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

The efficacy and safety of amlodipine was evaluated in 20 patients of mild to moderate hypertension in a single blind, placebo controlled, noncomparative study. Patients with a baseline diastolic blood pressure of > 90 and < 115 mmHg while on placebo were admitted to a 4 week active treatment phase. Amlodipine produced a significant (p < 0.05) reduction in mean systolic (177 mmHg to 145 mmHg) and diastolic blood pressure (106 mmHg to 84 mmHg) after 4 weeks treatment in all patients. 95% of the patients had their diastolic blood pressure reduced to < or = 90 mmHg by the end of the study period. There was no significant change in heart rate or in the laboratory parameters with amlodipine therapy. Seven patients reported mild to moderate adverse events which did not require discontinuation of therapy. This combination of efficacy and tolerability, together with convenience of once daily dosing, should ensure the usefulness of amlodipine in the treatment of hypertension.
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PMID:Amlodipine monotherapy in mild to moderate hypertension. 807 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

The chemistry, pharmacology, pharmacokinetics, efficacy, and adverse effects of amlodipine are reviewed. Amlodipine belongs to the dihydropyridine subclass of calcium antagonists. Amlodipine is a potent peripheral and coronary vasodilator with high selectivity for vascular smooth muscle and minimal effect on myocardial contractility or cardiac conduction. Absorption after oral administration is slow, and the duration of action is long, with a half-life of 36-45 hours. Amlodipine has FDA-approved labeling for use in the treatment of hypertension, chronic stable angina, and vasospastic angina. The agent is also indicated for use in hypertensive or anginal patients who also have congestive heart failure due to systolic dysfunction (New York Heart Association classes II and III). Clinical trials suggest that effective 24-hour control of hypertension and angina is provided by once-daily administration of amlodipine 5-10 mg alone or in combination with other drugs. No clinically important drug interactions have been observed to date. Amlodipine has not shown any unfavorable effects on serum glucose or lipid levels. The most common adverse effect is peripheral edema. Amlodipine is effective and well tolerated when given alone or in combination with other drugs for the treatment of hypertension and angina. Amlodipine may offer advantages over verapamil, diltiazem, and nifedipine in patients with hypertension or angina with associated congestive heart failure due to systolic dysfunction.
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PMID:Amlodipine: a new calcium antagonist. 813 60

Amlodipine is a calcium channel blocker used in the management of angina and hypertension. We report 3 cases of gingival overgrowth in adult dentate patients associated with chronic usage of this drug. Gingival changes occurred within 3 months of dosage and appeared to be compounded by the patient's existing periodontal condition. In all 3 patients, there was sequestration of amlodipine in their crevicular fluid. The significance of this finding in relation to the pathogenesis of this unwanted effect remains to be elucidated.
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PMID:Amlodipine-induced gingival overgrowth. 819 45

In an open, non-comparative, variable-dose study, 20 outpatients with mild to moderate essential hypertension were treated with 5-10 mg amlodipine once daily for 4 weeks, after their blood pressures had stabilized on placebo. Amlodipine produced a significant decrease in blood pressure (P < 0.05) from the initial mean of 162/100 mm Hg to 139/85 mm Hg at 4 weeks. 80% of the patients reached the goal diastolic blood pressure of < or = 90 mm Hg with a once-daily dose of 5 mg amlodipine within 2 weeks. The remaining 20% also attained the goal diastolic blood pressure within 4 weeks, with a one-step increase in the dose to 10 mg at 2 weeks. Amlodipine maintained blood pressure reduction throughout the 24-hours dosing interval with a once-daily dose. Notably, no side effects were observed; pulse rate, electrocardiogram, and laboratory parameters were not significantly altered with therapy. Amlodipine in a single daily dose of 5-10 mg is effective and well tolerated in the treatment of patients with mild to moderate hypertension.
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PMID:Amlodipine in mild and moderate hypertension: initial Indian experience. 829 30

Nifedipine is an effective compound for the treatment of hypertension. However, even as a tablet formulation it is relatively short acting requiring two or three times daily administration. Amlodipine is a long-acting calcium antagonist and effectively lowers BP in patients with essential hypertension. In the present study we compared the BP-lowering effect of nifedipine and amlodipine in patients with essential hypertension. Thirteen patients were studied. They had been on nifedipine tablets for at least four weeks and DBP had been consistently > 95 mmHg. After a further month run-in on nifedipine they entered a randomised double-blind crossover study of one month' treatment with either nifedipine tablet (20 mg twice daily) or amlodipine (5 mg once daily). BP was measured 12 and 2 hours after the last dose of nifedipine and 24 and 2 hours after the last dose of amlodipine. There was a significant peak/trough effect while on nifedipine tablets, the BP being significantly higher at 12 hours than at 2 hours after the last dose (155.2/90.9 +/- 4.6/1.7 vs. 136.1/84.8 +/- 4.3/1.7 mmHg; P < 0.001/P < 0.005). There was no overall difference in BP between nifedipine and amlodipine treatment when BPs were taken at the respective troughs (i.e. 12 hours and 24 hours). If anything, amlodipine tended to be slightly more effective at least on supine SBP (155.2/90.9 +/- 4.6/1.7 vs. 147.6/89.1 +2- 4.3/1.8 mmHg; P < 0.05, NS). In conclusion, amlodipine given once daily is at least as effective as nifedipine tablets given twice daily in patients with essential hypertension.
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PMID:Double-blind comparison between nifedipine and amlodipine for the treatment of essential hypertension. 841 Sep 27

In a multicentre crossover study of 97 patients with mild hypertension, the incidence and severity of adverse effects were observed during the first 14 days of treatment with amlodipine, nifedipine retard or placebo. Amlodipine (5 mg) once daily was equipotent to nifedipine retard (20 mg) twice daily. At these doses, the incidence of adverse effects was significantly greater during treatment with nifedipine retard (41%) than with amlodipine (27%, P < 0.05) or placebo (16%, P < 0.01). In particular, headache and flushing occurred significantly less frequently during the first 14 days of treatment with amlodipine than with nifedipine retard. The lower incidence and reduced severity of vasodilatory side-effects associated with amlodipine resulted in fewer withdrawals during initiation of therapy (2 on amlodipine compared with 7 on nifedipine retard).
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PMID:Early side-effects of antihypertensive therapy: comparison of amlodipine and nifedipine retard. 845 May 26

To determine the dose-response efficacy of once-daily administration of placebo or a new long-acting calcium channel blocker amlodipine in patients with mild to moderate hypertension, a randomized, multicenter, placebo-controlled, double-blind trial was conducted. The study included 210 patients with diastolic hypertension (blood pressure 95 to 114 mm Hg) without major hematologic, renal, hepatic, cardiac, or endocrine abnormalities. After a 4-week single-blind placebo run-in period, patients were given placebo or amlodipine (1.25, 2.5, 5, or 10 mg) daily for 4 weeks. To assess the antihypertensive effect of amlodipine over a 24-hour period, blood pressure and pulse rate at weeks 0 and 4 were recorded for 12 hours after the dose and then again at 24 hours. At the end of the study patients treated with all doses of amlodipine greater than 1.25 mg daily had significantly reduced diastolic blood pressure in both supine and standing than 1.25 mg daily had significantly reduced diastolic blood pressure in both supine and standing positions. Amlodipine, 1.25 mg daily, was also associated with a decrease in standing diastolic blood pressure. Response to treatment was greater in all amlodipine-treated patients than in those receiving placebo. Pulse rate in both the supine and standing positions was not significantly affected by amlodipine. At doses of 2.5, 5.0, or 10.0 mg daily, amlodipine maintained blood pressure below values obtained with placebo throughout the 24-hour period. Treatment with amlodipine was well tolerated and the incidence of side effects was low.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Double-blind evaluation of the dose-response relationship of amlodipine in essential hypertension. 849 14

Amlodipine belongs to the dihydropyridine class of calcium channel blockers. Both short and long term studies indicate that amlodipine effectively lowers mild to moderately elevated blood pressure and relieves symptoms of angina pectoris. In comparative studies, its antihypertensive efficacy is similar to that of other established agents such as beta-blockers, diuretics, ACE inhibitors and other calcium channel blockers (including the dihydropyridines); limited comparative data are, however, available in patients with angina pectoris. Amlodipine may offer potential in patients with congestive heart failure. Vasodilator adverse events such as oedema, headaches, and flushing are commonly observed with amlodipine. The drug does not appear to cause postural hypotension, reflex tachycardia or cardiac conduction disturbances. Comparative studies suggest that amlodipine is at least as well tolerated as other standard agents. Thus, amlodipine provides an attractive therapeutic option for the treatment of hypertension, and offers potential for patients with angina pectoris. Its beneficial effects in patients with congestive heart failure require confirmation in future studies.
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PMID:Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease. 852 73

The objective of this study was to determine whether the calcium antagonist amlodipine could slow the progression of chronic renal disease. We examined the effects of amlodipine on kidney structure and function in two experimental models of hypertension. In the first study, adult, male Munich Wistar rats underwent uninephrectomy and were given weekly injections of desoxycorticosterone and 1% saline for drinking. Rats ingested normal chow or chow containing amlodipine for 8 weeks. The drug reduced systemic blood pressure, but glomerular filtration rate, kidney weight, proteinuria, and morphological evidence of glomerular injury were not affected. In the second study, male spontaneously hypertensive rats underwent uninephrectomy at 5 weeks of age and were followed for 6 months, during which they received no therapy or amlodipine. The drug dose was determined in preliminary studies to be the highest dose not associated with marked growth retardation. Again, although systemic blood pressure was significantly reduced by amlodipine, proteinuria and the prevalence of glomerulosclerosis were similar in amlodipine-treated and control spontaneously hypertensive rats. Micropuncture studies revealed that glomerular pressure remained elevated in amlodipine-treated spontaneously hypertensive rats. Kidney weight and glomerular volume were also similar in amlodipine-treated and control rats. Amlodipine also failed to inhibit platelet aggregation. Therefore, antihypertensive therapy with amlodipine fails to reduce glomerular pressure in spontaneously hypertensive rats as well as glomerular size and injury in spontaneously hypertension rats and desoxycorticosterone-salt hypertension. Although other dihydropyridine calcium antagonists have been found to reduce experimental glomerular injury, these data suggest that amlodipine may not prevent hypertensive nephrosclerosis.
Hypertension 1996 Feb
PMID:Effects of amlodipine on glomerular filtration, growth, and injury in experimental hypertension. 856 47


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