Nicardipine

Nicardipine
Names
Trade namesCardene, others
Other namesNicardipine hydrochloride
IUPAC name
  • 2-[benzyl(methyl)amino]ethylmethyl-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Clinical data
Drug classCalcium channel blocker (dihydropyridine)[1]
Main usesHigh blood pressure, heart related chest pain[1]
Side effectsSwelling, headache, palpations, low blood pressure[1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Routes of
use		By mouth, intravenous
Onset of actionWithin 15 min[2]
Duration of actionAbout 1 hr[2]
External links
AHFS/Drugs.comMonograph
MedlinePlusa695032
Legal
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetics
Protein binding>95%
Elimination half-life8.6 hours
Chemical and physical data
FormulaC26H29N3O6
Molar mass479.533 g·mol−1
3D model (JSmol)
Melting point136–138 °C (277–280 °F)
SMILES
  • O=C(OCCN(Cc1ccccc1)C)\C2=C(\N/C(=C(/C(=O)OC)C2c3cccc([N+]([O-])=O)c3)C)C
InChI
  • InChI=1S/C26H29N3O6/c1-17-22(25(30)34-4)24(20-11-8-12-21(15-20)29(32)33)23(18(2)27-17)26(31)35-14-13-28(3)16-19-9-6-5-7-10-19/h5-12,15,24,27H,13-14,16H2,1-4H3 checkY
  • Key:ZBBHBTPTTSWHBA-UHFFFAOYSA-N checkY

Nicardipine, sold under the brand name Cardene among others, is a medication used to treat high blood pressure and heart related chest pain.[1] It is also used for Raynaud's phenomenon.[3] It is given by mouth and injected into a vein.[1]

Common side effects include swelling, headache, palpations, and low blood pressure.[1] It should not be used in those with severe aortic stenosis.[1] It may be used in pregnancy.[4] It is a calcium channel blocker of the dihydropyridine class.[1] It works by dilating peripheral arteries.[1]

Nicardipine was patented in 1973 and first approved for medical use in 1981.[5] It was approved in the United States in 1988.[1] It is available as a generic medication.[4] In the United Kingdom 4 weeks of medication costs the NHS about £10 as of 2021.[4] In the United States this amount costs about 130 USD.[6]

Medical uses

It has been used in percutaneous coronary intervention.[7]

Dosage

For angina or high blood pressure it is used at a dose of 20 to 30 mg three times per day.[4]

For a hypertensive emergency it is often started at a dose of 5 mg/hr as an intravenous infusion.[4][2] This may be increased by 2.5 mg/hr every half hour up to 15 mg/hr.[2]

Society and culture

The patent for both Cardene and Cardene SR expired in October 1995.[8]

References

  1. 1 2 3 4 5 6 7 8 9 10 "Nicardipine Monograph for Professionals". Drugs.com. Archived from the original on 21 September 2021. Retrieved 12 November 2021.
  2. 1 2 3 4 "Hypertensive emergency". EMCrit Project. Archived from the original on 8 July 2023. Retrieved 21 May 2024.
  3. ↑ Pope, J (10 October 2013). "Raynaud's phenomenon (primary)". BMJ clinical evidence. 2013: 1119. PMID 24112969.
  4. 1 2 3 4 5 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 176. ISBN 978-0857114105.
  5. ↑ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 464. ISBN 9783527607495. Archived from the original on 2021-08-29. Retrieved 2021-09-18.
  6. ↑ "Nicardipine Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 22 September 2021. Retrieved 13 November 2021.
  7. ↑ Huang RI, Patel P, Walinsky P, et al. (November 2006). "Efficacy of intracoronary nicardipine in the treatment of no-reflow during percutaneous coronary intervention". Catheterization and Cardiovascular Interventions. 68 (5): 671–6. doi:10.1002/ccd.20885. PMID 17034064. S2CID 37071966.
  8. ↑ "Nicardipine at Medline PLus". Archived from the original on 2016-07-05. Retrieved 2021-09-18.
Identifiers:
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