Zamzam water is obtained from zamzam well which is located in the Saudi Arabia’s divine locality called Mecca in the holy mosque Al-Haram. Usually in wells growth of microorganisms, their spores and plant vegetation occurs, but zamzam is free from biological contamination. Furthermore zamzam has significant health benefits; it produces healing and antimicrobial action due to presence of many minerals such as calcium, magnesium, zinc, fluoride and many others. Zamzam Studies and Research Center regulates demand and supply of water and also examines zamzam for its chemical and microbial composition. The composition of zamzam water showed the presence of calcium, magnesium, sodium, chloride in high concentration. Other constituents including zinc, antimony, beryllium, bismuth, bromine, cobalt, iodine, manganese, chromium and titanium are also found in zamzam water in traces. Heavy metals are also present in zamzam water such as arsenic, cadmium, lead, and selenium.The alkaline nature of zamzam water accounts for its various positive effects on health and the presence of antioxidant constituents in zamzam water could be related to its therapeutic efficacy in different diseases. Zamzam water has previously been studied for its therapeutic role in curing dental carries, diabetes, infertility and cancer.The purpose of this study was to explore the therapeutic efficacy and toxicological profile of zamzam water. In this study we determined the composition as well as effects of zamzam water on CNS profile (cage crossing, open field, stationary rod, head dip, light and dark, forced swimming test), brain biogenic amines estimation, anti-Parkinson activity, analgesic and anti-inflammatory activity, anticonvulsant activity, blood profile, lipid profile, liver profileand renal profile.Results suggest that zamzam water possesses remarkable therapeutic effects. Zamzam water can act as an anxiolytic, memory enhancer, antidepressant, anti-cataleptic, anticonvulsant, analgesic and anti-inflammatory agent. Furthermore it has positive effects on hematological, lipid and renal profile. The effects on liver profile should be further evaluated. It can be postulated that the presence of minerals and trace elements such as IX zinc, magnesium, iron, calcium, selenium and lithium in zamzam water can account for these beneficial effects. Our study further revealed that although arsenic level is high in zamzam water but even after chronic administration of zamzam water for 60 days adlibitum, there was no sign of toxicity shown in animals. This effect is due to unique composition of zamzam water. The presence of calcium, magnesium, selenium and zinc in zamzam water not only decreases arsenic absorption and its distribution in various organs but also neutralizes the arsenic induced toxicity on different organs. However further studies are required to explore the interaction of different elements and metals present in zamzam water and their effects. Thus we can conclude that zamzam water has not shown any toxic effects and it has remarkable therapeutic and beneficial effects on health even in the presence of arsenic in its composition.