NICARDIPINE HYDROCHLORIDE

NICARDIPINE HYDROCHLORIDE (ni-car'di-peen) Cardene, Cardene SR Classifications: calcium channel blocker; antihypertensive agent; Therapeutic:antihypertensive; calcium channel blocker Prototype: Nifedipine Pregnancy Category: C

Availability

20 mg, 30 mg capsules; 30 mg, 45 mg, 60 mg sustained release capsules; 2.5 mg/mL injection

Action

Calcium channel entry blocker that inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle, thus affecting contractility. Selectively affects vascular smooth muscle more than cardiac muscle; relaxes coronary vascular smooth muscle with little or no negative inotropic effect.

Therapeutic Effect

Significantly decreases systemic vascular resistance. It reduces BP at rest and during isometric and dynamic exercise.

Uses

Either alone or with beta blockers for chronic, stable (effort-associated) angina; either alone or with other antihypertensives for essential hypertension.

Unlabeled Uses

CHF, cerebral ischemia, migraine.

Contraindications

Hypersensitivity to nicardipine; advanced aortic stenosis; cardiogenic shock; hypotension; pregnancy (category C); lactation.

Cautious Use

CHF; renal and hepatic impairment; severe bradycardia; older adult; GERD; hiatal hernia; renal disease; renal impairment; acute stroke; acute myocardial infarction.

Route & Dosage

Hypertension, Angina Adult: PO 20–40 mg t.i.d. or 30–60 mg SR b.i.d. IV Initiation of therapy in a drug-free patient: 5 mg/h initially, increase dose by  2.5 mg/h q15min (or faster) (max: 15 mg/h); for severe hypertension: 4–7.5 mg/h; for postop hypertension: 10–15 mg/h initially, then 1–3 mg/h Substitute for Oral Nicardipine Adult: IV 20 mg q8h PO = 0.5 mg/h; 30 mg q8h PO = 1.2 mg/h; 40 mg q8h PO = 2.2 mg/h

Administration

Note: To prevent symptoms of withdrawal, do not abruptly discontinue drug.

Oral

• Give on empty stomach. High-fat meals may decrease blood levels.
• Ensure that sustained release form is not chewed or crushed. It must be swallowed whole.
• When converting from IV to oral dose, give first dose of t.i.d. regimen 1 h before discontinuing infusion.

Intravenous PREPARE: IV Infusion: Dilute each 25 mg ampule with 240 mL of D5W or NS to yield 0.1 mg/mL.   ADMINISTER: IV Infusion: For adults, usually initiated at 50 mL/h (5 mg/h) with rate increases of 25 mL/h (2.5 mg/h) q5–15min up to a maximum of 150 mL/h. Infusion is usually slowed to 30 mL/h once the target BP is reached. Substitute for oral doses: Oral 20 mg q8h, IV equivalent is 0.5 mg/h; oral 30 mg q8h, IV equivalent is 1.2 mg/h; oral 40 mg q8h, IV equivalent is 2.2 mg/h.   INCOMPATIBILITIES Solution/additive: Sodium bicarbonate. Y-site: Ampicillin, ampicillin/sulbactam, cefoperazone, furosemide, heparin, thiopental.

Adverse Effects (≥1%)

CNS: Dizziness or headache, fatigue, anxiety, depression, paresthesias, insomnia, somnolence, nervousness. CV: Pedal edema, hypotension, flushing, palpitations, tachycardia, increased angina. GI: Anorexia, nausea, vomiting, dry mouth, constipation, dyspepsia. Skin: Rash, pruritus. Body as a Whole: Arthralgia or arthritis.

Interactions

Drug: Adenosine prolongs bradycardia. Amiodarone may cause sinus arrest and AV block. Benazepril blunts increase in heart rate and increase in plasma norepinephrine and aldosterone seen with nicardipine. beta blockers cause hypotension and bradycardia. Cimetidine increases levels of nicardipine, resulting in hypotension. Concomitant nicardipine and cyclosporine result in significant increase in cyclosporine serum concentrations 1–30 d after initiation of nicardipine therapy; following withdrawal of nicardipine, cyclosporine levels decrease. Magnesium, when used to retard premature labor, may cause severe hypotension and neuromuscular blockade. Food: Grapefruit juice (>1 qt/d) may increase plasma concentrations and adverse effects.

Pharmacokinetics

Absorption: Immediately 35% of oral dose reaches systemic circulation. Onset: 1 min IV; 20 min PO. Peak: 0.5–2 h. Duration: 3 h IV. Distribution: 95% protein bound; distributed in breast milk. Metabolism: Rapidly and extensively in liver (CYP3A4); active metabolite has <1% activity of parent compound. Elimination: 35% in feces, 60% in urine; not affected by hemodialysis. Half-Life: 8.6 h.

Nursing Implications

Assessment & Drug Effects

• Establish baseline data before treatment is started including BP, pulse, and lab values of liver and kidney function.
• Monitor BP during initiation and titration of dosage carefully. Hypotension with or without an increase in heart rate may occur, especially in patients who are hypertensive or who are already taking antihypertensive medication.
• Avoid too rapid reduction in either systolic or diastolic pressure during parenteral administration.
• Discontinue IV infusion if hypotension or tachycardia develop.
• Observe for large peak and trough differences in BP. Initially, measure BP at peak effect (1–2 h after dosing) and at trough effect (8 h after dosing).

Patient & Family Education

• Record and report any increase in frequency, duration, and severity of angina when initiating or increasing dosage. Keep a record of nitroglycerin use and promptly report any changes in previous anginal pattern. Increased incidence and severity of angina has occurred in some patients using nicardipine.
• Do not change dosage regimen without consulting physician.
• Be aware that abrupt withdrawal may cause an increased frequency and duration of chest pain. This drug must be gradually tapered under medical supervision.
• Rise slowly from a recumbent position; avoid driving or operating potentially dangerous equipment until response to nicardipine is known.
• Notify physician if any of the following occur: Irregular heartbeat, shortness of breath, swelling of the feet, pronounced dizziness, nausea, or drop in BP.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug