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Monitoring of drug pharmacokinetics is used in personalized therapy, therapeutic drug monitoring (TDM), toxicology assessments, doping controls and clinical drug development. Drugs are predominantly measured in plasma, serum or urine. Monitoring of volatile organic compounds (VOCs) in breath has so far not received much attention, but nevertheless it has many advantages over conventional approaches. This chapter presents the principles of basic pharmacokinetics, focusing on volatiles and related physiological concepts. It also offers a comprehensive overview of drugs detected in exhaled breath. Finally, it also presents the necessary analytical and sensing tools to monitor volatile organic drugs, with selected pharmaceutical examples by which their potential is discussed.

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