NICARDIPINE HYDROCHLORIDE IN 0.83% 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 transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. It has greater selectivity for vascular smooth muscle than for cardiac muscle, leading to vasodilation and reduced peripheral vascular resistance. It does not significantly affect sinoatrial nodal or atrioventricular conduction.
| Metabolism | Primarily hepatic via cytochrome P450 isoenzymes CYP3A4 and CYP3A5, with minor contributions from CYP2C8. The drug undergoes extensive first-pass metabolism resulting in low oral bioavailability; however, intravenous administration bypasses first-pass metabolism. Metabolites are inactive and excreted primarily in urine (60%) and feces (35%). |
| Excretion | Primarily hepatic metabolism (>90%) with <1% unchanged drug excreted renally. Fecal excretion accounts for approximately 35% of metabolites via biliary elimination. |
| Half-life | Terminal elimination half-life is 8.6 hours (range 6-10 hours) in adults with normal hepatic function; prolonged in elderly or hepatic impairment. Clinical context: permits continuous IV infusion for stable hemodynamic control. |
| Protein binding | >95% bound to plasma proteins (primarily albumin, alpha-1-acid glycoprotein). High binding limits free drug concentration. |
| Volume of Distribution | 8.3 L/kg (0.08-0.17 L/kg in some sources; clinical meaning: extensive tissue distribution, particularly in vascular smooth muscle; Vd increases with hepatic impairment). |
| Bioavailability | Oral: ~35% (first-pass effect); IV: 100% (not applicable for this formulation, but provided for context). |
| Onset of Action | IV: 1-2 minutes (immediate dose-response); oral: 20-30 minutes (not applicable for this IV formulation). |
| Duration of Action | IV: 30-60 minutes (hemodynamic effects); clinical note: blood pressure declines gradually within 5-15 minutes of infusion start and returns to baseline within 30-60 minutes after cessation. |
| Molecular Weight | 515.99 |
Administer intravenously at an initial rate of 5 mg/h, titrated by increasing by 2.5 mg/h every 5-15 minutes to a maximum of 15 mg/h for hypertension. For substitution of oral therapy, start at 0.5 mg/h and titrate to achieve desired blood pressure.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment required for renal impairment; however, use with caution if GFR <30 mL/min due to risk of accumulation of nicardipine metabolites. |
| Liver impairment | In patients with cirrhosis and clinically significant portal hypertension (Child-Pugh class B or C), reduce initial dose to 0.5 mg/h and titrate cautiously. Monitor for hypotension and bradycardia. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: initial dose 0.5-1 mcg/kg/min continuous infusion, titrate up to 3-5 mcg/kg/min for hypertension. |
| Geriatric use | Start at lower initial infusion rate (3 mg/h) and titrate slowly due to decreased clearance and increased sensitivity to hypotension. Monitor closely for adverse effects. |
| 1st trimester | Limited human data; animal studies show fetal toxicity at high doses. Use only if potential benefit outweighs risk. |
| 2nd trimester | May cause fetal hypoxia and acidosis due to maternal hypotension. Avoid use during pregnancy, especially for chronic hypertension. |
| 3rd trimester | May inhibit labor and cause fetal distress. Use only for acute hypertensive emergencies when clearly needed. |
Clinical note
No significant drug interactions Can cause hypernatremia and fluid overload.
| FDA category | Animal |
| Placental transfer | Nicardipine crosses the placenta. Animal studies show placental transfer; human data limited but transfer confirmed with measurable fetal plasma concentrations. |
| Breastfeeding | Nicardipine is excreted into breast milk in low concentrations. A study reported relative infant dose of 2-3% of maternal weight-adjusted dose. Consider benefit of breastfeeding versus potential risk of adverse effects in infant, especially with high maternal doses or prolonged use. |
| Lactation Rating | L3: Probably Compatible |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate human studies; animal studies show teratogenicity (skeletal, cardiovascular) at high doses. Second/third trimesters: Risk of fetal hypoxia due to maternal hypotension; calcium channel blockers may inhibit uterine contractions. Use only if potential benefit outweighs risk. |
| Fetal Monitoring | Maternal: Blood pressure, heart rate, urine output, signs of hypotension. Fetal: Heart rate monitoring, ultrasound for growth restriction due to potential placental hypoperfusion. |
| Fertility Effects | No human data on fertility. In animal studies, high doses caused reduced fertility and implantation failure. Clinical significance unknown. |
■ FDA Black Box Warning
None
| Common Effects | fluid replacement |
| Serious Effects |
Advanced aortic stenosisHypersensitivity to nicardipine or any componentSevere hypotension (systolic BP < 90 mmHg)Cardiogenic shockPorphyria (acute intermittent porphyria)
| Precautions | Use caution in patients with coronary artery disease: may increase frequency, duration, or severity of angina during initiation or upward titration., Hypotension: monitor blood pressure closely; particularly in patients with reduced left ventricular function., Hepatic impairment: reduced clearance; consider dose reduction and monitor liver function., Renal impairment: may require dose adjustment; monitor renal function., Ventricular ectopy and ventricular tachycardia have been reported, especially in patients with preexisting conduction abnormalities., Avoid abrupt discontinuation; taper gradually to prevent rebound hypertension., Use with beta-blockers: increased risk of heart failure; monitor cardiac function. |
| Food/Dietary | Grapefruit and grapefruit juice are contraindicated as they increase nicardipine levels via CYP3A4 inhibition. High-fat meals may reduce absorption when taken orally, but IV route bypasses this. Avoid excessive sodium intake as it may counteract antihypertensive effects. |
| Clinical Pearls | For acute hypertension, administer as a continuous IV infusion (5 mg/hr, titrate up to 15 mg/hr). Monitor blood pressure every 5-15 minutes during titration. Use cautiously in advanced aortic stenosis; may precipitate angina. Extravasation can cause tissue necrosis; ensure central line access if peripheral infusion is prolonged. Nicardipine is photolabile; protect infusion bag from light and discard after 24 hours. In hepatic impairment or elderly, start at 3 mg/hr to avoid hypotension. |
| Patient Advice | Report any chest pain, irregular heartbeat, or dizziness immediately. · Avoid sudden standing to prevent orthostatic hypotension. · This medication is given intravenously; you will be monitored closely. · Notify nurse if you experience pain, redness, or swelling at the IV site. · Do not eat grapefruit or drink grapefruit juice while on this medication. |
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