Dexniguldipine

A detailed overview of the calcium channel blocker Dexniguldipine

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477241123 | IUPAC_name = 3-ethyl 5-methyl 2-[[3-[[2-(3,4,5-trimethoxyphenyl)ethyl]methylamino]propyl]methylamino]-4-(3-nitrophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate | image = Dexniguldipine.png | width = 250 | CAS_number = 99740-62-2 | ATC_prefix = none | PubChem = 65951 | ChemSpiderID = 59363 | UNII = 3X7Q2F3K0F | KEGG = D07865 | ChEMBL = 2104660 | C=30 | H=39 | N=3 | O=8 | molecular_weight = 569.65 g/mol }}

Dexniguldipine is a calcium channel blocker that belongs to the dihydropyridine class of medications. It is primarily investigated for its potential use in treating hypertension and other cardiovascular conditions.

Pharmacology

Dexniguldipine functions by inhibiting the influx of calcium ions through L-type calcium channels in the smooth muscle cells of the vascular system. This action results in the relaxation of vascular smooth muscle, leading to vasodilation and a subsequent decrease in blood pressure.

Mechanism of Action

The mechanism of action of dexniguldipine involves the selective blockade of L-type calcium channels. By preventing calcium ions from entering the cells, dexniguldipine reduces the contractility of the smooth muscle, thereby decreasing peripheral vascular resistance and lowering blood pressure.

Pharmacokinetics

Dexniguldipine is absorbed through the gastrointestinal tract and undergoes extensive first-pass metabolism in the liver. The bioavailability of dexniguldipine is relatively low due to this first-pass effect. It is metabolized primarily by the cytochrome P450 enzyme system, and its metabolites are excreted via the kidneys.

Clinical Use

While dexniguldipine has shown promise in preclinical studies, its clinical use is not widespread. It is primarily used in research settings to explore its potential benefits in managing hypertension and other cardiovascular disorders.

Side Effects

As with other calcium channel blockers, dexniguldipine may cause side effects such as:

• Headache
• Dizziness
• Flushing
• Peripheral edema
• Gastrointestinal disturbances

Research and Development

Research on dexniguldipine is ongoing, with studies focusing on its efficacy, safety, and potential applications in various cardiovascular conditions. Its role in combination therapies and its effects on different patient populations are also areas of active investigation.

Also see

• Calcium channel blocker
• Hypertension
• Dihydropyridine
• Vasodilation