Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0002962 (angina)
 21,142 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The long-term efficacy of amlodipine was assessed in 21 patients with chronic stable angina. After a 2-week run-in period, patients received 5 mg amlodipine once daily for 2 weeks. This was increased to 10 mg daily during the following 10-week dose-adjustment/maintenance phase, if angina attacks were not abolished. Patients were then followed up for an additional 21 months (total 24 months). During follow-up, patients were evaluated at least once a month, and sitting blood pressure and heart rate were monitored. Angina attack rate and nitroglycerin consumption were recorded in angina diaries throughout the study. Patients underwent a treadmill exercise test at baseline, at the end of the dose-adjustment phase and again during long-term follow-up at 20 months. Amlodipine (mean final daily dose, 8.2 mg) resulted in a significant reduction in angina attack rate and nitroglycerin consumption (both p < 0.001), which was maintained during follow-up. Systolic blood pressure was also reduced (p < 0.01) by amlodipine. Diastolic blood pressure and heart rate were not significantly affected. Amlodipine significantly increased mean exercise time (p < 0.001). ST-segment depression at maximum common load was reduced when compared with baseline values (p < 0.001), and the metabolic equivalent (MET) score at peak exercise was significantly improved by amlodipine (p < 0.001). All of these effects on exercise performance were sustained during follow-up. These data indicate that long-term treatment with amlodipine, in patients with severe coronary artery disease, reduced the number of angina attacks and nitroglycerin consumption and produced a sustained improvement in exercise performance.
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PMID:Long-term efficacy of amlodipine in patients with severe coronary artery disease. 752 84

The Circadian Anti-Ischemic Program in Europe (CAPE) trial was a large, multinational trial, taking place in ten countries and involving over 100 investigators. It was a double-blind, parallel, randomized, placebo-controlled trial comparing once-daily amlodipine with placebo in chronic stable angina pectoris. It consisted of two phases, the first being a 2-week, single-blind, placebo run-in phase during which stable doses of anti-anginal drugs were maintained (65% of patients were receiving beta-blockers), and the second an 8-week active treatment phase in which patients received either amlodipine or placebo, 5 mg once daily, for the first 4 weeks, increasing to 10 mg once daily for the second 4 weeks. Patients were randomized in a ratio of 2 patients receiving amlodipine to each patient receiving placebo. Out of an initial 1,160 patients screened, 315 entered the study, with 250 having complete efficacy-evaluable data. Patients were included if they experienced > or = 4 ambulatory ECG ischemic episodes (> or = 1 mm ST-segment depression for > or = 1 min) and/or > or = 20 min total ischemia time over 48 h. Data were obtained on the total frequency of ST-segment depression events, the ischemia area (ST-segment depression integral), the ischemic time and peak ST-segment depression. Patient diary information on angina attack rate and nitroglycerin tablet consumption was also collected. Patients in both groups were compared for age, blood pressure, heart rate, duration of angina and baseline ischemia at entry. Amlodipine and placebo had similar safety profiles, with 17.3% of amlodipine patients recording adverse events, compared with 13.3% of placebo patients.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Amlodipine and the total ischemic burden: circadian anti-ischemia program in Europe (CAPE) trial-methodology, safety and toleration. The Steering Committee members and all of the investigators. 773 84

Amlodipine 10 mg was evaluated for additional anti-ischaemic and anti-anginal efficacy in 14 patients pre-treated with a beta-blocker who had documented coronary artery disease, stable angina pectoris, and > or = 2 mm of exercise-induced ST segment depression. For 2 days the patients received open-label amlodipine and then, according to a randomized, placebo-controlled, cross-over and double-blind protocol, they were treated with amlodipine or placebo, respectively, once a day for 3 weeks each. Exercise tests and blood sampling for plasma concentrations of amlodipine were performed at 8 and at 24 h after dosing on both days of acute testing as well as on day 18 of chronic treatment. During chronic treatment, when plasma concentrations fluctuated between 23.5 ng.ml-1 at 8 h and 14 ng.ml-1 at 24 h post-dosing, ST segment depression at an individually comparable workload was significantly decreased by 28% compared with placebo (P < 0.005) at both points in time. Increases in ischaemia-free workload capacity amounted to 76% (P < 0.005) and to 81% (P < 0.01) at 8 and at 24 h, respectively. The number of anginal attacks was reduced by 39% (P < 0.05). Conversely, after initial dosing, i.e. when plasma concentrations declined from 4.7 ng.ml-1 to 3.9 ng.ml-1, influences upon ischaemic parameters compared to control values were markedly less at 24 h as opposed to 8 h. There were no untoward side effects observed at any point in time.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacokinetics and additional anti-ischaemic effectiveness of amlodipine, a once-daily calcium antagonist, during acute and long-term therapy of stable angina pectoris in patients pre-treated with a beta-blocker. 790 13

The efficacy and safety of amlodipine was evaluated in 20 patients with stable exertional angina. Patients with > or = 3 anginal attacks per week in the placebo run-in phase were admitted into a 4 weeks active treatment phase. Amlodipine was administered at a starting dose of 5 mg once daily at bed time, which could be adjusted after 2 weeks to 10 mg once daily if the patient continued to have even a single anginal attack/week. Four weeks of treatment with amlodipine produced a significant (p < 0.05) reduction from baseline in both the mean (+/- SE) number of anginal attacks/week (from 13.3 +/- 1.5 to 1.6 +/- 0.5) and the mean (+/- SE) number of isosorbide dinitrate tablets consumed per week (12.1 +/- 1.5 to 2.6 +/- 0.8). Eighty three percent of patients required an increase in dose to 10 mg daily. No significant change in heart rate, blood pressure, ECG and laboratory results were observed. One patient was withdrawn because of deteriorating angina and sinus tachycardia secondary to beta blocker withdrawal. Worsening of ankle odema was reported in 2 (10%) patients, which was tolerated and disappeared on completing therapy. Thus amlodipine is safe and effective when used as monotherapy in the treatment of chronic stable angina.
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PMID:Amlodipine monotherapy in chronic stable angina. 798 81

The efficacy of amlodipine, a calcium antagonist, was investigated in 12 patients with variant angina. Amlodipine was administered at a dose of 5 mg once daily, and efficacy was assessed from the frequency of anginal attacks, the frequency of ST elevation or depression, and the extent of ST segment changes [ST segment elevation or depression (mm) x duration (seconds)] on the Holter ECG before and after treatment. The frequency of ST elevation during the observation period was 1.67 +/- 0.33 times/day (symptomatic attacks: 1.17 +/- 0.21/day; asymptomatic attacks: 0.50 +/- 0.19/day), and this significantly decreased to zero per day (both symptomatic and asymptomatic attacks) after treatment (p < 0.05). The extent of ST segment elevation during the observation period was 507.5 +/- 156.6 mm.sec/day (symptomatic: 382.5 +/- 102.9 mm.sec/day; asymptomatic: 125.0 +/- 62.0 mm.sec/day), and such changes were completely suppressed (both symptomatic and asymptomatic) by treatment (p < 0.05). The frequency of ST depression was 2.08 +/- 0.42 times/day (symptomatic: 0.25 +/- 0.13/day; asymptomatic: 1.83 +/- 0.37/day) during the observation period, while it was 1.50 +/- 0.36 times/day (symptomatic: 0.25 +/- 0.13/day; asymptomatic: 1.25 +/- 0.30/day) after treatment. Although anginal attacks remained unchanged, asymptomatic attacks tended to decrease (p = 0.07).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Efficacy of amlodipine besilate therapy for variant angina: evaluation by 24-hour Holter monitoring. 801 72

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

Dihydropyridine calcium antagonists are established second line treatment for angina uncontrolled by beta-adrenergic blockers. Amlodipine is a recently introduced, dihydropyridine with a long half life. In a double blind, placebo controlled, cross over trial we assessed the efficacy and safety of amlodipine in 20 patients with persistent angina despite treatment with atenolol. 17 male patients (mean age 58 y) completed the study. Two patients were withdrawn during placebo because of worsening angina and one withdrew whilst on amlodipine because of palpitations. Compared with baseline, amlodipine prolonged exercise time to S-T segment depression by a median of 12.5%; significantly more than was found with placebo (median 0%). The improvement in exercise time and time to angina also tended to be greater for amlodipine than placebo. GTN consumption, at a median of 1.3/week, was significantly less with amlodipine than placebo (2.8). Attacks of angina were also reduced. Standing systolic and diastolic blood pressures and sitting systolic blood pressure were lower with amlodipine than placebo. Heart rate did not change. There was no change in cardiac output (measured by doppler aortovelography) when amlodipine was added to atenolol. Holter monitor measurements of 24 h maximum and minimum heart rate, heart rate variation and extrasystole counts were the same for amlodipine and placebo. In conclusion, amlodipine is effective in patients with angina inadequately controlled by atenolol alone, and does not interfere with cardiac rhythm or function.
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PMID:Amlodipine in patients with angina uncontrolled by atenolol. A double blind placebo controlled cross over trial. 822 29

Calcium antagonists are effective antianginal agents in the treatment of patients with stable exercise-induced angina pectoris. A series of randomized, double-blind, placebo-controlled studies with the novel, once-daily calcium antagonist amlodipine have been completed in a large number of patients with stable exercise-induced angina pectoris. Compared with placebo, once-daily amlodipine demonstrated a significant dose-related extension in exercise duration and workload accomplished, and reduction in number of anginal attacks and associated glyceryl trinitrate consumption. The clinical antianginal attributes of amlodipine were accompanied by significant reductions in electrocardiographic evidence of myocardial ischemia. In comparison with other antianginal drugs, once-daily amlodipine at a dosage range of 5-10 mg demonstrated antianginal activity comparable to thrice-daily diltiazem and once-daily nadolol. Amlodipine administered once daily achieves symptomatic and electrocardiographic amelioration of myocardial ischemic episodes induced by exercise in the majority of patients with stable angina pectoris. Amlodipine does not depress left ventricular pumping activity, and its side-effect profile does not differ substantially from that of placebo.
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PMID:Usefulness of amlodipine for angina pectoris. 831 Sep 73


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