Please sign in so that we can notify you about a reply
Indications/Uses
Moderate to severe hypertension where immediate correction of blood pressure (BP) is required (e.g., hypertensive emergency or urgencies).
Peri-operative and post-operative hypertension.
Short-term treatment of essential hypertension when oral therapy is not feasible or desirable.
Peri-operative and post-operative hypertension.
Short-term treatment of essential hypertension when oral therapy is not feasible or desirable.
Dosage/Direction for Use
Nicardipine injection is intended for intravenous injection. Dosage must be individualized depending on the seventy of hypertension and patient response during dosing.
Monitor BP and heart rate both during and after the infusion; avoid too rapid or excessive reduction in either systolic or diastolic BP during parenteral treatment.
Dosage as a Substitute for Oral Nicardipine: For patients who are maintained on oral nicardipine therapy and are being switched to IV therapy, the infusion rates necessary to produce an average plasma concentration equivalent to steady state oral doses.
Monitor BP and heart rate both during and after the infusion; avoid too rapid or excessive reduction in either systolic or diastolic BP during parenteral treatment.
Dosage as a Substitute for Oral Nicardipine: For patients who are maintained on oral nicardipine therapy and are being switched to IV therapy, the infusion rates necessary to produce an average plasma concentration equivalent to steady state oral doses.
Conditions Requiring Infusion Adjustment: Hypotension or Tachycardia: Discontinue infusion in case of hypotension or tachycardia. When BP and heart rate have stabilized, restart nicardipine IV infusion at low doses (e.g., 30 to 50 mL/hour) and adjust to maintain desired BP.
Infusion Site Changes: It is recommended that the infusion site be changed every 12 hours to minimize the risk of peripheral venous irritation.
Impaired Cardiac, Liver or Renal Function: Patients with congestive heart failure or impaired liver or renal function should be closely monitored when titrating nicardipine IV.
Transfer to Oral Antihypertensive: When transferring treatment to an oral antihypertensive other than nicardipine oral capsule or tablet, therapy should be started upon discontinuation of nicardipine IV.
If nicardipine tablets or capsules are to be used, the first dose of a thrice daily oral regimen should be taken 1 hour prior to discontinuation of nicardipine IV infusion.
Infusion Site Changes: It is recommended that the infusion site be changed every 12 hours to minimize the risk of peripheral venous irritation.
Impaired Cardiac, Liver or Renal Function: Patients with congestive heart failure or impaired liver or renal function should be closely monitored when titrating nicardipine IV.
Transfer to Oral Antihypertensive: When transferring treatment to an oral antihypertensive other than nicardipine oral capsule or tablet, therapy should be started upon discontinuation of nicardipine IV.
If nicardipine tablets or capsules are to be used, the first dose of a thrice daily oral regimen should be taken 1 hour prior to discontinuation of nicardipine IV infusion.
Overdosage
Studies in laboratory animals showed that lethal nicardipine overdose may cause systemic hypotension, bradycardia (following initial tachycardia) and progressive atrioventricular conduction block. Reversible hepatic function abnormalities and sporadic focal hepatic necrosis were also noted in test animals.
Standard measures including monitoring of cardiac and respiratory functions should be implemented as part of the management of nicardipine overdosage. Place the patient in supine position with legs elevated to avoid cerebral anoxia. If this is not adequate, increase plasma volume by infusion of glucose, saline or dextran. Frequent BP monitoring is essential. In case of accompanying bradycardia, administer atropine IV. Presser therapy and intravenous calcium gluconate should be reserved for patients with hypotension unresponsive to IV fluids.
Standard measures including monitoring of cardiac and respiratory functions should be implemented as part of the management of nicardipine overdosage. Place the patient in supine position with legs elevated to avoid cerebral anoxia. If this is not adequate, increase plasma volume by infusion of glucose, saline or dextran. Frequent BP monitoring is essential. In case of accompanying bradycardia, administer atropine IV. Presser therapy and intravenous calcium gluconate should be reserved for patients with hypotension unresponsive to IV fluids.
Contraindications
Known hypersensitivity to nicardipine.
Advanced aortic stenosis.
Advanced aortic stenosis.
Special Precautions
Excessive Pharmacologic Effects: Carefully monitor patient's BP and heart rate since nicardipine decreases peripheral vascular resistance and occasionally causes excessive and poorly tolerated hypotension or tachycardia.
Use with caution in patients with acute cerebral infarction or hemorrhage, and systemic hypotension should be avoided in these patients.
Rapid Decreases in BP: Although nicardipine IV has not been associated with adverse effects secondary to an excessively rapid decrease in BP, reduction of BP should be accomplished over as long a time period as is compatible with patient's clinical status.
Use in Patients with Angina: Increases in frequency, duration, or severity of angina have been observed in chronic oral nicardipine therapy. There have been reports of induction of exacerbation of angina in less than 1% of patients with coronary artery disease given nicardipine.
Use in Patients with Congestive Heart Failure: Use with caution in patients with congestive heart failure, especially in those receiving concomitant beta-adrenergic blocking agents, since nicardipine has been shown in some in vitro and clinical studies to have negative inotropic effect and may precipitate or worsen heart failure. If concomitant beta-blocker is intended to be withdrawn, beta-blocker withdrawal should be done by gradual dose reduction, preferably over 8 to 10 days.
Use in Patients with Impaired Liver Function: Use with caution in patient with impaired liver function or reduced hepatic blood flow since nicardipine is extensively metabolized in liver. Nicardipine bioavailability and elimination half-life are increased substantially in patients with severe hepatic impairment.
Use with caution in patients with acute cerebral infarction or hemorrhage, and systemic hypotension should be avoided in these patients.
Rapid Decreases in BP: Although nicardipine IV has not been associated with adverse effects secondary to an excessively rapid decrease in BP, reduction of BP should be accomplished over as long a time period as is compatible with patient's clinical status.
Use in Patients with Angina: Increases in frequency, duration, or severity of angina have been observed in chronic oral nicardipine therapy. There have been reports of induction of exacerbation of angina in less than 1% of patients with coronary artery disease given nicardipine.
Use in Patients with Congestive Heart Failure: Use with caution in patients with congestive heart failure, especially in those receiving concomitant beta-adrenergic blocking agents, since nicardipine has been shown in some in vitro and clinical studies to have negative inotropic effect and may precipitate or worsen heart failure. If concomitant beta-blocker is intended to be withdrawn, beta-blocker withdrawal should be done by gradual dose reduction, preferably over 8 to 10 days.
Use in Patients with Impaired Liver Function: Use with caution in patient with impaired liver function or reduced hepatic blood flow since nicardipine is extensively metabolized in liver. Nicardipine bioavailability and elimination half-life are increased substantially in patients with severe hepatic impairment.
Use In Pregnancy & Lactation
Pregnancy: Pregnancy Category C. There are no adequate and controlled studies to date using nicardipine in pregnant women. Nicardipine should be used in pregnancy only when the potential benefits justify the potential risks to the fetus.
There was increased embryolethality observed when nicardipine was administered orally to pregnant rabbit at a dose equivalent to a human oral dose of about 48 mg/kg/day (24 times the maximum recommended human oral dose and on associated with marked maternal body weight gain suppression). There were no adverse effects on the fetus, though there was increased maternal mortality, when nicardipine was given at a lower oral dose equivalent to a human dose of about 32 mg/kg/day (16 times the maximum recommended human oral dose) in a different strain of rabbit.
There was no evidence of embyrolethality or teratogenicity when pregnant rats were administered nicardipine orally at a dose equivalent to a human oral dose of about 16 mg/kg/day (8 times the maximum recommended human oral dose); however, dystocia, reduced birth weight, neonatal survival and neonatal weight gain were reported.
Lactation: Nicardipine is distributed into milk in high concentrations in rats. Because of the potential for serious adverse reactions to nicardipine in breastfeeding infants, it is recommended that women who breastfeed not be given the drug.
There was increased embryolethality observed when nicardipine was administered orally to pregnant rabbit at a dose equivalent to a human oral dose of about 48 mg/kg/day (24 times the maximum recommended human oral dose and on associated with marked maternal body weight gain suppression). There were no adverse effects on the fetus, though there was increased maternal mortality, when nicardipine was given at a lower oral dose equivalent to a human dose of about 32 mg/kg/day (16 times the maximum recommended human oral dose) in a different strain of rabbit.
There was no evidence of embyrolethality or teratogenicity when pregnant rats were administered nicardipine orally at a dose equivalent to a human oral dose of about 16 mg/kg/day (8 times the maximum recommended human oral dose); however, dystocia, reduced birth weight, neonatal survival and neonatal weight gain were reported.
Lactation: Nicardipine is distributed into milk in high concentrations in rats. Because of the potential for serious adverse reactions to nicardipine in breastfeeding infants, it is recommended that women who breastfeed not be given the drug.
Adverse Reactions
Adverse effects that have been reported with nicardipine IV are as follows: Body as a Whole: Asthenia, chest pain, fever, neck pain, malaise, fatigue, peripheral or facial edema, infection, arthralgia.
Cardiovascular: Hypotension, postural hypotension, exertional hypotension, tachycardia, ECG abnormality, ventricular extrasystoles, extrasystoles, hemopericardium, hypertension, supraventricular tachycardia, syncope, vasodilation, ventricular tachycardia, angina pectoris, atrioventricular block, ST segment depression, inverted T wave, deep-vein thrombophlebitis, sick sinus syndrome, flushing, palpitations, myocardial infarction, atrial fibrillation, pericarditis, peripheral vascular disorder.
Digestive: Abdominal pain, nausea, vomiting, dyspepsia, constipation, diarrhea, dry mouth, anorexia, heartburn.
Metabolic and Nutritional: Hypokalemia, hypophosphatemia, hyperglycemia, abnormal hepatic function test results, increased plasma renin concentration.
Nervous: Headache, dizziness, hypesthesia, intracranial hemorrhage, paresthesia, confusion, hypertonia, somnolence, insomnia, hot flashes, vertigo, hyperkinesia, impotence, mental depression, anxiety, cerebrovascular accident, cerebral ischemia, lassitude, nervousness, lightheadedness.
Hemic and Lymphatic: Thrombocytopenia.
Respiratory: Dyspnea, respiratory disorder, rhinitis, sinusitis.
Skin and Appendages: Sweating, injection site reaction and pain, rash.
Urogenital: Polyuria, hematuria, increased urinary frequency, nocturia, urinary retention.
Special Senses: Conjunctivitis, abnormal or blurred vision, ear disorder, tinnitus.
Cardiovascular: Hypotension, postural hypotension, exertional hypotension, tachycardia, ECG abnormality, ventricular extrasystoles, extrasystoles, hemopericardium, hypertension, supraventricular tachycardia, syncope, vasodilation, ventricular tachycardia, angina pectoris, atrioventricular block, ST segment depression, inverted T wave, deep-vein thrombophlebitis, sick sinus syndrome, flushing, palpitations, myocardial infarction, atrial fibrillation, pericarditis, peripheral vascular disorder.
Digestive: Abdominal pain, nausea, vomiting, dyspepsia, constipation, diarrhea, dry mouth, anorexia, heartburn.
Metabolic and Nutritional: Hypokalemia, hypophosphatemia, hyperglycemia, abnormal hepatic function test results, increased plasma renin concentration.
Nervous: Headache, dizziness, hypesthesia, intracranial hemorrhage, paresthesia, confusion, hypertonia, somnolence, insomnia, hot flashes, vertigo, hyperkinesia, impotence, mental depression, anxiety, cerebrovascular accident, cerebral ischemia, lassitude, nervousness, lightheadedness.
Hemic and Lymphatic: Thrombocytopenia.
Respiratory: Dyspnea, respiratory disorder, rhinitis, sinusitis.
Skin and Appendages: Sweating, injection site reaction and pain, rash.
Urogenital: Polyuria, hematuria, increased urinary frequency, nocturia, urinary retention.
Special Senses: Conjunctivitis, abnormal or blurred vision, ear disorder, tinnitus.
Drug Interactions
Beta-blockers (e.g. Propranolol): Beta-blockers result in excessive decrease in BP and a reduction in cardiac function in patients with congestive heart failure. Reduce dosage or discontinue use of either drug when necessary.
Cimetidine: Cimetidine increases nicardipine plasma levels. Patients receiving the two drugs concomitantly should be carefully monitored.
Digoxin: Nicardipine may increase plasma levels of digitalis preparations. Evaluate digoxin levels when concomitant therapy with nicardipine IV is initiated.
Fentanyl Anesthesia: Concomitant use of fentanyl anesthesia with a calcium channel blocker has been reported to cause hypotension. Although such interactions were not seen in studies with nicardipine IV, an increased volume of circulation fluids might be necessary in the occurrence of such interactions.
Ciclosporin: Concomitant administration increases ciclosporin plasma levels. Ciclosporin dosage should therefore be reduced accordingly in patients treated with nicardipine.
Other antihypertensive: Monitor patients to identify and treat promptly any undesirable effects from concomitant administration.
In vitro Interaction: No changes in plasma protein binding of nicardipine were observed when furosemide, propranolol, dipyridamole, warfarin, quinidine, or naproxen were added to human plasma in vitro.
Cimetidine: Cimetidine increases nicardipine plasma levels. Patients receiving the two drugs concomitantly should be carefully monitored.
Digoxin: Nicardipine may increase plasma levels of digitalis preparations. Evaluate digoxin levels when concomitant therapy with nicardipine IV is initiated.
Fentanyl Anesthesia: Concomitant use of fentanyl anesthesia with a calcium channel blocker has been reported to cause hypotension. Although such interactions were not seen in studies with nicardipine IV, an increased volume of circulation fluids might be necessary in the occurrence of such interactions.
Ciclosporin: Concomitant administration increases ciclosporin plasma levels. Ciclosporin dosage should therefore be reduced accordingly in patients treated with nicardipine.
Other antihypertensive: Monitor patients to identify and treat promptly any undesirable effects from concomitant administration.
In vitro Interaction: No changes in plasma protein binding of nicardipine were observed when furosemide, propranolol, dipyridamole, warfarin, quinidine, or naproxen were added to human plasma in vitro.
Caution For Usage
Preparation of Infusion Solution: Dilution Instructions: Nicardipine Injection must be diluted prior to administration. It is administered by slow continuous IV infusion at a concentration of 0.1 mg/mL. Nicardipine infusion solution is prepared by adding the necessary volume of nicardipine injection to a compatible infusion fluid.
Storage
Store at temperatures not exceeding 30°C. Protect from light.
Action
Pharmacology: Pharmacodynamics: Nicardipine is a dihyropyridine calcium channel antagonist that inhibits the transmembrane influx of calcium ions into cardiac muscle and vascular smooth muscle without changing serum calcium ion concentrations. Vascular smooth muscles are more sensitive to this effect than cardiac muscles because depolarization of vascular smooth muscle is dependent on calcium ion influx whereas cardiac muscle depolarization involves both sodium and calcium ion influx.
Nicardipine demonstrates strong coronary and cerebral vasodilatory activity. The selectivity for arterial and especially cardiac arterial vascular smooth muscle is reflected in relatively large and rapid changes in blood pressure (BP), with minimal inotropic cardiac effects and no significant venodilatory action.
Intravenous (IV) nicardipine produces dose-related decreases in mean arterial BP (up to 30% reduction) and increases in heart rate (by up to 13% to 26%). The duration of these effects, which may be as long as 3 hours, have generally been greater in patients at rest than in those at exercise. Nicardipine-induced increases in heart rate are due to reflex adrenergic stimulation following reduction in total peripheral resistance.
The degree of vasodilation and the resultant BP reduction were more prominent in hypertensive patients compared with normotensive volunteers given intra-arterial nicardipine. In normotensive volunteers, the administration of nicardipine 0.25 to 3 mg/hour for eight hours produced changes of <5 mmHg in systolic BP and <3 mmHg in diastolic BP.
Nicardipine exerts a vasorelaxing action on cerebrovascular smooth muscles thereby enhancing blood flow and oxygenation into the brain. Thus, nicardipine may be beneficial in the prevention of cerebrovascular accidents among hypertensive patients.
Hemodynamic studies in patients with coronary artery disease and normal or moderately abnormal left ventricular function have shown significant increases in cardiac output and coronary blood flow, with no significant change or a small decrease in left ventricular end-diastolic pressure (LVEDP). The ejection fraction is significantly increased by nicardipine.
Nicardipine demonstrates strong coronary and cerebral vasodilatory activity. The selectivity for arterial and especially cardiac arterial vascular smooth muscle is reflected in relatively large and rapid changes in blood pressure (BP), with minimal inotropic cardiac effects and no significant venodilatory action.
Intravenous (IV) nicardipine produces dose-related decreases in mean arterial BP (up to 30% reduction) and increases in heart rate (by up to 13% to 26%). The duration of these effects, which may be as long as 3 hours, have generally been greater in patients at rest than in those at exercise. Nicardipine-induced increases in heart rate are due to reflex adrenergic stimulation following reduction in total peripheral resistance.
The degree of vasodilation and the resultant BP reduction were more prominent in hypertensive patients compared with normotensive volunteers given intra-arterial nicardipine. In normotensive volunteers, the administration of nicardipine 0.25 to 3 mg/hour for eight hours produced changes of <5 mmHg in systolic BP and <3 mmHg in diastolic BP.
Nicardipine exerts a vasorelaxing action on cerebrovascular smooth muscles thereby enhancing blood flow and oxygenation into the brain. Thus, nicardipine may be beneficial in the prevention of cerebrovascular accidents among hypertensive patients.
Hemodynamic studies in patients with coronary artery disease and normal or moderately abnormal left ventricular function have shown significant increases in cardiac output and coronary blood flow, with no significant change or a small decrease in left ventricular end-diastolic pressure (LVEDP). The ejection fraction is significantly increased by nicardipine.
MedsGo Class
Calcium Antagonists
Features
Brand
Cardizef
Full Details
Dosage Strength
10 mg / 10 ml (1 mg / 1 ml)
Drug Ingredients
- Nicardipine
Drug Packaging
Solution for Injection (I.V.) 10's
Generic Name
Nicardipine Hcl
Dosage Form
Solution For Injection (I.V.)
Registration Number
DRP-8014-07
Drug Classification
Prescription Drug (RX)