Investigational Drug Details
| Drug ID: | D168 |
| Drug Name: | Labetalol |
| Synonyms: | |
| Type: | small molecule |
| DrugBank ID: | DB00598 |
| DrugBank Description: | Labetalol is a racemic mixture of 2 diastereoisomers where dilevalol, the R,R' stereoisomer, makes up 25% of the mixture.[L7730] Labetalol is formulated as an injection or tablets to treat hypertension.[L7727,L7730] Labetalol was granted FDA approval on 1 August 1984.[L7724] |
| PubChem ID: | 3869 |
| CasNo: | 36894-69-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | CC(CCC1=CC=CC=C1)NCC(O)C1=CC(C(N)=O)=C(O)C=C1 |
| Structure: |
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| InChiKey: | SGUAFYQXFOLMHL-UHFFFAOYSA-N |
| Molecular Weight: | 328.4055 |
| DrugBank Targets: | Beta-1 adrenergic receptor; Beta-2 adrenergic receptor; Alpha-1 adrenergic receptors |
| DrugBank MoA: | Labetalol non-selectively antagonizes beta-adrenergic receptors, and selectively antagonizes alpha-1-adrenergic receptors.[A181901] Following oral administration, labetalol has 3 times the beta-blocking ability than alpha-blocking ability.[A181901] This increases to 6.9 times following intravenous administration.[A181901] Antagonism of alpha-1-adrenergic receptors leads to vasodilation and decreased vascular resistance.[A181907] This leads to a decrease in blood pressure that is most pronounced while standing.[A181910] Antagonism of beta-1-adrenergic receptors leads to a slight decrease in heart rate.[L7727] Antagonism of beta-2-adrenergic receptors leads to some of the side effects of labetalol such as bronchospasms, however this may be slightly attenuated by alpha-1-adrenergic antagonism.[A181910] Labetalol leads to sustained vasodilation over the long term without a significant decrease in cardiac output or stroke volume, and a minimal decrease in heart rate.[A181907,A181910] |
| DrugBank Pharmacology: | Labetalol antagonizes various adrenergic receptors to decrease blood pressure.[A181901,A181907,A181910,L7727] The duration of action is long as it is generally given twice daily, and the therapeutic window is wide as patients usually take 200-400mg twice daily.[L7730] Patients susceptible to bronchospasms should not use labetalol unless they are unresponsive to or intolerant of other antihypertensives.[L7730] |
| DrugBank Indication: | Labetalol injections are indicated to control blood pressure in severe hypertension.[L7727] Labetalol tablets are indicated alone or in combination with antihypertensives like thiazides and loop diuretics to manage hypertension.[L7730] |
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