nicardipine

Absorption: Well absorbed following oral administration but extensively metabolized, resulting in ↓ bioavailability. IV administration results in complete bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Mostly metabolized by the liver; ≤10% excreted unchanged by kidneys.

Half-Life: 2–4 hr.

Time/Action Profile ⬆ ⬇

(cardiovascular effects)

ROUTE	ONSET	PEAK	DURATION
PO	20 min	0.5–2 hr	8 hr
IV	within min	45 min	50 hr‡

‡Following discontinuation.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Sick sinus syndrome;
2nd- or 3rd-degree AV block (unless an artificial pacemaker is in place);
SBP <90 mm Hg;
Advanced aortic stenosis;
Lactation: Lactation.

Use Cautiously in:

Severe hepatic impairment (dose ↓ recommended);
Severe renal impairment (dose ↓ may be necessary);
History of serious ventricular arrhythmias or HF;
OB: Other calcium channel blockers preferred in pregnancy;
Pedi: Safety and effectiveness not established in children;
Geri: Dose /slower IV infusion rates recommended in older adults due to risk of hypotension.

Adv. Reactions/Side Effects ⬆ ⬇

CV: peripheral edema, ARRHYTHMIA, bradycardia, chest pain, HF, hypotension, palpitations, syncope, tachycardia

Derm: dermatitis, erythema multiforme, flushing, ↑sweating, photosensitivity, pruritus/urticaria, rash, STEVENS-JOHNSON SYNDROME

EENT: blurred vision, disturbed equilibrium, epistaxis, tinnitus

Endo: gynecomastia, hyperglycemia

GI: anorexia, constipation, diarrhea, dry mouth, dyspepsia, ↑liver enzymes, nausea, vomiting

GU: dysuria, nocturia, polyuria, sexual dysfunction, urinary frequency

Hemat: anemia, leukopenia, thrombocytopenia

Metab: weight gain

MS: joint stiffness, muscle cramps

Neuro: abnormal dreams, anxiety, confusion, dizziness, drowsiness, dysgeusia, headache, jitteriness, nervousness, paresthesia, psychiatric disturbances, tremor, weakness.

Resp: cough, dyspnea, shortness of breath

Misc: gingival hyperplasia

Interactions ⬆ ⬇

Drug-drug:

Additive hypotension may occur when used concurrently with fentanyl, other antihypertensives, nitrates, acute ingestion of alcohol, or quinidine.
Antihypertensive effects may be ↓ by concurrent use of NSAIDs.
Cimetidine and propranolol may ↓ metabolism and ↑ risk of toxicity.
May ↓ the metabolism of and ↑ risk of toxicity from cyclosporine, prazosin, quinidine, tacrolimus, or carbamazepine.

Grapefruit and grapefruit juice↑ serum levels and effect.

Route/Dosage ⬆ ⬇

PO (Adults ): 20 mg 3 times daily, may ↑ every 3 days (range 20–40 mg 3 times daily).
IV (Adults ): Substitute for PO nicardipine: if PO dose is 20 mg every 8 hr, then infusion rate is 0.5 mg/hr; if PO dose is 30 mg every 8 hr, then infusion rate is 1.2 mg/hr; if PO dose is 40 mg every 8 hr, then infusion rate is 2.2 mg/hr. Patients not receiving PO nicardipine: initiate therapy at 5 mg/hr, may be increased by 2.5 mg every 5–15 min as needed (up to 15 mg/hr).

Availability ⬆ ⬇

(Generic available)

Capsules: 20 mg; 30 mg
Premixed infusion: 20 mg/200 mL dextrose 4.8% in water or 0.86% NaCl; 40 mg/200 mL 0.83% NaCl
Solution for injection: 2.5 mg/mL

Assessment ⬆ ⬇

Monitor BP and pulse prior to therapy, during dose titration, and periodically throughout therapy. Monitor ECG periodically during prolonged therapy.
- Monitor intake and output ratios and daily weight. Assess for signs of HF (peripheral edema, rales/crackles, dyspnea, weight gain, jugular venous distention).
Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
Angina: Assess location, duration, intensity, and precipitating factors of patient’s anginal pain.

Lab Test Considerations:

Total serum calcium concentrations are not affected by calcium channel blockers.
- Monitor serum potassium periodically. Hypokalemia↑ risk of arrhythmias; should be corrected.
- Monitor renal and hepatic functions periodically during long-term therapy. Several days of therapy may cause ↑ hepatic enzymes, which return to normal upon discontinuation of therapy.

Implementation ⬆ ⬇

Do not confuse Cardene with Cardizem. Do not confuse nicardipine with nifedipine or nimodipine.
- To transfer from IV nicardipine infusion to oral therapy with other antihypertensive, start oral therapy simultaneously with discontinuation of nicardipine infusion. If transferring to oral nicardipine therapy, administer first dose of a 3-times-a-day regimen 1 hr prior to discontinuation of infusion.
- Dose adjustments of nicardipine should be made no more frequently than every 3 days.
PO: May be administered without regard to meals. May be administered with meals if GI irritation becomes a problem.

IV Administration:

Diluent: Dilute each 25-mg vial with 240 mL of D5W, D5/0.45% NaCl, D5/0.9% NaCl, 0.45% NaCl, or 0.9% NaCl. Infusion is stable for 24 hr at room temperature.Concentration: 0.1 mg/mL.
Rate: Titrate rate according to BP response. Administer through large peripheral veins or central veins to reduce risk of venous thrombosis, phlebitis, local irritation, swelling, extravasation, and vascular impairment. Change infusion site every 12 hr to minimize risk of peripheral venous irritation.

Patient/Family Teaching ⬆ ⬇

Advise patient to take medication exactly as directed, even if feeling well. Take missed doses as soon as possible unless almost time for next dose; do not double doses. May need to be discontinued gradually.
- Instruct patient on technique for monitoring pulse. Instruct patient to contact health care professional if heart rate is <50 bpm.
- Advise patient to avoid grapefruit or grapefruit juice during therapy.
- Caution patient to change positions slowly to minimize orthostatic hypotension.
- May cause drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to the medication is known.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of alcohol or OTC medications and herbal products, especially NSAIDs and cold preparations, without consulting health care professional.
- Advise patient to notify health care professional if rash, irregular heartbeat, dyspnea, swelling of hands and feet, pronounced dizziness, nausea, constipation, or hypotension occurs or if headache is severe or persistent.
- Caution patient to wear protective clothing and to use sunscreen to prevent photosensitivity reactions.
- Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Angina: Instruct patient on concurrent nitrate or beta-blocker therapy to continue taking both medications as directed and to use SL nitroglycerin as needed for anginal attacks.
- Advise patient to contact health care professional if chest pain does not improve, worsens after therapy, or occurs with diaphoresis; if shortness of breath; or if persistent headache occurs.
- Caution patient to discuss exercise restrictions with health care professional prior to exertion.
Hypertension: Encourage patient to comply with other interventions for hypertension (weight reduction, low-sodium diet, smoking cessation, moderation of alcohol consumption, regular exercise, and stress management). Medication controls but does not cure hypertension.
- Instruct patient and family in proper technique for monitoring BP. Advise patient to take BP weekly and to report significant changes to health care professional.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇