General Information

Labetalol Impurities and Labetalol 

Daicel Pharma offers worldwide delivery options for custom synthesis of Labetalol impurities, including impurities such as (R, R)-Labetalol, (R, S)-Labetalol, (S, R)-Labetalol, (S, S)-Labetalol, 5-[2-[Bis(phenylmethyl)amino]-1-hydroxyethyl]-2-hydroxybenzamide (Labetalol-bisbenzyl base], 5,5-Dibromoacetyl Salicylamide, and Labetalol Impurity C. These impurities evaluate the purity and safety of Labetalol, an active pharmaceutical ingredient.

Labetalol [CAS: 36894-69-6], a non-selective beta-adrenergic and third-generation selective alpha-1-adrenergic antagonist, exhibits vasodilatory and antihypertensive effects. It treats high blood pressure, acting as an alpha-adrenergic and beta-adrenergic antagonist. Additionally, it functions as an antihypertensive agent and a sympatholytic agent.

Labetalol: Use and Commercial Availability 

Labetalol is a medication marketed under various brand names like Normodyne and Trandate. It is US FDA-approved to treat arterial hypertension, ranging from urgent/emergency cases to stable chronic hypertension. Labetalol also treats acute hypertension in pregnancy, hypertension associated with acute ischemic stroke, and intracranial hemorrhage, including subarachnoid hemorrhage.

Labetalol Structure and Mechanism of Action

The chemical name of Labetalol is 2-Hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]benzamide. Its chemical formula is C₁₉H₂₄N₂O₃, and its molecular weight is approximately 328.4 g/mol.

Labetalol inhibits the adrenergic stimulation of endothelial cell function. It acts on the beta-receptors in the bronchial and vascular smooth muscle leading to a decrease in adrenergic stimulation.

Labetalol Impurities and Synthesis

Labetalol treats high blood pressure. As with any pharmaceutical product, Labetalol may contain impurities. They can arise during manufacturing¹ or through external factors. Labetalol impurities can vary, but they are typically related to the synthesis or degradation of the drug. The common Labetalol impurities found in formulations include related compounds, such as diastereomers or enantiomers, and degradation products, that may result from exposure to light, heat, or moisture. Pharmaceutical manufacturers need to monitor and control the levels of impurities to ensure the safety and efficacy of Labetalol.

Daicel Pharma strictly adheres to cGMP standards and operates an analytical facility for preparing Labetalol impurities. We provide a range of Labetalol impurity standards, such as (R, R)-Labetalol, (R, S)-Labetalol, (S, R)-Labetalol, (S, S)-Labetalol, 5-[2-[Bis(phenylmethyl)amino]-1-hydroxyethyl]-2-hydroxybenzamide (Labetalol-bisbenzyl base], 5,5-Dibromoacetyl Salicylamide, and Labetalol Impurity C. Our impurities are accompanied by a detailed Certificate of Analysis (CoA) that includes a comprehensive characterization report. The CoA encompasses data obtained through techniques, 1H NMR, 13C NMR, IR, MASS, and HPLC purity analysis². Additional data, such as 13C-DEPT, can be provided upon request. We can synthesize unknown Labetalol impurities, degradation products, and labeled compounds to evaluate the efficacy of generic Labetalol. Each delivery has a comprehensive characterization report.