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Creatine is a naturally occurring compound found in muscle tissue that plays a vital role in cellular energy metabolism. While traditionally recognized for its benefits in enhancing skeletal muscle function and exercise performance, recent research has highlighted its potential therapeutic applications in various medical fields. This study reviews the available literature to assess the current state of knowledge regarding creatine’s medical uses and outlines directions for future research. Evidence has demonstrated a correlation between low creatine levels and reduced mental well-being, suggesting a role in the central nervous system. Notably, creatine has been explored as a potential antidepressant—both as a standalone treatment and as an adjunct to selective serotonin reuptake inhibitors (SSRIs)—owing to its newly discovered function as a neurotransmitter. Additionally, long-term investigations into creatine’s molecular mechanisms in the brain have prompted its study in stroke management, where it may support both prevention in high-risk populations and post-stroke rehabilitation. In the context of chronic heart failure, creatine has been linked to cardiomyocyte metabolic dysfunction, particularly regarding disruption of the creatine/phosphocreatine/ATP shuttle. Although studies examining creatine supplementation in cardiovascular disease have produced mixed results, the compound shows promise as a supportive therapy. However, further research is necessary to confirm its efficacy and safety across these medical applications.