Nisoldipine

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Nisoldipine
Nisoldipine structure.svg
Nisoldipine-3D-balls.png
Clinical data
Trade names Sular, Baymycard, Syscor
AHFS/Drugs.com Monograph
MedlinePlus a696009
Routes of
administration
Oral
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 4–8%
Protein binding >99%
Metabolism CYP3A4
Elimination half-life 7–12 hours
Excretion 70–80% via urine
Identifiers
  • (RS)-Isobutyl methyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.058.534 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C20H24N2O6
Molar mass 388.420 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
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Nisoldipine is a pharmaceutical drug used for the treatment of chronic angina pectoris and hypertension. It is a calcium channel blocker of the dihydropyridine class. It is sold in the United States under the proprietary name Sular. Nisoldipine has tropism for cardiac blood vessels. [1]

Contents

It was patented in 1975 and approved for medical use in 1990. [2]

Contraindications

Nisoldipine is contraindicated in people with cardiogenic shock, unstable angina, myocardial infarction, and during pregnancy and lactation. [3]

Adverse effects

Common side effects are headache, confusion, fast heartbeat, and edema. Hypersensitivity reactions are rare and include angioedema. [3]

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. [3]

Pharmacology

Mechanism of action

Nisoldipine is a calcium channel blocker that selectively inhibits L-type calcium channels. [3]

Related Research Articles

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References

  1. Knorr AM (April 1995). "Why is nisoldipine a specific agent in ischemic left ventricular dysfunction?". The American Journal of Cardiology. 75 (13): 36E–40E. doi:10.1016/S0002-9149(99)80446-9. PMID   7726122.
  2. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 464. ISBN   9783527607495.
  3. 1 2 3 4 Haberfeld H, ed. (2019). Austria-Codex (in German). Vienna: Österreichischer Apothekerverlag. Syscor 5 mg-Filmtabletten.

Further reading