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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The antihypertensive effect of nicardipine was evaluated in 89 ambulatory elderly patients with hypertension through a multicenter trial enrolling patients over the age of 65 years. After a baseline period during which they received placebo, subjects were randomized by an unbalanced assignment to a double-blind comparison of nicardipine (n = 57) and placebo (n = 32). The initial dose of nicardipine was 20 mg every 8 hours, which was then increased to 30 mg if needed. Blood pressure and heart rate were measured 1 and 8 hours after doses at each visit with subjects in both the supine and standing positions. Seventy-six per cent of patients who received nicardipine and 55% who received placebo responded (p less than 0.05). During standing, blood pressure did not decrease significantly from supine levels in either group, but a small, transient increase in heart rate occurred with nicardipine. Adverse reactions (apart from failure to respond) occurred in 8% of those who received nicardipine and 3% who received placebo. Three patients were withdrawn: two for symptoms, nausea, or flushing and one for transient and asymptomatic abnormalities on ECG. Nicardipine is effective and safe as monotherapy in elderly patients with hypertension, causing greater reduction in systolic than in diastolic pressure, but without orthostatic hypotension.
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PMID:Nicardipine monotherapy in ambulatory elderly patients with hypertension. 264 84

A double-blind, placebo-controlled clinical trial in France has studied the efficacy and safety of nicardipine in 31 elderly patients, aged 57 to 95 years (mean age 84 years), 16 of whom were actively treated with nicardipine, 10 to 30 mg three times a day (mean dose 69.4 mg/day). After 4 weeks, nicardipine lowered mean blood pressure (186/99 to 150/83 mm Hg; p less than 0.001), and the changes in systolic and diastolic blood pressure were significantly greater in the nicardipine group than in the placebo group. Nicardipine was well tolerated; orthostatic hypotension was not observed and there was no change in heart rate. Plasma renin activity (PRA) was measured in eight patients, but there was no correlation between PRA and the antihypertensive effect of nicardipine. Results of a pharmacokinetic study performed in 15 elderly patients showed a rapid rate of absorption and higher plasma levels than those observed in younger patients with hypertension (mean age 54 years). The results support those of the major French multicenter open study of 29, 104 elderly patients with hypertension (mean age 64 +/- 12 years) treated with nicardipine. The findings of this trial are reviewed and discussed, and recommendations made on the directions for future research in cardiovascular medicine with calcium channel blockers. Results of the trials discussed in this article show that nicardipine is an effective and well-tolerated drug in elderly patients and has wide-ranging effects on the cardiovascular system.
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PMID:Nicardipine in elderly patients with hypertension: a review of experience in France. 264 85

Nicardipine is an investigational dihydropyridine calcium channel blocking agent. One hundred fifty-one patients with hypertension received either 30 mg nicardipine t.i.d. or 25 mg hydrochlorothiazide b.i.d. in a double-blind, randomized, multicenter trial. After 4 weeks of therapy and at the end of the dosing interval, nicardipine reduced arterial pressure by 10/6 mm Hg and 12/6 mm Hg in the supine and standing positions, respectively (all p less than 0.01). In the hydrochlorothiazide group, the reductions were 12/6 mm Hg and 14/6 mm Hg, respectively (all p less than 0.01). The maximum reduction in blood pressure of 16/14 mm Hg supine and 20/15 mm Hg standing occurred within 1 hour after administration of nicardipine. The mean reduction in the hydrochlorothiazide group after 1 hour was 14/11 mm Hg supine and 16/12 mm Hg standing. Neither drug affected autonomic reflexes associated with maximum exercise. Nicardipine increased urinary sodium excretion during the 4-hour period after the first dose. Adverse effects of nicardipine were primarily extensions of its vasodilator effect and included flushing, headache, and edema.
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PMID:Nicardipine and hydrochlorothiazide in essential hypertension. 264

A new generation of dihydropyridine calcium antagonists which are related structurally to nifedipine is undergoing clinical investigation. Among these newer agents. nicardipine and nimodipine have become available for clinical use. In controlled trials, nicardipine is superior to placebo and equal to other antihypertensive agents for the treatment of systemic hypertension. Nicardipine is associated with a low incidence of adverse effects that are related primarily to its peripheral vasodilatory actions. In addition, nicardipine appears to have little if any negative effects on myocardial contractility or conduction.
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PMID:New therapeutic modalities in hypertension: focus on a new calcium antagonist-nicardipine. 266 49

The efficacy and safety of nicardipine were assessed in 29,104 hypertensive patients (mean age, 64 years) during a 90-day multicenter clinical trial. By treatment day 90, blood pressure was controlled in 60% of the patients taking nicardipine alone. The efficacy of nicardipine combined with another antihypertensive agent was examined in 6,479 of the patients. When nicardipine was added to their treatment regimen, blood pressure was controlled by day 90 in 63% of the patients taking beta-blockers, in 58% of those on diuretics, in 50% of those on angiotensin converting enzyme inhibitors, and in 49% of those taking centrally acting antihypertensive agents. Nicardipine was well tolerated; only 11% of the 29,104 patients discontinued treatment because of side effects. Most adverse reactions were transient and were related to vasodilation, and included peripheral edema in 7% of the patients, flushing in 7%, and headache in 4%. The results indicate that nicardipine is suitable as initial therapy in arterial hypertension.
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PMID:Efficacy and safety of nicardipine in 29,104 patients with hypertension. 267 15

Endothelin, an endothelium-derived vasoconstrictor peptide, and angiotensin II were intravenously injected into the femoral vein of normotensive Wistar-Kyoto (WKY) rats that had been anesthetized with urethane. Blood pressure and heart rate were recorded from a cannula inserted into the carotid artery. All experiments were carried out after treatment with adrenergic and cholinergic antagonists. Endothelin showed a potent, dose-dependent pressor action. The dose-response relations for the increase in blood pressure of rats receiving endothelin were comparable with those of rats receiving angiotensin II. However, endothelin showed far more long-lasting effects. Endothelin-induced responses consisted of three phases: a rapid and transient depressor phase and then two phases of pressor (transient and long-lasting) response. Nicardipine (0.1 mg/kg), a dihydropyridine Ca2+ channel blocker, markedly attenuated the slow phase of the pressor response but only slightly attenuated the rapid one. The pressor action of endothelin was not inhibited by continuous infusions of saralasin, which almost abolished the angiotensin II-induced pressor response. Endothelin-induced pressor response was also not attenuated by indomethacin, a prostaglandin synthesis inhibitor. These data provide evidence that endothelin produces a unique, potent, and long-lasting pressor response, which appears to be in part related to the activation of Ca2+ channels. In 12-week-old spontaneously hypertensive rats (SHR), the maximal pressor response to endothelin was slightly but significantly greater than that in age-matched WKY rats, but the dose dependency of the response was approximately consistent with that in WKY rats.(ABSTRACT TRUNCATED AT 250 WORDS)
Hypertension 1989 Oct
PMID:Characteristics of pressor response to endothelin in spontaneously hypertensive and Wistar-Kyoto rats. 267 62

1. A novel formulation of nicardipine (50% standard (short acting), 50% sustained release) was evaluated in mild hypertension in a double-blind, randomized, placebo-controlled study, using clinic measurements (Hawksley) augmented by home recorded blood pressures (Copal UA 251). 2. Nicardipine 60 mg twice daily for 28 days produced a highly significant reduction in sitting blood pressure compared with placebo both pre dose (mean difference 17/8 mm Hg) and 2 h post dose (mean difference 34/26 mm Hg). 3. Home recordings confirmed the hypotensive effect and also revealed a consistent 'peak' effect between 2-4 h after dosing (mean difference 32/22) mm Hg). 4. Doppler aortovelography at 2 h post-dose showed a significant increase in in stroke and minute distance (linear analogues of stroke volume and cardiac output respectively) compared with placebo. The increase in stroke distance was linearly related to change in plasma concentration of nicardipine. 5. Of the 14 patients enrolled in the study, nine experienced troublesome adverse effects on nicardipine (headaches, facial flushing, palpitations, ankle oedema) and two of these were unable to complete the study as a result. 6. This formulation of nicardipine, in the fixed dosage used in this study, is characterized by an effective antihypertensive action but also by an unacceptable adverse effect profile, presumably due to an excess of its 'short acting' component.
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PMID:Evaluation of a long acting formulation of nicardipine in hypertension by clinic and home recorded blood pressures and Doppler aortovelography. 275 80

Nicardipine, a calcium antagonist of the 1:4 dihydropyridine type, has been used to treat angina and hypertension and is currently being examined as an agent for treating ischemia of cerebral and myocardial tissue. Nicardipine shows high affinity for the dihydropyridine binding site (pKi = 9.7) and inhibits the L-type calcium ion channel as demonstrated by its ability to decrease the calcium ion-dependent action potential dose-dependently in ventricular papillary muscle (pIC50 = 7.15). Nicardipine shows greater potency in inhibiting the response of vascular smooth muscle (pIC50 = 8.20) than that of cardiac muscle (pIC50 = 7.15). The nicardipine selectivity for vascular smooth muscle is greater than that shown by other dihydropyridine calcium antagonists such as nifedipine and accounts for the efficacy of nicardipine in the treatment of angina and hypertension. Various mechanisms have been proposed to account for the beneficial action of nicardipine in treating animal models of cerebral ischemia and myocardial infarction. For example, it has been suggested that (1) nicardipine has a specific membrane-stabilizing effect on cell membranes, (2) the compound blocks certain sodium channels, (3) it may become concentrated in ischemic cells, or (4) it may stimulate calcium ion efflux from mitochondria, and these actions may account for the inhibition by nicardipine of veratrine-induced contraction of myocytes. In this study, some of these effects of nicardipine were examined. However, the suggestion that nicardipine concentrates in ischemic cells owing to the tertiary amine structure could not be conclusively demonstrated.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Cellular action of nicardipine. 280 73

Calcium channel blockers such as nicardipine act as arterial vasodilators and are effective in the treatment of hypertension. Although they are also effective tocolytic agents, fetal effects have not been fully studied. Fifteen chronically catheterized near-term ewes were studied. Maternal and fetal cardiorespiratory parameters were measured in the control period and again 15 minutes after maternal venous infusion of angiotensin II. Nicardipine 20 micrograms/kg/min was given over 2 minutes and maternal and fetal cardiorespiratory parameters and fetal blood flow were measured 5.30 and 60 minutes later. Nicardipine reversed maternal hypertension and produced transient tachycardia. Fetuses responded initially with transient bradycardia and then developed hypercapnia and acidemia (p less than 0.03) by 60 minutes after nicardipine. Fetal placental blood flow decreased and vascular resistance increased by 5 minutes after nicardipine but returned toward control values after 30 minutes. Unexpectedly we observed the death of five fetuses by 65 minutes after nicardipine. We conclude that the administration of nicardipine in the hypertensive ewe results in significant alterations of fetal cardiorespiratory status and placental function that may lead to acidemia.
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PMID:Fetal vascular responses to maternal nicardipine administration in the hypertensive ewe. 280 19

Calcium channel blockers are arterial vasodilators effective in the treatment of hypertension. Therefore nicardipine, a dihydropyridine calcium channel blocker, should modulate angiotensin II-induced vasoconstriction. Regional blood flows were measured with radioactive microspheres in five chronically catheterized near-term ewes both before and 15 minutes after maternal infusion of angiotensin II at 5 micrograms/min. Nicardipine was then administered intravenously at 20 micrograms/kg/min over 2 minutes while the angiotensin II infusion was maintained. Blood flows were measured after 5 minutes. Maternal blood pressure levels were increased by angiotensin II from 83 +/- 4 mm Hg to 114 +/- 5 mm Hg, and were decreased to 70 +/- 4 mm Hg by nicardipine (p less than 0.05). Nicardipine also reversed angiotensin II-induced vasoconstriction in the renal and endomyometrial vascular beds (p less than 0.05). Unexpectedly, however, nicardipine worsened placental vasoconstriction caused by angiotensin II, as placental blood flow fell from 242 +/- 32 ml.min-1.kg-1 fetal weight to 128 +/- 7 ml.min-1.kg-1 fetal weight (p less than 0.05), and placental resistance increased from 0.48 +/- 0.04 mm Hg.ml-1.min.kg-1 fetal weight to 0.55 +/- 0.05 mm Hg.ml-1.min.kg-1 fetal weight (p less than 0.05). Nicardipine reverses angiotensin II-induced vasoconstriction systemically and in the kidney and uterus of the pregnant ewe, but does not reverse placental vasoconstriction and may significantly alter fetal cardiorespiratory status.
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PMID:Placental vascular responses to nicardipine in the hypertensive ewe. 280 20


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