Nicardex

Nicardex

nicardipine

Manufacturer:

Dexa Medica
Full Prescribing Info
Contents
Nicardipine hydrochloride.
Description
Each ml injection contains: Nicardipine hydrochloride 1 mg.
Action
Pharmacology: Antihypertensive action: Antihypertensive action: Nicardipine hydrochloride showed a dose-dependent antihypertensive action in anesthetized dogs, and the gradient of the dose-response curve was low. Accordingly, it is estimated that nicardipine hydrochloride is unlikely to cause excessive hypotension in the control of blood pressure, demonstrating its excellent potency to control blood pressure. Further, nicardipine hydrochloride showed a dose-dependent antihypertensive action in conscious dogs without inhibiting the excitation conducting system.
Sudden hypertension-inhibiting action: Nicardipine hydrochloride dose-dependently inhibited hypertension due to endogenous vasopressors (norepinephrine, angiotensin II) regarded as a cause of incidental onset of sudden hypertension under anesthesia, in anesthetized dogs. Further, in conscious dogs in which hypertension was induced by continuous administration of vasopressors (angiotensin II), nicardipine hydrochloride dose-dependently decreased blood pressure without affecting the excitation conducting system.
Action on the cardiovascular system: Cardiac hemodynamics: Nicardipine hydrochloride, having a potent coronary vasodilatory activity produced an increase in coronary blood flow and a decrease in peripheral vascular resistance, and thus, by reducing afterload, resulted in a decrease in myocardial oxygen consumption in anesthetized dogs.
Action on the cardiovascular system in various anesthetized conditions: Nicardipine hydrochloride showed almost equivalent antihypertensive effects in dogs and monkeys anesthetized with pentobarbital, GOF or NLA. The dose which decreased blood pressure by about 30% caused slight increases in reflex heart rate and myocardial contractility under pentobarbital anesthesia and NLA anesthesia, but no such effects were seen under GOF anesthesia. However, higher doses decreasing blood pressure by 50% or more, caused a decrease in cardiac contractility and prolongation of atrioventricular conduction under any conditions of anesthesia.
Organ circulation and blood gas: Nicardipine hydrochloride decreased blood pressure and increased cardiac output in anesthetized cats, thereby increasing blood flow in various organs, including the brain and heart. Nicardipine hydrochloride caused almost no change in blood gases (PO2, PCO2, pH) in anesthetized human subjects and dogs.
Diuretic effects: Nicardipine hydrochloride increased the renal blood flow and glomerular filtration rate in both conscious and anesthetized human subjects, thereby increasing urinary volume.
Mechanism of Action: Nicardipine hydrochloride exhibits a vasodilatory effect by inhibition of Ca++ influx into vascular smooth muscle cells. Nicardipine hydrochloride showed 30,000-fold more potent Ca++ antagonistic action on vascular smooth muscle than the cardiac muscle and its vascular selectivity was higher than other Ca++ antagonists.
Pharmacokinetics: The pharmacokinetics of nicardipine hydrochloride injection is linear over the dosage range of 0.5 to 40 mg/hour. On termination of the infusion, nicardipine hydrochloride concentrations decrease rapidly, with at least a 50% decrease during the first two hours post-infusion. Plasma concentrations increase at a much slower rate after the first few hours, and approach steady state at 24 to 48 hours. Total plasma clearance (CI) is 4.0 l/hour·kg, and the apparent volume of distribution (Vd) using a noncompartment model is 8.3 l/kg. The effects of nicardipine hydrochloride on blood pressure significantly correlate with plasma concentrations.
Nicardipine hydrochloride has been shown to be rapidly and extensively metabolized by the liver. Nicardipine hydrochloride is highly protein bound (>95%) in human plasma over a wide concentration range.
Indications/Uses
Emergency treatment of acute hypertensive crises during surgery.
Hypertensive emergencies.
Dosage/Direction for Use
Emergency treatment of acute hypertensive crises during surgery: Nicardipine hydrochloride injection is diluted with 0.9% sodium chloride or 5% glucose to give 0.01-0.02% nicardipine hydrochloride (0.1-0.2 mg/ml) solution. The solution is administered by IV drip infusion at a starting rate of 2-10 mcg/kg/minute until the desired value is reached and adjusted thereafter with monitoring to maintain blood pressure. For rapid reduction, nicardipine hydrochloride may be administered intact at a dose of 10-30 mcg/kg by IV injection.
Hypertensive emergencies: Nicardipine hydrochloride injection is diluted 0.9% sodium chloride solution or 5% glucose to give 0.01-0.02% nicardipine hydrochloride (0.1-0.2 mg/ml) solution. The solution is administered by IV drip infusion at a velocity of 0.5-6.0 mcg/kg/minute. The solution is administered at a dosing rate of 0.5 mcg/kg/minute until the desired value is reached and adjusted thereafter with monitoring to maintain blood pressure.
Contraindications
Patients with suspected incomplete hemostasis following intracranial hemorrhage.
Patients with elevated intracranial pressure at the acute stage of cerebral stroke. Intracranial pressure may be further elevated.
Patients with medical history of hypersensitivity to nicardipine hydrochloride.
Special Precautions
In patients with hypertensive emergencies, if it is necessary to control blood pressure after arrival at the desired blood pressure and if oral administration is feasible, replacement with oral drugs should be undertaken.
In patients with hypertensive emergencies, it is reported that blood pressure may again increase on withdrawal of nicardipine hydrochloride. Therefore, the dose of nicardipine hydrochloride should be reduced gradually and blood pressure be controlled with caution after withdrawn. Further, after replacement with oral drugs, patients should be cautioned against a reincrease in blood pressure.
Patients with hepatic or renal dysfunction. In general, acute hypotension in patients with severe renal dysfunction may induce renal hypofunction.
Patients with aortic stenosis. The symptom may be exacerbated. Since the effects of nicardipine hydrochloride may differ in individual patients, nicardipine hydrochloride should be administered carefully under close monitoring of blood pressure and heart rate.
If marked hypotension is caused by overdosage of nicardipine hydrochloride, administration should be discontinued. If rapid recovery of blood pressure is necessary, a vasopressor (norepinephrine) should be administered.
If any pain or redness appears at the injection site after long-term administration of nicardipine hydrochloride, the injection site should be changed.
It is noted that some patients in the postsurgical monitoring period after open heart surgery may develop circulatory failure and show symptoms of heart failure. Efficacy of nicardipine hydrochloride for such patients has not yet been established.
As with all parenteral drugs, nicardipine hydrochloride injections should be inspected visually for particulate matter and discoloration prior to administration. Nicardipine hydrochloride is clear and pale yellow solution.
Special populations: Use in the elderly: Since the elderly often have physiological hypofunction (hepatic, renal, etc.), it is advisable to start the treatment at a low dose (e.g., IV drip infusion at 0.5 mcg/kg/minute) and continue with careful monitoring.
Use in pediatric: Safety of nicardipine hydrochloride in prematures, newborns, sucklings, infants and children has not been established.
Use in pregnancy & lactation: Nicardipine hydrochloride should only be used in pregnant women and women suspected of being pregnant provided that the expected therapeutic benefits outweigh the possible risk of treatment.
The use of nicardipine hydrochloride is not recommended during lactation. If its use during lactation is necessary, the patient should discontinue breastfeeding.
Use In Pregnancy & Lactation
Nicardipine hydrochloride should only be used in pregnant women and women suspected of being pregnant provided that the expected therapeutic benefits outweigh the possible risk of treatment.
The use of nicardipine hydrochloride is not recommended during lactation. If its use during lactation is necessary, the patient should discontinue breastfeeding.
Adverse Reactions
Emergency treatment of acute hypertensive crises during surgery: The main adverse reaction was tachycardia.
Hypertensive emergencies: The main adverse reaction was facial hot flush.
Significant adverse reactions: Paralytic ileus: paralytic ileus may occur. If abnormal signs develop, administration should be discontinued and appropriate measures should be taken.
Hypoxemia: hypoxemia may occur infrequently. If abnormal signs develop, administration should be discontinued and appropriate measures should be taken.
Anginal pain (cases in a foreign country): if such signs develop, administration should be discontinued and appropriate measures should be taken.
Thrombocytopenia: thrombocytopenia may occur. Patients should be carefully observed, and if abnormal signs develop, administration should be discontinued and appropriate measures should be taken.
Hepatic function disorder and jaundice: hepatic function disorder associated with elevation of AST (GOT), ALT (GPT) or γ-GTP and jaundice may occur. Patients should be carefully observed, and if abnormal signs develop, administration should be discontinued and appropriate measures should be taken.
Other adverse reactions: (See Table 1).


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Drug Interactions
Nicardipine hydrochloride injections should be administered with care when co-administered with the following drugs: See Table 2.


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Caution For Usage
Instruction for use: Preparation of the drip-injectable solutions: For IV drip infusion, a 0.01-0.02% nicardipine hydrochloride solution is prepared by adding the necessary volume of nicardipine hydrochloride injections to an infusion fluid which is suitable for concomitant use with nicardipine hydrochloride injections. (See Table 3.)


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In intravenous drip infusion of this product, nicardipine hydrochloride may crystallize due to a high pH of the infusion fluid or for other reasons. Therefore, careful attention should be paid to the possibility of such crystallizations.
Storage
STORE AT TEMPERATURES BELOW 30°C, PROTECT FROM LIGHT.
MIMS Class
ATC Classification
C08CA04 - nicardipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.
Presentation/Packing
Inj (amp) 1 mg/mL x 10 mL x 5's.
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