Zinc is one of the most abundant elements in the earth's crust and is widely used in the metal, rubber, chemical, paint, and agricultural industry, in addition to the usage in cosmetics ingredients, or for medical purposes. In this context, nano‐sized zinc oxide is used in personal care products, sensors, antibacterial creams, and biomedical applications. In fact, for various organisms, zinc is an essential component in the basic cellular functions. Furthermore, extracellular zinc has the potential to interact with and modulate many different synaptic targets, induce oxidative and nitrosative stress, leading to alteration in the inflammatory responses. It is normally absorbed from the intestine, and competes with Cu
2+
, Fe
2+
, and Ca
2+
for absorption and potentially induces copper deficiency. Consequences of zinc deficiency have been recognized for many years, however high exposure to zinc fumes, zinc compounds, and zinc nanoparticles via inhalation, ingestion, or dermal route may result in severe hematological, developmental, gastrointestinal, and nervous system toxicity. This chapter aims to summarize the knowledge on the regulations of occupational zinc exposure limits and manifestations of bulk and nano‐sized zinc toxicity.