Despite the increasing use of ginseng pharmacopuncture in clinical practice, evidence of its physiological effects, safety, and clinical outcomes is insufficient. The purpose of this review is to summarize previous studies and suggest future challenges for the clinical use of ginseng pharmacopuncture. We systematically searched clinical and animal studies that applied ginseng pharmacopuncture and reviewed the manufacturing processes of ginseng pharmacopuncture solution, safety, physiological responses, and clinical effects. Intravenous or point injection of the ginseng pharmacopuncture solution made by distillation extraction has been commonly used in studies. Ginseng pharmacopuncture does not show any toxicity in animals and humans, while it influenced the heart rate variability, pulse wave velocity, and protein synthesis in human subjects. In 25 case reports, patients with cancer, amyotrophic lateral sclerosis, skin wrinkles, and allergic rhinitis showed significant improvement of clinical outcomes. We found that more evidence is necessary to conclude that ginseng pharmacopuncture is safe and effective. First, the pharmacopuncture manufacturing process should be standardized on the basis of the safety and efficacy tests. Moreover, studies on the quantitative quality of the components of the solution and on the clinical comparison of various injection methods are required to improve clinical outcomes in the future.