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Transcript
ANNE ARUNDEL MEDICAL CENTER
CRITICAL CARE MEDICATION MANUAL
DEPARTMENT OF NURSING AND PHARMACY
Guidelines for Use of Intravenous
Nicardipine (Cardene IV)
MAJOR INDICATION
Management of hypertension; only use parenteral (IV) for short-term use when oral treatment is not
feasible nor desirable
MECHANISM OF ACTION
Nicardipine is a calcium channel blocker. It works by inhibiting calcium ion from entering the slow
channels of select voltage-sensitive areas of the vascular smooth muscle and myocardium during
depolarization. This causes relaxation of coronary vascular smooth muscle and coronary vasodilation. It
also increases myocardial oxygen delivery in patients with vasospastic angina.
PHARMACOKINETICS
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Nicardipine IV has a rapid onset of action. It acts within 1-2 minutes.
50% of the maximum effect is observed within 45 minutes with IV continuous infusion.
In treatment of acute hypertension in chronic hypertensives, discontinuation of infusion
produced a 50% decrease in effect in approximately 30 minutes with gradually decreasing effect
over the following 50 hours.
Nicardipine IV and oral nicardipine immediate release have duration of action of < 8 hours.
The volume of distribution is 8.3 L/kg.
More than 95% of nicardipine is bound to plasma protein.
100% of oral nicardipine is absorbed, but there is a large first-pass effect.
The peak effect of immediate capsules is 1-2 hours.
METABOLISM AND EXCRETION
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Nicardipine is metabolized by the liver. There is extensive first-pass effect and the major
pathway is via CYP3A4.
The half-life follows a dose-dependent (non-linear) pharmacokinetics. Calculated half-life is
dependent upon serum concentrations.
After IV infusion, serum concentrations decrease tri-exponentially:
o Alpha half-life: 2.7 minutes
o Beta half-life: 44.8 minutes
o Terminal half-life: 14.4 hours
Half-life over the first 8 hours after oral dosing is 2-4 hours. Terminal half-life (oral) is 8.6 hours.
60% of oral nicardipine is excreted in urine as metabolites. 49% of nicardipine IV is excreted in
urine as metabolites. <1% is excreted unchanged. 35% of oral nicardipine is excreted in feces
and 43% of nicardipine IV is excreted in feces.
ADMINISTRATION AND MONITORING
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For IV administration, nicardipine should be administered as a slow continuous infusion via
central line or via a large peripheral vein. To minimize peripheral venous irritation, change the
site of infusion every 12 hours.
Monitor blood pressure, heart rate, and EKG (for IV).
For premixed bags, do not combine or run in the same line as other medications.
Nicardipine IV is not compatible with Sodium Bicarbonate containing solutions or Lactated
Ringers.
Page 1 of 4
Last updated: July 2016
ANNE ARUNDEL MEDICAL CENTER
CRITICAL CARE MEDICATION MANUAL
DEPARTMENT OF NURSING AND PHARMACY


Guidelines for Use of Intravenous
Nicardipine (Cardene IV)
Injectable detail for administration:
o pH: vial: 3.5
o pH: Premixed bag: 3.7-4.7
For oral administration, administer without regards to meals. Avoid opening or cutting the
capsules.
DOSING
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The recommended dosing of IV nicardipine is 5 mg/hour initially with titration in 2.5 mg/hour
increments every 5-15 minutes until desired effect is achieved, up to a maximum of 15 mg/hour.
Dose
Infusion Rate
2.5 mg/hr
25 mL/hr
5 mg/hr
50 mL/hr
7.5 mg/hr
75 mL/hr
10 mg/hr
100 mL/hr
12.5 mg/hr
125 mL/hr
15 mg/hr (maximum)
150 mL/hr
Prolonged therapy with IV Nicardipine may require dosage reductions due to drug
accumulation.
The medication may exhibit a prolonged duration of effect in those patients with renal and/or
hepatic insufficiency. IV Nicardipine should be titrated carefully in patients with renal
dysfunction and severe hepatic dysfunction.
PO for Angina/Hypertension
o Immediate release (oral): 20 mg 3 times daily
o Usual dosage: 20-40 mg 3 times daily
o *Allow > 3 days between dose increases
o *Cardene SR has been discontinued in the United States for more than 1 year.
CONTRAINDICATIONS
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Hypersensitivity to nicardipine or any component of the formulation
Advanced aortic stenosis
Severe CHF
Severe hypotension or Cardiogenic Shock
PRECAUTIONS
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Increased angina and/or MI have occurred with initiation or dosage titration of dihydropyridine
calcium channel blockers.
Peripheral edema more common in oral therapy is a common side effect that occurs within 2-3
weeks of initiating therapy.
Tachycardia may occur; therefore, heart rate should be closely monitored.
Use with caution in patients with mild to moderate aortic stenosis. Nicardipine may reduce
coronary perfusion resulting in ischemia.
In concomitant use with a beta-blocker in patients with severe left ventricular dysfunction,
nicardipine may worsen symptoms of heart failure due to its negative inotropic effects.
Use with caution in patients with hepatic impairment or reduced hepatic blood flow.
Page 2 of 4
Last updated: July 2016
ANNE ARUNDEL MEDICAL CENTER
CRITICAL CARE MEDICATION MANUAL
DEPARTMENT OF NURSING AND PHARMACY





Guidelines for Use of Intravenous
Nicardipine (Cardene IV)
Use with caution in patients with hypertrophic cardiomyopathy and outflow tract obstruction
because a reduction in afterload may worsen symptoms.
Initiate at the lower end of the dosing range for elderly.
Peripheral infusion sites should be changed every 12 hours to minimize infusion site reactions.
Avoid use of small peripheral veins.
Rebound angina may occur in patients with CAD with abrupt withdrawal.
Hypotension or syncope
DRUG INTERACTIONS
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Antifungal agents (azole derivatives, systemic) may enhance adverse effects of nicardipine.
P-glycoprotein/ABCB1 inhibitors (nicardipine) may increase the serum concentration of
topotecan and vincristine (liposomal); therefore, avoid combination.
Carbamazepine may increase the metabolism of nicardipine. Therefore, for patients receiving
concomitant carbamazepine consider calcium channel blocker dose adjustments or alternative
therapy.
Nicardipine may enhance the hypotensive effect of carvedilol. Nicardipine may increase the
serum concentration of carvedilol and precipitate signs of heart failure in patients on carvedilol.
P-glycoprotein/ABCB1 inhibitors (nicardipine) may increase serum concentrations of the active
metabolites of dabigatran etexilate; therefore dose reductions of dabigatran may be needed.
Grapefruit juice may increase the serum concentration of nicardipine; therefore monitor
therapy.
Nicardipine may increase the serum concentrations of lacosamide; therefore, consider therapy
modification.
Many more drug interactions (CYP 3A4), please consult pharmacy as needed.
ADVERSE EFFECTS
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Cardiovascular: flushing (6-10%), pedal edema (dose-related; 7-8%), exacerbation of angina
pectoris (dose-related; 6%), hypotension (IV 6%), palpitations (3-4%), tachycardia (1-4%),
orthostatic hypotension, ventricular extrasystoles. Rarely: AV block, ST segment depression,
inverted T waves.
Central nervous system: headache (6-15%), dizziness (4-7%)
Gastrointestinal: nausea and vomiting (IV 5%)
Neuromuscular & skeletal: weakness (4-6%)
Miscellaneous: sweating, thrombocytopenia, injection site reactions
COMMENTS
 Avoid grape fruit juice.
 Cardene SR has been discontinued in the United States for more than 1 year.
 For treatment over dosage, the infusion should be stopped and standard measures including
monitoring of cardiac and respiratory functions should be implemented. The patient should be
positioned so as to avoid cerebral anoxia (Trendelenburg).
Page 3 of 4
Last updated: July 2016
ANNE ARUNDEL MEDICAL CENTER
CRITICAL CARE MEDICATION MANUAL
DEPARTMENT OF NURSING AND PHARMACY
Guidelines for Use of Intravenous
Nicardipine (Cardene IV)
REFERENCES
Nicardipine. In: Lexi-Drugs Online [Internet Database]. Hudson, OH: Lexi-Comp, Inc. Updated 2016 Jul 1.
IV Additive Service
Drug Name
(Generic)
Nicardipine
Premixed Bags
20 mg / 200 mL
Nicardipine 25
mg ampules (2.5
mg/mL, 10 mL) –
must be diluted
before use
Storage
Requirements
Store at room
temp. Protect
from light until
ready to use.
Ampules should be
protected from
light until used and
stored at room
temperature.
Preparation
None required
Resulting
Concentration
0.1 mg/mL
Stability
Per manufacturer’s
expiration date on
product
Inject 10 mL of
0.1 mg/mL
Resulting solution
Nicardipine
is stable at room
(Cardene) 2.5
temperature for 24
mg/mL into a
hours.
250 mL bag of NSS
or D5W. **
** Final concentration slightly less than 0.1mg/mL due to overfill in bag but close enough as will
titrate to response.
Page 4 of 4
Last updated: July 2016