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

Amlodipine, a potent long-acting dihydropyridine calcium antagonist, was compared with placebo in a parallel, randomized, double-blind study in 134 patients with chronic stable angina pectoris maintained on beta-adrenergic blocking agents. After a single-blind, two-week placebo period, patients were randomized to receive either amlodipine (2.5, 5, and 10 mg) or placebo once daily for four weeks. The effects of amlodipine on maximal exercise time, work, time to angina onset, and subjective indices including angina frequency, nitroglycerin tablet consumption, and patient and investigator ratings were assessed. Each dose of amlodipine produced increases in exercise time and calculated total work accomplished compared to baseline. Improvements at 5 and 10 mg were significantly greater than placebo which produced no significant change (p less than 0.05). Qualitative improvements in the severity of angina were produced by amlodipine at 5 and 10 mg daily assessed by patient-rating questionnaires (p less than 0.05). Reductions in angina frequency attacks per week and weekly nitroglycerin tablet consumption occurred but were not statistically significant when compared with placebo. Adverse effects observed during amlodipine treatment prompted discontinuation of treatment in only 2 out of 100 patients. Three patients discontinued treatment for reported lack of efficacy. No laboratory abnormalities prompted treatment discontinuation and minor side effects of dizziness, nausea, headache, and fatigue were observed infrequently. The results of this controlled, large-scale multicenter trial suggest that amlodipine significantly increased exercise capacity and was well tolerated when added to the antianginal regimen of patients remaining symptomatic while receiving beta-blocking agents.
 ...
PMID:Amlodipine combined with beta blockade for chronic angina: results of a multicenter, placebo-controlled, randomized double-blind study. 135 85

The effects of 5 and 10 mg of amlodipine and of placebo were compared in 21 patients with stable angina pectoris and multivessel coronary artery disease. The blind comparison was performed by means of bicycle ergometry and stress echocardiography using esophageal stimulation of the left heart atrium. All patients subsequently received placebo, amlodipine 5 mg and 10 mg for 2 weeks. In bicycle ergometry both doses of amlodipine in comparison with placebo significantly lowered the ST segment depression in lead V5 and prolonged the time to onset of angina. The exercise duration was significantly prolonged only after 10 mg of amlodipine. In stress echocardiography 10 mg of amlodipine significantly improved ejection fraction and reduced wall motion score during stimulation and increased peak velocity of relaxation of left ventricular posterior wall at rest and immediately after stimulation. In the patients with left ventricular end-diastolic pressure < or = 20 mmHg, amlodipine reduced the ratio of peak transmitral flow velocity in atrial contraction to that in early diastole (A/E) at rest and shortened deceleration time at rest and immediately after stimulation. Amlodipine in patients with stable angina pectoris significantly improved the exercise tolerance and the function of the left ventricle in a dose-dependent way. Amlodipine was well tolerated.
 ...
PMID:Amlodipine in patients with stable angina pectoris treated with nitrates and beta-blockers. The influence on exercise tolerance, systolic and diastolic functions of the left ventricle. 135 30

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.
 ...
PMID:[Amlodipine: pharmacokinetic and pharmacodynamic profile of a calcium antagonist with prolonged effect]. 153 45

Once-daily administration of amlodipine is a highly effective treatment for patients with angina pectoris. This study has confirmed its benefit in a relatively large subgroup of patients with post-myocardial infarction angina. Amlodipine reduced the number of angina attacks and nitroglycerin consumption and substantially improved the ability of the patient to perform physical exercise. The circadian pattern of angina attacks was markedly attenuated by amlodipine with patients reporting fewer attacks during the mid-morning peak that was clearly evident at baseline. The advantage of once-daily dosing, together with the excellent control of angina achieved in post-infarction patients, make amlodipine a good choice for therapy.
 ...
PMID:Amlodipine in post-infarction angina. 153 12

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.
 ...
PMID:Pharmacokinetics and pharmacodynamics of amlodipine. 153 13

The calcium antagonists are valuable and widely used agents in the management of essential hypertension and angina. There is an increasing number of new agents to add to the 3 prototype substances nifedipine, diltiazem and verapamil. These new agents are dihydropyridines structurally related to nifedipine. However, they tend to have longer elimination half-lives (t 1/2 beta) and may be suitable for twice-daily administration. Amlodipine is an exception with a t 1/2 beta in excess of 30h. Apart from elimination rates, however, the pharmacokinetic characteristics of the newer agents have a notable tendency to resemble those of the established agents. They are highly cleared drugs, are relatively highly protein bound. As they are subject to significant first-pass metabolism, old age and hepatic impairment will increase their plasma concentrations due to a reduced first-pass effect. Renal impairment does little to their pharmacokinetics since the fraction eliminated unchanged by the kidney is small. For most agents, plasma concentration-response relationships have been described. Interesting areas for further research include chronopharmacokinetics, stereoselective pharmacokinetics and lipid solubility. Drugs affecting hepatic blood flow and drug metabolising capacity have predictable interaction potential. Some of the newer calcium antagonists will, like verapamil, increase plasma digoxin concentrations. Verapamil and diltiazem decrease phenazone (antipyrine) metabolism and therefore tend to decrease the metabolism of other drugs.
 ...
PMID:Clinical pharmacokinetics of calcium antagonists. An update. 158 55

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.
 ...
PMID:Amlodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiovascular disease. 171 48

Sixty patients (31 male, 29 female) were studied in a 4-week double-blind parallel dose-response study. Patients received amlodipine 1.25 mg (n = 12), 2.5 mg (n = 12), 5 mg (n = 12), 10 mg (n = 12) or placebo (n = 12) once a day. Anti-anginal efficacy was assessed by sequential treadmill testing 24 h post-dose, frequency of anginal attacks and consumption of nitroglycerin, patient and investigator assessment. In the analysis of the final vs baseline total exercise time, the difference between those on amlodipine and those on placebo was significant (P less than 0.01), (all doses). Mean total exercise time increased by 24% in the amlodipine 10 mg group compared with a 20% decrease in the placebo group. The time to onset of angina increased by 37% in the amlodipine 10 mg group, compared with a 16.5% decrease in the placebo group. Differences were statistically significant for the 1.25, 5 and 10 mg amlodipine groups vs placebo. ST-segment charges and rate-pressure product were not affected significantly. There was a statistically significant difference in angina attack frequency and nitroglycerin tablet consumption (P less than 0.05) for all dose groups vs placebo. The majority of patients receiving amlodipine reported improvement in angina symptoms. Side-effects were frequent but mild and dose-related. Amlodipine has significant anti-anginal efficacy. The mechanisms underlying the anti-ischaemic effects of amlodipine are still under discussion.
 ...
PMID:A double-blind dose-response study of amlodipine in patients with stable angina pectoris. 182 20

Amlodipine is a dihydropyridine calcium antagonist that has unique pharmacokinetic properties. The drug is absorbed gradually after oral administration and so produces a gradual vasodilatation, reducing the incidence of side effects such as reflex tachycardia and headache, which can be troublesome with other calcium antagonists. Amlodipine also has a long elimination half-life, which makes it suitable for use on a once-daily basis. Controlled clinical studies have confirmed that a suitable dose regimen of amlodipine for use in angina is to start with 5 mg daily and increase this to 10 mg daily if required to control symptoms. Exercise testing carried out 24 hours post dose has confirmed that once-daily doses of amlodipine provide good anti-anginal and anti-ischaemic efficacy for a full 24 hours, a vital aspect of any therapy for ischaemic heart disease. Amlodipine has been shown to have comparable anti-anginal efficacy to the beta-blocker nadolol taken once daily and the calcium antagonist diltiazem taken 3 times daily. When added to the treatment regimen of patients with uncontrolled chronic stable angina despite treatment with nitrates, beta-blockers or both, amlodipine produces improved anti-anginal efficacy. Amlodipine has also been shown to be consistently effective in patients with vasospastic angina. There has been no evidence of tolerance to the anti-anginal effects of amlodipine in formal clinical trials involving treatment for up to 26 weeks.
 ...
PMID:The efficacy of amlodipine in the management of ischaemic heart disease. 183 71

Amlodipine is a dihydropyridine calcium antagonist with a unique pharmacokinetic profile providing advantages over other therapies of its kind. It has been shown to possess high oral absorption, long elimination half-life, smooth onset of action and long duration of pharmacodynamic activity. These properties result in gradual vasodilation, ensuring a low incidence of vasodilatory side effects and once-daily administration. In randomized, double-blind, placebo-controlled studies a dose of 5-10 mg once daily has been established as the most efficacious dose for the treatment of angina pectoris. Amlodipine was found to increase exercise capacity significantly and reduce electrocardiographic evidence of myocardial ischaemia after treadmill exercise testing 24 h after administration compared with placebo in patients suffering from angina pectoris. Angina attack rate and glyceryl trinitrate consumption were also significantly reduced. Amlodipine was shown to possess comparable anti-anginal efficacy with the calcium antagonist diltiazem and the beta-blocker nadolol. In combination with beta-blockers and/or nitrates the addition of amlodipine was found to produce enhanced anti-anginal efficacy with good tolerability. Amlodipine is also effective in reducing the angina attack rate in patients with vasospastic angina. In conclusion, amlodipine is an effective and well-tolerated therapeutic agent given once daily as monotherapy or in combination with beta-blockers and/or nitrates for the treatment of chronic stable angina pectoris and vasospastic angina.
 ...
PMID:A review of amlodipine in myocardial ischaemia. 183 40


1 2 3 4 5 6 7 Next >>