Nicardipine Hydrochloride

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

Pharmacology

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Inhibits movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle and myocardium.

Pharmacokinetics

Absorption

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%.

Distribution

Rapid early-distribution phase, intermediate phase, and a slow terminal phase. Vd is 8.3 L/kg; protein binding is approximately 95%.

Elimination

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).

Onset

Approximately 20 min (oral).

Special Populations

Reduction in glomerular filtration rate (GFR), decreased systemic Cl, and higher AUC.

In patients with severe hepatic function impairment, plasma concentrations are elevated and the half-life is prolonged.

Pharmacokinetics similar in hypertensive patients older than 65 yr of age compared with younger healthy individuals.

Plasma concentrations increased and half-life was prolonged to 19 h.

Indications and Usage

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).

Contraindications

Hypersensitivity to any component of the product; advanced aortic stenosis.

Dosage and Administration

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.

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.

PO Start with 30 mg twice daily (range, 30 to 60 mg twice daily).

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)

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.

General Advice

• Administer without regard to meals. Avoid giving with high-fat meals.
• Nicardipine IV is not compatible with sodium bicarbonate 5% injection or Ringer's lactate injection.
• Change site of infusion every 12 h to minimize the risk of peripheral venous irritation.

Storage/Stability

Store at 68° to 77°F. Protect from light.

Store at 68° to 77°F. Avoid exposure to elevated temperatures. Protect from light.

Protect from freezing.

Not adversely affected by freezing.

Store at 59° to 86°F. Protect from light.

Drug Interactions

Coadminister with caution when giving with nicardipine in patients with CHF.

Nicardipine plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions.

May cause increased cyclosporine levels, with possible toxicity.

Severe hypotension may occur.

May have additive effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension, increased angina, vasodilation (6%); palpitations, tachycardia (4%); ECG abnormality, postural hypotension, ventricular extrasystoles (1%).

CNS

Headache (15%); dizziness (7%); asthenia (6%); paresthesia, somnolence (1%).

Dermatologic

Flushing (10%); rash, sweating (1%).

GI

Nausea/vomiting (5%); dyspepsia, nausea (2%); dry mouth (1%).

Genitourinary

Polyuria (1%).

Local

Injection-site reaction (1%).

Musculoskeletal

Myalgia (1%).

Miscellaneous

Pedal edema (8%); edema (1%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

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.

Renal Function

Adjust dosage in patients with renal function impairment.

Hepatic Function

Adjust dosage and use drug with caution in patients with hepatic function impairment or reduced hepatic blood flow.

Special Risk Patients

Use with caution in patients who have sustained an acute cerebral infarction or hemorrhage, or in patients with pheochromocytoma.

Antiplatelet effects

Calcium channel blockers may inhibit platelet function.

Beta-blocker withdrawal

Patients withdrawn from beta-blockers while taking nicardipine may experience increased angina. Gradually taper beta-blocker dose.

CHF

Use drug with caution in patients with CHF.

Increased angina

Occasionally, patients have increased frequency, duration, or severity of angina when starting or increasing dose.

Withdrawal

Abrupt withdrawal may cause increased frequency and duration of angina.

Overdosage

Symptoms

Bradycardia, confusion, drowsiness, flushing, hypotension, palpitations, slurred speech.

Patient Information

• Instruct patient to swallow sustained-release capsules whole and not to crush or chew.
• Caution patient that increased angina may occur initially when starting, changing dose, or stopping medication.
• Advise patient not to stop taking drug abruptly.
• Instruct patient to report the following symptoms to health care provider: any unusual bleeding, bruising, change in angina, changes in gums, constipation, dizziness, irregular heartbeat, nausea, palpitations, rash, shortness of breath, or swelling in hands or feet.
• Advise patient that drug may cause dizziness or drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

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