Chemistry:Nicardipine

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Nicardipine (Cardene) is a medication used to treat angina and hypertension, especially for hemorrhagic stroke patients.[1] 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.[2]

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.[3][4] As its use may lead to reflex tachycardia, it is advisable to use it in conjunction with a beta-blocker.[4][3] In the setting of a ruptured brain aneurysm, nicardipine may be used (if nimodipine is unavailable) to reduce blood pressure and as prevention or treatment against cerebral vasospasm.[1]

It was patented in 1973 and approved for medical use in 1981.[5] Nicardipine was approved by the FDA in December 1988. The patent for both Cardene and Cardene SR expired in October 1995.[6]

Medical uses

Hypertensive emergency

Nicardipine is a calcium channel blocker used primarily for the management of hypertension and angina. It is particularly effective in the treatment of acute and severe hypertension, including hypertensive emergency.[7] This is due to the rapid onset and short half-life of this drug, which allows for precision in the control of blood pressure.

Other

Nicardipine is also used commonly in the perioperative setting for blood pressure fluctuations during surgery.[8] Other scenarios for usage of Nicardipine include subarachnoid hemorrhage and hypertensive crisis of pregnancy.[9]

Side effects

Nicardipine is associated to a wide range of side effects, due mainly to its vasodilatory effects. Common adverse effects include dizziness, fainting, flushing and peripheral edema.[10] This is a direct result to the relaxation of blood vessels and lower systemic vascular resistance.

Hypotension is another frequently observed side effect, particularly seen in scenarios when this medication is used intravenously for hypertensive emergencies.[11] Reflex tachycardia is a common compensatory response to vasodilation.[12] These side effects are usually mild and resolve following adjustment in dosage of the medication or discontinuation.

See also

References

  1. ↑ 1.0 1.1 "Chapter 429: Subarachnoid Hemorrhage". Harrison's Principles of Internal Medicine (21st ed.). New York: McGraw Hill. 2022. ISBN 978-1-264-26850-4. 
  2. ↑ "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. 
  3. ↑ 3.0 3.1 "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. 
  4. ↑ 4.0 4.1 "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. 
  5. ↑ (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. 
  6. ↑ "Nicardipine". Medline Plus. U.S. National Library of Medicine. https://www.medlineplus.gov/druginfo/meds/a695032.html. 
  7. ↑ "CLUE: a randomized comparative effectiveness trial of IV nicardipine versus labetalol use in the emergency department". Critical Care 15 (3). 2011-06-27. doi:10.1186/cc10289. PMID 21707983. 
  8. ↑ "Comparison of nicardipine versus esmolol in attenuating the hemodynamic responses to anesthesia emergence and extubation" (in English). Journal of Cardiothoracic and Vascular Anesthesia 21 (1): 45–50. February 2007. doi:10.1053/j.jvca.2006.08.005. PMID 17289479. 
  9. ↑ "Antihypertensive Medications for Severe Hypertension in Pregnancy: A Systematic Review and Meta-Analysis". Healthcare 10 (2): 325. February 2022. doi:10.3390/healthcare10020325. PMID 35206939. 
  10. ↑ "Intravenous nicardipine hydrochloride: treatment of patients with severe hypertension". American Heart Journal 119 (2 Pt 2): 434–437. February 1990. doi:10.1016/S0002-8703(05)80064-X. PMID 2405613. 
  11. ↑ "Hemodynamic effects of intravenous nicardipine in severely pre-eclamptic women with a hypertensive crisis". Ultrasound in Obstetrics & Gynecology 47 (1): 89–95. January 2016. doi:10.1002/uog.14836. PMID 25721057. 
  12. ↑ "Abstract WP328: Suppression of Tachycardia and Cost Effectiveness of Bisoprolol Transdermal Patch Addition to Intravenous Nicardipine in Antihypertensive Treatment for Acute Intracerebral Hemorrhage". Stroke 49 (Suppl_1): AWP328. 2018-01-22. doi:10.1161/str.49.suppl_1.WP328. https://www.ahajournals.org/doi/10.1161/str.49.suppl_1.WP328. 



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