Nisoldipine
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| Clinical data | |
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| Trade names | Sular, Baymycard, Syscor |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a696009 |
| Routes of administration | Oral |
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| Pharmacokineticdata | |
| Bioavailability | 4–8% |
| Protein binding | >99% |
| Metabolism | CYP3A4 |
| Eliminationhalf-life | 7–12 hours |
| Excretion | 70–80% via urine |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.058.534 |
| Chemical and physical data | |
| Formula | C20H24N2O6 |
| Molar mass | 388.420g·mol−1 |
| 3D model (JSmol) | |
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Nisoldipineis a pharmaceutical drug used for the treatment of chronicangina pectorisandhypertension.It is acalcium channel blockerof thedihydropyridineclass. It is sold in theUnited Statesunder theproprietary nameSular.Nisoldipine has tropism for cardiac blood vessels.[1]
It was patented in 1975 and approved for medical use in 1990.[2]
Contraindications
[edit]Nisoldipine is contraindicated in people withcardiogenic shock,unstable angina,myocardial infarction,and during pregnancy andlactation.[3]
Adverse effects
[edit]Common side effects are headache, confusion, fast heartbeat, andedema.Hypersensitivity reactions are rare and includeangioedema.[3]
Interactions
[edit]The substance is metabolized by the liver enzymeCYP3A4.Consequently, CYP3A4 inducers such asrifampicinorcarbamazepinecould reduce the effectiveness of nisoldipine, while CYP3A4 inhibitors such asketoconazoleincrease the amount of nisoldipine in the body more than 20-fold.Grapefruit juicealso increases nisoldipine concentrations by inhibiting CYP3A4.[3]
Pharmacology
[edit]Mechanism of action
[edit]Nisoldipine is a calcium channel blocker that selectively inhibitsL-type calcium channels.[3]
References
[edit]- ^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.PMID7726122.
- ^Fischer J, Ganellin CR (2006).Analogue-based Drug Discovery.John Wiley & Sons. p. 464.ISBN9783527607495.
- ^abcdHaberfeld H, ed. (2019).Austria-Codex(in German). Vienna: Österreichischer Apothekerverlag. Syscor 5 mg-Filmtabletten.
Further reading
[edit]- Mielcarek J, Grobelny P, Szamburska O (April 2005). "The effect of beta-carotene on the photostability of nisoldipine".Methods and Findings in Experimental and Clinical Pharmacology.27(3): 167–171.doi:10.1358/mf.2005.27.3.890873.PMID15834448.
- Missan S, Zhabyeyev P, Dyachok O, Jones SE, McDonald TF (November 2003)."Block of cardiac delayed-rectifier and inward-rectifier K+ currents by nisoldipine".British Journal of Pharmacology.140(5): 863–870.doi:10.1038/sj.bjp.0705518.PMC1574108.PMID14530219.
- Hamilton SF, Houle LM, Thadani U (1999). "Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure".Heart Disease.1(5): 279–288.PMID11720635.
External links
[edit]- Diseases Database(DDB):30009