Tygacil Tigecycline for Injection

1. Indications and Usage
Complicated Intra-abdominal Infections: Treatment of complicated intra-abdominal infections (cIAI) caused by susceptible strains of specific bacteria.
Complicated Skin and Skin Structure Infections: Treatment of complicated skin and skin structure infections (cSSSI) caused by susceptible strains.
2. Dosage and Administration
Adults: The recommended dosage is an initial dose of 100 mg, followed by 50 mg administered every 12 hours.
Administration: Intravenous infusion only. The infusion time for each dose should be approximately 30 to 60 minutes.
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment or those on hemodialysis.
Hepatic Impairment: For patients with severe hepatic impairment (Child-Pugh Class C), the dosage should be adjusted to an initial dose of 100 mg, followed by 25 mg every 12 hours.
3. Mechanism of Action
Protein Synthesis Inhibition: Tigecycline binds reversibly to the 30S ribosomal subunit of bacteria.
Resistance Overcoming: It inhibits bacterial protein synthesis by preventing the attachment of aminoacyl-tRNA to the ribosomal acceptor site.
Broad Spectrum: It is effective against organisms resistant to other tetracyclines because it is not affected by common tetracycline resistance mechanisms (ribosomal protection and efflux pumps).
4. Safety and Warnings
Mortality Risk: An increased risk of death was observed in patients treated with tigecycline compared to control groups in clinical trials.
Pregnancy: Use during the second and third trimesters may cause permanent discoloration of teeth and reversible inhibition of bone growth in the fetus.
Pediatric Use: Not recommended for patients under 18 years of age due to the mortality risk.
Superinfection: Prolonged use may result in the overgrowth of non-susceptible organisms, including fungi.
5. Adverse Reactions and Clinical Research
Common: Nausea and vomiting are the most frequently reported adverse reactions, typically occurring on the first or second day of treatment.
Clinical Research: Pivotal clinical trials have demonstrated non-inferiority compared to standard therapies (e.g., imipenem/cilastatin or vancomycin/aztreonam) in treating cIAI and cSSSI.
6. Drug Interactions
Warfarin: Tigecycline may increase the anticoagulant effect of warfarin; prothrombin time or INR should be monitored closely.
Oral Contraceptives: Concomitant use may lead to decreased efficacy of oral contraceptives.
Cyclosporine or Tacrolimus: Concomitant use may increase serum concentrations of these calcineurin inhibitors.
Digoxin: Tigecycline may slightly decrease digoxin peak concentration but does not significantly affect overall exposure or pharmacodynamics.
7. Pharmaceutical Information
Active Ingredient: Tigecycline (as free base).
Excipients: Glycine and hydrochloric acid.
Appearance: Orange lyophilized cake or powder.
Storage: Store at controlled room temperature and protect from light. Reconstituted and diluted solutions should be used promptly or stored under refrigeration as per stability guidelines.