Acupuncture has been widely used as alternative and complementary medicine for pain relief in and around East Asia about 2,000 years. Among various acupuncture techniques being newly developed, pharmacopuncture is a relatively novel acupuncture technique. While the conventional acupuncture treatment incorporates the physical stimulation of associated meridians and acupoints, pharmacopuncture is a form of acupuncture treatment which combines with injection of herbal medicine or animal product at the acupuncture points. The advantages of pharmacopuncture treatment are more rapid effects, synergistic effects, and the easy for controlling dosage compared to acupuncture treatment. Numerous types of pharmacopuncture are applied to treat diverse disorders; especially, it is frequently used to reduce an inflammatory response, thereby relieving the pain. Recently, it has been reported that medicinal materials used for pharmacopuncture treatment are prepared and applied by various methods of the operator at discretion, which has higher risks of adverse events than other treatments. In consideration of these problems, it is required to standardize the raw materials and the manufacturing process to provide safe, stable, and effective pharmacopuncture by enriching the effective components and removing the harmful factors. In vitro and in vivo as well as clinical trials have showed that bee venom(BV) may be an important source of pharmacopuncture to cure diverse diseases such as arthritis and rheumatism, pain, and cancer. Since BV contains several active ingredients with a wide variety of pharmaceutical properties, the identification of a single constituent, the possible mechanisms, and a standardization of the applicable route and formulation are needed. Our present results may be helpful to set priorities and directions for development of pharmacopuncture to target the clinical application.