NICARDIPINE HYDROCHLORIDE

Clinical safety rating: safe

Animal studies have demonstrated safety

How it works

Nicardipine is a dihydropyridine calcium channel blocker that inhibits the influx of extracellular calcium into myocardial and vascular smooth muscle cells, leading to coronary and peripheral vasodilation, reduced myocardial oxygen demand, and decreased systemic vascular resistance.

What the body does with it

Metabolism	Metabolized primarily by hepatic cytochrome P450 enzymes (CYP3A4) to inactive metabolites; undergoes extensive first-pass metabolism.
Excretion	Nicardipine is extensively metabolized in the liver; less than 1% of unchanged drug is excreted in urine. Approximately 60% of an administered dose is excreted in feces (primarily as metabolites) and 35% in urine (as metabolites).
Half-life	The terminal elimination half-life of nicardipine is approximately 8.6 hours. In clinical context, this supports twice-daily dosing for sustained-release formulations, though immediate-release forms require more frequent dosing due to shorter effective half-life.
Protein binding	Nicardipine is highly protein bound (>95%), primarily to albumin and alpha-1-acid glycoprotein.
Volume of Distribution	Volume of distribution is 1.2-2.2 L/kg, indicating extensive tissue distribution, with high affinity for adipose tissue and vascular smooth muscle.
Bioavailability	Oral immediate-release: approximately 35% (due to extensive first-pass metabolism). Oral sustained-release: approximately 35-40%. Intravenous: 100%.
Onset of Action	Intravenous: 1-2 minutes. Oral immediate-release: 20 minutes. Oral sustained-release: 30-60 minutes.
Duration of Action	Intravenous: 15-30 minutes after short infusion; continuous infusion required for sustained effect. Oral immediate-release: 3-6 hours. Oral sustained-release: 12 hours (supports twice-daily dosing).

Classification & Brands

Dosing & administration

20 mg orally three times daily; intravenously: 5 mg/hour initially, titrated to 15 mg/hour.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for mild to moderate renal impairment; not well studied in severe renal failure (CrCl <10 mL/min).
Liver impairment	Child-Pugh Class A and B: reduce oral dose to 20 mg twice daily; intravenous dose reduction to 1-2 mg/hour, titrate cautiously.
Pediatric use	Oral: initial 0.5-1 mg/kg/day in 3 divided doses, titrate up to 3 mg/kg/day (max 120 mg/day). Intravenous: 0.5-5 mcg/kg/min continuous infusion.
Geriatric use	Initiate at lower oral doses (e.g., 20 mg twice daily) due to increased bioavailability and prolonged half-life; monitor for hypotension.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Strong CYP3A4 inhibitors can significantly increase levels Can cause peripheral edema and reflex tachycardia.

Breastfeeding	Present in breast milk in low concentrations; M/P ratio unknown. Recommend caution due to potential adverse effects in infants (hypotension, bradycardia).
Teratogenic Risk	Limited human data; animal studies show no teratogenicity at therapeutic doses. First trimester: risk cannot be excluded; second/third trimester: associated with maternal hypotension and fetal hypoxia; use only if clearly needed.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Common Effects	angina
Serious Effects

Absolute Contraindications

["Hypersensitivity to nicardipine or any component","Advanced aortic stenosis (may reduce coronary perfusion)","Avoid in cardiogenic shock","Concurrent use with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin) may significantly reduce efficacy","Concurrent use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole) may increase toxicity"]

Clinical Precautions

Precautions

["Increased angina/acute myocardial infarction (especially during initiation or dose titration)","Beta-blocker withdrawal (taper beta-blockers slowly if discontinuing concurrent therapy)","Congestive heart failure (use caution in patients with severe left ventricular dysfunction)","Peripheral edema","Hepatic impairment (reduce dose in patients with decreased liver function)","Renal impairment (monitor renal function)"]

Clinical Tips & Counseling

Drug interactions

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