Labetalol is a combined α- and β-adrenoceptor antagonist, which is still currently used to treat hypertension. It acts as a nonselective competitive antagonist at β-adrenoceptors and a competitive antagonist of postsynaptic α-adrenoceptors. In this review, the pharmacokinetics, pharmacodynamics, pharmacological effects, mechanism of action, and indications of labetalol were revisited. Recent updates on the side effects and toxicities of labetalol on various bodily systems are also elaborated. A comparison between labetalol and other drugs, which are used for similar indications were also performed. Controversies regarding the usage of labetalol, either acutely or chronically, were also elaborated. Contraindications and precautions in the usage of labetalol were also discussed.