Pharmacokinetics, pharmacodynamics, safety and tolerability of tigecycline.

摘要

The pharmacokinetics and pharmacodynamics of tigecycline have been extensively studied in laboratory models and healthy volunteers. Tigecycline is available as a parenteral agent, exhibits linear pharmacokinetics, has a long terminal half-life, is extensively distributed into the tissues and attains steady-state levels in serum by day 7. The pharmacokinetics of tigecycline appear unaffected by age, renal disease and food. Clinical trials have shown that tigecycline (50 mg i.v. q12h) in adults is safe and generally well tolerated for up to 11.5 days. Drug-related adverse events, which are typically mild to moderate in intensity and of limited duration, mainly include nausea and vomiting. Tolerability of tigecycline in fasting subjects is improved by the use of antiemetics. C. difficile-related complications with tigecycline are uncommon. In the majority of patients, tigecycline has minimal adverse effects on blood chemistry or haematology.