Although magnesium sulfate is widely used as a tocolytic agent in the hope of preventing spontaneous preterm birth, there is a paucity of data from large well-designed randomized clinical studies demonstrating the efficacy of magnesium sulfate therapy. Given the potential for untoward side effects and the inherent risks of magnesium sulfate therapy, a thorough understanding of the potential risks and benefits of this agent is needed. To accomplish this understanding we have provided a detailed review the history, pharmacology, physiology, maternal/fetal side effects, and tocolytic efficacy of magnesium sulfate.