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Brand Name :
Cardene IV, Cardene SR
Synonyms :
nicardipine
Class :
Calcium Channel Blockers, Dihydropyridines
Dosage Forms & Strengths
Capsule
20 mg
30 mg
Capsule (extended release)
30 mg
45 mg
60 mg
Infusion solution
20mg/200ml
40mg/200ml
Injectable solution
2.5mg/ml
Take 20 to 40 mg orally every 8 hours
Administer dose of 5 mg/hr intravenously by slow infusion initially and it may be raised by 2.5 mg/hr every 15 minutes
Not more than 15 mg/hr
Take 20 to 40 mg orally every 8 hours
Start at 20 mg, and allow three days between dose raise to achieve steady-state plasma drug concentration
General daily dose range be 60 to 120 mg
Dosing Modifications
Renal impairment
Take a dose of 20 mg as immediate release orally every 8 hour initially and titrated in every three days
Take a dose of 30 mg as extended release orally every 12 hours initially and titrated in every three days
Use cautiously as intravenously
Hepatic impairment
Take a dose of 20 mg as immediate release orally every 12 hour initially and titrated in every three days
Daily immediate-release dose, may be not equivalent to daily extended-release dose
Use cautiously as intravenously
Pitt-Hopkins Syndrome (Orphan)
Orphan designation for treatment of Pitt-Hopkins Syndrome
Dosage Forms & Strengths
Capsule
20 mg
30 mg
Capsule (extended release)
30 mg
45 mg
60 mg
Infusion solution
20mg/200ml
40mg/200ml
Injectable solution
2.5mg/ml
Administer dose of 0.5 to 3 mcg/kg/min intravenously
Refer to adult dosing
nicardipine: they may enhance the serum concentration of CYP2D6 Inhibitors
nicardipine: they may enhance the serum concentration of CYP2D6 Inhibitors
nicardipine: they may enhance the serum concentration of CYP2D6 Inhibitors
nicardipine: they may enhance the serum concentration of CYP2D6 Inhibitors
nicardipine: they may enhance the serum concentration of CYP2D6 Inhibitors
CYP3A strong enhancers of the small intestine may reduce the bioavailability of nicardipine
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
may enhance the hypotensive effect of calcium channel blockers
bunazosin (Not available in the United States)
may enhance the hypotensive effect of calcium channel blockers
may enhance the hypotensive effect of calcium channel blockers
may enhance the hypotensive effect of calcium channel blockers
may enhance the hypotensive effect of calcium channel blockers
It may diminish the effect when combined with griseofulvin by CYP3A4 metabolism
it may diminish the therapeutic efficacy when combined with castor oil
nicardipine: they may diminish the serum concentration of CYP3A4 Inducers
nicardipine: they may diminish the serum concentration of CYP3A4 Inducers
nicardipine: they may diminish the serum concentration of CYP3A4 Inducers
nicardipine: they may diminish the serum concentration of CYP3A4 Inducers
nicardipine: they may diminish the serum concentration of CYP3A4 Inducers
has a synergistic effect over brentuximab vedotin by showing altered intestinal/hepatic CYP3A4 enzyme metabolism.
increase the therapeutic effect of daunorubicin by P-glycoprotein efflux transporter
the effect of nicardipine is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
increase the therapeutic effect of idarubicin by P-glycoprotein efflux transporter
metronidazole enhances the effect of nicardipine by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it may enhance the QTc-prolonging effect of levoketoconazole
QTc-prolongers increase the effect of levoketoconazole
nicardipine, when taken with ixazomib, alters the intestinal/hepatic CYP3A4 enzyme metabolism
Actions and Spectrum
nicardipine blocks the entry of calcium into smooth muscle cells in the walls of blood vessels and the heart.
This leads to a reduction in peripheral vascular resistance and a decrease in blood pressure.
Frequency defined
1-10%
Flushing (6-10%)
Headache (PO; 6.3%)
Hypotension (IV; 6%)
Polyuria (IV; 1%)
Nausea (PO; 1.6%)
Dizziness (1%)
Asthenia (PO; 3%)
Rash (PO; 1%)
Ventricular extrasystoles (IV; 1%)
Exacerbation of angina (6%)
Peripheral edema (PO; 6-8%)
Pedal edema (PO; 6.8%)
>10%
Headache (IV; 15%)
<1%
Facial edema
Myalgia (PO)
Tachycardia
Hypotension (PO)
Asthenia (IV)
Syncope (IV)
Black Box Warning
None
Contraindication/Caution:
Contraindication:
Caution:
Pregnancy consideration:
Pregnancy category: C
Lactation: Excretion into human milk is unknown
Pregnancy Categories:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category.
Pharmacology
Without affecting serum calcium concentrations, calcium-channel blockers prevent extracellular calcium ions from crossing the membranes of cardiac cells and vascular smooth muscle cells.
Pharmacodynamics
The primary pharmacodynamic effect of nicardipine is arterial vasodilation. By relaxing the smooth muscle cells in arterial walls, nicardipine reduces peripheral vascular resistance, allowing for increased blood flow and decreased blood pressure.
Pharmacokinetics
Absorption
nicardipine is absorbed after ingestion, but it undergoes significant first-pass metabolism in the liver, resulting in an oral bioavailability of approximately 35 to 55%.
Distribution
nicardipine has a volume of distribution, indicating distribution into tissues. It binds extensively to plasma proteins, albumin about 95%.
Metabolism
nicardipine undergoes hepatic metabolism through the cytochrome P450 enzyme.
Elimination and excretion
nicardipine is eliminated through the biliary and fecal routes. The elimination half-life is approximately 1 to 2 hours.
Administration
nicardipine is available in oral tablet form.
It is also available as an intravenous formulation.
Patient information leaflet
Generic Name: nicardipine
Why do we use nicardipine?
nicardipine is used for the treatment of hypertension (high blood pressure) and certain types of angina (chest pain).
nicardipine is used for treatment of smooth muscles in arterioles (smaller arteries) and peripheral resistance vessels.