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QuickView for Nisoldipine (compound)


PubChem
Name: Nisoldipine
PubChem Compound ID: 4499
Description: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.
Molecular formula: C20H24N2O6
Molecular weight: 388.414 g/mol
Synonyms:
Nisoldipine (JAN/USAN); 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2-methylpropyl ester, (+-)-; (+-)-Isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate; 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(2-nitrophenyl)-, methyl 2-methylpropyl ester; EINECS 264-407-7; Nisoldipine; 63675-72-9; Nisoldipino [INN-Spanish]; BRN 0454188; LS-131295.
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DrugBank
Identification
Name: Nisoldipine
Name (isomeric): DB00401
Drug Type: small molecule
Description: A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.
Synonyms:
Nisoldipin; Nisoldipino [INN-Spanish]; Nisoldipinum [INN-Latin]
Brand: Syscor, Zadipina, Sular, Baymycard, Nisocor
Category: Vasodilator Agents, Calcium Channel Blockers, Antihypertensive Agents
CAS number: 63675-72-9
Pharmacology
Indication: For the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
Pharmacology:
Nisoldipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Nisoldipine is similar to other peripheral vasodilators. Nisoldipine inhibits the influx of extra cellular calcium across the myocardial and...
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Mechanism of Action:
By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nisoldipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the m...
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Absorption: Relatively well absorbed into the systemic circulation with 87% of the radiolabeled drug recovered in urine and feces. The absolute bioavailability of nisoldipine is about 5%.
Protein binding: 99%
Biotransformation: Pre-systemic metabolism in the gut wall, and this metabolism decreases from the proximal to the distal parts of the intestine. Nisoldipine is highly metabolized; 5 major urinary metabolites have been identified. The major biotransformation pathway appears to be the hydroxylation of the isobutyl ester. A hydroxylated derivative of the side chain, present in plasma at concentrations approximately equal to the parent compound, appears to be the only active metabolite and has about 10% of the activity of the parent compound. Cytochrome P450 enzymes are believed to play a major role in the metabolism of nisoldipine. The particular isoenzyme system responsible for its metabolism has not been identified, but other dihydropyridines are metabolized by cytochrome P450 IIIA4.
Route of elimination: Although 60-80% of an oral dose undergoes urinary excretion, only traces of unchanged nisoldipine are found in urine.
Half Life: 7-12 hours
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Do not take with grapefruit juice as this has been shown to interfere with nisoldipine metabolism, resulting in a mean increase in Cmax of about 3-fold (up to about 7-fold) and AUC of almost 2-fold (up to 5-fold).
Drug interaction:
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of nisoldipine by decreasing its metabolism. Concomitant therapy should be avoided.
FosphenytoinPhenytoin decreases the efficiency of nisoldipine
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Nisoldipine. Avoid concurrent use of nisoldipine with strong inhibitors of CYP3A4, as the combination may lead to substantial increases in nisoldipine concentrations.
PhenytoinPhenytoin decreases the efficiency of nisoldipine
TelithromycinTelithromycin may reduce clearance of Nisoldipine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Nisoldipine if Telithromycin is initiated, discontinued or dose changed.
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