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

We evaluated the effect of nicardipine, a calcium channel blocker, on somatosensory evoked potentials (SEP) in 26 patients with acute cerebral infarction. Post treatment, 58% (15/26) of the N20 and P25 latencies were prolonged in the affected hemispheres; 8% (2/26) were shortened; and 35% (9/26) did not change. The mean N20 and P25 latencies were significantly prolonged two hours post treatment in the affected hemisphere (N20, P less than 0.01, P25 P less than 0.01). Nicardipine (Ni) had no effect on SEP components in the intact hemispheres. Seventy five per cent of the 12 patients with hypertension had a decrease in blood pressure (BP) after taking nicardipine, but there were no undesirable side effects or worsening of neurological signs. Our study demonstrates that nicardipine prolongs the latencies of short-latency components of SEP in the affected hemisphere after acute ischaemic stroke and also decreases BP. These observations suggest that nicardipine therapy might impair neuronal function in the ischaemic zone.
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PMID:Effect of nicardipine on somatosensory evoked potentials in patients with acute cerebral infarction. 226 63

Nicardipine is an investigational dihydropyridine calcium-channel blocker. In the present study, 21 patients with severe hypertension were treated with oral nicardipine, alone or in combination with beta-blockers and diuretics for 4-5 weeks, following initial control of their blood pressure with intravenous nicardipine. Each of the 21 patients had a satisfactory response to intravenous nicardipine which was administered as an infusion following initial blood pressure lowering. At 1 h prior to discontinuation of the intravenous treatment, oral nicardipine therapy was begun as a 40 mg dose. Oral nicardipine, 40 mg t.i.d., was continued for the remainder of hospitalization and for a 4-5-week outpatient follow-up period. The dose of oral nicardipine was downtitrated and additional antihypertensive drugs, beta-adrenergic blocking agents and/or diuretics, were added to maintain blood pressure in an acceptable range. Compared to baseline, mean supine systolic blood pressure was lowered significantly (p less than 0.001) by 57 mmHg at the end of intravenous maintenance and by 50 mmHg at the end of oral treatment. Likewise, significant (p less than 0.001) decreases in diastolic blood pressure of 43 and 32 mmHg, respectively, were observed for the same time periods. At the end of oral treatment, 6 patients remained on nicardipine monotherapy, 8 patients were on two-drug therapy and 7 patients required three-drug therapy. Side-effects were mild except for a moderate headache reported in one patient during intravenous treatment. From these observations we conclude that oral nicardipine is a useful new agent for initial, single treatment of chronic severe hypertension, although a significant number of patients eventually need additional antihypertensive therapy.
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PMID:Nicardipine in severe hypertension: oral therapy following intravenous treatment. 230 9

Cytosolic free calcium concentration ([Ca2+]i) and muscle tension were simultaneously measured in aortic tissue isolated from spontaneously hypertensive rats (SHR), normotensive Wistar-Kyoto (WKY) rats, and SHR chronically treated with a novel angiotensin converting enzyme inhibitor, CS-622. In the presence of 2.5 mM Ca2+ in the bathing solution, aortic [Ca2+]i measured with fura-2 was higher in SHR than in WKY rats, and it was almost the same in CS-622-treated SHR and untreated WKY rats. Increase of external Ca2+ concentration from zero to 2.5 mM elicited a contraction in SHR aortas but not in aortas from both CS-622-treated SHR and untreated WKY rats. When the aortas were contracted by 60 mM K+, however, [Ca2+]i as well as developed tension was similar in the three groups. CGP-28392 (10(-6) M), a Ca2+ channel activator, induced a rhythmic activity superimposed on a gradual increase of [Ca2+]i and tension in SHR aortas but not in the aortas of CS-622-treated SHR or untreated WKY rats. Nicardipine (10(-7) M) decreased the resting [Ca2+]i and the resting tone in SHR aortas, but not in WKY rat aortas. These results suggest that SHR aortas have a higher myogenic tone due to increased [Ca2+]i than WKY rat aortas and that the increased [Ca2+]i is attributed to alterations of dihydropyridine-sensitive Ca2+ channels in SHR aortas. Further, the decrease of the vascular tone induced by long-term administration of the angiotensin converting enzyme inhibitor may be due to a reduction of increased [Ca2+]i in SHR.
Hypertension 1990 Sep
PMID:Cytosolic free calcium of aorta in hypertensive rats. Chronic inhibition of angiotensin converting enzyme. 239 84

Nicardipine hydrochloride, a dihydropyridine calcium entry-blocking drug, was administered to 66 patients with severe hypertension during three protocols designed to examine the efficacy and safety of this investigation drug. It was shown that nicardipine was uniformly effective in lowering blood pressure to a therapeutic goal of 95 mm Hg. Time to achieve therapeutic effect was dose dependent, and steady-state blood levels were achieved after 8 to 12 hours. Reductions in both systolic and diastolic blood pressure but not changes in heart rate were correlated with plasma concentrations of nicardipine. In dose-ranging studies, the minimal effective dose of nicardipine appeared to be 2 mg/hr; 1 mg/hr was an ineffective dose, and little additional effect was seen above 4 mg/hr. Side effects were modest and consisted of those associated with vasodilation--headache, flushing, and feelings of warmth. In the initial group of patients studied, local thrombophlebitis occurred in a substantial number of patients. This was seen only after 14 hours of infusion. In subsequent studies, the infusion site was changed after 12 hours, and no further cases of thrombophlebitis were seen. Nicardipine appears to be therapeutic agent for parenteral use that shows promise in the treatment of severe hypertension.
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PMID:Intravenous nicardipine hydrochloride: treatment of patients with severe hypertension. 240 13

The incidence of postoperative hypertension after both cardiac and noncardiac surgery is a major concern. alpha-Adrenergic-blocking drugs, such as phentolamine, and direct-acting vasodilators, such as nitroglycerin and nitroprusside, are commonly used to treat hypertension. Nifedipine, a calcium channel blocker, may also be used, but because no intravenous preparation is available, its effects are not titratable. A new short-acting calcium channel blocker, nicardipine, is a potent vasodilator and produces more selective responses in the coronary versus the systemic vascular circulation. It is an effective cerebral vasodilator, increasing cerebral blood flow and oxygen delivery. Nicardipine can be administered as an intravenous loading infusion of 10 to 15 mg/hr for 25 minutes, followed by a maintenance infusion of 3 to 5 mg/hr. Nicardipine has a short duration factor, is easily titratable and is as effective as nitroglycerin or nitroprusside in the control of hypertension. In summary, nicardipine has many properties of an ideal drug for the treatment of postoperative hypertension.
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PMID:Clinical considerations for the use of intravenous nicardipine in the treatment of postoperative hypertension. 240 14

Nicardipine, a new calcium antagonist, was tested in a 14-week double-blind trial including 15 outpatients with uncomplicated essential hypertension. They were randomly assigned to nicardipine (20-30 mg three times daily) or placebo as first-step treatment. When necessary but always after a minimum of 4 weeks, pindolol (15 mg/day) was combined with nicardipine or placebo. At the end of step 1 (85 +/- 6 days with nicardipine vs. 58 +/- 6 days with placebo, p less than 0.01), nicardipine induced larger drops in supine systolic and diastolic blood pressure (SBP and DBP) than the placebo (21 +/- 2.5 vs 1.4 +/- 3 mm Hg, p less than 0.001, and 13 +/- 2 vs. 3.5 +/- 1.5 mm Hg, p less than 0.001, respectively). In the nicardipine group (n = 57), 53% of patients had controlled blood pressure (SBP less than 160 mm Hg and DBP less than 95 mm Hg) versus 17% in the placebo group (n = 47), p less than 0.001. There was no significant correlation between the decrease in blood pressure and the age of patients. The most common side effects in the nicardipine group were flushes (12%), headache (8%), ankle edema (5%), and asthenia (4%). When blood pressure was not brought under control and pindolol was prescribed as the second-step treatment, the nicardipine group (n = 52) displayed larger drops in SBP and DBP than the placebo group (n = 40) (27 +/- 5 vs. 15 +/- 3 mm Hg, p less than 0.01, and 18 +/- 1 vs. 9 +/- 2 mm Hg, p less than 0.001, respectively). These results show that a calcium antagonist is useful for first-step treatment of hypertension.
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PMID:First-step treatment of mild to moderate uncomplicated essential hypertension by a new calcium antagonist: nicardipine. 241 2

Nicardipine has high affinity for the dihydropyridine-binding site and has been shown to inhibit the influx of extracellular calcium through membrane slow channels. The calcium antagonist activity of nicardipine is greater in vascular smooth muscle than in cardiac muscle. Nicardipine has also been shown to possess greater activity in coronary than in peripheral vascular smooth muscle. This in vitro profile accounts for the decreased blood pressure and increased coronary blood flow in animal models in vivo. These pharmacologic properties are the basis for nicardipine's clinical utility in essential hypertension and acute myocardial ischemia. Nicardipine has been shown to be more vascular selective than other calcium antagonists and, therefore, possibly less inclined to produce negative inotropicity. This latter property has been confirmed in human hemodynamic studies. Nicardipine is effective in models of acute myocardial ischemia and hypertension. These results have been confirmed in antianginal and antihypertensive studies in humans. This new calcium antagonist has been shown to limit myocardial infarct size in both dogs and baboons subject to left anterior descending coronary artery ligation and to reduce the extent of ischemia-induced cerebral neuronal death in rats. Other protective effects of nicardipine have been demonstrated in paracetamol overdose in mice, chloroform-induced hepatotoxicity in rats and cerebral ischemia in gerbils and baboons. The mechanism of this cell protection of nicardipine may be related to physicochemical effects.
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PMID:Animal pharmacology of nicardipine and its clinical relevance. 244 Feb 94

Intracerebroventricular (i.c.v.) injection of the 1,4-dihydropyridine (DHP) calcium channel agonist, Bay K8644 (30 micrograms/kg) increased mean blood pressure and the K+-evoked release of [3H]acetylcholine ([3H]ACh) from hippocampal slices in spontaneously hypertensive rats (SHR). The Bay K8644-induced hypertension was inhibited by a pretreatment with methylatropine (80 micrograms/kg i.c.v.). In SHR, nicardipine, a DHP calcium channel antagonist, reduced mean blood pressure when i.c.v. injected (10 micrograms/kg). The nicardipine-induced hypotension was reduced by a pretreatment with hemicholinium-3 (20 micrograms, i.c.v.). Nicardipine (1 microM) did not modify, in SHR, the K+-evoked release of [3H]ACh, but inhibited the Bay K8644-induced increase in the ACh release. In normotensive rats, neither Bay K8644 nor nicardipine modify blood pressure, when centrally injected, or the stimulated release of [3H]ACh from hippocampal slices. The participation of central DHP sites in the cholinergic transmission in genetic hypertension is discussed.
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PMID:Central interactions between dihydropyridines and cholinergic systems in the control of blood pressure in rat. 244 12

Renal effects of CV-4093, a newly developed dihydropyridine calcium channel blocker, were examined using anesthetized stroke-prone spontaneously hypertensive rats, and the findings were compared with those of nicardipine. An intravenous injection of CV-4093 (2 micrograms/kg) produced long-lasting hypotension with a slow-onset accompanied by moderate renal vasodilation. There were no appreciable alterations in glomerular filtration rate (GFR) and urine formation, except that urine flow (UF) increased significantly during the first 10 min after injection. When CV-4093 was administered at 10 micrograms/kg, the hypotensive action was markedly augmented. Eighty minutes after the injection, a decrease in mean arterial pressure of about 45 mmHg was observed. Simultaneously, renal blood flow increased significantly from the control value of 5.76 +/- 0.46 ml/g.min to 6.94 +/- 0.28 ml/g.min. Renal vascular resistance decreased immediately after the injection, and the response lasted for over 3 hr, thereby indicating the marked and sustained renal vasodilating effect of CV-4093. GFR was constant throughout the experiment, but UF and urinary excretion of sodium were increased significantly. Fractional excretion of sodium was also elevated, thereby suggesting an inhibitory action of CV-4093 on renal tubular reabsorption of sodium. Nicardipine at a dose of 10 micrograms/kg, a dose producing an effective hypotensive action, caused no significant increases in RBF and urine formation. The renal vasodilating and diuretic actions of CV-4093 may provide a beneficial effect in the treatment of hypertension.
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PMID:Effects of CV-4093, a new dihydropyridine calcium channel blocker, on renal hemodynamics and function in stroke-prone spontaneously hypertensive rats (SHRSP). 259 83

The effects of monotherapy with nicardipine, 20 mg three times a day, have been investigated in a 1-year study of 26 elderly (greater than 60 years) patients with hypertension with various types of renal dysfunction and seven without renal dysfunction. Parameters measured included blood pressure, blood chemistry (serum creatinine, uric acid, blood urea nitrogen, blood glucose total cholesterol, and electrolytes), plasma renin activity, and plasma aldosterone concentration. Nicardipine was effective in reducing blood pressure in all patients with diabetic nephropathy, parenchymal renal diseases, or hypertensive nephropathy, and in those without renal dysfunction. Serum creatinine and blood urea nitrogen levels were slightly elevated in some patients whose pretreatment serum creatinine level was greater than 2 mg/dl, regardless of the type of nephropathy. However, it was not determined whether this effect was the result of a reduction in blood pressure induced by nicardipine. Serum sodium, potassium, total cholesterol, and blood glucose levels were unchanged by the administration of nicardipine. Changes in plasma renin activity and aldosterone levels were not significant. These results suggest that nicardipine can be used safely in elderly patients with hypertension with renal dysfunction, regardless of the type of nephropathy.
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PMID:Effects of nicardipine on blood pressure and renal function in elderly hypertensive patients with renal dysfunction. 264 83


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