Chemistry:Nicardipine

From HandWiki
Short description: Antihypertensive drug of the calcium channel blocker class
Nicardipine
Nicardipine.svg
Clinical data
Trade namesCardene
AHFS/Drugs.comMonograph
MedlinePlusa695032
Routes of
administration
Oral, intravenous
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding>95%
Elimination half-life8.6 hours
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC26H29N3O6
Molar mass479.533 g·mol−1
3D model (JSmol)
Melting point136–138 °C (277–280 °F)
  (verify)

Nicardipine (Cardene) is a medication used to treat high blood pressure and angina. It belongs to the dihydropyridine class of calcium channel blockers (CCBs). It is also used for Raynaud's phenomenon. It is available in by mouth and intravenous formulations. It has been used in percutaneous coronary intervention.[1]

Its mechanism of action and clinical effects closely resemble those of nifedipine and the other dihydropyridine calcium channel blockers (amlodipine, felodipine), except that nicardipine is more selective for cerebral and coronary blood vessels. It is primarily a peripheral arterial vasodilator, thus unlike the nitrovasodilators (nitroglycerin and nitroprusside), cardiac preload is minimally affected. It has the longest duration among parenteral CCBs. [2][3] As its use may lead to reflex tachycardia, it is advisable to use it in conjunction with a beta-blocker.[3][2]

It was patented in 1973 and approved for medical use in 1981.[4]

Nicardipine was approved by the FDA in December 1988. The patent for both Cardene and Cardene SR expired in October 1995.[5]

See also

References

  1. "Efficacy of intracoronary nicardipine in the treatment of no-reflow during percutaneous coronary intervention". Catheterization and Cardiovascular Interventions 68 (5): 671–676. November 2006. doi:10.1002/ccd.20885. PMID 17034064. 
  2. 2.0 2.1 "Vasodilators". Anesthesiology Core Review: Part One Basic Exam.. McGraw Hill. 2014. ISBN 978-0-07-182137-7. https://accessanesthesiology.mhmedical.com/content.aspx?bookid=974&sectionid=61590560. 
  3. 3.0 3.1 "Hypertensive urgencies & emergencies.". Current Medical Diagnosis & Treatment. McGraw Hill. 2022. ISBN 978-1-2642-6938-9. https://accessmedicine.mhmedical.com/content.aspx?bookid=3081&sectionid=258962164. 
  4. (in en) Analogue-based Drug Discovery. John Wiley & Sons. 2006. p. 464. ISBN 978-3-527-60749-5. https://books.google.com/books?id=FjKfqkaKkAAC&pg=PA464. 
  5. "Nicardipine". Medline Plus. U.S. National Library of Medicine. https://www.nlm.nih.gov/medlineplus/druginfo/meds/a695032.html.