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PubMed1991

Efficacy and safety of intravenous nicardipine in the control of postoperative hypertension. IV Nicardipine Study Group.

In a double-blind, randomized, multicenter study, the efficacy and safety of intravenous (IV) nicardipine was compared with placebo in the control of postoperative hypertension in cardiac and noncardiac surgical patients. One hundred twenty-two patients (17 cardiac and 105 noncardiac surgery) met the entry criteria (systolic BP greater than or equal to 140 mm Hg or diastolic BP greater than or equal to 95 mm Hg) and were randomized (3:2) to receive IV nicardipine (n = 71) or placebo (n = 51). Therapeutic response (greater than or equal to 15 percent reduction in BP from baseline) was achieved in 94 percent of patients treated with IV nicardipine vs 12 percent with placebo (p less than 0.001). The mean response time and infusion rate for IV nicardipine were 11.5 (+/- 0.8) minutes and 12.8 (+/- 0.3) mg/h, respectively. The magnitude of BP reduction was similar in both cardiac and noncardiac postsurgical patients. Blood pressure control was sustained with minimal dose adjustments of IV nicardipine (3.0 +/- 0.2 mg/h) during a prolonged maintenance infusion period of 6.8 +/- 0.5 h. A reflex mean increase in heart rate of 5 bpm was seen in patients treated with IV nicardipine. Sixteen patients (15 noncardiac and one cardiac surgery) had a sustained heart rate of greater than 100 bpm, with a mean increase of 24 bpm from the baseline. In all these patients except three, tachycardia was resolved while receiving nicardipine. None of these patients who had development of tachycardia during nicardipine therapy had exhibited ST segment changes indicative of ischemia. One patient with tachycardia at baseline had exhibited ST segment depression (3 to 4 mm) during nicardipine treatment, which was resolved following discontinuation of nicardipine therapy and application of nitroglycerin (Nitropaste). Hemodynamic evaluation revealed that IV nicardipine significantly decreased mean arterial pressure, systemic vascular resistance, and significantly increased cardiac index with no change in heart rate. These hemodynamic changes were similar in cardiac and noncardiac surgical patients. Adverse experiences reported with IV nicardipine included hypotension (4.5 percent), tachycardia (2.7 percent), and nausea/vomiting (4.5 percent). In the placebo group, the incidence of adverse experience was 6 percent, with an equal distribution of hypotension (2 percent), nausea/vomiting (2 percent), and headache (2 percent). No clinically important changes in laboratory variables related to IV nicardipine were reported. In conclusion, these findings indicate that nicardipine, a titratable intravenous calcium channel blocker, can rapidly and effectively control postoperative hypertension in cardiac and noncardiac surgical patients.

Adult↗
PubMed1995

Determination of (+)- and (-)-nicardipine concentrations in human serum and their correlation with the antihypertensive effect after oral administration of racemic nicardipine.

Serum (+)- and (-)-nicardipine concentrations were determined after oral administration of racemic nicardipine, and the relationship between the concentration of each enantiomer and the percentage change in blood pressure was investigated. Serum concentrations of (+) and (-)-nicardipine were assayed separately by a method combining high-performance liquid chromatography (HPLC) with gas chromatography - mass spectrometry (GS-MS). Linear relationships were found with serum concentrations of 0.25-80 mg x ml(-1) for both enantiomers of nicardipine with correlation coefficients of greater than 0.999. A single oral dose of 40 mg racemic nicardipine was given to 15 patients with essential hypertension. Serum (+)-nicardipine concentration was 2-3 times higher than the concentration of (-)-nicardipine 1, 2, and 3 after drug administration. The logarithmically transformed value of the serum (+)-nicardipine concentration was inversely correlated with the percentage change in systolic blood pressure, the correlation being statistically significant 1 and 2 h after drug administration, and also inversely correlated with the percentage change in diastolic blood pressure 1, 2 and 3 h after drug administration. However, the logarithmically transformed value of serum (-)-nicardipine showed no significant correlations with the percentage change in either systolic or diastolic blood pressure.

Administration, Oral↗
PubMed1987

Nicardipine in the treatment of essential hypertension controlled 6-month-study comparing nicardipine with propranolol at rest and during exercise.

Thirty patients with mild to moderate essential hypertension entered a randomised double-blind parallel group study for 6 months to compare the effects of the new calcium channel blocker nicardipine 90 mg/day and propranolol 240 mg/day. Both drugs reduced systolic and diastolic blood pressures significantly in the supine and in standing positions. After 6 months of treatment, nicardipine had reduced the supine systolic and diastolic blood pressures by 16 and 17 mm Hg, respectively, and propranolol by 15 and 12 mm Hg. While propranolol treatment led to a marked decline in heart rate, nicardipine caused a small but statistically significant increase in heart rate throughout the study. Both drugs reduced blood pressure during maximal exercise, but propranolol had a greater effect. During exercise nicardipine did not affect the heart rate, whereas propranolol dramatically reduced it. Nicardipine did not produce any ECG changes at rest or during exercise. The side-effects for nicardipine were mild and were related to the vasodilatation induced by the drug. No abnormalities in routine blood chemical tests were found for either of the drugs. Nicardipine appears to be an effective single drug treatment for mild to moderate hypertension.

Adult↗
PubMed2004

Bioequivalence study of nicardipine solution versus nicardipine tablets.

The bioequivalence of a solution (investigational product) and a tablet (reference product) formulation of the dihydropyridine-type derivative Ca2+ antagonist nicardipine were investigated by measuring plasma levels of the compound after single randomized administration of 20 mg of the two formulations. Drugs were given orally in a single dose to 24 healthy volunteers (12 males and 12 females) at the beginning of the experiment and after a two weeks wash-out. Nicardipine is available in oral and intravenous formulations, the second being used for the short-term treatment of hypertensive crises. Oral formulations of nicardipine most diffused include immediate release (20 or 30 mg, three times a day administration), sustained release (30 mg, 45 mg or 60 mg, twice a day administration) and modified release (80 mg, once a day administration) tablets. A nicardipine solution is available only in Spain, but no published studies on the kinetics of this formulation are available. In the last 15 years, the main efforts were aimed to develop sustained or controlled release formulations of nicardipine to improve patient compliance by reducing the number of doses required each day. However, the use of twice a day or once a day administration of Ca2+ antagonists should be not overemphasized in particular situations like those of possible risk of cerebrovascular and/or coronary steal effect primarily in the elderly. The oral formulation of nicardipine investigated with a bioequivalence range > 70% compared to nicardipine immediate release tablets may represent an additional resource for treating elderly patients with concomitant cerebrovascular or coronary heart disease.

Adult↗
PubMedDate not supplied

[An experimental, randomized, double-blind, placebo-controlled clinical trial to infestigate the effect of nicardipine on cognitive function in patients with vascular dementia. Spanish group of nicardipine study in vascular dementia].

INTRODUCTION AND OBJECTIVE: Experimental and clinical data suggest that calcium channel blockers could be effective in the treatment of vascular dementia (VD). The aim of this study is to evaluate the effect of nicardipine on the progression of cognitive impairment in patients with VD. PATIENTS AND METHODS: We selected outpatients, of both sexes, between 55 and 80 years old, with VD. Following a placebo wash-out period (4 weeks), the patients received nicardipine 20 mg t.i.d. or placebo for one year. The primary efficacy variable was the loss of over 10% of the basal score on the Mini-Mental State Examination after one year. The time it took to reach this degree of impairment, the evolution of Pfeiffer score, the effect on functional disability and the drug safety were also evaluated. RESULTS: 156 patients were included, 109 completed the study, and 142 underwent intent-to-treat analysis. At the end of the study, 34.6% of patients with placebo and 21.1% with nicardipine had lost over 10% of their basal MMSE score. Favorable effects of nicardipine were found on females (40.9% vs 10.5%, p = 0.01876), patients without previous treatments (46.2% vs 13.3%, p = 0.00748) and patients with concomitant antiplatelet treatment (35.0% vs 15.9; p = 0.03836). Survival analysis showed that the patients with nicardipine took longer to lose cognitive capacities (p = 0.031; RR = 1.15-3.99). CONCLUSION: Nicardipine did not reduce the cognitive decline at the stated period in the total group but it significantly delayed this decline and produces better evolution in females, in patients without previous treatments, and those with antiplatelet treatment.

Aged↗
PubMed1997

Determining the optimum dose for the intravenous administration of nicardipine in the treatment of acute heart failure--a multicenter study. The Nicardipine Heart Failure Study Group.

Nicardipine is a potent arteriolar vasodilator with a negligible negative inotropic effect. Although intravenous administration of this drug has been reported to be effective in the treatment of heart failure, the optimal dose by this route is not clear. This study was designed to determine the optimum dose for the intravenous infusion of nicardipine in the treatment of heart failure. In Trial 1, nicardipine was administered intravenously at a dose of 0.5 microgram/kg per min to 14 patients with acute heart failure. The dose was increased to 1.0 microgram/kg per min in 13 cases with marked improvement at 2 h. In Trial 2, nicardipine was administered in a double-blind manner to 53 patients at 3 different rates of infusion for 2 h: 1.0 (Group 1, n = 19), 2.0 (Group 2, n = 15), and 3.0 (Group 3, n = 19) micrograms/kg per min. Neither heart rate nor mean right atrial pressure changed in any of the 3 groups. Favorable hemodynamic effects were evident in all groups beginning 30 min after the start of infusion, with an increase in cardiac index (control vs 2 h after infusion, L/min per m2) (Group 1: 2.2 +/- 0.4 vs 3.1 +/- 0.8, Group 2: 2.2 +/- 0.4 vs 2.9 +/- 0.5, Group 3: 2.3 +/- 0.3 vs 3.1 +/- 0.7, all p < 0.01 compared to the control) and a decrease in diastolic pulmonary artery pressure (Group 1: 26 +/- 10 vs 19 +/- 7, Group 2: 27 +/- 10 vs 20 +/- 8, Group 3: 26 +/- 7 vs 18 +/- 5 mmHg, all p < 0.01). The decrease in systolic pressure was greatest in Group 3 (Group 1: 141 +/- 31 vs 119 +/- 18, Group 2: 149 +/- 25 vs 118 +/- 17, Group 3; 147 +/- 27 vs 107 +/- 14 mmHg, all p < 0.01 compared to control, and p < 0.05 between Groups 1 and 3). The intravenous drip infusion of nicardipine is effective in the treatment of heart failure by inducing an increase in cardiac output and a decrease in pulmonary artery wedge pressure. The optimal dose in this study was 1.0 microgram/kg per min.

Acute Disease↗
PubMed1995

Adsorptive stripping voltammetry of nicardipine at a HMDE; determination of trace levels nicardipine in blood and urine.

The redox behaviour of nicardipine, a 1,4-dihydropyridine calcium antagonist, has been studied in different media on mercury, glassy carbon, gold and platinum electrodes using various voltammetric techniques. A highly sensitive adsorptive stripping voltammetric method for the determination of nicardipine based on adsorption of the drug onto mercury, followed by differential pulse voltammetric determination of the surface species, is described. All factors (pH, supporting electrolyte, accumulation potential and time, etc.) influencing adsorption as well as voltammetric response are discussed. The application of adsorptive stripping voltammetry at the hanging mercury drop electrode (HMDE) to the determination of trace levels of nicardipine in human urine and blood is illustrated, without an extraction procedure being necessary prior to the voltammetric measurement. A limit of detection of 4.8 ng per ml urine and 34 ng per ml blood is found with a mean recovery of nicardipine in urine and blood of 97%. The mean relative error does not exceed 6.5%.

Calcium Channel Blockers↗
PubMed1990

Randomized double-blind comparison of side effects of nicardipine and nifedipine in angina pectoris. The Nicardipine Investigators Group.

Nicardipine and nifedipine are structurally similar dihydropyridine calcium channel blockers with demonstrated efficacy in the treatment of stable angina pectoris. The present study was a prospective randomized trial designed to evaluate the relative incidence of dizziness, flushing, headache, pedal edema, and palpitations during use of these drugs in patients with angina pectoris. Of 250 patients who entered into the comparative treatment part of the study, 140 patients were susceptible to developing symptoms to nifedipine as identified during a 1-month open-label treatment with nifedipine. These patients were compared with a parallel cohort of 110 patients, who were identified during the same open-label period, but remained mostly asymptomatic. After a 1-week washout of nifedipine, equal numbers of patients in each cohort began an 8-week period of randomized, double-blind treatment with nifedipine (20 mg three times daily) or nicardipine (30 mg three times daily). Patients who experienced these symptoms during the open-label nifedipine treatment had a higher incidence of the same symptoms during the blinded treatment regimen. Nicardipine-treated patients had a lower incidence of each of the symptoms than did the nifedipine-treated patients. Statistically significant differences were reported for dizziness, the most common of the side effects. Patients who were free of these symptoms in the open-label period usually remained free of them in the blinded comparison. However, even among those free of dizziness during the open-label nifedipine treatment, more patients reported experiencing dizziness in the blinded phase from nifedipine than from nicardipine (18% vs 6%; p = 0.02).

Adult↗
PubMed1988

[Comparison of protective effects induced by the ultrasonic mist of nicardipine + fenoterol versus nicardipine + fenoterol + ipratropium bromide].

A comparison is presented of the protective effect of ultrasound mist induced by nicardipine + fenoterol and nicardipine + fenoterol + ipratropium bromide in a group of 11 patients with chronic bronchial asthma in a phase of relative clinical stability. The data collected show that the three-drug combination was more effective than the use of nicardipine and fenoterol.

Aerosols↗
PubMedDate not supplied

Nicardipine hydrochloride injectable phase IV open-label clinical trial: study on the anti-hypertensive effect and safety of nicardipine for acute aortic dissection.

We performed a multicentre, phase IV, open-label clinical trial to examine the clinical usefulness of a continuous infusion of nicardipine hydrochloride to control hypertension in 31 patients with acute aortic dissection. Target blood pressure levels were reached within 15 min in 16 patients; in 15-30 min in 10 patients; in 30-45 min in three patients; and in 45-60 min in two patients. Baseline average systolic, diastolic and mean arterial blood pressures were 147 +/- 23 mmHg, 82 +/- 18 mmHg and 104 +/- 18 mmHg, respectively, with third-day pressures significantly reduced at 119 +/- 12 mmHg, 69 +/- 9 mmHg and 86 +/- 8 mmHg. Blood pressures after discontinuation of the infusion were not significantly different from those measured on the third day of infusion and no definite adverse effects attributable to the treatment were observed. Nicardipine hydrochloride was both effective and safe at controlling blood pressure in patients with acute aortic dissection.

Antihypertensive Agents↗
PubMed1987

[Double-blind evaluation of slow-release nicardipine using different methods of blood pressure measurement. Predictive value of the acute response to intravenous nicardipine].

Forty hypertensive patients (diastolic greater than 95 mmHg) were included after 15 days of a single blind placebo period in a randomized placebo controlled double-blind study to assess the antihypertensive effect of a new galenic form of nicardipine (N) administered 50 mg b.i.d. for 3 weeks. They comprised 27 men and 13 women aged from 27 to 72 years (mean: 53 +/- 10). Blood pressure (BP) was measured in hospital before morning drug intake by an automatic recorder (Sentron) in supine position for 30 minutes (min) and by a mercury sphygmomanometer. Ambulatory BP was assessed by a portable patient activated recorder (Remler 2000). Mercury sphygmomanometer supine BP under N fell from 160 +/- 21/104 +/- 6 mmHg to 151 +/- 14/98 +/- 8 mmHg (n = 20; p less than 0.01/p less than 0.01) whereas BP under placebo (P) was respectively 158 +/- 14/103 +/- 6 mmHg and 156 +/- 20/102 +/- 9 mmHg (NS). Sentron BP under N fell from 158 +/- 17/96 +/- 8 mmHg to 148 +/- 13/90 +/- 7 mmHg (p less than 0.001/p less than 0.01) with no BP change under P (152 +/- 12/93 +/- 7 mmHg to 151 +/- 14/93 +/- 8 mmHg NS). BP recorder every 30 min for 12 hours revealed a decrease under N (160 +/- 18/105 +/- 10 mmHg to 142 +/- 16/94 +/- 10 mmHg; p less than 0.001/p less than 0.001) with a placebo effect in the control group on the diastolic BP (160 +/- 15/103 +/- 7 mmHg to 156 +/- 16/100 +/- 8 mmHg/NS/p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed2000

Effects of grapefruit juice on the stereoselective disposition of nicardipine in humans: evidence for dominant presystemic elimination at the gut site.

OBJECTIVES: To assess relative roles of the intestinal and hepatic stereoselective metabolism of nicardipine in an oral first-pass disposal with and without grapefruit juice intake. METHODS: The kinetic profiles of (+)- and (-)-nicardipine were studied in the six normal healthy male volunteers who received oral (40 mg) and intravenous (2 mg) racemic nicardipine, first with water and second with grapefruit juice. Both the enantiomers were determined by the stereoselective high-performance liquid chromatographic method, and hemodynamic parameters (arterial blood pressure, heart rate, and electrocardiogram) were assessed when each blood sample was taken. RESULTS: Grapefruit juice compared with water intake caused a significant (P < 0.05) increase in the mean oral (+)- and (-)-nicardipine bioavailability (Fobs) (48.6+/-5.0% and 105.6+/-7.8%) and dose-absorbed (Fabs) available fraction unmetabolized at the gut (Fg) (48.2+/-5.6% and 110.9+/-8.8%, respectively) with no significant change in the hepatic first-pass effect. However, all of the mean kinetic parameters of both the enantiomers after the intravenous dosing of racemic nicardipine did not differ between the grapefruit juice- and water-intake trial phases. The mean percentage changes in oral AUC (43.1+/-3.4% in [+]-nicardipine and 90.9 6.4% in [-]-nicardipine, or Fobs) and Fabs Fg by grapefruit juice tended to be greater for (-)-nicardipine than for (+)-nicardipine and the mean oral (+)/(-)-nicardipine AUC ratio was significantly reduced by grapefruit juice (from 2.25+/-0.37 to 1.75+/-0.28) (P < 0.05). Except for heart rates, which were greater with grapefruit juice (P < 0.05) at 1 and 2 h after the oral dose of nicardipine, the mean hemodynamic variables did not differ between the two trial phases. CONCLUSION: We conclude that the gut is the major presystemic disposal site of racemic nicardipine in humans. Grapefruit juice appears to affect this metabolic disposal of (-)-nicardipine to a somewhat greater extent compared with that of (+)-nicardipine, with an early postdose transient tachycardia after the oral dosing of racemic nicardipine.

Adult↗
PubMed2003

Intravenous nicardipine for treatment of postcoarctectomy hypertension in children.

Our objective was to evaluate the efficacy of intravenous (IV) nicardipine for the treatment of postcoarctectomy hypertension in children with coarctation of the aorta. We carried out a retrospective review in a pediatric intensive care unit at a tertiary care children's hospital. The patients were children with coarctation of the aorta treated for postcoarctectomy hypertension. Children with postcoarctectomy hypertension defined as a systolic blood pressure >95th percentile for age measured by indwelling arterial catheter were treated with IV nicardipine. We measured change in mean arterial blood pressure (MAP), mean systolic and diastolic blood pressure, and mean heart rate (HR) from baseline after initiating treatment with IV nicardipine. The outcome measure was a reduction in MAP and mean systolic and diastolic blood pressure after treatment with IV nicardipine. During a 4-year period, 10 children met the study criteria. Median age was 3.25 months (range, 0.25 to 180 months). Initial median treatment dose of IV nicardipine was 1.0 micro g/kg/min (range, 0.5 to 6 micro g/kg/min); median dose used to control hypertension was 1.5 micro g/kg/min (range, 0.25 to 6 micro g/kg/min). Median duration of therapy was 26.3 h (range, 13 to 49 h). Treatment with IV nicardipine resulted in a 26.5% decrease in MAP from baseline during the first hour of treatment ( p = 0.0006). Mean systolic blood pressure decreased from 133 to 105 mmHg ( p = 0.005), and mean diastolic blood pressure decreased from 75 to 52.5 mmHg ( p = 0.001) during the first hour of therapy with nicardipine. There was a significant reduction ( p = 0.0005) in MAP during continued treatment with IV nicardipine. The mean HR of 150 remained unchanged during the first hour of therapy with nicardipine, and no significant change in mean HR or adverse effects was noted during continued therapy. Two children receiving other antihypertensive therapy demonstrated further reduction in their blood pressure when IV nicardipine was initiated. Tachycardia and hypotension were not observed in any child treated with IV nicardipine. We concluded that IV nicardipine reduced MAP with no significant change in mean HR and no adverse effects in patients with postcoarctectomy hypertension. Nicardipine produced a further reduction in MAP in children receiving other antihypertensive agents. Nicardipine is an effective agent for treatment of postcoarctectomy hypertension in children with coarctation of the aorta.

Antihypertensive Agents↗
PubMed1987

Nicardipine for systemic hypertension: effects on blood pressure and target organ function.

Nicardipine has been shown to lower blood pressure in patients with uncomplicated hypertension as well as in patients with concomitant renal impairment, coronary artery disease or congestive heart failure. The decrease in blood pressure induced by nicardipine is related to a concurrent decrease in total peripheral vascular resistance. The antihypertensive actions of nicardipine are maintained during long-term administration without the development of tachyphylaxis. In patients receiving diuretics or beta blockers, the addition of nicardipine has been shown to produce an additional decrease in blood pressure. The combined use of nicardipine and beta blockers may be beneficial in the treatment of hypertension: the increase in peripheral vascular resistance during beta blockade may be prevented by nicardipine-induced vasodilation; conversely, beta blockers may prevent reflex tachycardia and other consequences of peripheral vasodilatation. Although nicardipine may increase the heart rate acutely, tachycardia does not occur during long-term therapy. Preliminary data suggest that nicardipine exerts potent antihypertensive effects in patients with renal insufficiency without altering renal parameters. In patients with normal renal function, nicardipine has been shown to cause acute natriuresis and an increase in renal blood flow and glomerular filtration rate. Nicardipine also has a favorable effect on peripheral and cerebral blood flow. Like other dihydropyridines, nicardipine appears to have an antiatherogenetic effect in the experimental model. Short-term therapy with nicardipine does not affect serum lipid levels. Results from several studies suggest that nicardipine is an effective antihypertensive agent that can be used as monotherapy or in combination with other drugs such as beta blockers or diuretics.(ABSTRACT TRUNCATED AT 250 WORDS)

Aged↗
PubMed1985

Short- and long-term treatment of stable effort angina with nicardipine, a new calcium channel blocker: a double-blind, placebo-controlled, randomised, repeated cross-over study.

This study evaluated 1 year the efficacy of therapy with nicardipine in patients with chronic stable angina pectoris. Twenty-five male patients were entered. After a placebo run-in phase, the patients received nicardipine 30 mg, nicardipine 40 mg, and placebo, three times daily given in random, double-blind manner for 8 weeks. A double-blind, cross-over study comparing nicardipine with placebo was then undertaken. After 5 months of open treatment with nicardipine 90 or 120 mg day-1, patients received either placebo or nicardipine for 3 weeks, each followed by the alternative treatment for an additional 3 weeks and further open-label treatment with nicardipine for another 3-5 months. There were no significant changes in the PR, QRS or QT intervals, or in the QRS pattern during the short-term and long-term studies. There were no significant differences in mean heart rate after nicardipine compared with baseline. During treatment with nicardipine 120 mg day-1, patients reported significantly fewer anginal attacks compared with placebo, and nitroglycerin consumption also decreased. Nicardipine increased treadmill time, time to onset of angina, and time to one mm ST segment depression. These effects were maintained after 6 months of continued nicardipine therapy. Adverse effects were minor and well tolerated and included headache, dizziness, gastrointestinal upset, flushing paraesthesia and pedal oedema. Abrupt withdrawal of nicardipine at the end of the study resulted in a rapid return of the original symptoms but without further deterioration from the baseline measurements. Nicardipine was effective in the treatment of stable effort angina pectoris; this benefit was maintained for the entire year of treatment.

Adult↗
PubMed1992

Comparison of sustained-release formulations of nicardipine and verapamil for mild to moderate systemic hypertension.

In this double-blind, parallel, multicenter study, sustained-release (SR) preparations of 2 calcium antagonists, nicardipine and verapamil, were compared for the treatment of mild to moderate systemic hypertension. Two hundred eighteen patients with supine diastolic blood pressures (BP) 95 to 114 mm Hg were randomly assigned to receive nicardipine-SR 45 mg twice daily (n = 73), nicardipine-SR 60 mg twice daily (n = 73) or verapamil-SR 240 mg once daily in the morning (n = 72). All 3 regimens significantly reduced supine and sitting systolic and diastolic BPs compared with baseline values (p < 0.005). The efficacy of drugs became apparent after 2 weeks of therapy, and was sustained throughout the 12-week study. Reductions in sitting diastolic BP and supine and sitting systolic BPs were statistically greater with nicardipine-SR 60 mg twice daily compared with verapamil, and nicardipine-SR 45 mg twice daily was equivalent to verapamil. Asthenia and constipation occurred more frequently in patients treated with verapamil (9.7 and 11.1%, respectively, compared with 6.8 and 4.1% in either nicardipine group). Adverse events reported more frequently with nicardipine were headache (17.8% with nicardipine-SR 60 mg and 15.1% with nicardipine-SR 45 mg vs 13.9% with verapamil) and edema (15.1% in the nicardipine-SR 60 mg group, 8.2% with nicardipine-SR 45 mg vs 4.2% with verapamil). Verapamil, but not nicardipine, produced significant reductions in heart rate. SR preparations of calcium antagonists offer options for effective monotherapy of systemic hypertension. Side-effect profiles differ and may affect choice of therapy.

Delayed-Action Preparations↗
PubMed1988

Intravenous nicardipine for the treatment of severe hypertension.

PURPOSE: Severe hypertension responds to treatment with nifedipine given orally or sublingually. Nicardipine hydrochloride, a water soluble dihydropyridine analogue similar to nifedipine, has less of a negative ionotropic effect and produces less reflex tachycardia than nifedipine. Our purpose was to assess the antihypertensive efficacy and safety of intravenous nicardipine in a group of patients with severe hypertension (defined as a supine diastolic blood pressure of more than 120 mm Hg). PATIENTS AND METHODS: Eighteen patients with severe hypertension received treatment with intravenous nicardipine. Nicardipine titration was performed using doses of 4 to 15 mg/hour to achieve therapeutic goal (diastolic blood pressure 95 mm Hg or less or decrease in diastolic blood pressure of more than 25 mm Hg). After this therapeutic end-point was reached, patients received maintainance therapy with nicardipine for varying lengths of time: one hour (Group I), six hours (Group II), or 24 hours. When blood pressure control was lost, patients in Groups I and II entered a second maintenance period lasting a maximum of 24 hours. Onset and offset of action of nicardipine at various infusion rates and times of infusion were measured. RESULTS: Onset time to achieve therapeutic response was rapid at 15 mg/hour (0.31 +/- 0.13 hours) when compared with lower doses (1.11 +/- 0.36 hours at 4 mg/hour; 0.54 +/- 0.09 hours at 5 mg/hour; 0.52 +/- 0.09 hours at 7 to 7.5 mg/hour). Those who showed a therapeutic response received maintenance infusions with nicardipine for one (n = 7), six (n = 6), or 24 (n = 5) hours. Sustained blood pressure control at a constant rate of nicardipine infusion was seen in all patients during the maintenance period. After discontinuation of nicardipine, the time for offset of action (increase in diastolic blood pressure of 10 mm Hg or more) was independent of duration of infusion. Decreases in both systolic and diastolic pressures correlated well with plasma nicardipine levels. Heart rate increased by about 10 beats/minute, but this increase did not correlate with plasma nicardipine levels. Side effects were minimal, consisting of headache and flushing. In seven patients, local phlebitis developed at the site of infusion. This occurred after at least 14 hours of infusion at a single site, and the incidence can probably be reduced by shortening the infusion time at a single site. CONCLUSION: Nicardipine appears to be a safe and effective drug for intravenous use in the treatment of severe hypertension.

Adult↗
PubMed1999

Post-tetanic count and train-of-four responses during neuromuscular block produced by vecuronium and infusion of nicardipine.

We have examined onset and recovery of neuromuscular block produced by vecuronium using either post-tetanic count (PTC), or the first twitch of the train-of-four (TOF) (T1/T0) and TOF ratio (T4/T1) during continuous infusion of nicardipine. Sixty adult patients were allocated to one of four groups of 15 patients each: nicardipine-PTC, nicardipine-TOF, control-PTC and control-TOF. In the nicardipine-PTC and nicardipine-TOF groups, nicardipine 0.03 mg kg-1 was given before vecuronium 0.1 mg kg-1 and a continuous infusion of nicardipine was started immediately at a rate of 2 micrograms kg-1 min-1. Mean time from administration of vecuronium to onset of neuromuscular block in the nicardipine-PTC and nicardipine-TOF groups was significantly shorter than in the control-PTC and control-TOF groups (166 (SD 39) vs 220 (28) s; P < 0.05). There was no significant difference in recovery of PTC between the nicardipine-PTC and control-PTC groups or in recovery of TOF ratio in the nicardipine-TOF and control-TOF groups. However, during recovery, T1/T0 in the nicardipine-TOF group was significantly less than that in the control-TOF group, 60-100 min after administration of vecuronium.

Adult↗