Plant species have long been regarded as possessing the principal ingredients used in widely disseminated ethnomedical practices. Different surveys showed that medicinal plant species used by the inhabitants for the traditional treatment of diseases are inadequately screened for their therapeutic/preventive potential and phytochemical findings. The genus Nepeta L., which belongs to the family Lamiaceae, are widely used in traditional medicine. In this review, Nepeta species, which are used as traditional herbal medicine pursued indigenously, have reported several pharmacological effects as antimicrobial, antioxidant, antiinflammatory, sedative, relaxant, cholesterol lowering, antiasthmatic, carminative, diuretic, diaphoretic, febrifuge, vermifuge, herbicidal, insecticidal and insect repellent, all of them directly related to the specific chemical composition. According to the Nepeta genus phytochemistry, there exist two main essential oil chemotypes. The first is the nepetolactone chemotype, and the second is the 1,8-cineole and/or linalool chemotype. The active constituents from Nepeta genus may provide the opportunity for the production of antidepressive, antidiabetes, analgestic, anti-inflammatory, lipid-lowering and cardioprotective drugs. Due to the effects of Nepeta species on improving the complications of various diseases, the need for doing more extensive and comprehensive clinical trials for the use of Nepeta species in the treatment of diseases is necessary. Recommended future directives incurring the design and conduct of comprehensive trials are pointed out to validate the usefulness of these active plant species and bioactive secondary metabolites either alone or in combination with existing conventional therapies.