Drug intelligence / Profile preview

nicardipine + labetalol + urapidil

Development stage
Unknown
Lead developer
Chiesi
Modality
Small Molecules
Administration
Intravenous
01

Overview

This is a combination of three antihypertensive agents—nicardipine, labetalol, and urapidil—used together for the rapid management of severe hypertension or hypertensive emergencies. - **Nicardipine** is a dihydropyridine calcium channel blocker that inhibits the influx of calcium ions into vascular smooth muscle and cardiac muscle, leading to vasodilation and reduced blood pressure. - **Labetalol** is a combined alpha-1 adrenergic receptor antagonist and non-selective beta-adrenergic receptor antagonist; it decreases systemic vascular resistance (via alpha blockade) while also reducing heart rate and contractility (via beta blockade). - **Urapidil** acts as an alpha-1 adrenergic receptor antagonist causing vasodilation, but also as a serotonin 5-HT1A receptor agonist which further reduces sympathetic outflow from the central nervous system. Urapidil’s dual mechanism allows effective blood pressure reduction with minimal reflex tachycardia[5][6][7]. This combination may be used in critical care settings where rapid titration of intravenous antihypertensives is required to achieve target blood pressures in conditions such as hypertensive emergencies, acute intracerebral hemorrhage, pre-eclampsia/eclampsia, or perioperative hypertension[1][2].

02

Targets

ADORA2A (Adenosine A₂A Receptor)ADRB1 (β1)TRPA1 (Transient receptor potential cation channel subfamily A member 1)ADORA3 (Adenosine A3 receptor)ADRB2 (β2)ADRA1A (α1A)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))ADORA1 (Adenosine receptor A1 subtype)CYP3A4 (Cytochrome P450 3A4)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)

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