Labetalol
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| Pronunciation | /ləˈbɛtəlɔːl/ |
| Trade names | Normodyne, Trandate |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a685034 |
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| Routes of administration |
oral, iv |
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| Pharmacokinetic data | |
| Bioavailability | 25% |
| Protein binding | 50% |
| Metabolism | hepatic pass metabolism, |
| Biological half-life | Tablet: 6-8 hours; IV: 5.5 hours |
| Excretion | Excreted in urine, not removed by hemodialysis |
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| ECHA InfoCard | 100.048.401 |
| Chemical and physical data | |
| Formula | C19H24N2O3 |
| Molar mass | 328.406 g/mol |
| 3D model (Jmol) | |
| Chirality | Racemic mixture |
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Labetalol, sold under the trade names Normodyne among others, is a mixed alpha/beta adrenergic antagonist that is used to treat high blood pressure. It can be given intravenously in severe hypertensive situations, or by mouth for long term hypertension management. Its dose and use is limited by its main side effect—postural hypotension, where there is a substantial drop in blood pressure when standing up.
Labetalol's dual alpha- and beta- blockade has different physiological effects in short- and long-term situations. In short-term, acute situations, labetalol decreases blood pressure by decreasing systemic vascular resistance with little effect on stroke volume, heart rate and cardiac output. During long-term use, labetalol can reduce heart rate during exercise while maintaining cardiac output by an increase in stroke volume.
Labetalol is effective in the management of hypertensive emergencies, postoperative hypertension, pheochromocytoma-associated hypertension, and rebound hypertension from beta blocker withdrawal.
It has a particular indication in the treatment of pregnancy-induced hypertension which is commonly associated with pre-eclampsia.
It is also used as an alternative in the treatment of severe hypertension.
Pregnancy: Studies in lab animals showed no harm to the fetus. However, a comparable well-controlled study has not been performed in pregnant women.
Nursing: Breast milk has been shown to contain small amounts of labetalol (0.004% original dose). Prescribers should be cautious in the use of labetalol for nursing mothers.
Pediatric: No studies have established safety or usefulness in this population.
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Wikipedia