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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 |
| ATC code | |
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| Pharmacokinetic data | |
| Bioavailability | 4–8% |
| Protein binding | >99% |
| Metabolism | CYP3A4 |
| Eliminationhalf-life | 7–12 hours |
| Excretion | 70–80% via urine |
| Identifiers | |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.058.534 |
| Chemical and physical data | |
| Formula | C20H24N2O6 |
| Molar mass | 388.420 g·mol−1 |
| 3D model (JSmol) | |
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Nisoldipine is a pharmaceutical drug used for the treatment of chronicangina pectoris andhypertension. It is acalcium channel blocker of thedihydropyridine class. It is sold in theUnited States under theproprietary nameSular. Nisoldipine has tropism for cardiac blood vessels.[1]
It was patented in 1975 and approved for medical use in 1990.[2]
Nisoldipine is contraindicated in people withcardiogenic shock, unstable angina,myocardial infarction, and during pregnancy andlactation.[3]
Common side effects are headache, confusion, fast heartbeat, andedema. Hypersensitivity reactions are rare and includeangioedema.[3]
The substance is metabolized by the liver enzymeCYP3A4. Consequently, CYP3A4 inducers such asrifampicin orcarbamazepine could reduce the effectiveness of nisoldipine, while CYP3A4 inhibitors such asketoconazole increase the amount of nisoldipine in the body more than 20-fold.Grapefruit juice also increases nisoldipine concentrations by inhibiting CYP3A4.[3]It has also been reported to bindtubulin, blocking its polymerization.[4]
Nisoldipine is a calcium channel blocker that selectively inhibitsL-type calcium channels.[3]