This is an update to a previously published article discussing the neuropsychopharmacology of pathological gambling (PG) . In the prior manuscript, we described how cortico-limbic circuitry and neurotransmitter systems (norepinephrine, serotonin, dopamine, opioids, glutamate, and gamma-aminobutyric acid (GABA)) have been implicated in PG. These systems represent potential targets for psychopharmacological treatments for PG, with opioid antagonists arguably showing the most consistent benefit in RCTs. In the past year and half since this publication was prepared, there has been one additional randomized clinical trial (RCT) published along with a single case study. Our original manuscript did not describe in detail findings from case studies or open-label studies so in addition to the new RCT data and a new case report involving naltrexone, here we describe case and open-label findings. A PubMed search was conducted using terms such as “pathological gambling treatment”, “clinical trials and gambling”, and “gambling psychopharmacology.” Using these search terms, numerous results were obtained, necessitating further search modifiers. For example, using just “pathological gambling treatment” results in over 1600 hits. In order to focus in on the search modalities, we searched within the initial results for specific phrases such as “psychopharmacology, clinical trial, medication, serotonergic, dopaminergic, etc.” in addition to searching for specific medications. Results not directly related to the treatment of pathological gambling were not included. The study of pathological gambling is relatively new. As such, our search did not exclude any studies due to age of material, but with a few exceptions, the majority of the studies discussed were published later than 2000. This resulted in 24 case studies and/or RCTs not previously included in our original review article. These findings in conjunction with our prior publication provide a comprehensive overview of controlled investigations and exploratory reports of pharmacotherapies for PG.