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

Diuretics and calcium blockers are particularly effective in the treatment of hypertension in Blacks, who, characteristically, have low-renin hypertension. The efficacy and tolerable of lacidipine (a calcium) blocker of the dihydropyridine class) and hydrochlorothiazide (a diuretic) were compared in a 12 week double-blind randomised parallel group study of Nigerians with essential hypertension. Lacidipine was given at a starting dose of 4 mg daily by mouth and increased to 6 mg if there was no satisfactory response at 4 weeks, and hydrochlorothiazide was stared at 25 mg daily by mouth and increased to 50 mg if necessary. Twenty-four patients (8 male) in the lacidipine group and 17 (5 male) in the hydrochlorothiazide group were evaluable at the end of the trial. In the lacidipine group, SBP was significantly reduced from 157 +/- 14 mmHg to 146 +/- 24 mmHg (P < 0.00001) and DBP from 90 +/- 9 mmHG to 87 +/- 15 mmHg (P < 0.00001) with BP normalisation rates of 67% and 79% at 4 weeks and 12 weeks, respectively. In the hydrochlorothiazide group, SBP was significantly reduced from 16.4 +/- 19 mmHg to 141 +/- 17 mmHg (P < 0.00001) and DBP from 102 +/- 6 mmHG to 89 +/- 7 mmHg (P < 0.00001) with normalisation rates of 77% and 82% at 4 weeks and 12 weeks respectively. The groups did not differ in BP reduction nor normalisation rates. There were no reported side effects.
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PMID:Evaluation of lacidipine (a calcium blocker) in the treatment of hypertension in black African people: a double-blind comparison with hydrochlorothiazide. 1045 35

The aim of this study was to investigate the therapeutic effectiveness of lacidipine in stroke-prone spontaneously hypertensive rat (SHRSP) with cerebrovascular lesions in comparison with nicardipine. SHRSP were fed 1% saline as drinking water. After the onset of stroke, saline was replaced with water and each drug was administered orally once a day for 3 weeks. In the drug-untreated group, recurrence of stroke was repeated, deterioration and amelioration of neurological deficits (ND) were repeated, and histological examination and measurement of regional blood flow (rBF) using nonradioactive colored microspheres performed at the end of treatment revealed severe damages and significantly decreased rBF in brain and kidney, respectively. In kidney, not only lacidipine (1 mg/kg) but also nicardipine (30 mg/kg) decreased vascular lesions and ameliorated low-rBF significantly. Both drugs also inhibited the recurrence of stroke completely even at a low dose that did not ameliorate severe hypertension. Neuronal damages and ND in each lacidipine-treated group were ameliorated significantly, whereas those in each nicardipine-treated group were slightly improved. Lacidipine at 1 mg/kg alone ameliorated the cerebral low-rBF significantly even at 24 hr after administration. These results suggest that a long-lasting improvement of low-rBF after stroke may be useful in the treatment of SHRSP with cerebrovascular lesions.
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PMID:Therapeutic effects of a calcium antagonist, lacidipine, on stroke-prone spontaneously hypertensive rats with cerebrovascular lesions. 1046 64

Calcium antagonists are uniquely suitable for managing hypertension by virtue of their efficacy, metabolic neutrality and their ability to countervail counterregulatory adaptive changes, thereby enhancing blood pressure lowering. Recent evidence has accrued underscoring the concept that calcium antagonists are heterogeneous and consist of chemically dissimilar agents. The difference in formulations and pharmacokinetics affect clinical events including the effect on blood pressure, heart rate and the degree with which sympathetic activity is activated. Lacidipine is a new calcium antagonist that is the prototype of the lipophilic dihydropyridines. Of great importance, lacidipine has a slow onset of vasodilator/antihypertensive effect and does not promote an excessive sympathetic drive. These attributes commend its selection as an antihypertensive agent.
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PMID:Role of a third generation calcium antagonist in the management of hypertension. 1052 76

An increasing amount of data suggests that systolic blood pressure (SBP) and pulse pressure (PP) may more closely relate to and thus favour the atherogenic process than does diastolic blood pressure (DBP). The baseline data from the ongoing European Lacidipine Study on Atherosclerosis (ELSA) recently indicated that carotid artery atherosclerosis in normocholesterolaemic patients with mild or moderate essential hypertension is more closely related to SBP and more so PP than to DBP and lipid variables. Other new data point to the effects of hypertension on arterial compliance, as well as the effects of 24-h blood pressure variability on arterial compliance and distensibility. When viewed in their entirety, these data present a compelling case for the closer monitoring of SBP and PP with respect to arterial compliance, and the need for aggressive blood pressure treatment to control and perhaps reverse the underlying pathological changes in arterial structure and function in hypertensive patients.
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PMID:Systolic blood pressure and pulse pressure: role of 24-h mean values and variability in the determination of organ damage. 1070 28

This is an open trial investigating the efficacy and metabolic effects of 3 months' treatment with lacidipine in 25 Nigerian Africans with mild to moderate hypertension. There was a significant fall in sitting diastolic blood pressure, with treatment (p = 0.01). There were no significant weight changes. The heart rate initially rose significantly with the drug but this normalised with time. All biochemical and haematological indices remained essentially unchanged during therapy. Lacidipine therefore proved an efficacious and metabolically neutral antihypertensive in mild to moderate hypertension in Africa.
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PMID:Lacidipine in the treatment of hypertension in black African people: antihypertensive, biochemical and haematological effects. 1119 Oct 8

Endothelium-dependent vasorelaxation is defective in hypertensive rats, especially in conduit arteries. In the stroke-prone spontaneously hypertensive rat, impaired endothelium-dependent vasorelaxation appears to contribute to the pathogenesis of stroke independent of blood pressure. Because treatment with lacidipine, a long-acting calcium channel blocker, protects against stroke and cardiovascular remodeling in this model, we investigated the effect of this treatment on endothelium-dependent vasorelaxation in the aorta. Stroke-prone rats were exposed to a salt-rich diet (1% NaCl in drinking water) with or without lacidipine (1 mg. kg(-1). d(-1)) for 6 weeks. A high-sodium diet (1) increased systolic blood pressure, aortic weight, and wall thickness and plasma renin activity (P<0.05); (2) markedly reduced nitric oxide (NO)-mediated, endothelium-dependent relaxation of aortic rings to acetylcholine and the sensitivity to the relaxing effect of S-nitroso-N-acetylpenicillamine, an NO donor (P<0.001); and (3) induced an elevation of preproendothelin-1 mRNA levels in aortic tissue (P<0.01) without affecting endothelial NO synthase mRNA levels. Lacidipine treatment prevented the salt-dependent functional and structural alterations of the aorta, including the overexpression of the preproendothelin-1 gene, and increased endothelial NO synthase mRNA levels in aortic tissue (P<0.01). In conclusion, lacidipine protects stroke-prone hypertensive rats against the impairment of endothelium-dependent vasorelaxation evoked by a salt-rich diet, and this effect may contribute to its beneficial effect against end-organ damage and stroke.
Hypertension 2001 Apr
PMID:Lacidipine prevents endothelial dysfunction in salt-loaded stroke-prone hypertensive rats. 1130 13

Cyclosporine (CsA) treatment in solid organ transplantation has represented one of the greatest advances in the past 20 years, reducing acute rejection and increasing long-term survival. However, CsA has an important side effect, producing renal vasoconstriction and systemic hypertension. The main histological findings in the kidney are vascular lesions in the endothelium and smooth muscle cells. On proximal tubule cells, severe atrophy, vacuolization and thickening of the basal membrane can be found. The main mechanisms of vasoconstriction are secondary to endothelium disorders, increasing vasoconstrictor substances like endothelin, thromboxane, free radicals, etc., and reducing vasodilator substances like nitric oxide and prostaglandins. CsA acute nephrotoxicity produces haemodynamic changes with minor histological lesions, which will disappear when the medication is discontinued. Long-term CsA nephrotoxicity has been widely discussed in the literature. For some authors, a limited number of patients can develop end-state renal failure but others did not suffer these complications. Nevertheless, it seems clear that high doses of CsA can produce renal lesion and renal insufficiency, being difficult to evaluate in renal transplant patients because of the frequent association with chronic rejection lesions. Several types of drugs have been used to treat CsA nephrotoxicity in renal transplant patients but calcium antagonists and angiotensin converting enzyme-inhibitors are the most frequently used, especially the former due to their effect on the afferent arteriole vasodilatation, their natriuretic properties and their reducing intracellular calcium. The greatest experience has been with nifedipine, but other drugs like verapamil, diltiazem, amlodipine, felodipine, isradipine, etc., have also been used. Lacidipine, a 1,4-dihydropiridine, has demonstrated a beneficial effect during the short term after renal transplantation, and a multicentre, multinational, double-bind, placebo-controlled clinical trial for the long term currently ongoing.
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PMID:Calcium antagonists and renal protection from cyclosporine nephrotoxicity: long-term trial in renal transplantation patients. 1134 60

The photostability of Lacidipine, a dihydropyridine drug used in the treatment of mild and moderate hypertension, was studied in solutions exposed to UV-A radiations. The effects of the solvent (ethanol, acetone, dichloromethane), drug concentration and radiation wavelength on the drug photostability were evaluated. Lacidipine and its photoproducts were separated by a selective liquid chromatographic (HPLC) method, under normal phase conditions (CN-column), using n-hexane:ethanol 97:3 (v/v) as mobile phase, at a flow rate of 2.0 ml/min. The main photodegradation products were isolated and characterised and a photodegradation pathway was proposed for Lacidipine in solution. The cis-isomer and a photocyclic isomer proved to be the main photodegradation products.
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PMID:Photodegradation studies on lacidipine in solution: basic experiments with a cis-trans reversible photoequilibrium under UV-A radiation exposure. 1181 21

Dihydropyridines can inhibit gene expression in-vitro and may have a protective vascular effect independent of blood pressure reduction. We tested the hypothesis that lacidipine prevents induction of inducible NO synthase (iNOS), influences leukocyte adhesion and infiltration, inhibits nuclear factor (NF)-kappaB transcription factor activity, and ameliorates end-organ damage in a transgenic rat model of angiotensin (Ang) II--dependent organ sclerosis. We treated rats transgenic for human renin and angiotensinogen (dTGR) from week 4 to 7 with lacidipine (0.3 or 3 mg/kg by gavage). Blood pressure was measured by tail cuff. Organ damage was assessed by histology and immunohistochemistry. Adhesion molecules and cytokines were analyzed by immunohistochemistry. Transcription factors were analyzed by mobility shift assays. Untreated dTGR developed moderate hypertension, cardiac hypertrophy, and severe renal damage with albuminuria. Lacidipine decreased blood pressure slightly at the low dose and substantially at the higher dose. However, both treatments reduced albuminuria and plasma creatinine to the same degree (P<0.05). Intercellular adhesion molecule-1 (ICAM-1) was markedly reduced by lacidipine as well as renal neutrophil and monocyte infiltration. Lacidipine reduced mitogen-activated protein (MAP) kinase phosphorylation and iNOS expression in both cortex and medulla. NF-kappaB and AP-1 were activated in dTGR but reduced by lacidipine. Lacidipine ameliorates Ang II-induced end-organ damage independent of blood pressure lowering, perhaps by inhibiting the MAP kinase pathway and NF-kappaB activation.
Hypertension 2002 Feb
PMID:Lacidipine inhibits adhesion molecule and oxidase expression independent of blood pressure reduction in angiotensin-induced vascular injury. 1188 31

Lacidipine is a clinically active, antihypertensive calcium antagonist of the 1,4 dihydropyridine (DHP) class. It is also capable of vascular protection when administered (prophylactically and therapeutically) at nonsustained antihypertensive doses to salt-sensitive Dahl-S rats: useful animal models for studying the vasoprotective effect of calcium antagonists. In our previous work using voltammetry with selective biosensors, we observed that lacidipine implements endothelial nitrogen monoxide (NO) in normal rats. These experiments, performed in aortic rings obtained from Dahl-S rats analyzed with voltammetry and specific biosensors, further demonstrate that lacidipine, given at doses that do not control the development of hypertension (1 mg/kg), enhance endothelial NO activity. Taken together with the observation that 1 mg/kg lacidipine, and not its vehicle, is able to prevent vascular damage and concomitant increases in mortality (accelerated by a salt diet), this voltametric data suggest that NO acts as a component of positive influence of this DHP on vascular structure and function.
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PMID:Evidence that lacidipine at nonsustained antihypertensive doses activates nitrogen monoxide system in the endothelium of salt-loaded Dahl-S rats. 1190 20


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