Drimia genus includes plants that used from ancient time for various ailments such as dropsy, respiratory ailment, bone and joint complications,skin disorders, epilepsy and cancer. Toxic properties of some Drimia species also were noted by ancient scientists and these plants have been traditionally used for rat control. Bufadienolides have been identified as the main constituents in the genus of Drimia. Phenolics, sterols, protein and some of other phytochemicals have been also isolated from these plants. Pharmacological and clinical studies have strongly approved their effect on cardiovascular system. Extracts and compounds isolated from Drimia species showed biological activities such as antibacterial, antifungal, antiviral, antioxidant, anti-inflammatory and insecticidal effects throughseveral in vivo and in vitro studies. Moreover, cytotoxic and antitumor activities which may be related to bufadienolide content of these plants have been considered by many researchers. Traditional therapeutic values of these plants for treating respiratory and rheumatic ailments as well as skin disorders are needed to be validated through more researches. Toxic effects of these plants and isolated compounds have been investigated through several in vivo studies. Drimia plants and their isolated compounds have narrow therapeutic index, so patients should be prohibited from applying these plants without medical supervision and should be informed about the main intoxication symptoms before starting treatment. Moreover, interaction of Drimia plants with other constituents of traditional herbal mixtures as well as chemical and biological modalities for reducing toxicity of bufadienolide compounds can be subjected for future studies. Drimia genus includes plants that used from ancient time for various ailments such as dropsy, respiratory ailment, bone and joint complications, skin disorders, epilepsy and cancer. Toxic properties of some Drimia species also were noted by ancient scientists and these plants have been traditionally used for rat control. Bufadienolides have been identified as the main constituents in the genus of Drimia. Phenolics, sterols, protein and some of the other phytochemicals have been also isolated from these plants. Pharmacological and clinical studies have strongly approved their effect on cardiovascular system. and compounds isolated from Drimia species showed biological activities such as antibacterial, antifungal, antiviral, antioxidant, anti-inflammatory and insecticidal effects through serum in vivo and in vitro studies. Moreover, cytotoxic and antitumor activities which may be related to bufadienolide content of these plants have been considered by many researchers. Traditional t herapeutic values ​​of these plants for treating respiratory and rheumatic ailments as well as skin disorders are needed to be validated through more researches. Toxic effects of these plants and isolated compounds have been investigated through several in vivo studies. Drimia plants and their isolated compounds have narrow therapeutic index, so patients should be prohibited from applying these plants without medical supervision and should be informed about the main intoxication symptoms before starting treatment. Moreover, interaction of Drimia plants with other constituents of traditional herbal mixtures as well as chemical and biological modalities for reducing toxicity of bufadienolide compounds can be subjected for future studies.