Nisoldipine CAS NO.63675-72-9
Active Pharmaceutical Ingredients 2025-03-03
Catalog ID80017143
CAS NO.63675-72-9
Purity 98%
MDL NumberMFCD00478055
EINEC264-407-7
Molecular formula C20H24N2O6
Molecular weight 388.4144
Melting point: 151~152℃
| Aspect | Details |
|---|---|
| Mechanism of Action | Nisoldipine is a dihydropyridine calcium channel blocker that inhibits the influx of calcium into vascular smooth muscle and cardiac muscle cells by blocking voltage-gated calcium channels. This action results in vasodilation, reduced peripheral vascular resistance, and decreased blood pressure. |
| Clinical Uses | It is primarily used to manage hypertension and can be used alone or in combination with other antihypertensive agents such as ACE inhibitors, diuretics, or beta-blockers. It is also used off-label for ischemic heart conditions like stable angina and Prinzmetal angina. |
| Pharmacokinetics | Nisoldipine has low oral bioavailability (about 5%) due to extensive first-pass metabolism. It is metabolized via the hepatic CYP3A4 pathway and excreted primarily through the kidneys. The elimination half-life is approximately 13.7 ± 4.3 hours. |
| Dosage Forms | Available as extended-release tablets in doses of 8.5 mg, 17 mg, and 34 mg for once-daily oral administration. |
| Side Effects | Common side effects include headache, dizziness, flushing, and peripheral edema. These effects are generally mild and transient. |
| Contraindications | It should be used with caution in patients with severe aortic stenosis and may not be suitable for those with a history of heart failure. |
| Interactions | Nisoldipine may interact with other drugs metabolized by the CYP3A4 enzyme, such as certain antifungal agents and macrolide antibiotics, which can increase its plasma concentration. |
| Special Considerations | It can penetrate the blood-brain barrier, which may be relevant in certain clinical scenarios. |
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