nicardipine (Rx)

Brand and Other Names:Cardene, Cardene IV, more...Cardene SR
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule

  • 20mg
  • 30mg

capsule, extended release

  • 30mg
  • 45mg
  • 60mg

infusion solution

  • 20mg/200mL
  • 40mg/200mL

injectable solution

  • 2.5mg/mL
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Hypertension

PO: 20-40 mg (conventional) q8hr or 30-60 mg (extended release) q12hr

Extended-release form preferred because of less frequent dosing, potentially smoother BP control, and concerns raised by short-acting nifedipine

IV: 5 mg/hr by slow infusion (50 mL/hr) initially; may be increased by 2.5 mg/hr every 15 minutes; not to exceed 15 mg/hr

IV as substitute for conventional PO

  • PO dose: 20 mg q8hr; equivalent IV infusion: 0.5 mg/hr
  • PO dose: 30 mg q8hr; equivalent IV infusion: 1.2 mg/hr
  • PO dose: 40 mg q8hr; equivalent IV infusion: 2.2 mg/hr
  • If transitioning to PO nicardipine, initiate PO dosing 1 hr before discontinuance of IV

Chronic Stable Angina

20-40 mg (conventional) PO q8hr

Start at 20 mg, and allow 3 days between dose increases to achieve steady-state plasma drug concentration; usual dosage range, 60-120 mg/day

Dosing Modifications

Renal impairment

  • Immediate release: 20 mg PO q8hr initially; titrated to effect every 3 days
  • Extended release: 30 mg PO q12hr initially; titrated to effect every 3 days
  • IV: Use with caution; guidelines for dose adjustments not available; monitor and adjust as necessary

Hepatic impairment

  • Immediate release: 20 mg PO q12hr initially; titrated to effect every 3 days
  • Daily immediate-release dose may not be directly equivalent to daily extended-release dose; use caution in converting
  • IV: Use with caution; guidelines for dose adjustments not available; monitor and adjust as necessary

Dosage Forms & Strengths

capsule

  • 20mg
  • 30mg

capsule, extended release

  • 30mg
  • 45mg
  • 60mg

infusion solution

  • 20mg/200mL
  • 40mg/200mL

injectable solution

  • 2.5mg/mL
more...

Hypertension (Off-label)

Not approved by FDA; limited data available

0.5-3 mcg/kg/min IV  

Use with caution; initiate at low end of adult dosing range; monitor closely

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Interactions

Interaction Checker

and nicardipine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (IV; 15%)

            1-10%

            Flushing (6-10%)

            Peripheral edema (PO; 6-8%)

            Pedal edema (PO; 6.8%)

            Headache (PO; 6.3%)

            Hypotension (IV; 6%)

            Exacerbation of angina (6%)

            Asthenia (PO; 3%)

            Nausea (PO; 1.6%)

            Ventricular extrasystoles (IV; 1%)

            Dizziness (1%)

            Rash (PO; 1%)

            Polyuria (IV; 1%)

            <1% (selected)

            Asthenia (IV)

            Facial edema

            Hypotension (PO)

            Myalgia (PO)

            Syncope (IV)

            Tachycardia

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            Warnings

            Contraindications

            Hypersensitivity to nicardipine or other calcium-channel blockers

            Advanced aortic stenosis

            Cautions

            May cause symptomatic hypotension or tachycardia; titrate slowly to avoid systemic hypotension and possible negative inotropic effects with congestive heart failure (CHF), angina, and left ventricular dysfunction (particularly during treatment initiation, after dose increase, or after withdrawal of beta blocker)

            To reduce possibility of venous thrombosis, phlebitis, and vascular impairment, do not use small veins, such as those on dorsum of hand or wrist; avoid intraarterial administration or extravasation

            Caution should be exercised when using the drug in congestive heart failure patients, particularly in combination with a beta-blocker; nicardipine gives no protection against dangers of abrupt beta-blocker withdrawal; any such withdrawal should be by gradual reduction of dose of beta-blocker, preferably over 8 to 10 days

            Closely monitor response in patients with angina, congestive heart failure, impaired hepatic function, portal hypertension, and renal impairment and pheochromocytoma

            Peripheral edema may occur

            Exacerbation of angina or MI reported with dosage titration of dihydropyridine calcium-channel blockers

            With acute cerebral infarction or hemorrhage, titrate slowly to avoid systemic hypotension

            Use with caution in patients with hypertrophic cardiomyopathy and mild-to-moderate aortic stenosis

            Use with caution in hepatic or renal impairment; lower doses may be required

            Use with caution in hypertension associated with pheochromocytoma and portal hypertension when administering IV

            Change infusion site every 12 hr to minimize risk of peripheral venous irritation

            Blood pressure starts to fall within min of infusion; calcium channel blockers, may occasionally produce symptomatic hypotension; caution is advised to avoid systemic hypotension when administering drug to patients who have sustained acute cerebral infarction or hemorrhage

            Extended-release form not recommended for angina

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Unknown whether drug is excreted in breast milk; avoid use

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Calcium-channel blocker (dihydropyridine); inhibits transmembrane influx of extracellular calcium ions across membranes of myocardial cells and vascular smooth muscle cells without changing serum calcium concentrations; this inhibits cardiac and vascular smooth muscle contraction, thereby dilating main coronary and systemic arteries

            Produces vasodilation and decreases peripheral resistance  

            Absorption

            Bioavailability: 35%

            Onset: PO, 0.5-2 hr; IV, 10-20 min

            Duration: Immediate release and IV, 8 hr; extended release, 8-12 hr

            Peak plasma time: Immediate release, 0.5-2 hr; extended release, 2-4 hr

            Distribution

            Protein bound: 95%

            Vd: 8.3 L/kg

            Metabolism

            Metabolized in liver by CYP3A4 (first pass)

            Metabolites: Pyridine analogue (inactive)

            Elimination

            Half-life: 2-4 hr

            Dialyzable: HD, no

            Total plasma clearance: IV, 0.3-0.9 L/hr/kg; PO, 1.62-7.86 L/hr/kg

            Excretion: Urine (60%), feces (35%)

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            Administration

            IV Incompatibilities

            Solution: Lactated Ringer solution, sodium bicarbonate 5%

            Y-site: Ampicillin, ampicillin-sulbactam, cefoperazone, furosemide, heparin (may be compatible at low concentrations of both), thiopental

            IV Compatibilities

            Solution: D5/NS, D5/LR, D5W, NS

            Additive: Potassium chloride

            Y-site (partial list): Amikacin, aminophylline, aztreonam, calcium gluconate, cefazolin, ceftazidime (incompatible at high concentrations of both), chloramphenicol, cimetidine, clindamycin, diltiazem, dobutamine, dopamine, enalapril, epinephrine, erythromycin, esmolol, famotidine, fentanyl, gentamicin, hydrocortisone, labetalol, lidocaine, lorazepam, magnesium sulfate, methylprednisolone, metronidazole, midazolam, morphine, nitroglycerin, nitroprusside sodium, penicillin G, phosphate, piperacillin, potassium chloride, ranitidine, tobramycin, trimethoprim-sulfamethoxazole, vancomycin

            IV Preparation

            Dilute ampules before infusion: 25 mg diluted in 240 mL IV fluid (yielding 250 mL of 0.1 mg/mL solution)

            Premixed infusion solution requires no dilution

            IV Administration

            Administer by slow continuous infusion

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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