Angina: Oral: 20 mg 3 times daily; usual dosage: 20 to 40 mg 3 times daily (allow ≥3 days between dose increases).
Hypertension: Oral: Initial: 20 mg 3 times daily; usual dosage: 20 to 40 mg 3 times daily (allow ≥3 days between dose increases).
Acute hypertension: Continuous IV infusion: 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; adjust infusion rate as needed to maintain desired response; in rapidly titrated patients, consider reduction to 3 mg/hour after response is achieved. Discontinue infusion if unacceptable hypotension or tachycardia occurs.
Acute ischemic stroke, BP management with reperfusion therapy (off-label use):
Note: Prior to reperfusion therapy (thrombolytic and/or mechanical thrombectomy), maintain a target BP of ≤185/110 mm Hg. If BP remains >185/110 mm Hg, do not administer thrombolytic. During and 24 hours after start of thrombolytic therapy, maintain a target BP of ≤180/105 mm Hg; if hypertension is refractory or diastolic BP >140 mm Hg, consider alternative therapy (AHA/ASA [Powers 2019]).
Continuous IV infusion: Initial: 5 mg/hour; titrate by 2.5 mg/hour at 5- to 15-minute intervals (maximum dose: 15 mg/hour) (AHA/ASA [Powers 2019]).
Hypertensive emergency:
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 (ACC/AHA [Whelton 2018]; Elliott 2021).
Continuous IV infusion: 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) (ACC/AHA [Whelton 2018]; Peixoto 2019).
Intracerebral hemorrhage, blood pressure management (off-label use):
Note: In patients who present within 6 hours of acute intracerebral hemorrhage and have systolic BP between 150 and 220 mm Hg, decreasing systolic BP to <140 mm Hg is not beneficial and can be harmful (ACC/AHA [Whelton 2018]).
Patients who present with systolic BP >220 mm Hg:
Continuous IV infusion: Initiate 5 mg/hour; titrate by 2.5 mg/hour at 5- to 15-minute intervals to recommended target systolic BP (maximum dose: 15 mg/hour) (AHA/ASA [Broderick 2007]; Mocco 2006; Ortega-Gutierrez 2013).
Subarachnoid hemorrhage, blood pressure management (off-label use):
Note: Optimal therapy is not well established. Cautious use of antihypertensive therapy to decrease the risk of rebleeding may be appropriate in some patients with systolic BP >160 mm Hg or mean arterial pressure >110 mm Hg with adequate cerebral perfusion pressure (AHA/ASA [Connolly 2012]; Diringer 2011).
Continuous IV infusion: Initiate 5 mg/hour; titrate by 2.5 mg/hour at 5- to 15-minute intervals to goal target systolic BP or mean arterial pressure (maximum dose: 15 mg/hour) (Mocco 2006).
Substitution for oral therapy (approximate equivalents):
20 mg every 8 hours oral, equivalent to 0.5 mg/hour IV infusion.
30 mg every 8 hours oral, equivalent to 1.2 mg/hour IV infusion.
40 mg every 8 hours oral, equivalent to 2.2 mg/hour IV infusion.
Conversion to oral antihypertensive agent: Initiate oral antihypertensive at the same time that IV nicardipine is discontinued; if transitioning to oral nicardipine, start oral nicardipine 1 hour prior to IV discontinuation.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Oral: Initial: 20 mg 3 times daily; titrate slowly.
IV: There are no specific dosage adjustments provided in the manufacturer's labeling; titrate slowly with careful monitoring; dosage adjustment may be necessary.
Oral: Initial: 20 mg twice daily; titrate slowly.
IV: There are no specific dosage adjustments provided in the manufacturer's labeling; titrate slowly with monitoring; dosage adjustment may be necessary.
(For additional information see "Nicardipine: Pediatric drug information")
Hypertension: Note: Use should be reserved for acute severe hypertension: Limited data available: Infants, Children, and Adolescents: Continuous IV infusion: Bolus dose (optional): Initial: 30 mcg/kg, maximum dose: 2 mg/dose; followed by 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 dose: 4 to 5 mcg/kg/minute (AAP [Flynn 2017]; Flynn 2000; Flynn 2001). In a retrospective analysis (n=29; mean age: 7.8 ± 6 years [range: 2 days to 17.9 years]), the mean initial dose was 0.8 ± 0.3 mcg/kg/minute (range: 0.2 to 1.3 mcg/kg/minute), the mean effective dose was 1.8 ± 1 mcg/kg/minute (range: 0.3 to 4 mcg/kg/minute); blood pressure was controlled within 2.7 ± 2.1 hours (range: 0.5 to 9 hours) after starting nicardipine continuous infusion (Flynn 2001).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
IV: Infants, Children, and Adolescents: There are no dosage adjustments provided in the manufacturer's labeling; based on experience in adult patients, titrate slowly; monitor closely, dosing adjustment may be necessary.
IV: Infants, Children, and Adolescents: There are no dosage adjustments provided in the manufacturer's labeling; however, nicardipine is extensively metabolized by the liver. Based on experience in adult patients, consider initiating at lower doses and titrating slowly; careful monitoring is warranted and dosing adjustment may be necessary.
Initiate at the low end of the dosage range. Specific guidelines for adjustment of nicardipine are not available, but careful monitoring is warranted and adjustment may be necessary.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral, as hydrochloride:
Generic: 20 mg, 30 mg
Solution, Intravenous [preservative free]:
Generic: 20 mg/200 mL in NaCl 0.9% (200 mL); 40 mg/200 mL in NaCl 0.9% (200 mL)
Solution, Intravenous, as hydrochloride:
Cardene IV: 20 mg (200 mL); 40 mg (200 mL)
Generic: 2.5 mg/mL (10 mL)
Solution, Intravenous, as hydrochloride [preservative free]:
Generic: 2.5 mg/mL (10 mL)
Yes
Oral: Administer without regards to meals.
IV:
Administer as a slow continuous infusion via central line or through a large peripheral vein. Peripheral venous irritation may be minimized by changing the site of infusion every 12 hours.
Premixed bags: Do not combine or run in the same line as other medications.
IV: Administer by slow IV continuous infusion through a central line or large peripheral vein; avoid extravasation. Peripheral infusion sites should be changed every 12 hours to minimize venous irritation.
Vial: Must be diluted prior to administration.
Premixed solutions: No further dilution needed. For single use only, discard any unused portion. Use only if solution is clear; per manufacturer's labeling, do not add nicardipine solution with other medications in the same line or in premixed container.
Note: Premixed solutions available
IV infusion: 25 mg in 250 mL (total volume) (concentration: 0.1 mg/mL) of D5W, D51/2NS, D5NS, NS, or 1/2NS
Note: Premixed solutions available.
IV infusion: 100 mcg/mL, 200 mcg/mL, or 500 mcg/mL.
Angina: Management of chronic stable angina (oral only).
Hypertension: Management of hypertension (oral and IV); parenteral only for short-term use when oral treatment is not feasible or not desirable.
Acute ischemic stroke, BP management with reperfusion therapy; Intracerebral hemorrhage, blood pressure management; Subarachnoid hemorrhage, blood pressure management
NiCARdipine may be confused with niacinamide, NIFEdipine, niMODipine
Cardene may be confused with Cardizem, Cardura, codeine
Cardene I.V. may be confused with Nexterone
Significant differences exist between oral and IV dosing. Use caution when converting from one route of administration to another.
Cardene [US, Great Britain, Netherlands] may be confused with Cardem brand name for celiprolol [Spain]; Cardin brand name for simvastatin [Poland]
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Cardiovascular: Flushing (6% to 10%), pedal edema (dose related; 7% to 8%), exacerbation of angina pectoris (dose related; 6%), hypotension (IV 6%), palpitations (3% to 4%), tachycardia (1% to 4%), chest pain (IV 1%), extrasystoles (IV 1%), hemopericardium (IV 1%), hypertension (IV 1%), supraventricular tachycardia (IV 1%), edema (≤1%)
Central nervous system: Headache (6% to 15%), dizziness (4% to 7%), hypoesthesia (1%), intracranial hemorrhage (1%), pain (1%), somnolence (1%)
Dermatologic: Diaphoresis (1%), skin rash (≤1%)
Endocrine & metabolic: Hypokalemia (IV 1%)
Gastrointestinal: Nausea and vomiting (IV 5%), nausea (2%), dyspepsia (≤2%), abdominal pain (IV 1%), xerostomia (≤1%)
Genitourinary: Hematuria (1%)
Local: Injection site reaction (IV 1%), pain at injection site (IV 1%)
Neuromuscular & skeletal: Weakness (4% to 6%), myalgia (1%), paresthesia (1%)
<1%, postmarketing, and/or case reports: Abnormal dreams, abnormal hepatic function tests, abnormal vision, angina pectoris, anxiety, arthralgia, atrial fibrillation (not distinguishable from natural history of atherosclerotic vascular disease), atrioventricular block, atypical chest pain, blurred vision, cerebral ischemia (not distinguishable from natural history of atherosclerotic vascular disease), confusion, conjunctivitis, constipation, deep vein thrombophlebitis, depression, depression of ST segment on ECG, dyspnea, ear disease, ECG abnormal, fever, gingival hyperplasia, heart block (not distinguishable from natural history of atherosclerotic vascular disease), hot flash, hyperkinesia, hypersensitivity reaction, hypertonia, hypophosphatemia, impotence, infection, insomnia, inversion T wave on ECG, malaise, myocardial infarction (chronic therapy; may be due to disease progression), neck pain, nervousness, nocturia, orthostatic hypotension, oxygen saturation decreased (possible pulmonary shunting), parotitis, pericarditis (not distinguishable from natural history of atherosclerotic vascular disease), peripheral vascular disease, psoriasis (Song 2021), respiratory tract disease, rhinitis, sinus node dysfunction (chronic therapy; may be due to disease progression), sinusitis, sore throat, sustained tachycardia, syncope, thrombocytopenia, tinnitus, tremor, urinary frequency, ventricular extrasystoles, ventricular tachycardia, vertigo, vomiting
Hypersensitivity to nicardipine or any component of the formulation; advanced aortic stenosis
Concerns related to adverse effects:
• Angina/MI: Increased angina (frequency, duration, or severity) and/or MI has occurred. Reflex tachycardia may occur resulting in angina and/or MI in patients with obstructive coronary disease, especially in the absence of concurrent beta blockade.
• Hypotension/syncope: Symptomatic hypotension with or without syncope may rarely occur; blood pressure must be lowered at a rate appropriate for the patient's clinical condition. Avoid systemic hypotension in acute cerebral infarction or hemorrhage. Close monitoring of heart rate and blood pressure, especially during initial therapy and dosage titration, is required.
• Peripheral edema: A common side effect is peripheral edema (dose-dependent); occurs within 2 to 3 weeks of starting therapy.
• Tachycardia: May occur; close monitoring of heart rate is required.
Disease-related concerns:
• Aortic stenosis: Use with caution in patients with mild to moderate aortic stenosis; may reduce coronary perfusion resulting in ischemia. Use is contraindicated in patients with advanced aortic stenosis.
• Heart failure: Use in patients with heart failure (HF) or severe left ventricular dysfunction, particularly with concomitant beta-blockade, may experience worsened symptoms of HF due to mild negative inotropic effects of nicardipine. The ACC/AHA heart failure guidelines recommend to avoid use in patients with heart failure due to lack of benefit and/or worse outcomes with calcium channel blockers in general (ACC/AHA [Yancy 2013]).
• Hepatic impairment: Use with caution in patients with hepatic impairment or reduced hepatic blood flow. Consider lower starting dose and closely monitor response.
• Hypertrophic cardiomyopathy with left ventricular outflow tract obstruction: Use with caution in patients with hypertrophic cardiomyopathy and left ventricular outflow tract obstruction since reduction in afterload may worsen symptoms associated with this condition (AHA/ACC [Ommen 2020]).
• Renal impairment: Use with caution in patients with renal impairment. Increase dose cautiously in patients with renal impairment since clearance of nicardipine is diminished in this population.
Dosage form specific issues:
• Propylene glycol: Some dosage forms may contain propylene glycol; large amounts are potentially toxic and have been associated hyperosmolality, lactic acidosis, seizures and respiratory depression; use caution (AAP 1997; Zar 2007).
Other warnings/precautions:
• Infusion sites: To minimize infusion site reactions, peripheral infusion sites (for IV therapy) should be changed every 12 hours; use of arteries or small peripheral veins should be avoided.
• Withdrawal: Abrupt withdrawal may cause rebound angina in patients with CAD.
Substrate of CYP1A2 (minor), CYP2C8 (minor), CYP2C9 (minor), CYP2D6 (minor), CYP2E1 (minor), CYP3A4 (minor), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP2D6 (weak)
Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Alpha1-Blockers: May enhance the hypotensive effect of Calcium Channel Blockers. Risk C: Monitor therapy
Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification
Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy
Atosiban: Calcium Channel Blockers may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. Risk C: Monitor therapy
Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Risk C: Monitor therapy
Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination
Calcium Salts: May diminish the therapeutic effect of Calcium Channel Blockers. Risk C: Monitor therapy
Cimetidine: May increase the serum concentration of Calcium Channel Blockers. Risk C: Monitor therapy
Clopidogrel: Calcium Channel Blockers may diminish the therapeutic effect of Clopidogrel. Risk C: Monitor therapy
CycloSPORINE (Systemic): Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May decrease the serum concentration of NiCARdipine. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of NiCARdipine. Risk C: Monitor therapy
Dantrolene: May enhance the hyperkalemic effect of Calcium Channel Blockers. Dantrolene may enhance the negative inotropic effect of Calcium Channel Blockers. Risk X: Avoid combination
Dapoxetine: May enhance the orthostatic hypotensive effect of Calcium Channel Blockers. Risk C: Monitor therapy
Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy
Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy
Grapefruit Juice: May increase the serum concentration of NiCARdipine. Risk C: Monitor therapy
Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy
Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Risk C: Monitor therapy
Levoketoconazole: NiCARdipine may enhance the QTc-prolonging effect of Levoketoconazole. Risk X: Avoid combination
Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Magnesium Sulfate: May enhance the adverse/toxic effect of Calcium Channel Blockers (Dihydropyridine). Specifically, the risk of hypotension or muscle weakness may be increased. Risk C: Monitor therapy
Melatonin: May diminish the antihypertensive effect of Calcium Channel Blockers (Dihydropyridine). Risk C: Monitor therapy
Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy
Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Neuromuscular-Blocking Agents (Nondepolarizing): Calcium Channel Blockers may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). Risk C: Monitor therapy
Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy
Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider therapy modification
Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Risk D: Consider therapy modification
SUNItinib: NiCARdipine may increase the serum concentration of SUNItinib. Risk C: Monitor therapy
Tacrolimus (Systemic): Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Thioridazine: CYP2D6 Inhibitors (Weak) may increase the serum concentration of Thioridazine. Management: Consider avoiding concomitant use of thioridazine and weak CYP2D6 inhibitors. If combined, monitor closely for QTc interval prolongation and arrhythmias. Some weak CYP2D6 inhibitors list use with thioridazine as a contraindication. Risk D: Consider therapy modification
Serum concentrations/toxicity of nicardipine may be increased by grapefruit juice. Management: Monitor for excessive hemodynamic (ie, blood pressure, heart rate) response to nicardipine in patients who consume grapefruit juice.
Nicardipine has limited placental transfer following maternal oral and IV administration (Bartels 2007; Carbonne 1993; Matsumura 2014).
Nicardipine has been shown to decrease maternal blood pressure without significant changes on placental perfusion or fetal hemodynamics (Cornette 2016). Although effective for the treatment of hypertension in pregnancy, nicardipine may have an increased risk of adverse maternal events (eg, headache, nausea, tachycardia) in comparison to other agents (Nooij 2014). Cases of acute pulmonary edema have been reported following use as a tocolytic (Melis 2015).
Chronic maternal hypertension may increase the risk of birth defects, low birth weight, preterm delivery, stillbirth, and neonatal death. Actual fetal/neonatal risks may be related to duration and severity of maternal hypertension. Untreated hypertension may also increase the risks of adverse maternal outcomes, including gestational diabetes, myocardial infarction, preeclampsia, stroke, and delivery complications (ACOG 203 2019).
Calcium channel blockers may be used to treat hypertension in pregnant women; however, agents other than nicardipine are more commonly used for chronic hypertension (ACOG 203 2019; ESC [Regitz-Zagrosek 2018]). Females with preexisting hypertension may continue their medication during pregnancy unless contraindications exist (ESC [Regitz-Zagrosek 2018]). Nicardipine may be used as an alternative agent for the treatment of acute onset, severe hypertension in pregnant females (ACOG 203 2019; ACOG 767 2019).
Nicardipine is present in breast milk.
In one study of 11 women administered various doses of oral or IV nicardipine 4 to 14 days postpartum, peak milk concentrations ranged from 1.9 to 18.8 mcg/L. The highest breast milk concentration was observed following a maternal dose of nicardipine 120 mg IV. Using the highest breast milk concentration (18.8 mcg/L) the relative infant dose (RID) of nicardipine was calculated by the authors of the study to be 0.14% of the weight-adjusted maternal dose, providing an estimated daily infant dose via breast milk of 2,823 ng/kg/day (Jarreau 2000). A second study administered IV nicardipine 0.8 to 4.6 days' postpartum (dosage range at delivery: 1 to 7 mg/hour) to women with preeclampsia. A total of 34 breast milk samples were obtained from seven women; in 82% of samples, nicardipine was undetectable. The highest breast milk concentration (18.5 mcg/L) was observed following a maternal dose of nicardipine IV 5.5 mg/hour (Bartels 2007). In a third study, breast milk concentrations of nicardipine were found to correlate with maternal plasma concentrations in 16 women treated with IV nicardipine for preeclampsia. The highest milk concentration was 38 mcg/L (measured 2 to 7 days' postpartum) and the highest maternal dose was 1.33 mg/kg/day. In this study, the average RID was also calculated to be <1% of the weight-adjusted maternal dose (range: 0.006 to 0.33%) (Matsumura 2014).
In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
BP, heart rate; consult individual institutional policies and procedures.
BP goals: May vary depending on clinical condition, different clinical practice guidelines, and expert opinion. Refer to "Clinical Practice Guidelines" for specific treatment goals.
Inhibits calcium ion from entering the “slow channels” or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization, producing a relaxation of coronary vascular smooth muscle and coronary vasodilation; increases myocardial oxygen delivery in patients with vasospastic angina
Onset of action: IV: Within minutes (constant infusion); Oral: 0.5 to 2 hours.
Peak effect: Oral: 1 to 2 hours; IV continuous infusion: 50% of the maximum effect is seen by 45 minutes.
Duration:
IV: ≤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.
Oral: ≤8 hours.
Absorption: Oral: ~100%, but large first-pass effect.
Distribution: Vd: 8.3 L/kg.
Protein binding: >95%.
Metabolism: Hepatic; extensive first-pass effect (saturable); major pathway is via cytochrome P450 isoenzyme CYP3A4, 2C8, and 2D6.
Bioavailability: Oral: ~35%.
Half-life elimination: Follows dose-dependent (nonlinear) pharmacokinetics; “apparent” or calculated half-life is dependent upon serum concentrations.
Oral: Half-life over the first 8 hours is 2 to 4 hours; terminal half-life: 8.6 hours.
IV: After IV infusion, serum concentrations decrease tri-exponentially; alpha half-life: 3 minutes; beta half-life: 45 minutes; terminal half-life: 14 hours (Note: Terminal half-life can only be seen after long-term infusions).
Time to peak, serum: Oral: 30 to 120 minutes (mean: 1 hour).
Excretion: Urine (oral: 60% as metabolites; IV: 49% as metabolites; <1% as unchanged drug); feces (oral: 35%; IV: 43%)
Clearance: Decreased in patients with hepatic impairment; may be decreased in patients with renal impairment
Renal function impairment:
IV: Significantly lower systemic clearance and higher AUC in patients with mild to moderate renal impairment.
Oral: Cmax and AUC were ~2-fold higher in patients with mild renal impairment.
Hepatic function impairment: In patients with severe hepatic impairment, plasma concentrations were elevated and the half-life was prolonged.
Capsules (niCARdipine HCl Oral)
20 mg (per each): $2.23 - $15.49
30 mg (per each): $3.19 - $22.19
Solution (Cardene IV Intravenous)
20 mg/200 mL 0.86% (per mL): $0.61
20 mg/200 mL 4.8% (per mL): $0.61
40 mg/200 mL 0.83% (per mL): $1.22
Solution (niCARdipine HCl in NaCl Intravenous)
20 mg/200 mL 0.9% (per mL): $0.61
40 mg/200 mL 0.9% (per mL): $1.22
Solution (niCARdipine HCl Intravenous)
2.5 mg/mL (per mL): $2.10 - $25.29
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