Labetalol blocks two kinds of receptors that respond to adrenaline and similar stress chemicals. Blocking alpha-1 receptors lets blood vessels relax, which lowers the resistance the heart pumps against. Blocking beta receptors keeps the heart from racing during exercise or stress. Together these effects lower blood pressure without setting off a fast pulse, and the resting heart rate drops only a little.
Taken by mouth, it reaches its peak effect within 2 to 4 hours, and one dose lasts at least 8 hours, longer with bigger doses. Given by IV, each injection reaches its full effect within about 5 minutes. Because of the alpha-1 blocking, blood pressure falls more when standing than lying down, so people can feel dizzy or faint when they get up, most of all after an IV dose. The beta blocking can also slow the heart too much, tighten the airways in people with lung disease, and hide the racing heartbeat that warns of low blood sugar.