Capsicum peppers are great herbal medicine bestowed with natural pharmacological bioactive compounds majorly Phytochemicals, capsaicin, essential oils and a rich mix of organic micronutrients with potential health benefits. They play nutritional roles in diets and possess medicinal properties. These bioactive agents manifest their usefulness over mono-therapy by working in consortium and exert synergistic, polyvalent and pharmacological effects in humans as nutraceutical that serve as functional foods; as crude drugs for health benefits including prevention and treatments of chronic metabolic diseases such as coronary heart disease, diabetes and obesity. The synergistic effects of the phyto-nutrients of Capsicum peppers are thought to make them potentially effective anti-microbial, anti-inflammatory, anticancerous, anti-tumor, anti-mutagenic and possess good antioxidants with scavenging ability for singlet oxygen, free radical inhibitors, peroxide decomposers and metal chelating agents which are implicated in favoring of the onset of degenerative diseases including mucosa degeneration. While capsaicin imparts the ability for Capsicum peppers to function as topical agents, for the relief of various forms of pains as pain medicine; its activity as neurotoxic and cytotoxic agent is suggested to give various potential environmental health benefits and also benefiting man as a potential effective anesthesia. The presence of Phytochemicals in Capsicum pepper makes them not only useful and much cheaper alternatives to synthetic drugs but the Phytochemicals can be harnessed as crude drugs for the production of novel drugs. However, clinical studies on the consumption of Capsicum peppers are insufficient and needed to confirm some of the findings from animal studies.