Trade Names:Cardene I.V.- Injection 2.5 mg/mL- Injection, solution, premixed 0.2 mg/mL in dextrose 5%- Injection, solution, premixed 0.2 mg/mL in sodium chloride 0.83%
Trade Names:Cardene SR- Capsules, sustained-release 30 mg- Capsules, sustained-release 45 mg- Capsules, sustained-release 60 mg
Trade Names:Nicardipine hydrochloride- Capsules 20 mg- Capsules 30 mg
Inhibits movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle and myocardium.
Nicardipine is absorbed approximately 100% following oral administration. C max is 28 to 50 mg/mL; steady state is 24 to 48 h (IV), 2 to 30 h (oral); T max is 0.5 to 2 h (oral); absolute bioavailability is 35% (less for oral administration because of first-pass metabolism). T max (sustained-release capsules) is 1 to 4 h. Food is administered 3 h after high-fat meal. C max is less than 20% and AUC is less than 30%.
Rapid early-distribution phase, intermediate phase, and a slow terminal phase. Vd is 8.3 L/kg; protein binding is approximately 95%.
Eliminated by urine (less than 1% unchanged, 49% of dose recovered) and feces (43%). Plasma Cl is 0.4 L/h/kg; plasma half-life is 8.6 h (oral); half-life is 2 to 4 h (oral); alpha half-life is 2.7 min (IV); beta half-life is 44.8 min (IV); gamma half-life is 14.4 h (IV).
Approximately 20 min (oral).
Reduction in glomerular filtration rate (GFR), decreased systemic Cl, and higher AUC.Hepatic Function Impairment
In patients with severe hepatic function impairment, plasma concentrations are elevated and the half-life is prolonged.Elderly
Pharmacokinetics similar in hypertensive patients older than 65 yr of age compared with younger healthy individuals.Severe hepatic function impairment
Plasma concentrations increased and half-life was prolonged to 19 h.
Treatment of chronic stable (effort-associated) angina (immediate-release capsules); management of hypertension (immediate- and sustained-release capsules; IV when oral therapy not feasible or desirable).
Hypersensitivity to any component of the product; advanced aortic stenosis.
PO Usual initial dosage is 20 mg 3 times daily (range, 20 to 40 mg 3 times daily). Allow at least 3 days before increasing the dose.HypertensionAdults Immediate-release
PO Start with 20 mg 3 times daily (range, 20 to 40 mg 3 times daily). Allow at least 3 days before increasing the dose.Sustained-release
PO Start with 30 mg twice daily (range, 30 to 60 mg twice daily).IV
IV Individualize dose based on severity of hypertension and response of patient during dosing. As a substitute for oral therapy, the following may be given: For an oral nicardipine dosage of 20 mg every 8 h, an equivalent IV infusion rate is 0.5 mg/h. For an oral nicardipine dosage of 30 mg every 8 h, an equivalent IV infusion rate is 1.2 mg/h. For an oral nicardipine dosage of 40 mg every 8 h, an equivalent IV infusion rate is 2.2 mg/h. For initiation of therapy in a drug-free patient, administer slow continuous infusion at a concentration of 0.1 mg/mL ( Cardene I.V. ) or 0.2 mg/mL ( Cardene I.V. premixed)Titration
For gradual reduction in blood pressure, initiate therapy at 5 mg/h (25 mL/h of Cardene I.V. premix or 50 mL/h of Cardene I.V. ); may increase by 2.5 mg/h (12.5 mL/h of Cardene I.V. premix or 25 mL/h of Cardene I.V. ) every 15 min up to a max of 15 mg/h (75 mL/h of Cardene I.V. premix or 150 mL/h of Cardene I.V. ) until desired blood pressure is achieved. For more rapid blood pressure reduction, initiate therapy at 5 mg/h (25 mL/h of Cardene I.V. premix or 50 mL/h of Cardene I.V. ); may increase by 2.5 mg/h (12.5 mL/h of Cardene I.V. premix or 25 mL/h of Cardene I.V. ) every 5 min up to a max of 15 mg/h (75 mL/h of Cardene I.V. premix or 150 mL/h of Cardene I.V. ) until desired blood pressure is achieved.
Store at 68° to 77°F. Protect from light.IV
Store at 68° to 77°F. Avoid exposure to elevated temperatures. Protect from light.Premixed solution
Protect from freezing.Injection
Not adversely affected by freezing.Sustained-release capsules
Store at 59° to 86°F. Protect from light.
Coadminister with caution when giving with nicardipine in patients with CHF.Cimetidine, grapefruit
Nicardipine plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions.Cyclosporine
May cause increased cyclosporine levels, with possible toxicity.Fentanyl anesthesia
Severe hypotension may occur.Other hypertensive agents
May have additive effects.
None well documented.
Hypotension, increased angina, vasodilation (6%); palpitations, tachycardia (4%); ECG abnormality, postural hypotension, ventricular extrasystoles (1%).
Headache (15%); dizziness (7%); asthenia (6%); paresthesia, somnolence (1%).
Flushing (10%); rash, sweating (1%).
Nausea/vomiting (5%); dyspepsia, nausea (2%); dry mouth (1%).
Injection-site reaction (1%).
Pedal edema (8%); edema (1%).
Category C .
Safety and efficacy not established.
Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Adjust dosage in patients with renal function impairment.
Adjust dosage and use drug with caution in patients with hepatic function impairment or reduced hepatic blood flow.
Use with caution in patients who have sustained an acute cerebral infarction or hemorrhage, or in patients with pheochromocytoma.
Calcium channel blockers may inhibit platelet function.
Patients withdrawn from beta-blockers while taking nicardipine may experience increased angina. Gradually taper beta-blocker dose.
Use drug with caution in patients with CHF.
Occasionally, patients have increased frequency, duration, or severity of angina when starting or increasing dose.
Abrupt withdrawal may cause increased frequency and duration of angina.
Bradycardia, confusion, drowsiness, flushing, hypotension, palpitations, slurred speech.
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