NICARDIPINE HYDROCHLORIDE IN 0.9% SODIUM CHLORIDE
Clinical safety rating
safeNo 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. |
| Molecular Weight | 479.61 |
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 | Limited human data; animal studies show no teratogenicity but use only if clearly needed during first trimester. |
| 2nd trimester | Calcium channel blockers may cause uterine relaxation; use with caution due to potential for hypotension and fetal hypoxia. |
| 3rd trimester | May inhibit labor; use only if benefit outweighs risk. Monitor maternal blood pressure and fetal heart rate. |
Clinical note
No significant drug interactions Can cause hypernatremia and fluid overload.
| FDA category | Animal |
| Placental transfer | NICARDIPINE crosses the placenta (fetal-to-maternal ratio approximately 0.14–0.17). |
| Breastfeeding | NICARDIPINE is excreted into breast milk in small amounts (estimated relative infant dose <2%). No adverse effects reported in breastfed infants; however, caution is advised, especially in preterm or neonates with impaired renal function. |
| Lactation Rating | L2 (Probably Compatible) |
| 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. |
| 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. |
■ FDA Black Box Warning
None.
| Common Effects | fluid replacement |
| Serious Effects |
Advanced aortic stenosisHypersensitivity to nicardipine or any componentSystolic blood pressure <90 mmHgAcute porphyria (if using IV formulation due to propylene glycol)
| 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 |
| Food/Dietary | NO FOOD INTERACTIONS DUE TO INTRAVENOUS ROUTE. HOWEVER, GRAPEFRUIT JUICE MAY INCREASE SYSTEMIC EXPOSURE IF TAKEN ORALLY; IV ADMINISTRATION NOT AFFECTED. |
| Clinical Pearls | NICARDIPINE IS A DIHYDROPYRIDINE CALCIUM CHANNEL BLOCKER WITH HIGH VASCULAR SELECTIVITY. INTRAVENOUS ADMINISTRATION ALLOWS PRECISE TITRATION FOR HYPERTENSIVE URGENCY OR EMERGENCY. IT IS METABOLIZED BY CYP3A4; CAUTION WITH STRONG INHIBITORS/INDUCERS. CONTINUOUS BLOOD PRESSURE MONITORING REQUIRED. MAY CAUSE REFLEX TACHYCARDIA. AVOID IN ADVANCED AORTIC STENOSIS. SOLUTION IS LIGHT-SENSITIVE; PROTECT FROM LIGHT DURING INFUSION. TITRATE TO TARGET BP; ONSET ~5 MIN, DURATION 3-4 HOURS. |
| Patient Advice | This medication is given intravenously to quickly lower your blood pressure. · Your blood pressure will be monitored continuously during infusion. · Report any symptoms of dizziness, headache, or ankle swelling. · Do not stop the medication abruptly; it is administered by healthcare professionals. · Inform your healthcare provider if you have liver disease or aortic stenosis. |
Loading safety data…