CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER
Clinical safety rating
cautionComprehensive clinical and safety monograph for CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER (CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER).
Nicardipine is a dihydropyridine calcium channel blocker that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. It causes vasodilation and decreases systemic vascular resistance.
| Metabolism | Extensively metabolized in the liver via cytochrome P450 (CYP) enzymes, primarily CYP3A4 and CYP2C8, to inactive metabolites. |
| Excretion | Primarily hepatic metabolism to inactive metabolites; <1% excreted unchanged in urine. Biliary/fecal excretion of metabolites accounts for approximately 60-70% of total elimination, with renal excretion of metabolites approximately 30-40%. |
| Half-life | 2 to 4 hours in healthy subjects; increased in hepatic impairment (up to 7 hours) and in elderly. No significant change in renal impairment. |
| Protein binding | >95% bound to plasma proteins (primarily albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | 8.4 L/kg (0.084 L/kg for a 70 kg adult? Please check: typical Vd is 8.4 L/kg? Actually nicardipine Vd is about 8.4 L/kg, which is large, indicating extensive tissue distribution). Correct: Vd = 8.4 L/kg (range 0.6-8.4 L/kg? Standard value is ~8.4 L/kg). |
| Bioavailability | Oral: 35% (extensive first-pass metabolism); intravenous: 100%. |
| Onset of Action | Intravenous infusion: within 5-15 minutes; oral administration: 20-30 minutes. |
| Duration of Action | Intravenous infusion: 2-4 hours (blood pressure reduction); oral: 6-8 hours for extended-release formulation. |
| Molecular Weight | 515.56 Da (nicardipine hydrochloride) |
Intravenous infusion: initial dose 5 mg/hour, titrate by 2.5-5 mg/hour every 15-30 minutes as needed; maximum 15 mg/hour. Oral: 20 mg three times daily initially, then 30-40 mg three times daily.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: maximum IV infusion rate 8 mg/hour; CrCl <30 mL/min: maximum IV infusion rate 5 mg/hour. Oral: no adjustment specified but monitor closely. |
| Liver impairment | Child-Pugh Class A: start with 50% of usual dose; Class B: start with 25% of usual dose; Class C: avoid use or use extreme caution. |
| Pediatric use | Limited data; for IV infusion, start at 0.5 mcg/kg/min and titrate to effect; typical range 0.5-5 mcg/kg/min. Oral: 0.5-1 mg/kg/dose three times daily (max 30 mg/dose). |
| Geriatric use | Start at lower end of dosing range; IV infusion initial rate 3 mg/hour; oral initial dose 20 mg twice daily; monitor blood pressure closely. |
| 1st trimester | Cardene (nicardipine) is a dihydropyridine calcium channel blocker. In first trimester, data are limited; animal studies show embryotoxicity at high doses. Use only if benefit outweighs risk. |
| 2nd trimester | Second trimester use may be associated with risk of fetal hypoxia and metabolic acidosis; consider alternative agents. |
| 3rd trimester | Third trimester use may cause uteroplacental hypoperfusion and fetal distress; avoid use in pregnancy for chronic hypertension. May be used intravenously in preeclampsia for blood pressure control. |
Clinical note
Comprehensive clinical and safety monograph for CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER (CARDENE IN 5.0% DEXTROSE IN PLASTIC CONTAINER).
| Placental transfer | Nicardipine crosses the placenta; umbilical cord/maternal plasma ratio approximately 1.0. |
| Breastfeeding | Nicardipine is excreted into breast milk in small amounts; estimated infant dose <5% of maternal weight-adjusted dose. Monitor infant for hypotension and constipation. |
| Lactation Rating | L2 (Probably Compatible) |
| Teratogenic Risk | NICARDIPINE (CARDENE) is a calcium channel blocker. Animal studies (rats, rabbits) showed embryotoxicity, fetotoxicity, and teratogenicity at doses ≥10× human dose. In humans, no adequate controlled studies; first trimester: potential for teratogenic risk (class C). Second and third trimesters: may cause fetal hypoxia, metabolic acidosis, and hypotension due to maternal hypotension. Use only if benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of hypotension. Monitor fetal heart rate and uterine activity during intravenous infusion. Assess for fetal growth restriction if used long-term. |
| Fertility Effects | In animal studies, high doses caused impaired fertility and reduced spermatogenesis. Human data insufficient; potential for transient hormonal effects. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to nicardipine or any componentAdvanced aortic stenosis
| Precautions | Use caution in patients with coronary artery disease due to risk of increased angina or myocardial infarction, May cause hypotension, hepatic impairment, and elevated liver enzymes, May exacerbate congestive heart failure, Use with caution in patients with impaired renal function, Monitor blood pressure and heart rate during infusion |
| Food/Dietary | Grapefruit and grapefruit juice may increase nicardipine levels; avoid concurrent use. No other significant food interactions. Maintain a heart-healthy, low-sodium diet as recommended for hypertension management. |
| Clinical Pearls | Cardene (nicardipine) IV infusion in D5W is a dihydropyridine calcium channel blocker used for short-term treatment of hypertension when oral therapy is not feasible. It is photosensitive; protect from light. Administer via central line due to peripheral vein irritation. Titrate based on blood pressure response; onset within minutes. Use with caution in patients with severe aortic stenosis, heart failure, or hepatic impairment. Avoid in patients with advanced aortic stenosis due to risk of reducing coronary perfusion. |
| Patient Advice | This medication is given intravenously to lower blood pressure quickly. · Your blood pressure and heart rate will be monitored closely during infusion. · Report any pain, redness, or swelling at the IV site immediately. · Avoid sudden position changes to prevent dizziness or fainting. · Do not stop the infusion without medical guidance. · Inform your healthcare provider if you have liver disease, heart failure, or aortic stenosis. |
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