Opioids are routinely used in the management of moderate to severe pain. However, in the acute care setting, consistently undertreated and suboptimally managed pain continues to be a problem. Given the potential for opioids to result in lifethreatening situations, and the increasing complexity of the patients that are cared for in acute care facilities, a thorough understanding of intravenous opioid therapy is a necessity for hospital-based clinicians. Opioids can be classified by chemical structure and/or drug effect (i.e. action on Mu, Kappa, and Delta opioid receptors throughout the body). Endogenous opioids include endorphins, enkephalins, and dynorphins, which moderate the body's natural response to pain. Commonly used exogenous intravenous opioids include morphine, hydromorphone, fentanyl, meperidine, methadone, buprenorphine, butorphanol, and nalbuphine, which vary greatly in potency, duration of action, metabolism, and in their adverse effect profile. A growing body of evidence suggests that patient controlled analgesia may be superior to conventional methods (need for analgesia determined by clinicians) of treating pain in the acute care setting. Newer pump delivery systems may also decrease the risks of human and equipment errors as well as enhance patient safety and satisfaction. The purpose of this review is to help guide clinicians in the safe and effective management of pain in patients requiring intravenous opioid therapy in the acute care setting.