In this review we overview the mechanisms responsible for uterine contractility and relaxation. We then use this as the basis for discussing the two major uterotonins, oxytocin and prostaglandins followed by currently available (although often unlicensed) tocolytics; progesterone, magnesium, calcium channel blockers, oxytocin receptor blockers, β-adrenergic receptor agonists, prostaglandin synthesis inhibitors and nitric oxide donors. In this brief review we have concentrated on the most important mechanisms of action and data obtained on human tissue. By focussing on mechanisms, meta-analyses and Cochrane literature reviews, our aim is to provide insight for clinical usefulness, and highlight where further research is required and where the targets may be.