous
Community-acquired pneumonia

Intravenous
Complicated intra-abdominal infections, Complicated skin and skin structure infections

No dosage adjustment needed.

Mild to moderate: No dosage adjustment. Severe: 100 mg as a single dose, then 25 mg 12 hrly.

Reconstitute 50 mg vial w/ 5.3 mL of NaCl 0.9% inj or dextrose 5% inj or Lactate Ringer's inj to achieve a concentration of 10 mg/mL. For IV bag infusion: Further dilute a 5 mL reconstituted soln w/ 100 mL of IV bag for infusion. For a 100 mg dose: Reconstitute two 50 mg vials and dilute 10 mL of the reconstituted soln in 100 mL of IV infusion soln. For a 50 mg dose: Further dilute a 5 mL reconstituted soln w/ 100 mL of NaCl 0.9% inj or dextrose 5% inj. Concentration of infused soln should not exceed 1 mg/mL. The reconstituted soln should be yellow to orange only.

Y-site: Amphotericin B, amphotericin B lipid complex, diazepam, omeprazole , esomeprazole or any IV soln that may result in a pH above 7.

Hypersensitivity. Hospital-acquired pneumonia and ventilator-associated pneumonia. Use during tooth development.

Hypersensitivity to tetracyclines. Use tigecycline in situations when alternative treatments are not suitable. Patients w/ complicated intra-abdominal infections secondary to clinically apparent intestinal perforation. Hepatic impairment. Pregnancy and lactation.

Nausea, vomiting, diarrhoea, abdominal pain, anorexia, headache, dizziness, jaundice, abscess, dyspepsia, acidosis, hypoproteinemia, thrombophlebitis, photosensitivity, inj site reactions, pruritus, rash, overgrowth of nonsusceptible organisms (e.g. fungi), Clostridium-difficile associated diarrhoea, prolonged prothrombin time (PT) and aPTT increased ALT, AST, alkaline phosphatase and bilirubin.
Potentially Fatal: Sepsis or septic shock. Anaphylaxis and anaphylactoid reactions. Acute pancreatitis. Fatal colitis. Liver impairment w/ fatal liver failure.

IV/Parenteral: D

Increased warfarin serum levels. May decrease efficacy of oral contraceptives.

Description: Tigecycline is a glycylcycline antibiotic which prevents protein synthesis of the susceptible bacteria by binding to its 30s ribosomal subunit. It is generally considered as bacteriostatic agent; w/ bactericidal activity against S. pneumonia and L. pneumophilia. Tigecycline antibacterial activity covers facultative gm+ve (including MRSA, vancomycin-susceptible Enterococcus faecalis) and gm-ve bacteria, and anaerobic bacteria.
Pharmacokinetics:
Absorption: Bioavailability: 100%.
Distribution: Widely distributed; crosses the placenta. Volume of distribution: 7-9 L/kg. Plasma protein binding: 71-89%.
Metabolism: Not extensively metabolised, resulting in trace amount of glucuronide, N-acetyl metabolite and tigecycline epimer.
Excretion: Via faeces: 60% (mainly as unchanged drug); urine: 33% (approx 22% as unchanged drug). Elimination half-life: 42 hr (following multiple doses).

Unopened vial: Store between 20-25°C. Reconstituted soln: 24 hr at room temperature (up to 6 hr in vial). IV infusion bag diluted w/ NaCl 0.9% inj or dextrose 5% inj: 48 hr between 2-8°C.

Tetracyclines

Anon. Tigecycline. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/11/2013.

Buckingham R (ed). Tigecycline. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/11/2013.

Joint Formulary Committee. Tigecycline. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/11/2013.

McEvoy GK, Snow EK, Miller J et al (eds). Tigecycline. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 11/11/2013.

Tygacil (tigecycline): Drug Safety Communication - Increased Risk of Death. U.S. FDA. https://www.fda.gov/. Accessed 11/11/2013.