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

Fourteen patients with vascular disease were studied to evaluate the efficacy of nicardipine hydrochloride as a hypotensive agent in the treatment of acute hypertension occurring during anaesthesia. Five patients received a bolus injection of nicardipine hydrochloride 0.5 mg. Another nine patients received bolus injections of nicardipine 1 and 2 mg. Nicardipine 0.5 mg significantly decreased systemic arterial pressure (by about 24%), systemic vascular resistance (SVR), left ventricular stroke work index (LVSWI) and rate-pressure product (RPP). Nicardipine 1 or 2 mg had twice the effect in decreasing arterial pressure as did 0.5 mg, without significant change in heart rate or right and left ventricular filling pressures. Cardiac index and stroke volume index increased and SVR, pulmonary vascular resistance, LVSWI and RPP decreased significantly.
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PMID:Haemodynamic effects of nicardipine hydrochloride. Studies during its use to control acute hypertension in anaesthetized patients. 646 25

Nicardipine, a new calcium antagonist, was given to an insulin-treated diabetic patient with severe hypertension that had resisted ordinary antihypertensive treatment. After substitution of treatment with nicardipine, his blood pressure decreased from 210/110 to 142/76 mmHg. Despite this significant decrease in blood pressure, the patient's renal blood flow, as estimated by endogenous creatinine clearance, increased. His daily requirement of insulin and his degree of proteinuria remained unchanged by the use of nicardipine.
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PMID:Effect of nicardipine in a hypertensive patient with diabetes mellitus. 647 68

Nicardipine is the first intravenously administered dihydropyridine calcium channel blocker. Its primary physiological actions include vasodilatation with limited effects on the inotropic and dromotropic function of the myocardium. Several reports have documented its use in adult patients for pharmacological control of blood pressure. We present our experience with the perioperative use of nicardipine in children to treat intraoperative hypertension, as an agent for controlled hypotension during spinal fusion and LeFort I maxillary osteotomies and to treat postoperative hypertension. Dosing regimens and possible applications in paediatric anaesthesia are discussed.
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PMID:Nicardipine: perioperative applications in children. 748 37

The positive inotropic agents, including beta-adrenergic receptor agonists and PDE III inhibitors, are reviewed to explain their mechanisms of action, pharmacology, and clinical usage. New cardiotonic drugs, such as dopexamine and dobutamine (beta-adrenergic receptor agonists) and amrinone, milrinone, and enoximone (PDE III inhibitors), have important roles for the treatment of perioperative acute heart failure or acute deterioration of congestive heart failure. PDE III inhibitors have important roles as effective inodilator agents, and understanding their actions, pharmacology, and appropriate usage is important. Nicardipine, the first dihydropyridine calcium-channel blocker available for intravenous use, represents an arterial-specific vasodilator that offers an important therapeutic approach to treat perioperative hypertension.
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PMID:New cardiac drugs. 763 56

Nicardipine is a second generation dihydropyridine-type Ca2+ antagonist with high vascular selectivity and strong cerebral and coronary vasodilatory activity. The compound is used in the treatment of hypertension, primarily in the elderly. In this review the main evidence of the cerebrovascular activity of nicardipine in preclinical studies using in vitro and in vivo models is detailed. A particular physico-chemical property of nicardipine is the almost complete protonation in acid environment. This allows its accumulation in ischemic brain regions and makes it a candidate for the treatment of cerebrovascular disorders characterised by impaired brain perfusion. The main clinical data on the use of nicardipine in cerebral ischemia and related disorders, subarachnoid haemorrhage and stroke, are also reviewed. These studies included 5940 patients affected by chronic cerebrovascular insufficiency (cerebral ischemia, cerebral atherosclerosis mainly associated with hypertension, transient ischemic attacks, sequelae of cerebral infarction, thrombosis or embolia, hypertensive encephalopathy), 1540 patients affected by sequelae of subarachnoid haemorrhage and 206 patients affected by stroke. Both preclinical studies and clinical trials have shown that nicardipine is a safe Ca2+ antagonist with powerful cerebrovascular activity. This suggests its possible use in cerebrovascular disorders in which blockade of Ca2+ channels of the L-type and/or selective cerebral vasodilatation is desirable. Further studies are necessary to establish if modulation of neuronal Ca2+ channels of the L-type by nicardipine may have a neuroprotective effect independent by the cerebrovascular activity of the compound.
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PMID:Nicardipine and treatment of cerebrovascular diseases with particular reference to hypertension-related disorders. 765 45

Calcium metabolism appears to be altered in human and experimental hypertension, which represents an important risk factor for thrombotic events. We investigated the possible effect of the calcium antagonist nicardipine on a model of experimental venous thrombosis in spontaneously hypertensive rats (SHR). Thrombus formation was highly enhanced in SHR with respect to normotensive Wistar Kyoto rats (WKY). Nicardipine, when administered orally (10 mg kg-1) at a single dose or once a day for three days, completely counteracted the increase in thrombus size caused by hypertension. Furthermore, a significant rise in prostacyclin production from aortic tissue [19.2 +/- 1.5 vs 13.2 +/- 2.4 ng (mg dry tissue)-1], associated with a fall in thromboxane A2 release from activated platelets (328.3 +/- 74.6 vs 705.0 +/- 88.1 ng ml-1), was observed in nicardipine-treated SHR. Plasma triglyceride and free fatty acid levels were also lowered by drug administration. Our results suggest that the actions of nicardipine on calcium metabolism result in antithrombotic effect through an increased availability of vasodilating eicosanoids in vessel walls and through a reduced amount of prothrombotic agents (thromboxane, free fatty acids).
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PMID:Antithrombotic activity of nicardipine in spontaneously hypertensive rats. 786 21

Concern over negative inotropic effects has limited the use of calcium blockers in patients with congestive heart failure. Nicardipine, a second generation dihydropyridine calcium channel blocker, has demonstrated positive hemodynamic effects in short-term therapy in patients with congestive heart failure. Prolonged use of calcium channel blockers remains contraindicated in patients with congestive heart failure due to the potential for activation of the renin-angiotensin system. However, acute intravenous nicardipine administration has important clinical applications (as in the management of surgical hypertension or hypertensive emergencies). Nicardipine may be safely used for these indications even in the presence of congestive heart failure.
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PMID:Nicardipine in heart failure: distinguishing its acute beneficial from its chronic effects. 812 55

Today calcium antagonists (Ca-antagonists) are widely used agents in the management of various diseases of the circulatory system. More than 20 years ago the Ca-antagonists of the so-called 1st generation (Verapamil, Diltiazem, Nifedipine) were introduced for treatment of angina pectoris and later of essential hypertension. In the last decade an increasing number of agents structurally related to dihydropyridines were developed for the treatment of hypertension and/or coronary heart disease or cerebral disorders; the main target was to reduce side effects and to guarantee once or at least twice daily administration. Therefore the Ca-antagonists of the so-called 2nd generation (e.g. Amlodipine, Felodipine, Isradipine, Nitrendipine, Nicardipine, Nimodipine, Nisoldipine) tend to longer elimination-half-lives; Amlodipin is an exception with an elimination-half-life of 30 hours on the average. Apart from elimination rates, however, the biopharmaceutical and pharmacokinetic characteristics of all Ca-antagonists are similar: they are highly cleared drugs and are relatively highly protein bound. As they are subject to significant hepatic first-pass-metabolism old age and hepatic disease will increase their plasma-concentrations. Renal impairment affects little their pharmacokinetics since the fraction eliminated unchanged by the kidneys is small. For most agents, plasma-concentration-response relationships have been described. With exception of nicardipine a linear pharmacokinetic in all Ca-antagonists was demonstrated. Drugs and food affecting hepatic blood flow and drug metabolising capacity have predictable interaction potential. With regard to the acute pharmacodynamic effects the Ca-antagonists show similar qualitative effects, though there are quantitative differences. Orally administered dihydropyridine-derivatives induce acute hypotensive effects, whereas the other compounds show clinically relevant hypotensive effects only when administered chronically per os or less pronounced when given as intravenous infusion.
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PMID:[Principles of the pharmacokinetics and pharmacodynamics of calcium antagonists]. 813 31

Fourteen hypertensive patients hospitalized in a paediatric intensive care unit were studied to evaluate safety and hypotensive efficacy of intravenous nicardipine. Systolic and diastolic blood pressure significantly decreased 1 h after the beginning of the treatment (1 microgram/kg per minute). Mean decrease in systolic blood pressure during the first 24 h was between 9.9% and 13.4% of the initial value. Mean lowering of diastolic blood pressure was between 16.7% and 25.6%. Nicardipine did not significantly affect heart rate with dose of 1 microgram/kg per minute. No clinical side-effects were observed. Nicardipine could be a first line drug for the treatment of hypertension in paediatric intensive care units.
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PMID:Intravenous nicardipine in hypertensive children. 822 97

Thirty-six patients (17 males and 19 females), aged between 40 and 70 years old (mean age 55.9), suffering from slight or moderate arterial hypertension, were monitored for four weeks after 14 days of placebo treatment. In a double-blind and random study 24 patients were treated with Nicardipine Retard (40 mg twice a day) whereas a further 12 received placebo twice a day. Sphigomanometric controls carried out after two and four weeks showed a significant reduction in arterial pressure only in those patients receiving active treatment. 24-hour out-patient monitoring of arterial pressure, carried out using Spacelabs 5300, showed a reduction in both systolic and diastolic arterial pressure throughout the day in subjects treated with calcium-antagonists compared to the placebo group. The normal physiological 24-hour trend of arterial pressure was always taken into account. The pressure response to a cold pressor test, mental arithmetic test, isometric and dynamic effort tests, measuring using a cycloergometer, was not modified by anti-hypertensive treatment, thus confirming the preservation of normal physiological behaviour during daily activities. There was no significant change in heart rate and the drug was well tolerated.
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PMID:[Antihypertensive action of nicardipine retard in 24 hours and its effect on stress]. 824 8


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