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

Amlodipine is a new calcium antagonist of the 1.4-dihydropyridine group for treatment of hypertension and angina pectoris. Amlodipine is distinct from other calcium antagonists by its pharmacokinetic profile: slower onset of action with less acute vasodilatation associated side effects and a sustained antihypertensive and anti-anginal efficacy over 24 hours.
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PMID:[Amlodipine: pharmacokinetic and pharmacodynamic profile of a calcium antagonist with prolonged effect]. 153 45

The efficacy and safety of amlodipine in the long term treatment of outpatients with mild to moderate hypertension were examined in an open, non-comparative study. 87 patients were enrolled in the study, 62 (71%) of whom were observed for 27 months under controlled conditions. Daily doses of 5-10 mg amlodipine led to a statistically significant decrease in systolic and diastolic blood pressure (-30.5/-20.7 mmHg, p less than 0.01) while there was no substantial influence on heart rate or decrease in efficacy. Amlodipine was tolerated very well; only 17% of the patients reported side effects, most of which were either mild or moderate and were tolerated or disappeared with continued treatment. No clinically significant changes were noted in clinical laboratory or ECG examinations. Based on its special pharmacological and pharmacokinetic properties, amlodipine is a novel calcium antagonist from the dihydropyridine class which has proved to be effective in the treatment of hypertension. The antihypertensive effect, which is sustained for more than 24 hours, parallels the circadian variations in blood pressure and thus induces beneficial pharmacodynamic effects. Due to the low incidence of side effects and the once-daily dosage regimen, an improvement in patient compliance can be expected.
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PMID:[Effectiveness and tolerance of amlodipine in treatment of patients with mild to moderate hypertension. Results of a long-term study with a new calcium antagonist]. 153 8

Amlodipine, a novel dihydropyridine calcium-antagonist, was compared to slow-release nifedipine in a short-term study on 40 patients with mild to moderate essential hypertension, in order to assess the efficacy and tolerability of two different dihydropyridine calcium-antagonists with short and long half-life. After a two-week single-blind placebo period, patients were given, in a randomized sequence, amlodipine (5 or 10 mg/day od, 20 patients) or nifedipine s.r. (20 or 40 mg BID, 20 patients). At the end of treatment (12 weeks) a significant lowering of arterial pressure was obtained after 24h from the administration of amlodipin (-34/-17 mmHg) and after 12h from the administration of nifedipine s.r. (-33/-16 mmHg). Furthermore, with both drugs, no significant changes in heart rate and ECG have been reported. Amlodipine was better tolerated than nifedipine, as shown by the lower incidence of side effects. Therefore amlodipine proved to be an effective and well tolerated drug in the therapy of mild to moderate hypertension.
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PMID:[A comparison between amlodipine and nifedipine retard in patients with essential arterial hypertension]. 153 44

Amlodipine is a low-clearance, dihydropyridine calcium antagonist. The slow rate of elimination (elimination half-life of 40-60 h) confers several pharmacokinetic characteristics that are not seen with other calcium-antagonist drugs. It has high oral bioavailability (60-80%) and accumulates to a steady-state with once-daily administration over a period of 1-1 1/2 weeks. Fluctuation of plasma drug concentration between doses is between 20 and 25% when once-daily dosing is used. Onset of effect is gradual after oral administration which is due, in part, to an intermediate rate of drug absorption (peak plasma drug concentration occurs 6-8 h after dosing) and perhaps also to the physicochemical characteristics of the drug-cell membrane-receptor interaction. The pharmacodynamic profile of the drug in hypertensive patients is consistent with the disposition of the drug. After single doses, blood pressure decreases gradually over 4-8 h and may slowly return to baseline over 24-72 h. No change in heart rate is noted after the dose as the onset is gradual and physiological reflexes are not activated. During chronic, oral, once-daily dosing blood pressure is decreased from pretreatment baseline with little fluctuation over the 24-hour dose interval. Discontinuation of amlodipine treatment results in a slow return of blood pressure to baseline over 7-10 days, with no evidence of a 'rebound' effect. Amlodipine is a low-clearance, dihydropyridine calcium antagonist which is effective for the treatment of hypertension and angina pectoris with once-daily dosing.
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PMID:Pharmacokinetics and pharmacodynamics of amlodipine. 153 13

Amlodipine and nitrendipine are calcium antagonists of the 1,4-dihydropyridine group which differ in their pharmacokinetic and pharmacodynamic properties. The clinical relevance of these differences was investigated in a study designed to compare the efficacy and safety of once-daily amlodipine (5 mg) and nitrendipine (20 mg) in patients with mild-to-moderate essential hypertension. Ambulatory blood pressure monitoring and conventional measurements showed that amlodipine and nitrendipine produced comparable reductions in blood pressure after 4 weeks of treatment. However, the onset of the antihypertensive effect was gradual for amlodipine, while most of the reduction achieved at the end of treatment with nitrendipine was seen after the first dose. There were no significant changes in heart rate with amlodipine, but significant increases occurred during the first 6 h of nitrendipine treatment. Amlodipine was associated with a significantly lower incidence of vasodilator-related adverse effects at initiation of therapy (headache, flushing, tachycardia) compared with nitrendipine, which may reflect its slower onset of action. The different pharmacodynamic and toleration profiles of amlodipine and nitrendipine at therapeutically equivalent doses suggest that amlodipine may have advantages in the treatment of hypertension, especially in terms of the low incidence of acute side effects, which may ultimately translate into improved patient compliance.
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PMID:Amlodipine compared to nitrendipine in hypertensive patients: the effects on toleration in relationship to the onset of action. 153 15

The frequency and severity of adverse effects during the first 14 days of treatment with amlodipine (5 mg once daily), nifedipine retard (20 mg twice daily) or placebo were compared in a multicentre, three-way, cross-over study involving 97 patients with mild-to-moderate hypertension. All three groups of patients were well matched for age, sex and baseline blood pressure. Amlodipine and nifedipine retard produced highly significant and comparable reductions in blood pressure, indicating that the doses were therapeutically equivalent. The incidence of adverse effects considered to be definitely or probably related to nifedipine retard treatment (41%) was significantly higher than for placebo (16%, p less than 0.01) or amlodipine (27%, p less than 0.05). There were no significant differences in the incidence of vasodilator-related adverse effects between amlodipine and placebo. In contrast, headache, flushing and dizziness were reported more frequently by patients while on nifedipine retard than on placebo or amlodipine. The convenience of once-daily dosing, together with a lower incidence of adverse effects, with consequently fewer withdrawals from therapy, suggests that amlodipine has clinical advantages over nifedipine retard in the treatment of hypertension.
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PMID:Comparison of early side effects with amlodipine and nifedipine retard in hypertension. 153 16

Amlodipine, a basic dihydropyridine derivative, inhibits the calcium influx through 'slow' channels in peripheral vascular and coronary smooth muscle cells, thus producing marked vasodilation in peripheral and coronary vascular beds. Short to medium term clinical trials indicate that amlodipine is effective as both an antianginal agent in patients with stable angina pectoris and an antihypertensive agent in patients with mild to moderate hypertension. In small comparative studies amlodipine was at least as effective as 'standard' agents, including atenolol, verapamil, hydrochlorothiazide or captopril in hypertension, and diltiazem or nadolol in angina pectoris. Amlodipine is well tolerated, and does not appear to cause some of the undesirable effects often associated with other cardiovascular agents (e.g. adverse changes in serum lipid patterns, cardiac conduction disturbances, postural hypotension). The most common adverse effects associated with amlodipine therapy--oedema and flushing--are related to the vasodilatory action of the drug, and are generally mild to moderate in severity. Thus, amlodipine seems to provide a useful alternative to other agents currently available for the treatment of essential hypertension and chronic stable angina pectoris, with certain pharmacodynamic and tolerability properties that should be advantageous in many patients.
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PMID:Amlodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiovascular disease. 171 48

Abnormalities in regulatory mechanisms for calcium handling play a key role in cell death and tissue necrosis. In the cardiovascular system this applies to the vasculature and the myocardium alike. In the aged population, where hypertension is a known risk factor, manifestations of vascular injury include atherogenesis and stroke. The newly developed dihydropyridine-based calcium antagonist amlodipine was used in investigations to determine whether calcium antagonists with sustained activity, in addition to lowering blood pressure, slow the development of atherogenesis in rabbits receiving high cholesterol diets, or reduce mortality in stroke-prone hypertensive rats. To establish whether this drug protects the vasculature against excessive atheroma formation in the presence of high cholesterol intake, rabbits were given 2% cholesterol in addition to their normal food intake and either 0, 1, or 5 mg/kg/day amlodipine orally for either 8 or 12 weeks. One day after the conclusion of the treatment protocol, the thoracic aorta was excised, assayed for calcium or cholesterol concentrations, and stained to identify sudanophilic-positive lesions. Amlodipine caused a time- and dose-dependent reduction in lesion formation, calcium overload, and cholesterol level. In the second series of experiments, amlodipine (5 mg/kg/day) was added to the diets of stroke-prone hypertensive rats. Treatment was initiated at age 5 weeks and continued for 30 weeks. During the treatment period, systolic blood pressure was reduced in the amlodipine-treated rats (166 +/- 9 mm Hg) versus those treated with placebo (248 +/- 12 mm Hg) (p less than 0.001). A significant reduction in mortality was observed in the amlodipine-treated rats (p less than 0.001), with 93% surviving versus only 26% in the placebo group at the end of the 30-week treatment period. Concomitantly, cardiac hypertrophy was attenuated in the treated group compared with the placebo group (heart-to-body weight ratios of 4.5 +/- 0.01 vs 5.8 +/- 0.6, respectively [p less than 0.01]). These results extend the evidence that calcium antagonists provide vascular protection in animal models. This finding may become increasingly important in the management of an aging hypertensive population.
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PMID:Vascular injury: mechanisms and manifestations. 182 8

Amlodipine is a 1,4-dihydropyridine calcium antagonist which, although structurally related to nifedipine, has a number of important distinguishing properties. A high oral bioavailability of amlodipine has been demonstrated in a number of animal species and man, together with a long elimination half-life. In vitro studies have demonstrated a slow onset of action which is consistent with the findings from receptor binding studies which show that amlodipine binds to receptor sites with slow rates of association and dissociation. These studies have also shown that amlodipine may interact with both dihydropyridine and diltiazem binding sites. In vivo animal experiments have confirmed the gradual onset of action observed in vitro and have shown amlodipine to have sustained antihypertensive effects with no change in heart rate. Amlodipine has also been shown to attenuate the cardiac hypertrophy associated with the development of hypertension in spontaneously hypertensive rats. Animal studies have clearly demonstrated the mild natriuretic and diuretic properties of amlodipine. The pharmacodynamic and pharmacokinetic properties of amlodipine make this drug an optimal choice of treatment for the control of hypertension with once daily administration.
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PMID:Amlodipine: a once daily calcium antagonist. 183 46

Amlodipine is a dihydropyridine calcium antagonist which can be used once daily in hypertension. The pharmacokinetics of the molecule mean that effective blood levels and hence good control of blood pressure are maintained throughout the dosing interval. Dose-ranging studies have shown the most appropriate starting dose is 5 mg once daily, with simple adjustment to 10 mg if necessary. Comparative studies with other agents have shown amlodipine to have antihypertensive efficacy superior to verapamil and comparable with atenolol, hydrochlorothiazide, captopril or nitrendipine. When used in combination with angiotensin converting enzyme inhibitors, beta-blockers or thiazide diuretics, amlodipine can produce important additional antihypertensive effects. Studies involving long-term use of amlodipine in hypertension indicate that no tolerance appears, and that amlodipine is a well tolerated drug.
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PMID:Amlodipine: an effective once-daily antihypertensive agent. 183 48


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