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In the past two decades, lung transplantation has become an increasingly important surgical option for the patient with end stage lung disease. Compared with the other solid organ transplants (heart, liver and kidney), lung transplantation carries immense clinical and logistic challenges; long-term organ viability is particularly problematic, with an expected five-year mortality of 40-50%. The number of lung transplants performed in the U.S. has been increasing steadily since 1988, when UNOS (United Network for Organ Sharing) started recording statistical data. In that year, 33 cases of lung transplantation were performed. As of today, a total of 23,815 lung transplants have been performed, and the largest number of yearly lung transplants (n=1,822) was performed in 2009. From appropriate patient selection, to optimal organ selection, surgical procedure, and immediate and long-term postoperative care, the medical process involves multiple healthcare providers and requires a very well-organized and committed healthcare system to achieve optimal surgical results. Understanding the pharmacology involved in the care of the lung transplant patient is of utmost importance to achieve appropriate organ preservation, immunosuppression, hemodynamic stability, and adequate anesthetic depth, while avoiding drug toxicity and side effects. The purpose of this review is to summarize the pharmacokinetics and pharmacodynamics of the medications most commonly administered to this patient population, throughout the perioperative period.