NICARDIPINE HYDROCHLORIDE IN 0.9% SODIUM CHLORIDE
Clinical safety rating: safe
No significant drug interactions Can cause hypernatremia and fluid overload.
Nicardipine is a dihydropyridine calcium channel blocker that inhibits the influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, resulting in vasodilation and reduced systemic vascular resistance.
| Metabolism | Hepatic via CYP3A4; undergoes extensive first-pass metabolism. |
| Excretion | Primarily hepatic metabolism; <1% excreted unchanged in urine. Metabolites are excreted renally and fecally. Fecal excretion accounts for approximately 35% of total elimination. |
| Half-life | Terminal elimination half-life is 8.6 hours (range 6–10 hours). In patients with hepatic impairment, half-life may be prolonged up to 14 hours. No significant change in renal impairment. |
| Protein binding | >95% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd is approximately 0.4 L/kg in healthy subjects, indicating moderate tissue distribution. Increased Vd in patients with hepatic cirrhosis (up to 1.0 L/kg). |
| Bioavailability | Oral bioavailability is approximately 35% due to extensive first-pass hepatic metabolism. Intravenous bioavailability is 100%. |
| Onset of Action | Intravenous administration: onset of hypotensive effect within 1–2 minutes. Oral: onset within 20 minutes. |
| Duration of Action | Intravenous: duration of hypotensive effect is 3–6 hours after discontinuation of infusion. Oral: duration of antihypertensive effect is 8 hours. |
Intravenous infusion: Initial rate 5 mg/hour, titrate by 2.5 mg/hour every 5-15 minutes to a maximum of 15 mg/hour. For hypertension, typical maintenance 3-5 mg/hour.
| Dosage form | INJECTABLE |
| Renal impairment | No specific GFR-based dose adjustment required; use with caution in severe renal impairment (CrCl <30 mL/min) and monitor closely. |
| Liver impairment | Child-Pugh Class A: Reduce initial dose to 2.5 mg/hour; titrate cautiously. Class B or C: Avoid use or use very low doses under close monitoring. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: Continuous infusion 0.5-5 mcg/kg/min, titrate to effect. Initiate at 0.5-1 mcg/kg/min. |
| Geriatric use | Elderly patients: Initiate at lower infusion rates (e.g., 2.5 mg/hour) and titrate slowly due to increased sensitivity and higher risk of hypotension. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
No significant drug interactions Can cause hypernatremia and fluid overload.
| FDA category | Animal |
| Breastfeeding | Excreted in breast milk in small amounts (M/P ratio unknown); use with caution, monitor infant for hypotension. |
| Teratogenic Risk | First trimester: Limited data; no clear evidence of major malformations in humans, but animal studies show fetotoxicity at high doses. Second/third trimester: Potential fetal hypoxia due to maternal hypotension; consider risk-benefit. |
■ FDA Black Box Warning
None.
| Common Effects | fluid replacement |
| Serious Effects |
["Known hypersensitivity to nicardipine or any component of the formulation","Patients with severe aortic stenosis (may reduce coronary perfusion pressure)","Patients with advanced aortic stenosis (may precipitate left ventricular failure)"]
| Precautions | ["May cause hypotension, especially in patients with compromised cardiac function","Use with caution in patients with hepatic impairment or reduced hepatic blood flow","May exacerbate angina in patients with obstructive coronary artery disease","Monitor blood pressure, heart rate, and ECG continuously during infusion","Risk of peripheral edema, headache, and reflex tachycardia"] |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate; fetal heart rate and uterine activity during IV infusion. |
| Fertility Effects | No significant adverse effects on fertility reported in animal studies; limited human data. |