Monoterpenoids, being a valuable component of essential oils, constitute important groups of natural compounds. They contain two isoprenoid units in their structure. Monoterpenoids are the secondary metabolites of the plants and they do not exert primary function in the plants. Owing to their higher abundance in the plant kingdom, they find wide application in the perfumery industry, food, and health care products for human beings. Monoterpenoids either in direct form or modified form exert diverse pharmacological effects. The present review reports wide pharmacological activities of monoterpenoids like learning and memory enhancer, antidepressant, anxiolytic, antinociceptive, anticonvulsant, and neuroprotective indicating the promising potential of monoterpenoids to treat a wide range of complex diseases.