Nicarson

Each 10 mL Solution for Injection contains: Nicardipine HCl 10 mg.

Moderate to severe hypertension where immediate correction of blood pressure is required (ie, hypertensive emergencies or urgencies). Peri-operative and post-operative hypertension. Short-term treatment of essential hypertension when oral therapy is not feasible or desirable.

Nicardipine injection is intended for IV infusion. Dosage must be individualized depending on the severity 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.
Adults: Initial dose: Treatment should start with the continuous administration of nicardipine at the rate of 3-5 mg/h for 15 minutes. Rates can be increase by increments of 0.5 or 1 mg every 15 minutes. The infusion rate should not exceed 15 mg/hr.
Maintenance dose: When the target pressure is reached, the dose should be reduced progressively, usually to between 2 and 4 mg/h, to maintain the therapeutic efficacy.
Transition to an oral antihypertensive agent: discontinue nicardipine or titrate download while appropriate oral therapy is established. When an oral hypertensive agent is being instituted, consider the lag time of onset of the oral agent's affect. Continue blood pressure monitoring until desired effect is achieved.
A switch can also be made to oral nicardipine 20 mg capsules at dosage of 60 mg/day in 3 daily doses or to nicardipine 50 mg extended-release tablets, at dosage of 100 mg/day in 2 daily doses.
SPECIAL POPULATION: Older patients: Elderly may be more sensitive to nicardipine effects because of impaired renal &/or hepatic function. It is recommended to provide a continuous infusion of nicardipine starting at the dose of 1 to 5 mg/h, depending on the blood pressure and clinical situation. After 30 minutes, depending on the effect observed, the rate should be increased or decreased by increments of 0.5 mg/h. The rate should not exceed 15 mg/h.
Pregnancy: It is recommended to provide a continuous infusion of nicardipine starting at 1 to 5 mg/h, depending on the blood pressure and clinical situation. After 30 minutes, depending on the effect observed, this rate can be increased or decreased by increments of 0.5 mg/h.
Doses higher than 4 mg/h are generally not exceeded in the treatment of pre-eclampsia, however the rate should not exceed 15 mg/h.
Nicardipine should be used with particular caution in these patients. Since nicardipine is metabolized in the liver, it is recommended to use the same dose regimens as for elderly patients in patients with impaired liver function or reduced hepatic blood flow.
Renal Impairment: Infusion site reactions can occur, particularly with prolonged duration of administration and in peripheral veins.
It is advised to change the infusion site in case of any suspicion of infusion site irritation. The use of central venous line or of a greater dilution of the solution could reduce the risk of occurrence of infusion site reaction.
Pediatric population: The safety and efficacy of nicardipine IV has not been tested in controlled clinical trials in infants or children, thus special care is required in this population.

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. Pressor therapy and calcium gluconate IV should be reserved for patients with hypotension unresponsive to IV fluids.

Known hypersensitivity to nicardipine or to any of the excipients; advanced aortic stenosis; compensatory hypertension; unstable angina Patients with rare hereditary problems of fructose intolerance should not take this medicine.

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 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 or exacerbation of angina in <1% of patients with coronary artery disease given nicardipine.
Use in Patients with Congestive Heart Failure: Especially in those receiving concomitant β-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 blocker is intended to be withdrawn, β-blocker withdrawal should be done by gradual dose reduction, preferably over 8-10 days.
Use in Patients with Impaired Liver Function: Use with caution in patients with impaired liver function or reduced hepatic blood flow since nicardipine is extensively metabolized in the liver. Nicardipine bioavailability and elimination t½ are increased substantially in patients with severe hepatic impairment.
Use in Patients with Impaired Renal Function: Nicardipine IV should be used with caution and dosage titrated carefully in patients with impaired renal function.
Use in Patients with Pheochromocytoma: Administer with caution in patients with pheochromocytoma since there is limited clinical experience on the use of nicardipine IV in hypertension associated with pheochromocytoma.
Central Vein infusion Site: Nicardipine IV should be administered through central veins rather than arteries or small peripheral veins (eg, those on the dorsum of the hand or wrist) to decrease the possibility of venous thrombosis, phlebitis, local irritation, swelling, extravasation and rarely, vascular impairment.
Use in Children: The safety and effectiveness of nicardipine in patients <18 years have not been established.
Use in the Elderly: In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function and of concomitant disease or other drug therapy.

Use in 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 risk to the fetus.
There was an increased embryo lethality observed when nicardipine was administered orally to pregnant rabbits at a dose equivalent to a human oral dose of about 48 mg/kg/day (24 times the maximum recommended human oral dose and one 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 embryo lethality 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.
Use in 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 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, MI, 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.

Beta-blockers (Eg. Propranolol): Result in an 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: Increases nicardipine plasma levels. Patients receiving the 2 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 circulating 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 Agents: 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.

Store below 30°C. Protected from light.

Calcium Antagonists

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