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QuickView for Nifedipine (compound)

Name: Nifedipine
PubChem Compound ID: 10383105
Description: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.
Molecular formula: C17H18N2O6
Molecular weight: 348.327 g/mol
Name: Nifedipine
Name (isomeric): DB01115
Drug Type: small molecule
Description: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.
Brand: Ecodipi, Zenusin, Nifar, Cordipin, Adalat Retard, Depin, Cardifen, Oxcord, Kordafen, Adalat Gits 30, Coral, Adalat 10, Corynphar, Dilafed, Alonix, Fenihidin, Alonix S, Cordicant, Calcigard, Nifidine, Aldipin, Introcar, Apo-Nifed, Adapine, Nifedipres, Corotrend, Nifedepat, Aprical, Cordalat, Nifedipine Retard, Corinfar, Nifangin, Adapress, Adalat LP, Camont, Fenamon, Pidilat, Tibricol, Fedcor, Hexadilat, Megalat, Nifdemin, Coracten, Nifelat, Nifelat Q, Hadipin, Orix, Chronadalate, Macorel, Nedipin, Alfadal, Adalat LA, Adalat CR, Nifipen, Adalat 20, Nifecor, Adalat CC, Calcibloc, Fenihidine, Sepamit, Nifecard, Anifed, Adalat, Glopir, Procardia XL, Procardia, Adalat 5, Nifedicor, Nifedin, Fenamon Sr, Adalate, Myogard, Cordafen, Ecodipin, Adalat Oros, Chronadalate Lp, Nifelan, Nicardia, Fedcor Retard, Cardionorm, Nifedine, Bonacid, Alpha-Nifedipine Retard, Anpine, Cardilat, Adalat Gits, Nifebene, Nificard, Nifedirex LP, Cordaflex, Adalat PA, Alat, Duranifin, Nifensar XL, Citilat, Dipinkor, Niphedipine, Dilcor, Adalat Ft, N1fedilat, Cordilan, Adalat Crono, Calcilat, Angipec, Nifelate, Ecodipin E, Dignokonstant
Category: Vasodilator Agents, Tocolytic Agents, Calcium Channel Blockers, Dihydropyridines
CAS number: 21829-25-4
Indication: For the management of vasospastic angina, chronic stable angina, hypertension, and Raynaud's phenomenon. May be used as a first line agent for left ventricular hypertrophy and isolated systolic hypertension (long-acting agents).
Nifedipine, the prototype of the dihydropyridine class of calcium channel blockers (CCBs), is similar to other dihydropyridines including amlodipine, felodipine, isradipine, and nicardipine. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channe...
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Mechanism of Action:
Nifedipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes ...
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Absorption: Rapidly and fully absorbed following oral administration.
Protein binding: 92-98%
Biotransformation: Hepatic metabolism via cytochrome P450 system. Predominantly metabolized by CYP3A4, but also by CYP1A2 and CYP2A6 isozymes.
Route of elimination: Nifedipine is extensively metabolized to highly water-soluble, inactive metabolites accounting for 60 to 80% of the dose excreted in the urine. The remainder is excreted in the feces in metabolized form, most likely as a result of biliary excretion.
Half Life: 2 hours
Toxicity: Symptoms of overdose include dizziness, drowsiness, nausea, severe drop in blood pressure, slurred speech, and weakness. LD50=494 mg/kg (orally in mice); LD50=1022 mg/kg (orally in rats)
Affected organisms: Humans and other mammals
Food interaction:
Grapefruit down-regulates post-translational expression of CYP3A4, the major metabolizing enzyme of nifedipine. Grapefruit, in all forms (e.g. whole fruit, juice and rind), can significantly increase serum levels of nifedipine and may cause toxicity. Avoid grapefruit products while on this medication.
Avoid alcohol.
Take with low fat meal.
Avoid natural licorice.
Drug interaction:
MelatoninMelatonin can possibly decrease the effect of nifedipine
TalbutalThe barbiturate, talbutal, decreases the effect of the calcium channel blocker, nifedipine.
QuinupristinSynercid increases the effect of ziprasidone
MethohexitalThe barbiturate, methohexital, decreases the effect of the calcium channel blocker, nifedipine.
QuinidineDecreased quinidine effect, increased nifedipine effect
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