Context: Primary care providers can play a significant role in the management of gambling disorder (GD). However, they usually lack sufficient training in this area, including the potential utilisation of pharmacotherapy. Objective: The objective of this study is to evaluate and summarize the effectiveness and safety information for the use of pharmacological agents in GD. Study Design: Narrative review. Dataset: Embase (via Ovid), Medline and Cochrane Central (Via EBSCO), Prospero, Clinicaltrials.gov, Epistemonikos. A specific search strategy was used in each database, which included a combination of the following subject headings and keywords: gamble, drug therapy, medicine, therapeutics, treatment, intervention, therapy, management, pharm, medication, drug, antidepressants, SSRI, opioid, naltrexone, lithium. Population Studied: Articles were included if: 1) pharmacotherapy was discussed as the main focus of the study or as part of a broader strategy in GD treatment, 2) the publication type was systematic review, meta-analysis, or if it was a review that analyzed data from multiple clinical trials; all articles, regardless of publication type, published since 2019 on the topic were screened for eligibility. Results: The preliminary search identified 1925 articles (1508 articles in Medline, 508 articles in Embase, 201 articles in Cochrane Central, and 1 article through citation searchings). Out of 67 articles evaluated for potential eligibility, 19 were included in full-text review. Conclusions: Pharmacotherapy can achieve a small to medium improvement in patients with GD. Six pharmacological agents showed various degrees of efficacy and safety across a limited number of studies. Conducting future and more rigorous trials that address the limitations in the existing literature (e.g. inclusion of GD patients with the common comorbid psychiatric disorders), can set the stage for an FDA approval of medications in GD with confirmed efficacy data.