A-Z Drug Facts > Nicardipine Hydrochloride

Nicardipine Hydrochloride

Pronouncation: (NYE-CAR-dih-peen HIGH-droe-KLOR-ide)
Class: Calcium channel blocking agent

Trade Names:
Cardene
- Capsules 20 mg
- Capsules 30 mg

Trade Names:
Cardene I.V.
- Injection 2.5 mg/mL

Trade Names:
Cardene SR
- Capsules, sustained-release 30 mg
- Capsules, sustained-release 45 mg
- Capsules, sustained-release 60 mg

Pharmacology

Feedback for Nicardipine Hydrochloride As a treatment for... Avg User Ratings [?] High Blood Pressure Be the first to rate it 0 comments   Heart Failure Be the first to rate it 0 comments   Angina Pectoris Prophylaxis Be the first to rate it 0 comments   Compare with other drugs.

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). 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: 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 t _{1/ 2} is 8.6 h (oral); t _{1/ 2} is 2 to 4 h (oral); alpha t _{1/ 2} is 2.7 min (IV); beta t _{1/ 2} is 44.8 min (IV); gamma t _{1/ 2} is 14.4 h (IV).

Onset

Approximately 20 min (oral).

Special Populations

Renal Function Impairment

Significant reduction in glomerular filtration rate (GFR), significant systemic Cl, and higher AUC.

Severe Liver Insufficiency

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

Sick sinus syndrome; second- or third-degree atrioventricular (AV) block except with functioning pacemaker; advanced aortic stenosis.

Dosage and Administration

Angina (Immediate-Release Only)
Adults

PO Usual initial dose 20 mg 3 times daily (range, 20 to 40 mg 3 times daily).

Hypertension
Adults Immediate-release

PO Usual dose 20 mg 3 times daily (range, 20 to 40 mg 3 times daily).

Sustained-release

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

IV Individualize dosage based on severity of hypertension and response of patient during dosing.

General Advice

• Administer without regard to meals. Avoid giving with high-fat meals.

Storage/Stability

Store at controlled room temperature (56° to 86°F).

Drug Interactions

Cyclosporine

May cause increased cyclosporine levels with possible toxicity.

Other hypertensive agents

May have additive effects.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Peripheral edema; palpitations; AV block; MI; angina; tachycardia; abnormal ECG.

CNS

Dizziness; lightheadedness; asthenia; psychiatric disturbances; headache; paresthesia; somnolence; weakness.

Dermatologic

Rash.

GI

Nausea; abdominal discomfort; cramps; dyspepsia; dry mouth; thirst.

Miscellaneous

Flushing; allergic reaction; myalgia.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Adjust dose 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.

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 on starting or increasing dose.

Withdrawal

Abrupt withdrawal may cause increased frequency and duration of angina.

Overdosage

Symptoms

Nausea, weakness, dizziness, drowsiness, confusion, slurred speech, marked and prolonged hypotension, bradycardia, functional rhythms, second- or third-degree AV block, palpitations, flushing, nervousness, vomiting.

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, rash, palpitations, irregular heartbeat, shortness of breath, nausea, change in angina, constipation, changes in gums, dizziness, 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.

Link to this page

Printable Version

Email Page

Add to my drug list