Drug intelligence / Profile preview

labetalol + nicardipine

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous
01

Overview

Labetalol + nicardipine is a combination of two antihypertensive agents used together, primarily in acute care settings for the management of severe hypertension or hypertensive emergencies. Labetalol is a non-selective beta-adrenergic blocker with additional selective alpha-1 adrenergic blocking activity, resulting in decreased blood pressure through vasodilation and reduced heart rate. Nicardipine is a dihydropyridine calcium channel blocker that inhibits calcium ion influx into vascular smooth muscle and myocardium, leading to arterial vasodilation and reduction in systemic vascular resistance. The combination may be used when rapid blood pressure control is required or when monotherapy does not achieve target pressures, such as during hypertensive crises or perioperative management. Both drugs are administered intravenously in acute settings; labetalol typically by bolus injection and nicardipine by continuous infusion[1][2][3][4].

02

Targets

ADRA1A (α1A)ADRB1 (β1)ADRB2 (β2)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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