Objective: The primary objective of this article is to review the basic science of nonsteroidal anti-inflammatory drugs (NSAIDs), their clinical effects, indications, potential complications, and ethical issues associated with the use of injectable NSAIDs in the treatment of athletes. These objectives are presented taking into consideration the contemporaneous issues associated with the treatment of amateur and professional athletes. Data Sources: A nonformal review of the published medical literature and lay media focusing on the use of injectable NSAIDs in athletes was used for this article. Main Results: All NSAIDs work through the inhibition of the cyclooxygenase (COX) pathway (either one or both subtypes) to reduce inflammation and inhibit pain by reducing prostaglandin and thromboxane synthesis. Complications related to NSAID use involve primarily the gastrointestinal, renal, and cardiovascular systems through this COX pathway inhibition. Ketorolac is the only NSAID currently available in an injectable form. Despite its analgesic efficacy comparable with opioid medication, injectable ketorolac has the potential to cause bleeding in collision athletes resulting from impaired hemostasis. Conclusions: Nonsteroidal anti-inflammatory drug medications are currently used at every level of competition. Injectable ketorolac is an effective analgesic and anti-inflammatory drug. However, its potential effectiveness must be weighed against the risk of potential complications in all athletes, especially those who participate in contact/collision sports. The team physician must balance the goal of treating pain and inflammation with the ethical implications and medical considerations inherent in the administration of injectable medications solely to prevent pain and/or return the athlete to competition.