NICARDIPINE HYDROCHLORIDE IN 0.86% 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 across the myocardial and vascular smooth muscle cell membranes, leading to vasodilation and reduced myocardial contractility.
| Metabolism | Primarily hepatic via cytochrome P450 3A4, with minor contribution from 2C8 and 2D6. Metabolites are inactive. |
| Excretion | Primarily hepatic metabolism; <1% excreted unchanged in urine. Biliary/fecal excretion accounts for approximately 35% of metabolites. |
| Half-life | Terminal elimination half-life is 2 to 4 hours; prolonged in hepatic impairment or with continuous infusion. |
| Protein binding | >95% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 0.7 L/kg (range 0.6-0.8 L/kg). Large Vd indicates extensive tissue distribution, including central nervous system. |
| Bioavailability | Oral: approximately 35% (extensive first-pass metabolism). IV: 100%. |
| Onset of Action | Intravenous: 1-2 minutes; oral: 20-30 minutes; onset after IV bolus is rapid due to direct vascular effect. |
| Duration of Action | Intravenous: 30-60 minutes after bolus; continuous infusion effects persist during infusion. Oral immediate-release: 4-6 hours; sustained-release: 12 hours. |
| Molecular Weight | 515.99 |
Intravenous infusion: initial rate 5 mg/hour, titrate by 2.5 mg/hour every 15 minutes as needed up to 15 mg/hour. For acute hypertension, 5 mg/hour initial, increase by 2.5 mg/hour every 5-15 minutes to maximum 15 mg/hour.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for GFR >= 30 mL/min. For GFR < 30 mL/min, use with caution and consider starting at lower doses (e.g., 3-5 mg/hour) due to potential accumulation. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B or C: Reduce initial dose by 50% (e.g., start at 2.5 mg/hour) and titrate slowly. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: intravenous infusion starting at 0.5-1 mcg/kg/min, titrate as needed; maximum 3-5 mcg/kg/min. Alternatively, for hypertensive emergencies: 0.5-3 mcg/kg/min continuous infusion. |
| Geriatric use | Start at lower end of dosing range (3-5 mg/hour intravenous) and titrate slowly due to increased sensitivity and potential for hypotension. Monitor closely. |
| 1st trimester | Limited human data; use only if benefit outweighs risk. Animal studies show teratogenicity at high doses. |
| 2nd trimester | May cause fetal hypoxia and acidosis; use cautiously. Avoid in preeclampsia due to risk of maternal hypotension and fetal distress. |
| 3rd trimester | May cause fetal hypoxia and acidosis; avoid for tocolysis. Use only if clearly needed. |
Clinical note
No significant drug interactions Can cause hypernatremia and fluid overload.
| FDA category | Animal |
| Placental transfer | Crosses placenta; fetal serum concentrations approximately 10-15% of maternal levels. |
| Breastfeeding | Excreted in breast milk in small amounts; use with caution. Monitor infant for hypotension and bradycardia. Consider alternative agents for chronic hypertension. |
| Lactation Rating | L3: Limited data, potential adverse effects |
| Teratogenic Risk | Pregnancy Category C. First trimester: Limited human data; animal studies show embryotoxicity and fetotoxicity at doses 4-10 times the maximum recommended human dose. Second and third trimesters: May cause maternal hypotension and fetal hypoxia; avoid use unless potential benefit outweighs risk. No adequate well-controlled studies in pregnant women. |
| Fetal Monitoring | Monitor maternal blood pressure and heart rate continuously during infusion. Assess fetal heart rate and uterine activity if used near term. Monitor for maternal hypotension, reflex tachycardia, and signs of preeclampsia. |
| Fertility Effects | No specific studies in humans. Animal studies at high doses (≥10 mg/kg/day) showed impaired fertility with reduced conception rates and increased resorptions. Clinical relevance unknown. |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | fluid replacement |
| Serious Effects |
Hypersensitivity to nicardipine or any componentAdvanced aortic stenosisCerebral edema or increased intracranial pressureCardiogenic shockConcurrent use with rifampin
| Precautions | May cause hypotension, especially with rapid dose escalation or in patients with compromised cardiac function, Use with caution in patients with heart failure, as negative inotropic effects may worsen symptoms, Avoid in patients with severe aortic stenosis due to risk of reduced coronary perfusion |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they inhibit CYP3A4 metabolism, increasing nicardipine levels and risk of adverse effects. |
| Clinical Pearls | Nicardipine is a dihydropyridine calcium channel blocker used for rapid blood pressure reduction in hypertensive emergencies. Administer as a continuous IV infusion, titrating by 0.5-1 mg/hour every 15 minutes; maximum dose 15 mg/hour. Monitor for reflex tachycardia, hypotension, and peripheral edema. Compatible with 0.86% sodium chloride; do not mix with other medications in the same IV line. Use with caution in patients with heart failure, as negative inotropic effects may occur. |
| Patient Advice | This medication is given intravenously to quickly lower your blood pressure. · You will be monitored closely for changes in heart rate and blood pressure. · Report any chest pain, shortness of breath, or swelling in your legs or ankles. · Avoid grapefruit and grapefruit juice while on this medication due to increased risk of side effects. · Do not stop the medication abruptly without consulting your healthcare provider. |
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