Clinical pharmacokinetics and pharmacodynamics of tigecycline

Rapid emergence of resistance against antibacterials emphasizes the need for the development of novel and/or more potent antibacterials. Tigecycline is the first representative of a new drug class, the glycylcyclines, and was approved in 2005 by the US FDA for the treatment of complicated skin and skin structure infections, as well as complicated intra-abdominal infections. Tigecycline distributes extensively into the intracellular space of tissue and accumulates in cells, which may qualify it for the treatment of intracellular infections. The pharmacokinetics of tigecycline are complex with both linear and non-linear characteristics. The reason for this complexity is still not fully understood. Non-linearity can be found in the volume of distribution possibly due to extensive and variable tissue and/or plasma protein binding. In contrast, clearance and area under the plasma concentration-time curve are dose-independent. Tigecycline has a high incidence of mild adverse effects, mainly nausea and vomiting, but is otherwise well tolerated.