This review describes a comprehensive investigation focusing on syntheses of analytical reagents, followed by their utilization in development of analytical methods, and leading to practical applications for rational use of medicaments centering on abused drugs. Many kinds of analytical reagents for fluorescence and chemiluminescence detections have been synthesized with the intention of improving sensitivity. By properly combining the developed analytical reagents with an HPLC separation technique, one could determine ultra-small amounts of abused drugs such as stimulants, narcotics and obesity drugs in various matrices. Furthermore, chiral analyses of some abused drugs and evaluation of their potential for drug-drug interaction were also performed. The developed methods might be useful for forensic and toxicological studies on drug abuse. Also, the results obtained in our study might contribute to the prediction of and the protection of human health from risks of abused drugs.