Capsaicin, a well known vanilloid, has shown evidence of an ample variety of biological effects which make it the target of extensive research ever since its identification. In spite of the fact that capsaicin causes health hazards in quite a few ways, yet, the verity cannot be ignored that capsaicin has several therapeutic implications. In patients with hypersensitive bladders, vesical instillation of 1 mM capsaicin markedly improved urinary frequency and urge incontinence. Again, administration of capsaicin favors an augmentation in lipid mobilization and a decrease in adipose tissue mass. Topical capsaicin cream as well decreases postsurgical neuropathic pain and is preferred by patients over a placebo among other therapies. Several in vitro studies have revealed that capsaicin results in growth arrest in some transformed cell lines. Furthermore, capsaicin has been proven to be an undeniably exciting molecule and remains a valuable drug for alleviating pain and itch. It has been recognized that capsaicinoids are the most potential agonists of capsaicin receptor (TRPV1). However, vanilloids could exert the beneficial effects not only through the receptor-dependent pathway but also through the receptor-independent one. The involvement of serotonin, neuropeptide Substance P and somatostatin in the pharmacological actions of capsaicin has been expansively investigated. Better understanding of the established TRPV1 receptor mechanism as well as exploring other possible receptor mechanism may publicize other new clinical efficacies of capsaicin. Further, clinical studies are required in several of these conditions to establish the efficacy of capsaicin.