Onset of action:Within minutes (constant infusion)
Peak effect: 50% of the maximum effect is seen by 45 minutes
Duration: <8 hours; upon discontinuation of continuous infusion, a 50% decrease in effect is seen in ~30 minutes with gradual discontinuing antihypertensive effects for ~50 hours.
Distribution: Vd 8.3 L/kg.
Protein binding: >95%.
Metabolism: Hepatic; extensive first-pass effect (saturable); major pathway is via CYP3A4, 2C8, and 2D6.
Half-life elimination: Follow dose-dependent (nonlinear) pharmacokinetics; apparent or calculated half-life is dependent upon serum concentrations. alpha half-life 3 minutes; beta half-life 45 minutes; terminal half-life 14 hours
Excretion: Urine (IV: 49% as metabolites; <1% as unchanged drug); feces (IV: 43%)
Clearance: Decreased in patients with hepatic impairment; may be decreased in patients with renal impairment
禁忌症
Hypersensitivity to nicardipine or any component of the formulation; advanced aortic stenosis
懷孕分類
C 1. Limited placental transfer following maternal IV administration
2. Risk of adverse maternal events: headache, nausea, tachycardia, acute pulmonary edema (have been reported following use as a tocolytic)
3. Females with preexisting hypertension may continue their medication during pregnancy unless contraindications exist. Nicardipine may be used as an alternative agent for the treatment of acute onset, severe hypertension in pregnant females.
Acute hypertension (Continuous IV infusion):
1. Initial 5 mg/hour; may increase by 2.5 mg/hour every 5 minutes (for rapid titration) to every 15 minutes (for gradual titration) up to a maximum of 15 mg/hour
2. Adjust infusion rate as needed to maintain desired response; in rapidly titrated patients, consider reduction to 3 mg/hour after response is achieved
3. Discontinue infusion if unacceptable hypotension or tachycardia occurs.
Hypertensive emergency (Continuous IV infusion):
Note : In general, reduce mean arterial BP ~10% to 20% over the first hour, then 5% to 15% over the next 23 hours, unless there is a compelling indication (eg, acute aortic dissection, severe preeclampsia, eclampsia) for more rapid BP and heart rate control.
1. Initiate 5 mg/hour; titrate by 2.5 mg/hour at 5- to 15-minute intervals to goal target mean arterial pressure (maximum dose: 15 mg/hour).
小兒調整劑量
1. Bolus(optional): Initial 30 mcg/kg, maximum 2 mg/dose
2. Continuous infusion: Initial 0.5 to 1 mcg/kg/minute, titrate dose according to blood pressure; rate of infusion may be increased every 15 to 30 minutes; maximum: 4-5 mcg/kg/minute
腎功能調整劑量
There are no specific dosage adjustments provided in the manufacturer's labeling; titrate slowly with careful monitoring; dosage adjustment may be necessary.
肝功能調整劑量
There are no specific dosage adjustments provided in the manufacturer's labeling; titrate slowly with monitoring; dosage adjustment may be necessary.