- Guide to PHARMACOLOGY
Synonyms: (R,S)-nicardipine | Cardene®
nicardipine is an approved drug (FDA (1988))
Compound class: Synthetic organic
Comment: One of the dihydropyridine class of drugs.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: nicardipine
|No information available.|
|Summary of Clinical Use|
|Nicardipine acts as a vasodilator and has anti-hypertensive properties. Used in the treatment of angina and coronary spasms, nicardipine has also been used in asthma treatment.|
|Mechanism Of Action and Pharmacodynamic Effects|
|Nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes, by means of three mechanisms: deforming calcium channels, inhibiting ion-control gating mechanisms and and interfering with the release of calcium from the sarcoplasmic reticulum. This results in a decrease in intracellular calcium which inhibits the contractile processes of the myocardial smooth muscle, which leads to dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure and decreased afterload.
Due to the complex nature of this drug's MMOA, and the paucity of (human) affinity data, we do not tag a primary drug target.
For extended ADME data see the following: