There is a dramatic rise of novel drug use due to the increased popularity of so-called designer drugs. These synthetic drugs can be illegal in some countries, but legal in others and novel compounds unknown to drug chemistry emerge monthly. This thoughtfully constructed edited reference presents the main chromatographic methodologies and strategies used to discover and analyze novel designer drugs contained in diverse biological materials. The methods are based on molecular characteristics of the drugs belonging to each individual class of compounds, so it will be clear how the current methods are adaptable to future new drugs that appear in the market.