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

Nitrendipine (BAY e 5009) is a new calcium channel blocker with a marked effect on excitation-contraction coupling in different types of muscle cells. It has many similarities to the established agent, nifedipine. In the present study, nitrendipine was evaluated in a double-blind within-patient comparison. Twelve patients with essential hypertension were given nitrendipine 20 mg or 40 mg orally for three weeks following a 1-week placebo period. After a second 1-week placebo period, there was a crossover to the alternative dosage (20 or 40 mg respectively), and active therapy was again given for 3 weeks. Both doses of nitrendipine caused a significant and equal reduction of arterial pressure, which persisted for at least 24 hours. Only the highest dose caused an increase in heart rate. There were a few reports of headaches, flushing, and palpitation, particularly after the 40 mg dose. There was a significant correlation between the reduction of mean arterial pressure and the log plasma concentration (20 mg: r = -0.88, p less than 0.01; 40 mg: r = -0.94, p less than 0.001). There was a linear relationship between the area under the curve and the oral dose, indicating that liver enzyme saturation had not occurred. There was no accumulation of nitrendipine in plasma during 3 weeks of treatment.
Hypertension
PMID:Pharmacokinetic and pharmacodynamic parameters in patients treated with nitrendipine. 634 73

We compared the efficacy and safety of nitrendipine with that of hydralazine in 21 subjects with essential hypertension. Nitrendipine or hydralazine was given in a double-blind manner after a placebo period. Dose was titrated to diastolic blood pressure (BP) less than or equal to 90 mm Hg and the dose established during titration was continued for 5 to 7 wk. Both supine and erect BP were decreased by both drugs, but heart rate was affected only minimally. Myocardial oxygen demand decreased only with nitrendipine (P less than 0.05), although the change may have been the result of somewhat higher systolic BP while on placebo. Hydralazine induced minimal changes in levels of plasma catecholamines, but plasma norepinephrine levels rose in subjects on nitrendipine. Side effects encountered with both drugs were much the same, although nitrendipine was more often associated with mild fatigue. There were mild elevations in liver function parameters in two subjects on nitrendipine. There was little difference between the effects of nitrendipine and hydralazine in hypertension.
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PMID:Effects of nitrendipine and hydralazine on plasma catecholamines in essential hypertension. 647 32

Weekly subcutaneous implantation of 25-mg nitrendipine pellets prevented onset of both spontaneous and deoxycorticosterone-salt hypertension in rats. Discontinuance of implantation led to reappearance of hypertension after about 2 weeks in the former and led to rising though still normotensive pressures after about 3 weeks in the latter. A new implant caused blood pressures in both to drop within a day or two to normotensive levels in the case of spontaneously hypertensive rats. Nitrendipine prevented cardiac hypertrophy in steroid hypertensive rats, but not in spontaneous hypertensives. A nitrendipine pellet given 1 day before or a 30 mg/kg injection given 1 h prior to the administration of a water, Na+, and K+ load, prevented the diabetes insipidus-like syndrome resulting from deoxycorticosterone-salt treatment, and lowered sodium but not potassium excretion. Nitrendipine did not affect steroid-induced hypernatremia and hypokalemia.
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PMID:Control of spontaneous and deoxycorticosterone-salt hypertension and polyuria by nitrendipine pellets. 673 89

Nitrendipine is a calcium antagonistic 1,4-dihydropyridine derivative with a pronounced antihypertensive activity in animal experiment. Similar to other calcium entry blockers, nitrendipine decreases blood pressure by lowering the elevated peripheral vascular resistance. However, its long-term effect differs from that of vasodilators such as hydralazine and minoxidil. In contrast to vasodilators, nitrendipine reduces heart hypertrophy in various forms of experimental hypertension in rats. Nitrendipine is highly effective in normalizing blood pressure, reducing heart hypertrophy, and preventing mortality in salt-related hypertension (two-kidney renal hypertension, salt-induced hypertension in Dahl rats), which are rather refractory to the effect of vasodilators. Nitrendipine reduces renovascular resistance in spontaneously hypertensive rats but has no effect on that of normotensive rats. In conscious renal hypertensive dogs, nitrendipine decreases blood pressure more than does hydralazine. The reflex tachycardia is more pronounced after hydralazine than after nitrendipine; blood pressure decrease is greater and the duration of the effect is longer than that of nifedipine. Nitrendipine is thus predicted as an effective drug for antihypertensive monotherapy.
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PMID:Nitrendipine and other calcium entry blockers (calcium antagonists) in hypertension. 682 91

Nitrendipine (Bay e 5009) is a new calcium antagonist antihypertensive agent similar in structure and function to nifedipine. Nitrendipine was tested in a range of single and repeated doses in 10 adult males with uncomplicated mild to moderate hypertension. The treatment goal was reduction of diastolic blood pressure to 90 mm Hg or less. The dose that achieved goal blood pressure ranged between 10 and 30 mg. Systolic and diastolic blood pressure began to fall within 15 minutes following ingestion of single oral doses of nitrendipine. The maximum effect of the drug was achieved in 60 to 90 minutes and remained at approximately this level for 6 to 8 hours. The average reduction in supine diastolic was more than twice as great as the fall in systolic blood prere began to fall within 15 minutes following ingestion of single oral doses of nitrendipine. The maximum effect of the drug was acheived in 60 to 90 minutes and remained at approximately this level for 6 to 8 hours. The average reduction in supine diastolic was more than twice as great as the fall in systolic blood pressure. With continuous doses given three times daily, all patients' blood pressures were as low or lower than the maximal effect observed after single doses. The reduction in blood pressure was sustained for the full 3 weeks of treatment. There was a sustained small increase in pulse rate averaging 6 beats/min. The drug was generally well tolerated by most patients. Mild to moderate headache that resolved with continued treatment was the most frequent side effect. This preliminary trial indicates that nitrendipine is an effective antihypertensive agent that merits further study.
Hypertension
PMID:Acute and short-term effects of new calcium antagonist in hypertension. 706 6

To clarify whether angiotensin converting enzyme (ACE) inhibitors prevent progressive renal injury directly by their antihypertensive effect we administered the ACE inhibitor lisinopril to male MWF/Ztm rats as a single daily dose that lowered blood pressure for only 9 of 24 h. We investigated the effects of this treatment in short- and long-term studies and compared them with another antihypertensive drug, the calcium channel blocker nitrendipine, given to partially control blood pressure as done with the ACE inhibitor. In untreated animals systemic hypertension, proteinuria, and glomerulosclerosis developed spontaneously with age, and lisinopril reduced systemic hypertension and prevented proteinuria and glomerular lesions. Nitrendipine, despite similar blood pressure control, was ineffective in preventing both proteinuria and glomerulosclerosis. After 2 mo of treatment glomerular capillary pressure was significantly reduced by lisinopril and slightly but significantly increased by nitrendipine, compared with untreated controls. The ultrafiltration coefficient was significantly higher in lisinopril than in controls and not significantly changed by nitrendipine. With both drugs, however, glomerular hemodynamic effects were observed only at a few hours after administration and were abolished before the next administration. No significant changes in glomerular tuft volume were observed in treated and untreated animals after 2 and 6 mo of observation. Thus ACE inhibitor, despite only partial control of systemic blood pressure, effectively prevented proteinuria and glomerular injury. Comparable blood pressure control obtained with a calcium channel blocker was not associated with renal protection. These results suggest that ACE inhibitors could protect glomerular microcirculation by a mechanism that is not directly related to their antihypertensive action.
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PMID:Dissociation between antiproteinuric and antihypertensive effect of angiotensin converting enzyme inhibitors in rats. 752 85

In this study we evaluated the delayed effects of a calcium entry blocker on blood pressure and on vascular structural and functional alterations in mesenteric resistance arteries of spontaneously hypertensive rats (SHR). The calcium entry blocker nitrendipine was administered (30 mg/kg per day) according to three different schedules: in one group of SHR from 4 to 8 weeks of age (n = 12), in a second group from 8 to 12 weeks of age (n = 12), and in a third group from 4 to 12 weeks of age (n = 12). Twelve untreated SHR and 12 untreated Wistar-Kyoto rats served as controls. Half the animals of each group were killed at 13 weeks, and the remaining were killed at 38 weeks. After death, relative left ventricular mass was calculated. Vascular morphology and function (responses to norepinephrine and acetylcholine) in mesenteric small arteries were then assessed using a micromyographic technique. Nitrendipine treatment delayed the development of hypertension and determined the regression of structural alterations of mesenteric resistance arteries in SHR. These favorable effects were maintained for several weeks after treatment withdrawal, provided that treatment was started at 4 weeks of age. Considering the functional alterations of mesenteric arteries in SHR (responses to norepinephrine and acetylcholine), nitrendipine treatment determined an improvement of both these dysfunctions as long as reductions of the media-to-lumen ratio and blood pressure, respectively, were maintained.
Hypertension 1994 Jul
PMID:Delayed development of hypertension after short-term nitrendipine treatment. 802 Oct 1

Twenty patients (12 males, 8 females, mean age 51 +/- 10 years) with mild to moderate arterial hypertension were treated with nitrendipine (mean daily dose 17 mg) during a 6 month period. Patients were evaluated with blood measurement and with 24-hour ambulatory blood pressure monitoring. In 16 patients who completed the study, systolic and diastolic blood pressure decreased of 13-15% and 18-20% respectively after at least 1 month of therapy. Mean 24-hour blood pressure was reduced of 9.7% (p < 0.01) at the end of the third month and of 13.9% (p < 0.01) at the end of the sixth month. Both systolic and diastolic 24-hour blood pressure were significantly reduced. Nitrendipine was active on day time and night time pressure. Only 1 patient had edema of the legs. Heart rate was not increased by the drug. Total cholesterol and LDL cholesterol were reduced.
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PMID:[Evaluation of the chronic antihypertensive effect of nitrendipine using ambulatory monitoring]. 803 97

Lesions of the arterial wall constitute one of the main complications of essential hypertension. The final objective of all antihypertensive drugs is to reduce the cardiovascular morbidity and mortality rates, but their short and medium term objectives must be to normalise blood pressure values and to correct the functional and structural abnormalities consecutive to arterial hypertension. In this double-blind drug versus placebo study conducted in 20 patients (14 men, 6 women) aged over 40, the effects of nitrendipine on regional arterial haemodynamics (aortic territory, upper limb, lower limb) and carotid circulation were evaluated. Nitrendipine was administered daily in doses of 20 mg during 1 month. After 4 weeks of treatment, the treated group showed a fall in blood pressure and an improvement in the pulse wave propagation (an index of arterial distensibility) in the carotido-femoral territory (11.4 +/- 1.7 vs 9.9 +/- 1.6 m/s; P < 0.01) and in the humero-radial territory (12.9 +/- 2.0 vs 11.6 +/- 2.1 m/s; P < 0.05); there was no change in the femoro-tibial territory (13.2 +/- 1.8 vs 12.5 +/- 1.7 m/s; NS). The haemodynamics of the common carotid artery showed no change in carotid diameter or blood velocity, and small lowering of local resistances (28.1 +/- 9.1 vs 24.6 +/- 4.9 mmHg.s.ml-1; P < 0.05). This study demonstrates that in patients older than 40 years a long-term treatment with nitrendipine lowers blood pressure, does not alter the common carotid flow and improves arterial distensibility. The arterial effects seem to vary according to the arterial territories considered.
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PMID:[Regional arterial hemodynamics and carotid circulation in essential arterial hypertension. Effect of nitrendipine in patients over 40 years of age]. 811 16

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


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