Tigecycline

Indications
Intravenous
Complicated intra-abdominal infections
Adult: 100 mg as a single dose, followed by 50 mg every 12 hr for 5 to 14 days. Infuse dose over 30-60 minutes.
Hepatic impairment: Child-pugh classes A and B: no dosage adjustment. Child-Pugh class C: 100 mg as a single dose, then 25 mg every 12 hr.
Intravenous
Complicated skin and skin structure infections
Adult: 100 mg as a single dose, followed by 50 mg every 12 hr for 5 to 14 days. Infuse dose over 30-60 minutes.
Hepatic impairment: Child-pugh classes A and B: no dosage adjustment. Child-Pugh class C: 100 mg as a single dose, then 25 mg every 12 hr.
Intravenous
Community-acquired pneumonia
Adult: 100 mg as a single dose, followed by 50 mg every 12 hr for 7 to 14 days. Infuse dose over 30-60 min.
Hepatic impairment: Child-pugh classes A and B: no dosage adjustment. Child-Pugh class C: 100 mg as a single dose, then 25 mg every 12 hr.

Reconstitution: Reconstitute 50 mg vial with 5.3 ml of 0.9% sodium chloride inj or 5% dextrose inj or Lactate Ringer's inj to achieve a concentration of 10 mg/ml. Swirl the vial gently till the drug dissolves and immediately withdraw 5 ml of the reconstituted solution and dilute in 100 ml of IV bag for infusion. For a 100 mg dose, reconstitute two 50-mg vials and dilute 10 ml of the reconstituted solution in 100 ml of IV infusion solutions. Concentration of infused solutions should not exceed 1 mg/ml. The reconstituted solutions should be yellow to orange only. Otherwise, it should be discarded.
Incompatibility: Incompatible (Y-site): Amphotericin B, amphotericin B lipid complex, diazepam, omeprazole , esomeprazole. Compatible (Y-site): Amikacin, dobutamine, dopamine HCl, gentamicin, haloperidol, Lactated Ringer's, lidocaine HCl, metoclopramide, morphine, norepinephrine, piperacillin/tazobactam (EDTA formulation), potassium chloride, propofol, ranitidine HCl, theophylline, and tobramycin. Compatible IV solutions: 0.9% Sodium chloride inj, 5% Dextrose inj, and Lactated Ringer's inj.
Contraindications
Hypersensitivity to Tigecycline or tetracycline class of antibiotics.
Warnings / Precautions
Pregnancy (use may cause fetal harm), lactation, children <18 yr (safety and efficacies not established). Hepatic dysfunctions, liver failure and pancreatitis (including fatalities) have been reported. Not to be use during tooth development (last half of pregnancy, infancy, and childhood up to 8 yr) as it may cause permanent teeth discolouration. Treatment may cause superinfection and Clostridium difficile associate diarrhoea. An increase in all-cause mortality has been observed in Tigecycline-treated patients versus comparator-treated patients (cause of increase has not been established). Not recommended for treatment of hospital-acquired pneumonia and ventilator-associated pneumonia. Caution in patients with complicated intra-abdominal infections secondary to clinically apparent intestinal perforation.
Adverse Reactions
Nausea, vomiting, diarrhoea, abdominal pain, anorexia, headache, dizziness, pancreatitis, jaundice, hepatic cholestasis, liver failure, Clostridium-difficile associated diarrhoea, infection, abscess, thrombophlebitis, injection site reactions, pruritus, rash, hypoproteinemia, thrombocytopenia, prolonged prothrombin time (PT), prolonged activated partial thromboplastin time (aPTT), increased INR, increased creatinine; increased ALT, AST, alkaline phosphatase and bilirubin.
Potentially Fatal: Sepsis and anaphylaxis.
Overdose Reactions
Increased nausea and vomiting were observed when healthy volunteers were given 300 mg of IV single dose. No information available on treatment of overdose; Tigecycline is not removed significantly by haemodialysis.
Drug Interactions
Warfarin serum concentrations may be increased due to reduced clearance; monitor PT if both drugs are used concurrently.
See Below for More tigecycline Drug Interactions
Mechanism of Actions
Tigecycline is a glycylcycline antibiotic and exhibits its antibacterial action by reversible binding to the 30S subunits of the ribosome, thus preventing the binding of aminoacyl tRNA and the incorporation of amino acids into the elongating peptide chains. It is generally considered as bacteriostatic agent; with bactericidal activity against S. pneumonia and L. pneumophilia. Tigecycline antibacterial activity covers facultative Gram-positive (including MRSA, vancomycin-susceptible Enterococcus faecalis) and Gram-negative bacteria, and anaerobic bacteria.
Distribution: Widely distributed, Vd: 7-9 L/kg. Plasma protein binding: 71-89% (in vitro).
Metabolism: Not extensively metabolised, resulting in trace amount of glucuronide, N-acetyl metabolite and Tigecycline epimer (each constitutes <10% of dose).
Excretion: Via faeces: 60% (mainly as unchanged drug); Via urine: 33%(about 22% as unchanged drug). Terminal elimination half-life: 42 hr (following multiple doses).
Storage Conditions
Intravenous: Unopened vial: Store at 20-25°C, excursions permitted to 15-30°C. Reconstituted solutions: Stable up to 24 hr at room temperature (up to 6 hr in vial, the remaining time in IV infusion bag); stable up to 48 hr if reconstituted with 0.9% Sodium chloride inj or 5% Dextrose inj, and store at 2-8°C (following immediate transfer into IV infusion bag).
ATC Classification
J01AA12 - tigecycline ; Belongs to the class of tetracyclines. Used in the systemic treatment of infections.
Storage
Intravenous: Unopened vial: Store at 20-25°C, excursions permitted to 15-30°C. Reconstituted solutions: Stable up to 24 hr at room temperature (up to 6 hr in vial, the remaining time in IV infusion bag); stable up to 48 hr if reconstituted with 0.9% Sodium chloride inj or 5% Dextrose inj, and store at 2-8°C (following immediate transfer into IV infusion bag).
Available As
  • Tigecycline 50 mg
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