Nanomaterials play an important role in the fabrication of many devices and modified materials, due to their unique properties, such as a large surface area/volume ratio and their high mechanical strength. The applicability of nanomaterials in drug determinations is being well investigated. This review provides a summary of the synthesis methods, characterization routes, and applications toward drugs. Nanomaterials have been investigated for their applications with electrochemical and spectroscopic systems for drug determinations. Most of the applications described in the literature are concerned with pushing the limits of how few molecules can be detected in a given volume of solution. Nanomaterials based methods are useful because of their excellent electrical, thermal, magnetic, and optical properties. The real value of the designed method lies in their detection limit range, sensitivity, and other merits that can be enhanced by the nanomaterials modified electrodes or surfaces.