Pharmacological neuroenhancement and mood enhancement are gaining tremendous importance in society. The main motivation for neuroenhancement and mood enhancement is the anticipated increase in attention and vigilance, better performance in learning and memory and mood stability to meet the complex demands of an exacerbating meritocracy. Most users apply drugs originally designated for attention disorders, sleep disorders or dementia. Application of related drugs in terms of enhancement strategies in healthy individuals is off-label per se, the acquisition and distribution illegal. Here, we first provide an overview of the basic physiological mechanisms underlying vigilance, learning and memory, and emotional states. We then present the different pharmacological classes, i. a. purines and methylxanthines, phenylethylamine, modafinil, nootropics and antidepressants and elaborate their pharmacodynamics profile. Special attention will be paid to the norepinephrine/dopamine and cholinergic receptors and transporter systems but also to functional interaction with adenosine, serotonine and the glutamate receptor systems. Metaanalysis revealed that efficacy reported in, e. g. ADHD or dementia patients cannot be translated to healthy individuals. A validated positive effect on attention and vigilance has only been reported for some phenylethylamines and modafinil. It is likely that new developments, particularly in the field of antidementives will dramatically enhance neuroenhancement and mood enhancement. Drug regulatory actions, public and political discussions are necessary to meet the ethical and legal challenges of neuroenhancement and mood enhancement in the future.