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Various pharmacotherapies in drug addiction have been developed to target two primary neurobiological processes of addiction: 1) dopaminergic and opioid systems found to be involved in the rewarding effects of various drugs of abuse and 2) the enduring neuroplasticity mediating the vulnerability to relapse that largely includes glutamatergic mechanisms. Drug development is a costly, slow process and, thus far, pharmacotherapeutic treatment of drug addiction is not highly efficacious. Issues of compliance to both behavioural and pharmacological treatment remain of primary concern, and indeed reduce the efficacy of treatments developed thus far. Tools to improve compliance and treatment efficacy, including pharmacogenetics, hold promise but are novel and the full extent of their clinical utility has not yet been shown. In this chapter, we will discuss the current state of pharmacotherapy in addiction, as well as the various targets that have been identified as having a role in drug use and relapse.

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