Nisoldipine

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Nisoldipine
Skeletal formula of nisoldipine
Ball-and-stick model of the nisoldipine molecule
Names
Pronunciationnye sol' di peen[1]
Trade namesSular, Baymycard, Syscor, others
  • (RS)-Isobutyl methyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Clinical data
Drug classCalcium channel blocker (dihydropyridine)[2]
Main usesHigh blood pressure[2]
Side effectsSwelling, headache, palpitations, nausea, rash[2]
Pregnancy
category
  • US: C (Risk not ruled out)
Routes of
use		By mouth
External links
AHFS/Drugs.comMonograph
MedlinePlusa696009
Legal
Legal status
Pharmacokinetics
Bioavailability4–8%
Protein binding>99%
MetabolismCYP3A4
Elimination half-life7–12 hours
Excretion70–80% via urine
Chemical and physical data
FormulaC20H24N2O6
Molar mass388.414 g·mol−1
3D model (JSmol)
  • CC1=C(C(C(=C(N1)C)C(=O)OCC(C)C)c2ccccc2[N+](=O)[O-])C(=O)OC
  • InChI=1S/C20H24N2O6/c1-11(2)10-28-20(24)17-13(4)21-12(3)16(19(23)27-5)18(17)14-8-6-7-9-15(14)22(25)26/h6-9,11,18,21H,10H2,1-5H3
  • Key:VKQFCGNPDRICFG-UHFFFAOYSA-N

Nisoldipine, sold under the brand name Sular, is a medication used to treat high blood pressure.[2] It may be used by itself or with other medications.[2] It is taken by mouth.[2]

Common side effects include swelling, headache, palpitations, nausea, and rash.[2] Other side effects may include angina, low blood pressure], and allergic reactions.[2] While use during pregnancy is not well studied, risk is low.[3] It is a calcium channel blocker (CCB) of the dihydropyridine class.[2] It works by resulting in vasodilation of arteries.[1]

Nisoldipine was patented in 1975 and approved for medical use in 1990.[4] It was approved in the United States in 1995.[2] It is available as a generic medication.[1] In the United States it costs about 54 USD per month.[5]

Medical use

Dosage

It is often started at 17 mg per day and may be increased to 34 mg per day.[2]

Contraindications

Nisoldipine is contraindicated in people with cardiogenic shock, unstable angina, myocardial infarction, and during pregnancy and lactation.[6]

Side effects

Common side effects are headache, confusion, fast heartbeat, and edema. Hypersensitivity reactions are rare and include angioedema.[6]

Interactions

The substance is metabolized by the liver enzyme CYP3A4. Consequently, CYP3A4 inducers such as rifampicin or carbamazepine could reduce the effectiveness of nisoldipine, while CYP3A4 inhibitors such as ketoconazole increase the amount of nisoldipine in the body more than 20-fold. Grapefruit juice also increases nisoldipine concentrations by inhibiting CYP3A4.[6]

Pharmacology

Mechanism of action

Further information: Calcium channel blocker § Mechanism of action

Nisoldipine is a calcium channel blocker that selectively inhibits L-type calcium channels.[6] It has tropism for cardiac blood vessels.[7]

It is a second generation CCB.[1]

References

  1. ↑ 1.0 1.1 1.2 1.3 "Nisoldipine". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Archived from the original on 13 November 2021. Retrieved 13 November 2021.
  2. ↑ 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 "Nisoldipine Monograph for Professionals". Drugs.com. Archived from the original on 21 September 2021. Retrieved 13 November 2021.
  3. ↑ "Nisoldipine (Sular) Use During Pregnancy". Drugs.com. Archived from the original on 22 September 2021. Retrieved 13 November 2021.
  4. ↑ 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 2020-12-04.
  5. ↑ "Nisoldipine Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 13 November 2021.
  6. ↑ 6.0 6.1 6.2 6.3 Haberfeld, H, ed. (2019). Austria-Codex (in Deutsch). Vienna: Österreichischer Apothekerverlag. Syscor 5 mg-Filmtabletten.
  7. ↑ Knorr, Andreas M. (1995). "Why is nisoldipine a specific agent in ischemic left ventricular dysfunction?". The American Journal of Cardiology. 75 (13): E36–E40. doi:10.1016/S0002-9149(99)80446-9. PMID 7726122.

External links

Identifiers:
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